320 results on '"Bonina, F."'
Search Results
152. ChemInform Abstract: SOME AROYLHYDRAZONES OF HALOBENZALDEHYDES AND HALO-SUBSTITUTED 2,5-DIARYL-1,3,4-OXADIAZOLES
- Author
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MAZZONE, G., primary, BONINA, F., additional, and FORMICA, F., additional
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- 1979
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153. ChemInform Abstract: Reactivity of 3‐Aryl‐4‐amino‐5‐mercapto‐4H‐1,2,4‐triazoles: Synthesis and Biological Evaluation of 3,6‐Diaryl Derivatives of 7H‐1,2,4‐Thiazolo(3,4‐b)(1,3,4)thiadiazine and of 3‐Aryl‐4‐amino‐5‐carboxymethylthio4H‐1,2,4‐triazoles.
- Author
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MAZZONE, G., primary, BONINA, F., additional, PANICO, A. M., additional, AMICO‐ROXAS, M., additional, CARUSO, A., additional, BLANDINO, G., additional, and VANELLA, A., additional
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- 1988
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154. ChemInform Abstract: 3-METHYLTHIO-, 3-(SUBSTITUTED-AMINO)ETHYLTHIO-, 3-CARBOXYMETHYLTHIO-, AND 3,3′-(DITHIOBIS)-5-ARYL-4H(R)-1,2,4-TRIAZOLES AND N-SUBSTITUTED 2-AMINOMETHYL DERIVATIVES OF 5-ARYL-4H(R)-1,2,4-TRIAZOLINE-3-THIONES: SYNTHESIS AND BIOLOGICAL A
- Author
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MAZZONE, G., primary, BONINA, F., additional, and BLANDINO, G., additional
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- 1982
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155. ChemInform Abstract: Synthesis and Pharmacological Activity of 2-Arylethenylthiazol-4-acetic Acids and -4-carboxylic Acids.
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BONINA, F., primary, GUERRERA, F., additional, PAPPALARDO, F., additional, SIRACUSA, M. A., additional, CARUSO, A., additional, TROMBADORE, S., additional, and AMICO-ROXAS, M., additional
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- 1986
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156. ChemInform Abstract: A NEW SYNTHESIS OF SYMMETRICAL 2,5-DIARYL-1,3,4-THIADIAZOLES
- Author
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MAZZONE, G., primary, PUGLISI, G., additional, BONINA, F., additional, and CORSARO, A., additional
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- 1984
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157. ChemInform Abstract: SYNTHESIS AND BIOLOGICAL ACTIVITY OF 3-AMINOMETHYL DERIVATIVES OF SOME 5-ARYL-1,3,4-OXADIAZOL-2-ONES
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MAZZONE, G., primary, BONINA, F., additional, and ARRIGO REINA, R., additional
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- 1980
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158. ChemInform Abstract: Synthesis, Stability and Anticonvulsant Activity of Two New GABA Prodrugs.
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PALAGIANO, F., BONINA, F. P., MONTENEGRO, L., BIONDI, A., SORRENTINO, L., CAPASSO, A., and DE CAPRARIIS, P.
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- 1997
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159. In vitro percutaneous absorption evaluation of phenobarbital through hairless mouse, adult and premature human skin
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Bonina, F. P., Montenegro, L., Micali, G., and West, D. P.
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- 1993
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160. In vitro evaluation of N-acyllactam esters of indomethacin as dermal prodrugs
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Bonina, F. P., Montenegro, L., Trapani, G., and Franco, M.
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- 1995
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161. Flavonoid-biomembrane interactions: A calorimetric study on dipalmitoylphosphatidylcholine vesicles
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Saija, A., Bonina, F., Trombetta, D., and Tomaino, A.
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- 1995
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162. Effects of some non-toxic penetration enhancers on in vitro heparin skin permeation from a gel vehicles
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Bonina, F. P. and Montenegro, L.
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- 1994
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163. Partitioning and differential scanning calorimetry studies of N-alkyllactame ester dermal prodrugs of indomethacin
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Bonina, F. P., Castelli, F., Montenegro, L., and Mazzone, G.
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- 1994
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164. Vehicle effects on in vitro heparin release and skin penetration from different gels
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Bonina, F. P. and Montenegro, L.
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- 1994
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165. Assay of vitamin A palmitate and vitamin E acetate in cosmetic creams and lotions by supercritical fluid extraction and HPLC
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Scalia, S., Renda, A., Ruberto, G., and Bonina, F.
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- 1995
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166. Effects of phospholipid based formulations on in vitro and in vivo percutaneous absorption of methyl nicotinate
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Bonina, F. P., Montenegro, L., Scrofani, N., and Esposito, E.
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- 1995
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167. In vitro and in vivo evaluation of polyoxyethylene indomethacin esters as dermal prodrugs
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Bonina, F. P., Montenegro, L., Caprariis, P. De, and Palagiano, F.
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- 1995
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168. Naproxen l-alkylazacycloalkan-2-one esters as dermal prodrugs: in vitro evaluation
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Bonina, F. P., Montenegro, L., and Guerrera, F.
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- 1993
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169. Vehicle effects on in vitro skin permeation of and stratum corneum affinity for model drugs caffeine and testosterone
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Bonina, F. P., Carelli, V., Colo, G. Di, and Montenegro, L.
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- 1993
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170. Evaluation of Alternative Strategies to Optimize Ketorolac Transdermal Delivery
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Antonella Peduto, Francesco Bonina, Luisa Rizza, Carmelo Puglia, Rosanna Filosa, Paolo Blasi, Paolo De Caprariis, Puglia C., Filosa R., Peduto A., de Caprariis P., Rizza L., Bonina F., Blasi P., Puglia, C, Filosa, Rosanna, Peduto, A, de Caprariis, P, Rizza, L, Bonina, F, and Blasi, P.
- Subjects
Drug ,Chemistry, Pharmaceutical ,Skin Absorption ,media_common.quotation_subject ,Pharmaceutical Science ,ketorolac ,02 engineering and technology ,Aquatic Science ,030226 pharmacology & pharmacy ,Article ,03 medical and health sciences ,Drug Delivery Systems ,0302 clinical medicine ,Drug Discovery ,medicine ,Stratum corneum ,Humans ,Organic chemistry ,Prodrugs ,Drug Carrier ,Ecology, Evolution, Behavior and Systematics ,media_common ,Transdermal ,Drug Carriers ,Chromatography ,Ecology ,Chemistry ,Ketorolac ,Lipid carrier ,Prodrug ,Anti-Inflammatory Agents, Non-Steroidal ,lipid carrier ,General Medicine ,Permeation ,021001 nanoscience & nanotechnology ,body regions ,NLC ,prodrug ,transdermal delivery ,medicine.anatomical_structure ,Drug reservoir ,Female ,0210 nano-technology ,Drug carrier ,Drug Delivery System ,Agronomy and Crop Science ,Human ,medicine.drug - Abstract
In the present study, 2 alternative strategies to optimize ketorolac transdermal delivery, namely, prodrugs (polyoxyethylene glycol ester derivatives, I–IV) and nanostructured lipid carriers (NLC) were investigated. The synthesized prodrugs were chemically stable and easily degraded to the parent drug in human plasma. Ketorolac-loaded NLC with high drug content could be successfully prepared. The obtained products formulated into gels showed a different trend of drug permeation through human stratum corneum and epidermis. Particularly, skin permeation of ester prodrugs was significantly enhanced, apart from ester IV, compared with ketorolac, while the results of drug release from NLC outlined that these carriers were ineffective in increasing ketorolac percutaneous absorption owing to a higher degree of mutual interaction between the drug and carrier lipid matrix. Polyoxyethylene glycol esterification confirmed to be a suitable approach to enhance ketorolac transdermal delivery, while NLC seemed more appropriate for sustained release owing to the possible formation of a drug reservoir into the skin.
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- 2006
171. PEG-crosslinked-chitosan hydrogel films for in situ delivery of Opuntia ficus-indica extract
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Paola Laurienzo, Antonella D’Agostino, Rosa Lanzetta, Giovanna Gomez d'Ayala, Ovidio Catanzano, Francesco Bonina, F. Di Lorenzo, Mario Malinconico, Chiara Schiraldi, Catanzano, O, Gomez d'Ayala, G, D'Agostino, A, Di Lorenzo, F, Schiraldi, C, Malinconico, M, Lanzetta, R, Bonina, F, and Laurienzo, P
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Opuntia ficus-indica ,Polymers and Plastics ,Kinetics ,Biocompatible Materials ,Wound-healing assay ,macromolecular substances ,02 engineering and technology ,010402 general chemistry ,01 natural sciences ,Polyethylene Glycols ,Chitosan ,chemistry.chemical_compound ,Drug Delivery Systems ,Elastic Modulus ,Tensile Strength ,PEG ratio ,Ultimate tensile strength ,Monolayer ,Spectroscopy, Fourier Transform Infrared ,Materials Chemistry ,medicine ,HaCaT Cells ,Humans ,Fourier transform infrared spectroscopy ,Skin ,Wound Healing ,Crosslinking ,Poly(ethylene glycol) ,Plant Extracts ,Organic Chemistry ,technology, industry, and agriculture ,Opuntia ,Hydrogels ,021001 nanoscience & nanotechnology ,Methylgalactosides ,Bandages ,0104 chemical sciences ,Cross-Linking Reagents ,chemistry ,Swelling ,medicine.symptom ,0210 nano-technology ,Ethylene glycol ,Nuclear chemistry - Abstract
In the present study, chitosan-based wound dressings loaded with the extract of Opuntia ficus-indica (OPU) were prepared. OPU is known for its capability to accelerate skin injury repair. Chitosan (Ch) was crosslinked with a low molecular weight diepoxy-poly(ethylene glycol) (diePEG), and hydrogel films with different Ch/PEG composition and OPU content were prepared by casting. The occurrence of crosslinking reaction was confirmed by FTIR spectroscopy. FTIR and DSC analysis suggested that ionic interactions occur between chitosan and OPU. Tensile tests evidenced that the crosslinking caused a decrease of Young’s modulus, which approaches the value of the human skin modulus. Swelling characteristics, water vapor transmission rate, and release kinetics demonstrated that these films are adequate for the proposed application. Finally, a scratch test on a keratinocytes monolayer showed that the rate of cell migration in the presence of OPU-loaded samples is about 3-fold higher compared to unloaded films, confirming the repairing activity of OPU.
- Published
- 2020
172. In-vitro and in-vivo evaluation of oligoethylene esters as dermal prodrugs of 18β-glycyrrhetic acid
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Francesco Bonina, Carmine Ostacolo, Sonia Laneri, Antonia Sacchi, Carmelo Puglia, Puglia, C., Ostacolo, Carmine, Sacchi, Antonia, Laneri, Sonia, and Bonina, F.
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Adult ,Male ,Skin erythema ,Skin Absorption ,Anti-Inflammatory Agents ,Pharmaceutical Science ,Human skin ,In Vitro Techniques ,Administration, Cutaneous ,Permeability ,ethylene glycol derivative ,Polyethylene Glycols ,Hydrolysis ,Drug Stability ,glycyrrhetinic acid ,prodrug ,In vivo ,Enzymatic hydrolysis ,Stratum corneum ,medicine ,Humans ,Organic chemistry ,Prodrugs ,Chromatography, High Pressure Liquid ,Skin ,Pharmacology ,Chromatography ,integumentary system ,Chemistry ,Nicotinic Acids ,Esters ,Prodrug ,Membrane ,medicine.anatomical_structure ,Erythema ,Glycyrrhetinic Acid ,Female ,Dermatologic Agents ,Gels - Abstract
Novel polyoxyethylene esters of 18 β-glycyrrhetic acid (GA) were synthesized and evaluated as potential dermal prodrugs. The permeation of these prodrugs (1a-e) was studied in-vitro, using excised human skin membranes (SCE; stratum corneum/epidermis) mounted in Franz type cells, and in-vivo, evaluating the ability of these compounds to inhibit methyl nicotinate (MN)-induced skin erythema in healthy human subjects. All the esters synthesized showed a good water stability, while the enzymatic hydrolysis rate was significantly affected by the length of the polyoxyethylenic chain used as promoiety. In in-vitro percutaneous absorption studies, only esters 1b and 1c (respectively triethylen- and tetraethylenglycol derivatives) showed an increased flux through SCE membranes compared with GA. Furthermore, we observed an appreciable and sustained in-vivo topical anti-inflammatory activity of esters 1b and 1c compared with the parent drug.
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- 2006
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173. Synthesis and in vitro chemical and enzymatic stability of glycosyl 3′-azido-3′-deoxythymidine derivatives as potential anti-HIV agents
- Author
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Maria Grazia Rimoli, Enrico Abignente, Rosaria Meli, Paolo De Caprariis, L. Avallone, Giampiero Boatto, Michele Amorena, Carmelo Puglia, Maria Nieddu, Francesco Bonina, Bonina, F., Puglia, C., Rimoli, MARIA GRAZIA, Avallone, L., Abignente, E., Boatto, G., Nieddu, M., Meli, Rosaria, Amorena, M., DE CAPRARIIS, P., Rimoli, M. G., and ABIGNENTE DI FRASSELLO, Enrico
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Male ,Glycosylation ,Anti-HIV Agents ,Swine ,Stereochemistry ,viruses ,Pharmaceutical Science ,Esterase ,Chemical synthesis ,chemistry.chemical_compound ,Zidovudine ,Azidodeoxythymidine ,Chemical stability ,Sustained release ,Enzyme Stability ,medicine ,Animals ,Prodrugs ,heterocyclic compounds ,Glycosyl ,sustauned release ,Rats, Wistar ,Esterases ,Biological activity ,biochemical phenomena, metabolism, and nutrition ,Prodrug ,chemical stability ,Controlled release ,Rats ,chemistry ,Area Under Curve ,medicine.drug - Abstract
New glycosyl derivatives of 3'-azido-3'-deoxythymidine (AZT) (1 and 2) were synthesized in order to improve AZT retention in the blood and to guarantee its sustained release, overcoming the necessity of multiple drug administrations. The esters synthesized (1 and 2) link AZT, by a succinyl linker, to the C-3 position of glucose and to C-6 of galactose. Furthermore, the chemical and enzymatic stabilities of esters 1 and 2 were evaluated in order to determine both their stability in aqueous medium and their feasibility to undergo enzymatic cleavage by esterase to regenerate the original drug. The pharmacokinetic profiles of esters 1 and 2, obtained after systemic administration, showed an interesting controlled release, in particular for ester 2, compared to the pharmacokinetic profile of AZT.
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- 2002
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174. Lipid nanoparticles as carrier for octyl-methoxycinnamate: in vitro percutaneous absorption and photostability studies
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Elisabetta Damiani, Carmelo Puglia, Aurelie Marie Madeleine Schoubben, Luisa Rizza, Francesco Bonina, Maria Stella Tarico, Paolo Blasi, Rosario Emanuele Perrotta, Puglia C., Bonina F., Rizza L., Blasi P., Schoubben A., Perrotta R., Tarico M.S., and Damiani E.
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Adult ,Nanostructure ,Materials science ,Chemistry, Pharmaceutical ,Skin Absorption ,Sonication ,Analytical chemistry ,Pharmaceutical Science ,Nanoparticle ,Nanoparticles ,Percutaneous ,Photodegradation ,Calorimetry (DSC) ,In vitro models ,Skin ,Particle size ,Ultrasound ,Permeability ,Photochemical Processe ,chemistry.chemical_compound ,Differential scanning calorimetry ,In vitro model ,Cinnamate ,Drug Stability ,Solid lipid nanoparticle ,Humans ,Microemulsion ,Solubility ,Drug Carrier ,Drug Carriers ,Calorimetry, Differential Scanning ,Emulsion ,skin ,photodegradation ,Octyl methoxycinnamate ,Lipid ,Photochemical Processes ,Oil ,Lipids ,Nanostructures ,chemistry ,Cinnamates ,Emulsions ,Percutaneou ,Oils ,Human ,Nuclear chemistry - Abstract
The aim of the present study was the evaluation of lipid nanoparticles (solid lipid nanoparticles, SLN, and nanostructured lipid carriers, NLC) as potential carriers for octyl-methoxycinnamate (OMC). The release pattern of OMC from SLN and NLC was evaluated in vitro, determining its percutaneous absorption through excised human skin. Additional in vitro studies were performed in order to evaluate, after UVA radiation treatment, the spectral stability of OMC-loaded lipid nanoparticles. From the obtained results, ultrasonication method yielded both SLN and NLC in the nanometer range with a high active loading and a particle shape close to spherical. Differential scanning calorimetry data pointed out the key role of the inner oil phase of NLC in stabilizing the particle architecture and in increasing the solubility of OMC as compared with SLN. In vitro results showed that OMC, when incorporated in viscosized NLC dispersions (OMCNLC), exhibited a lower flux with respect to viscosized SLN dispersions (OMCSLN) and two reference formulations: a microemulsion (OMC-ME) and a hydroalcoholic gel (OMC-GEL). Photostability studies revealed that viscosized NLC dispersions were the most efficient at preserving OMC from ultraviolet-mediated photodegradation. (c) 2011 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:301-311, 2012
- Published
- 2012
175. Lipid nanoparticles for brain targeting I. Formulation optimization
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Carlo Rossi, Francesco Bonina, Paolo Blasi, Maurizio Ricci, Stefano Giovagnoli, Carmelo Puglia, Aurelie Marie Madeleine Schoubben, Blasi P., Giovagnoli S., Schoubben A., Puglia C., Bonina F., Rossi C., and Ricci M.
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Materials science ,Palmitates ,Pharmaceutical Science ,Nanoparticle ,Lipid nanoparticle ,Nanotechnology ,Palmitate ,Triglyceride ,Blood–brain barrier ,chemistry.chemical_compound ,Colloid ,Drug Delivery Systems ,High pressure homogenization ,Response surface methodology ,Colloids ,Infusions, Intravenou ,Particle Size ,Infusions, Intravenous ,Brain targeting ,Lipid nanoparticles ,Drug Carrier ,Triglycerides ,Blood-brain barrier ,Drug Carriers ,Cetyl palmitate ,Fatty Acids ,Temperature ,Brain ,Lipid ,Lipids ,chemistry ,Neurovascular unit ,Computer-Aided Design ,Nanoparticles ,Particle size ,Drug Delivery System ,Fatty Acid - Abstract
The aim of this study was to optimize the formulation of lipid nanoparticles (NPs), intended for brain targeting, with the aid of a computer generated experimental design. The high pressure homogenization technique, selected for this purpose, was suitable to formulate the 3 investigated lipids (i.e., Softisan (R) 142, SOFT; Compritol (R) 888 ATO, COMP; cetyl palmitate, CP) into nanometre-length particles, while the computer generated experimental design helped to individuate the best preparation conditions with a small number of experimental assay. Even though all the 3 optimized formulations were suitable for intravenous infusion, CP NPs showed the smallest particle size and the appropriate thermal behaviour to be used as carriers in brain targeting applications. (C) 2011 Elsevier B.V. All rights reserved.
- Published
- 2011
176. Lipid nanoparticles for prolonged topical delivery: An in vitro and in vivo investigation
- Author
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Francesco Bonina, Maurizio Ricci, Carlo Rossi, Carmelo Puglia, Aurelie Marie Madeleine Schoubben, Paolo Blasi, Luisa Rizza, Puglia C., Blasi P., Rizza L., Schoubben A., Bonina F., Rossi C., and Ricci M.
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Adult ,Male ,Naproxen ,Administration, Topical ,Chemistry, Pharmaceutical ,Skin Absorption ,Pharmaceutical Science ,Nanoparticle ,Lipid nanoparticle ,SLN ,Human skin ,Pharmacology ,In Vitro Techniques ,Dosage form ,Ketoprofen ,Lipid nanoparticles ,Drug Delivery Systems ,In vivo ,medicine ,Humans ,Ultrasonics ,NLC ,Dermal targeting ,Microparticle ,Particle Size ,Skin ,Active ingredient ,Gel ,integumentary system ,Calorimetry, Differential Scanning ,Chemistry ,In Vitro Technique ,Anti-Inflammatory Agents, Non-Steroidal ,Lipid ,Controlled release ,Lipids ,Biophysics ,Nanoparticles ,Female ,Gels ,Drug Delivery System ,medicine.drug ,Human - Abstract
Dermal therapy is still a challenge due to the difficulties in controlling the active pharmaceutical ingredient (API) fate within the skin. Recently, lipid nanoparticles have shown a great potential as vehicle for topical administration of active substances, principally owing to the possible targeting effect and controlled release in different skin strata. Ketoprofen and naproxen loaded lipid nanoparticles were prepared, using hot high pressure homogenization and ultrasonication techniques, and characterized by means of photo correlation spectroscopy and differential scanning calorimetry. Nanoparticle behavior on human skin was assessed, in vitro, to determine drug percutaneous absorption (Franz cell method) and, in vivo, to establish the active localization (tape-stripping technique) and the controlled release abilities (UVB-induced erythema model). Results demonstrated that the particles were able to reduce drug penetration increasing, simultaneously, the permeation and the accumulation in the horny layer. A prolonged anti-inflammatory effect was observed in the case of drug loaded nanoparticles with respect to the drug solution. Direct as well as indirect evidences corroborate the early reports on the usefulness of lipid nanoparticles as carriers for topical administration, stimulating new and deeper investigations in the field. (c) 2008 Elsevier B.V. All rights reserved.
- Published
- 2008
177. NEW OLIGOETHYLENE ESTER DERIVATIVES OF 5-IODO-2’-DEOXYURIDINE AS DERMAL PRODRUGS : SYNTHESIS, PHYSICOCHEMICAL PROPERTIES, AND SKIN PERMEATION STUDIES
- Author
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Francesco Bonina, Marzia Amato, Maurizio Ricci, L. Avallone, Maria Grazia Rimoli, Carmelo Puglia, Paolo De Caprariis, Francesco Barbato, Bonina, F. P., Rimoli, MARIA GRAZIA, Avallone, L., Barbato, Francesco, Amato, M., Puglia, C., Ricci, M., and DE CAPRARIIS, P.
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Adult ,Swine ,Skin Absorption ,Dermal prodrugs ,Pharmaceutical Science ,IDU ,In vitro ,Administration, Cutaneous ,Chemical synthesis ,Esterase ,chemistry.chemical_compound ,Idoxuridine ,Organic chemistry ,Animals ,Humans ,Prodrugs ,Nucleic Acid Synthesis Inhibitors ,Chromatography ,Chemistry ,virus diseases ,Esters ,Prodrug ,Permeation ,Ethylenes ,Middle Aged ,Deoxyuridine ,Partition coefficient ,Succinic acid ,Lipophilicity - Abstract
Five new oligoethylene ester derivatives (9-13) of 5-iodo-2'-deoxyuridine (IDU) were synthesized and assayed to determine their lipophilicity by both experimental lipophilicity indices (log K') and calculated partition coefficients (CLOGP). In vitro experiments were carried out to evaluate the chemical and enzymatic stability and fluxes through excised human skin of these new IDU derivatives. Esters 9-13 showed increased lipophilicity compared with the parent drug (IDU), had good stability in phosphate buffer (pH 7.4), and were readily hydrolyzed by porcine esterase. No correlation between lipophilicity and skin permeation fluxes of synthesized esters 9-13 was observed. Results from in vitro percutaneous absorption studies showed that, among all esters synthesized, only esters 9 and 10 significantly increased the cumulative amount of IDU that penetrated through excised human skin compared with the parent drug (IDU).
- Published
- 2002
178. IN VITRO AND IN VIVO EVALUATION OF POLYOXYETHYLENE ESTERS AS DERMAL PRODRUGS OF KETOPROFEN, NAPROXEN AND DICLOFENAC
- Author
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Maria Grazia Rimoli, Carmelo Puglia, Paolo De Caprariis, Tony Barbuzzi, Francesco Bonina, Antonella Saija, F. Palagiano, BONINA F., P, Puglia, C., Barbuzzi, T., DE CAPRARIIS, P., Palagiano, F., Rimoli, MARIA GRAZIA, and Saija, A.
- Subjects
Ketoprofen ,Adult ,Male ,Skin erythema ,Naproxen ,Diclofenac ,Skin Absorption ,Pharmaceutical Science ,Administration, Cutaneous ,Esterase ,Polyethylene Glycols ,chemistry.chemical_compound ,Controlled release ,Dermal prodrug ,Skin permeation ,In vivo ,medicine ,Organic chemistry ,Humans ,Prodrugs ,Chromatography ,Chemistry ,Anti-Inflammatory Agents, Non-Steroidal ,Prodrug ,Middle Aged ,Solubility ,Succinic acid ,Erythema ,Area Under Curve ,Solvents ,Female ,Gels ,medicine.drug - Abstract
Novel polyoxyethylene esters of ketoprofen (1(a-e)), naproxen (2(a-e)) and diclofenac (3(a-e)) were synthesized and evaluated as potential dermal prodrugs of naproxen, ketoprofen and diclofenac. These esters were obtained by coupling these drugs with polyoxyethylene glycols by a succinic acid spacer. The aqueous solubilities, lipophilicities and hydrolysis rates of esters 1(a-e), 2(a-e) and 3(a-e) were determined in a buffered solution and in porcine esterase. The permeation of these prodrugs through excised human skin was studied in vitro. Furthermore we investigated the in vivo topical anti-inflammatory activity of esters 1(d), 2(e) and 3(e), which showed the best in vitro profile, evaluating the ability of these compounds to inhibit methyl nicotinate (MN)-induced skin erythema on healthy human volunteers. Esters 1(a-e), 2(a-e) and 3(a-e) showed good water stability and rapid enzymatic cleavage and their hydrolysis rates, both chemical and enzymatic, were not significantly affected by the length of the polyoxyethylenic chain used as promoiety. Concerning in vitro percutaneous absorption studies, only esters 1(d-e), 2(d-e) and 3(c-e) showed an increased flux through stratum corneum and epidermis membranes compared to their respective parent drugs. In vivo results showed an interesting delayed and sustained activity of esters 1(d) and 3(e) compared to the parent drugs. In conclusion polyoxyethylene glycols could prove to be suitable promoieties for ketoprofen, naproxen and diclofenac design since esters 1(d-e), 2(d-e) and 3(c-e) showed some requirements (chemical stability, enzymatic lability and an increased skin permeation) needed to obtain successful dermal prodrugs. Furthermore, was observed an appreciable and sustained in vivo topical anti-inflammatory activity of esters 1(d) and 3(e), compared to the parent drugs, using MN-induced erythema in human volunteers as inflammation model.
- Published
- 2001
179. Synthesis and pharmacological evaluation of oligoethylene ester derivatives as indomethacin oral prodrugs
- Author
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Michele D'Amico, Lucia Montenegro, Francesco Rossi, F. Palagiano, Franco Bonina, Paolo De Caprariis, De Caprariis, P, Palagiano, F, Bonina, F, Montenegro, L, D'Amico, Michele, Rossi, F., DE CAPRARIIS, P, and Rossi, Francesco
- Subjects
Male ,Analgesic ,Pharmaceutical Science ,Pharmacology ,Carrageenan ,Chemical synthesis ,Mice ,indomethacin ,Oral administration ,Edema ,Gastric mucosa ,medicine ,Organic chemistry ,Animals ,Humans ,Prodrugs ,Stomach Ulcer ,Chromatography, High Pressure Liquid ,Pain Measurement ,chemistry.chemical_classification ,Chemistry ,Hydrolysis ,Anti-Inflammatory Agents, Non-Steroidal ,Biological activity ,Esters ,Prodrug ,Rats ,medicine.anatomical_structure ,Enzyme ,prodrug ,bioavailability ,medicine.symptom - Abstract
Five indomethacin oligoethylene ester derivatives ( 3 – 7 ) were synthesized and evaluated for their anti‐inflammatory, analgesic, and ulcerogenic activity after oral administration. The molecular weight of the oligoethylene glycols used for synthesizing esters 3 – 7 ranged from 106 to 282. The chemical and enzymatic stabilities of esters 3 – 7 were evaluated in pH 7.4 and 2.0 buffers and in human plasma, respectively. All the prodrugs showed a good stability both in pH 7.4 phosphate buffer and in pH 2.0 buffer, and they were readily hydrolyzed by human plasma. Esters 3 – 7 showed an anti‐inflammatory activity, determined as the percent inhibition of carrageenan‐induced edema, similar to that of indomethacin, although at higher doses. From writhing test results, we observed that all the prodrugs exhibited better or similar analgesic activity compared to indomethacin. Esters 3 – 7 were significantly less irritating to the gastric mucosa than indomethacin, after oral administration, and esters 3 – 5 did not show any ulcerogenic activity, although they were administered at higher doses than indomethacin.
- Published
- 1994
180. Hydroxytyrosol from olive fruits prevents blue-light-induced damage in human keratinocytes and fibroblasts.
- Author
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Avola R, Graziano ACE, Pannuzzo G, Bonina F, and Cardile V
- Subjects
- Antioxidants isolation & purification, Cell Line, Cell Survival drug effects, Cell Survival radiation effects, Collagen Type I genetics, Collagen Type I metabolism, DNA Damage, Elastin metabolism, Fibroblasts metabolism, Fibroblasts pathology, Fibroblasts radiation effects, Humans, Keratinocytes metabolism, Keratinocytes pathology, Keratinocytes radiation effects, Matrix Metalloproteinase 1 genetics, Matrix Metalloproteinase 1 metabolism, Matrix Metalloproteinase 12 genetics, Matrix Metalloproteinase 12 metabolism, Oxidative Stress drug effects, Oxidative Stress radiation effects, Phenylethyl Alcohol isolation & purification, Phenylethyl Alcohol pharmacology, Proliferating Cell Nuclear Antigen metabolism, Radiation-Protective Agents isolation & purification, Reactive Oxygen Species metabolism, Skin metabolism, Skin pathology, Skin radiation effects, Skin Aging radiation effects, Time Factors, Antioxidants pharmacology, Fibroblasts drug effects, Fruit chemistry, Keratinocytes drug effects, Light adverse effects, Olea chemistry, Phenylethyl Alcohol analogs & derivatives, Radiation-Protective Agents pharmacology, Skin drug effects, Skin Aging drug effects
- Abstract
Skin aging is a complex biological process influenced by a combination of endogenous or intrinsic and exogenous or extrinsic factors due to environmental damage. The primary environmental factor that causes human skin aging is the ultraviolet irradiation from the sun. Recently, it was established that the long-term exposure to light-emitting-diode-generated blue light (LED-BL) from electronic devices seems to have a relevant implication in the molecular mechanisms of premature photoaging. BL irradiation induces changes in the synthesis of various skin structures through DNA damage and overproduction of reactive oxygen species (ROS), matrix metalloproteinase-1 and -12, which are responsible for the loss of the main components of the extracellular matrix of skin like collagen type I and elastin. In the current study, using human keratinocytes and fibroblasts exposed to specific LED-BL radiation doses (45 and 15 J/cm
2 ), we produced an in vitro model of skin photoaging. We verified that, compared with untreated controls, the treatment with LED-BL irradiation results in the alteration of metalloprotease-1 (collagenase), metalloprotease-12 (elastase), 8-dihydroxy-2'-deoxyguanosine, proliferating cell nuclear antigen, and collagen type I. Moreover, we showed that the photoaging prevention is possible via the use of hydroxytyrosol extracted from olive fruits, well known for antioxidant properties. Our results demonstrated that hydroxytyrosol protects keratinocytes and fibroblasts from LED-BL-induced damage. Thus, hydroxytyrosol might be proposed as an encouraging candidate for the prevention of BL-induced premature photoaging., (© 2018 Wiley Periodicals, Inc.)- Published
- 2019
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181. A Randomized, Double-Blinded, Clinical Trial on Effects of a Vitis vinifera Extract on Cognitive Function in Healthy Older Adults.
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Calapai G, Bonina F, Bonina A, Rizza L, Mannucci C, Arcoraci V, Laganà G, Alibrandi A, Pollicino C, Inferrera S, and Alecci U
- Abstract
Introduction: Gradual population aging is creating a new set of needs in the general population. Memory capacity decreases with age, and memory deficits are considered an early symptom of Alzheimer's Disease (AD), one of the most prevalent cognitive disorders in older people. Numerous studies have shown that grape polyphenolic compounds (GPs) are able to attenuate cognitive impairment and reduce brain lesions in experimental AD animal models. These GP effects are associated with improvement in brain antioxidant status and prevention of free radical-induced neuronal damage. We designed a randomized, double-blind, placebo-controlled clinical trial to investigate the potential beneficial effects of a Vitis vinifera- based dietary supplement on cognitive function and neuropsychological status in healthy older adults. Methods: One-hundred eleven subjects were recruited and randomly divided in two groups: one group received the V. vinifera- based dietary supplement Cognigrape
® for 12 weeks (250 mg/day) and the second group received placebo over the same period of time. Before and after the end of the supplementation period, cognitive function and neuropsychological status were evaluated using the Mini-Mental State Examination (MMSE), Beck Depression Inventory (BDI), Hamilton Anxiety Rating Scale (HARS), and Repeatable Battery for the Assessment of Neuropsychological Status (RBANS) evaluations. Results: MMSE scores were significantly improved after supplementation with Cognigrape® in comparison with baseline levels ( p < 0.0001) and placebo ( r = 0.59, 0.95% CI 0.11, 1.22; p < 0.0001). Cognigrape® supplementation produced a significant reduction in BDI (-15.8%) and HARS (-24.9%) scores with respect to baseline levels ( p < 0.0001) and placebo ( p < 0.0001 for BDI and p < 0.05 for HARS). RBANS total score was significantly improved by Cognigrape® with respect to baseline levels and placebo ( r = 0.55, 0.95% CI 0.48, 6.07; p < 0.0001). The comparison with the placebo revealed improvements in several parameters among participants receiving Cognigrape® : attention ( p < 0.001); language ( p < 0.05); immediate memory ( p < 0.0001); and delayed memory ( p < 0.0001). Visuospatial/constructional abilities were not modified. During the study, no adverse effects were detected. Conclusion: The results show that 12 weeks of Cognigrape® supplementation is safe, can improve physiological cognitive profiles, and can concurrently ameliorate negative neuropsychological status in healthy older adults.- Published
- 2017
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182. Modern drug delivery strategies applied to natural active compounds.
- Author
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Puglia C, Lauro MR, Tirendi GG, Fassari GE, Carbone C, Bonina F, and Puglisi G
- Subjects
- Biological Availability, Drug Carriers chemistry, Humans, Nanoparticles, Pharmaceutical Preparations administration & dosage, Solubility, Biological Products administration & dosage, Drug Delivery Systems, Nanotechnology
- Abstract
Introduction: Colloidal drug delivery systems (CDDSs) are innovative carriers that have been studied in pharmaceutical field from many years to overcome unfavorable physical and chemical features of synthetic drugs. Recently the use of CDDS as carriers for phytochemicals has seen an exponential increase which, in some cases, has led to the rediscovery of ancient and forgotten natural molecules. Area covered: This article focuses on the main features of CDDS, particularly micro- and nanoemulsions, vesicular carriers and micro- and nanoparticles, loaded with natural active compounds. A detailed review of the literature is presented, introducing the importance of these systems in terms of their capability to optimize the stability of phytochemicals, their absorption through biological membranes and their bioavailability. Expert opinion: The delivery of phytochemicals is problematic due to poor solubility, poor permeability, low bioavailability, instability in biological milieu and extensive first-pass metabolism. Global research efforts investigating nanotechnology have attempted to overcome these limitations rediscovering and, in some cases, 'discovering ex novo' unexpected virtues and benefits associated to these compounds. The 'nanotechnological approach' can definitely enhance the pharmacokinetics and therapeutic index of natural active compounds and improve their performance in therapy.
- Published
- 2017
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183. Nanostructured Lipid Carriers (NLC) as Vehicles for Topical Administration of Sesamol: In Vitro Percutaneous Absorption Study and Evaluation of Antioxidant Activity.
- Author
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Puglia C, Lauro MR, Offerta A, Crascì L, Micicchè L, Panico AM, Bonina F, and Puglisi G
- Subjects
- Administration, Topical, Adult, Antioxidants pharmacology, Benzodioxoles chemistry, Benzodioxoles pharmacology, Humans, In Vitro Techniques, Lipids, Molecular Structure, Particle Size, Phenols chemistry, Phenols pharmacology, Skin Absorption, Antioxidants administration & dosage, Benzodioxoles administration & dosage, Nanostructures, Pharmaceutical Vehicles, Phenols administration & dosage
- Abstract
Sesamol is a natural phenolic compound extracted from Sesamum indicum seed oil. Sesamol is endowed with several beneficial effects, but its use as a topical agent is strongly compromised by unfavorable chemical-physical properties. Therefore, to improve its characteristics, the aim of the present work was the formulation of nanostructured lipid carriers as drug delivery systems for topical administration of sesamol.Two different nanostructured lipid carrier systems have been produced based on the same solid lipid (Compritol® 888 ATO) but in a mixture with two different kinds of oil phase such as Miglyol® 812 (nanostructured lipid carrier-M) and sesame oil (nanostructured lipid carrier-PLUS). Morphology and dimensional distribution of nanostructured lipid carriers have been characterized by differential scanning calorimetry and photon correlation spectroscopy, respectively. The release pattern of sesamol from nanostructured lipid carriers was evaluated in vitro determining drug percutaneous absorption through excised human skin. Furthermore, an oxygen radical absorbance capacity assay was used to determine their antioxidant activity.From the results obtained, the method used to formulate nanostructured lipid carriers led to a homogeneous dispersion of particles in a nanometric range. Sesamol has been encapsulated efficiently in both nanostructured lipid carriers, with higher encapsulation efficiency values (> 90 %) when sesame oil was used as the oil phase (nanostructured lipid carrier-PLUS). In vitro evidences show that nanostructured lipid carrier dispersions were able to control the rate of sesamol diffusion through the skin, with respect to the reference formulations.Furthermore, the oxygen radical absorbance capacity assay pointed out an interesting and prolonged antioxidant activity of sesamol, especially when vehiculated by nanostructured lipid carrier-PLUS., (Georg Thieme Verlag KG Stuttgart · New York.)
- Published
- 2017
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184. The polysaccharide and low molecular weight components of Opuntia ficus indica cladodes: Structure and skin repairing properties.
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Di Lorenzo F, Silipo A, Molinaro A, Parrilli M, Schiraldi C, D'Agostino A, Izzo E, Rizza L, Bonina A, Bonina F, and Lanzetta R
- Subjects
- Humans, Molecular Weight, Keratinocytes drug effects, Opuntia chemistry, Polysaccharides chemistry, Wound Healing drug effects
- Abstract
The Opuntia ficus-indica multiple properties are reflected in the increasing interest of chemists in the identification of its natural components having pharmaceutical and/or cosmetical applications. Here we report the structural elucidation of Opuntia ficus-indica mucilage that highlighted the presence of components differing for their chemical nature and the molecular weight distribution. The high molecular weight components were identified as a linear galactan polymer and a highly branched xyloarabinan. The low molecular weight components were identified as lactic acid, D-mannitol, piscidic, eucomic and 2-hydroxy-4-(4'-hydroxyphenyl)-butanoic acids. A wound healing assay was performed in order to test the cicatrizing properties of the various components, highlighting the ability of these latter to fasten dermal regeneration using a simplified in vitro cellular model based on a scratched keratinocytes monolayer. The results showed that the whole Opuntia mucilage and the low molecular weight components are active in the wound repair., (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Published
- 2017
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185. Regio- and Stereoselective Aliphatic-Aromatic Cross-Benzoin Reaction: Enzymatic Divergent Catalysis.
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Beigi M, Gauchenova E, Walter L, Waltzer S, Bonina F, Stillger T, Rother D, Pohl M, and Müller M
- Subjects
- Acetone chemical synthesis, Acetone chemistry, Aldehyde-Lyases chemistry, Aldehydes chemistry, Benzoin chemistry, Biocatalysis, Carboxy-Lyases chemistry, Hydroxypropiophenone chemistry, Stereoisomerism, Thiamine Pyrophosphate chemistry, Acetobacter enzymology, Acetone analogs & derivatives, Chemistry Techniques, Synthetic methods, Hydroxypropiophenone chemical synthesis, Lactococcus lactis enzymology, Pseudomonas fluorescens enzymology, Pseudomonas putida enzymology
- Abstract
The catalytic asymmetric synthesis of chiral 2-hydroxy ketones by using different thiamine diphosphate dependent enzymes, namely benzaldehyde lyase from Pseudomonas fluorescens (PfBAL), a variant of benzoylformate decarboxylase from Pseudomonas putida (PpBFD-L461A), branched-chain 2-keto acid decarboxylase from Lactococcus lactis (LlKdcA) and a variant of pyruvate decarboxylase from Acetobacter pasteurianus (ApPDC-E469G), was studied. Starting with the same set of substrates, substituted benzaldehydes in combination with different aliphatic aldehydes, PfBAL and PpBFD-L461A selectively deliver the (R)- and (S)-2-hydroxy-propiophenone derivatives, respectively. The (R)- and (S)-phenylacetylcarbinol (1-hydroxy-1-phenylacetone) derivatives are accessible in a similar way using LlKdcA and ApPDC-E469G, respectively. In many cases excellent stereochemical purities (>98 % enantiomeric excess) could be achieved. Hence, the regio- and stereochemistry of the product in the asymmetric aliphatic-aromatic cross-benzoin reaction can be controlled solely by choice of the appropriate enzyme or enzyme variant., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2016
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186. In vitro Percutaneous Absorption of Niacinamide and Phytosterols and in vivo Evaluation of their Effect on Skin Barrier Recovery.
- Author
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Offerta A, Bonina F, Gasparri F, Zanardi A, Micicche L, and Puglia C
- Subjects
- Administration, Topical, Adult, Chemistry, Pharmaceutical methods, Drug Carriers chemistry, Epidermis metabolism, Female, Humans, Lecithins chemistry, Lipids chemistry, Male, Nanoparticles chemistry, Nicotinic Acids chemistry, Permeability, Niacinamide chemistry, Niacinamide metabolism, Phytosterols chemistry, Phytosterols metabolism, Skin metabolism, Skin Absorption
- Abstract
In this study, we evaluated different strategies to optimize the percutaneous absorption of niacinamide (NA) and soy phytosterols (FITO) by making use of solid lipid nanoparticles (SLN) and penetration enhancers, such as the hydrogenated lecithin. The evaluation of the skin permeation of NA and FITO has been effected in vitro using excised human skin (i.e., stratum corneum-epidermis or SCE). Furthermore, we evaluated the in vivo effect that NA and FITO has on skin barrier recovery after the topical application; using the extent of methyl nicotinate (MN)-induced erythema in damaged skin as a parameter to determine the rate of stratum corneum recovery. Results pointed out the importance of these strategies as valid tools for NA and FITO topical delivery. In fact, soy lecithin based formulations were able to increase the percutaneous absorption of the two active ingredients, while SLN guaranteed an interesting delayed and sustained release of FITO. In vivo evaluation showed clearly that the formulation containing both the actives (NA and FITO) is able to recover about 95% of skin barrier integrity eight days after tape stripping. This effect is probably due to the "synergistic effect" of NA and FITO.
- Published
- 2016
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187. Design of solid lipid nanoparticles for caffeine topical administration.
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Puglia C, Offerta A, Tirendi GG, Tarico MS, Curreri S, Bonina F, and Perrotta RE
- Subjects
- Administration, Topical, Adult, Algorithms, Caffeine chemistry, Central Nervous System Stimulants chemistry, Drug Carriers, Drug Delivery Systems, Drug Design, Humans, In Vitro Techniques, Particle Size, Skin Absorption, Caffeine administration & dosage, Caffeine pharmacokinetics, Central Nervous System Stimulants administration & dosage, Central Nervous System Stimulants pharmacokinetics, Lipids chemistry, Nanoparticles chemistry
- Abstract
Context: Solid lipid nanoparticles (SLN) are drug carriers possessing numerous features useful for topical application. A copious scientific literature outlined their ability as potential delivery systems for lipophilic drugs, while the entrapment of a hydrophilic drug inside the hydrophobic matrix of SLN is often difficult to obtain., Objective: To develop SLN intended for loading caffeine (SLN-CAF) and to evaluate the permeation profile of this substance through the skin once released from the lipid nanocarriers. Caffeine is an interesting compound showing anticancer and protective effects upon topical administration, although its penetration through the skin is compromised by its hydrophilicity., Materials and Methods: SLN-CAF were formulated by using a modification of the quasi-emulsion solvent diffusion technique (QESD) and characterized by PCS and DSC analyses. In vitro percutaneous absorption studies were effected using excised human skin membranes (i.e. Stratum Corneum Epidermis or SCE)., Results: SLN-CAF were in a nanometric range (182.6 ± 8.4 nm) and showed an interesting payload value (75% ± 1.1). DSC studies suggest the presence of a well-defined system and the successful drug incorporation. Furthermore, SLN-CAF generated a significantly faster permeation than a control formulation over 24 h of monitoring., Discussion and Conclusions: SLN-CAF were characterized by valid dimensions and a good encapsulation efficiency, although the active to incorporate showed a hydrophilic character. This result confirms the suitability of the formulation strategy employed in the present work. Furthermore, the in vitro evidence outline the key role of lipid nanoparticles in enhancing caffeine permeation through the skin.
- Published
- 2016
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188. A Citrus bergamia Extract Decreases Adipogenesis and Increases Lipolysis by Modulating PPAR Levels in Mesenchymal Stem Cells from Human Adipose Tissue.
- Author
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Lo Furno D, Graziano AC, Avola R, Giuffrida R, Perciavalle V, Bonina F, Mannino G, and Cardile V
- Abstract
The aim of this research was to assess the impact of a well-characterized extract from Citrus bergamia juice on adipogenesis and/or lipolysis using mesenchymal stem cells from human adipose tissue as a cell model. To evaluate the effects on adipogenesis, some cell cultures were treated with adipogenic medium plus 10 or 100 μg/mL of extract. To determine the properties on lipolysis, additional mesenchymal stem cells were cultured with adipogenic medium for 14 days and after this time added with Citrus bergamia for further 14 days. To verify adipogenic differentiation, oil red O staining at 7, 14, 21, and 28 days was performed. Moreover, the expression of peroxisome proliferator-activated receptor gamma (PPAR-γ), adipocytes fatty acid-binding protein (A-FABP), adipose triglyceride lipase (ATGL), hormone-sensitive lipase (HSL), monoglyceride lipase (MGL), 5'-adenosine monophosphate-activated protein kinase (AMPK)α1/2, and pAMPKα1/2 was evaluated by Western blot analysis and the release of glycerol by colorimetric assay. Citrus bergamia extract suppressed the accumulation of intracellular lipids in mesenchymal stem cells during adipogenic differentiation and promoted lipolysis by repressing the expression of adipogenic genes and activating lipolytic genes. Citrus bergamia extract could be a useful natural product for improving adipose mobilization in obesity-related disorders.
- Published
- 2016
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189. Efficacy and Safety of a Natural Remedy for the Treatment of Gastroesophageal Reflux: A Double-Blinded Randomized-Controlled Study.
- Author
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Alecci U, Bonina F, Bonina A, Rizza L, Inferrera S, Mannucci C, and Calapai G
- Abstract
Gastroesophageal reflux (GER) is a common, chronic, relapsing symptom. Often people self-diagnose and self-treat it even though health-related quality of life is significantly impaired. In the lack of a valid alternative approach, current treatments focus on suppression of gastric acid secretion by the use of proton pump inhibitors (PPIs), but people with GER have a significantly lower response rate to therapy. We designed a randomized double-blinded controlled clinical study to evaluate the efficacy and the safety of a formulation based on sodium alginate/bicarbonate in combination with extracts obtained from Opuntia ficus-indica and Olea europaea associated with polyphenols (Mucosave®; verum ), on GER-related symptoms. Male/female 118 (intention to treat) subjects with moderate GER and having at least 2 to 6 days of GER episodes/week were treated with verum (6 g/day) or placebo for two months. The questionnaires Gastroesophageal Reflux Disease-Health-Related Quality of Life (GERD-HRQoL) and Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) were self-administered by participants before the treatment and at the end of the treatment. Verum produced statistically significant reduction of GERD-HRQoL and GSAS scores, -56.5% and -59.1%, respectively, in comparison to placebo. Heartburn and acid regurgitation episodes for week were significantly reduced by verum ( p < 0.01). Results indicate that Mucosave formulation provides an effective and well-tolerated treatment for reducing the frequency and intensity of symptoms associated with gastroesophageal reflux.
- Published
- 2016
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190. Lipid nanocarriers (LNC) and their applications in ocular drug delivery.
- Author
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Puglia C, Offerta A, Carbone C, Bonina F, Pignatello R, and Puglisi G
- Subjects
- Animals, Eye Diseases drug therapy, Eye Diseases genetics, Humans, Drug Carriers chemistry, Eye metabolism, Lipids chemistry, Nanomedicine methods, Nanostructures
- Abstract
The peculiar physio-anatomical structure of the eye and the poor physico-chemical properties of many drug molecules are often responsible for the inefficient treatment of ocular diseases by conventional dosage forms, and justify the development of innovative ocular drug delivery systems. Lipid-based nanocarriers (LNC) are among the newer and interesting colloidal drug delivery systems; they show the capability to improve the local bioavailability of drugs administered by various ocular routes and, therefore, their therapeutic efficacy. Furthermore, their extreme biodegradability and biocompatible chemical nature have secured them the title of 'nanosafe carriers.' This review treats the main features of LNC [namely, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and lipid-drug conjugates (LDC)]; examples and advantages of the application of these colloidal carrier systems for the ophthalmic administration of drugs are presented.
- Published
- 2015
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191. Evaluation of nanostructured lipid carriers (NLC) and nanoemulsions as carriers for UV-filters: characterization, in vitro penetration and photostability studies.
- Author
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Puglia C, Damiani E, Offerta A, Rizza L, Tirendi GG, Tarico MS, Curreri S, Bonina F, and Perrotta RE
- Subjects
- Chemistry, Pharmaceutical methods, Drug Stability, Humans, Particle Size, Permeability, Skin metabolism, Skin Absorption physiology, Drug Carriers chemistry, Lipids chemistry, Nanostructures chemistry, Sunscreening Agents chemistry, Sunscreening Agents pharmacology, Ultraviolet Rays adverse effects
- Abstract
The increased awareness of protection against UV radiation damages has led to a rise in the use of topically applied chemical sunscreen agents and to an increased need of innovative carriers designed to achieve the highest protective effect and reduce the toxicological risk resulting from the percutaneous absorption of these substances. In this paper, nanostructured lipid carriers (NLC) and nanoemulsions (NE) were formulated to optimize the topical application of different and widespread UVA or UVB sun filters (ethyl hexyltriazone (EHT), diethylamino hydroxybenzoyl hexyl benzoate (DHHB), bemotrizinol (Tinosorb S), octylmethoxycinnamate (OMC) and avobenzone (AVO)). The preparation and stability parameters of these nanocarriers have been investigated concerning particle size and zeta potential. The release pattern of the sunscreens from NLC and NE was evaluated in vitro, determining their percutaneous absorption through excised human skin. Additional in vitro studies were performed in order to evaluate, after UVA radiation treatment, the spectral stability of the sunfilters once formulated in NLC or NE. From the results obtained, when incorporated in NLC, the skin permeation abilities of the sun filter were drastically reduced, remaining mainly on the surface of the skin. The photostability studies showed that EHT, DHHB and Tinosorb S still retain their photostability when incorporated in these carriers, while OMC and AVO were not photostable as expected. However, no significant differences in terms of photoprotective efficacy between the two carriers were observed., (Copyright © 2013 Elsevier B.V. All rights reserved.)
- Published
- 2014
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192. Optimization of curcumin loaded lipid nanoparticles formulated using high shear homogenization (HSH) and ultrasonication (US) methods.
- Author
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Puglia C, Offerta A, Rizza L, Zingale G, Bonina F, and Ronsisvalle S
- Subjects
- Calorimetry, Differential Scanning, Curcumin chemistry, Lipids chemistry, Nanoparticles, Ultrasonics
- Abstract
Lipid nanoparticles (LN) are drug carriers possessing advantages with respect to stability, drug release profile, and biocompatibility. There are several production methods for lipid nanoparticles. Recently high shear homogenization (HSH) and ultrasound (US) techniques have been used to produce these systems in a cheaper and easier way. The objective of the present study was to evaluate the effect of same important instrumental parameters, such as homogenization time (HT) and ultrasonication time (UT), on particle size (MD) and polydispersity index (PDI) of LNs obtained by HSH-US techniques. Curcumin was used as a model drug to be incapsulated in the LNs. LN were prepared by HSH-US technique using tripalmitin (Dynasan 116) and poloxamer 188 (Lutrol F68) as solid lipid and surfactant, respectively. The preparations were characterized and then evaluated using a factorial design study. From the results obtained, LNs produced by HSH-US method were characterized by nanodimension, high homogeneity and encapsulation efficiency. US technology plays an important role in controlling the final dimension of LN dispersion, while longer times of HSH seem mainly to exert a positive effect on the final homogeneity of particle dispersion. Additional studies are in progress to evaluate drug release profile from LNs, for further in vitro/in vivo correlation studies.
- Published
- 2013
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193. Formulation strategies to modulate the topical delivery of anti-inflammatory compounds.
- Author
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Puglia C, Rizza L, Offerta A, Gasparri F, Giannini V, and Bonina F
- Subjects
- Administration, Topical, Adult, Anti-Inflammatory Agents metabolism, Drug Carriers, Emulsions, Erythema drug therapy, Erythema etiology, Erythema pathology, Female, Gels, Glycyrrhetinic Acid metabolism, Glycyrrhetinic Acid pharmacology, Glycyrrhizic Acid metabolism, Humans, Hydrogenation, Male, Nanoparticles, Particle Size, Permeability, Skin drug effects, Skin metabolism, Skin pathology, Skin Absorption, Ultraviolet Rays adverse effects, Anti-Inflammatory Agents pharmacology, Glycyrrhetinic Acid analogs & derivatives, Glycyrrhizic Acid pharmacology, Lecithins metabolism
- Abstract
The aim of this study was to assess the ability of some vehicles (emulsion and emulgel), containing hydrogenated lecithin as penetration enhancer, in increasing the percutaneous absorption of the two model compounds dipotassium glycyrrhizinate (DG) and stearyl glycyrrhetinate (SG). Furthermore SG-loaded solid lipid nanoparticles (SLNs) were prepared and the effect of this vehicle on SG permeation profile was evaluated as well. Percutaneous absorption has been studied in vitro, using excised human skin membranes (i.e., stratum corneum epidermis or [SCE]), and in vivo, determining their anti-inflammatory activity. From the results obtained, the use of both penetration enhancers and SLNs resulted in being valid tools to optimize the topical delivery of DG and SG. Soy lecithin guaranteed an increase in the percutaneous absorption of the two activities and a rapid anti-inflammatory effect in in vivo experiments, whereas SLNs produced an interesting delayed and sustained release of SG.
- Published
- 2013
194. Emerging role of colloidal drug delivery systems (CDDS) in NSAID topical administration.
- Author
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Puglia C, Tirendi GG, and Bonina F
- Subjects
- Administration, Topical, Animals, Anti-Inflammatory Agents, Non-Steroidal chemistry, Colloids chemistry, Humans, Anti-Inflammatory Agents, Non-Steroidal administration & dosage, Colloids administration & dosage, Drug Delivery Systems methods
- Abstract
NSAIDs are the most commonly prescribed category of drugs for the treatment of musculoskeletal pain and inflammation associated with many conditions. Topical administration of these drugs is always the best choice since adverse effects occur commonly with systemic NSAID therapy. Colloidal drug delivery systems (CDDS) are interesting systems, which are able to improve the duration of drug residence in the skin and to allow an achievable drug sustained and controlled release compared to conventional topical formulations. This review focuses on micro and nanoemulsions, vesicular carriers and nanoparticles as novel high efficiency delivery systems of NSAIDs in topical applications.
- Published
- 2013
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195. Ceramides as possible nutraceutical compounds: characterization of the ceramides of the Moro blood orange ( Citrus sinensis ).
- Author
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Valsecchi M, Mauri L, Casellato R, Ciampa MG, Rizza L, Bonina A, Bonina F, and Sonnino S
- Subjects
- Ceramides chemistry, Chromatography, High Pressure Liquid, Mass Spectrometry, Sicily, Spectrometry, Mass, Electrospray Ionization, Ceramides analysis, Citrus sinensis chemistry, Dietary Supplements analysis, Fruit chemistry
- Abstract
Ceramides are presented as nutraceutical compounds for protection of colon carcinoma and as important cosmetic preparation components, increasing absorption through the skin. Therefore, the ceramide (Cer) content of Moro blood oranges was determined by mass spectrometry. A total of 114 Cer species were identified: ∼160 mg in the peels and ∼140 mg in the pulp per kilogram of oranges, expressed as "milligram equivalents of d18:1,17:0 Cer". The predominant ceramides contained 4-hydroxy-8-sphingenine (t18:1(Δ8)) and 4-hydroxysphinganine (t18:0) as long-chain bases (LCBs) and fatty acids (FAs) with different structures. In the pulp, t18:1(Δ8)- and t18:0-containing Cer species comprised 50.5 and 33.5% of the total, respectively, 11.5 and 3.5% non-hydroxylated FAs, respectively, 32.0 and 21.0% α-hydroxylated FAs, respectively, and 7.0 and 9.0% α,β-hydroxylated FAs, respectively. In the peels, t18:1(Δ8)- and t18:0-containing species comprised 49.5 and 34.5% of the total, respectively, 16.0 and 1.5% non-hydroxylated FAs, respectively, 31.5 and 29.0% α-hydroxylated FAs, respectively, and 2.0 and 4.0% α,β-hydroxylated FAs, respectively.
- Published
- 2012
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196. Protective effects of an extract from Citrus bergamia against inflammatory injury in interferon-γ and histamine exposed human keratinocytes.
- Author
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Graziano AC, Cardile V, Crascì L, Caggia S, Dugo P, Bonina F, and Panico A
- Subjects
- Cell Survival drug effects, Cell Survival physiology, Cells, Cultured, Cytoprotection physiology, Humans, Inflammation chemically induced, Inflammation metabolism, Inflammation prevention & control, Interferon-gamma drug effects, Keratinocytes metabolism, Keratinocytes pathology, Plant Extracts isolation & purification, Plant Extracts therapeutic use, Citrus physiology, Cytoprotection drug effects, Histamine toxicity, Interferon-gamma toxicity, Keratinocytes drug effects, Plant Extracts pharmacology
- Abstract
Aims: The present work evaluated the anti-inflammatory/antioxidant activity of a well characterized extract from Citrus bergamia Risso and Poiteau (CBE), containing neoeriocitrin, naringin, neohesperidin and other flavonoids, on human NCTC 2544 keratinocytes treated with interferon-gamma (IFN-γ) and histamine (H)., Main Methods: High performance liquid chromatography (HPLC) coupled with diode array detectors was used to characterize and quantify phenolic compounds in CBE. Anti-inflammatory/antioxidant ability on keratinocytes was determined through evaluation of inter-cellular adhesion molecule-1 (ICAM-1) and inducible nitric oxide synthase (iNOS) expression by Western blot, production of nitric oxide (NO) with Griess reagent and concentration of reactive oxygen species (ROS) by fluorescent quantitative analysis with 2',7'-dichlorfluorescein-diacetate (DCFH-DA). Cell viability was assessed using 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Antioxidant activity was also measured by oxygen radical absorbance capacity (ORAC) assay. Glycosaminoglycans (GAGs) were quantified using 1.9-dimethyl methylene blue (DMB)., Key Findings: CBE exhibited high antioxidant activity confirmed by elevated ORAC values related to high capacity in oxygen radical scavenging. The assays on keratinocytes demonstrated that CBE does not inhibit cell proliferation and is shown to significantly reduce dose-dependently ICAM-1, iNOS, NO, ROS and GAG production in cells exposed to IFN-γ and H., Significance: Our study demonstrates that the pools of compounds of an extract from C. bergamia efficiently block the proinflammatory actions induced by IFN-γ and H on human keratinocytes. CBE may be used for topic employment in some inflammatory diseases of the skin and to represent an important opportunity for the essential oil processing industries., (Copyright © 2012 Elsevier Inc. All rights reserved.)
- Published
- 2012
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197. Curcumin loaded NLC induces histone hypoacetylation in the CNS after intraperitoneal administration in mice.
- Author
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Puglia C, Frasca G, Musumeci T, Rizza L, Puglisi G, Bonina F, and Chiechio S
- Subjects
- Acetylation, Animals, Biological Availability, Central Nervous System metabolism, Chemistry, Pharmaceutical methods, Drug Carriers administration & dosage, Drug Stability, Histone Acetyltransferases antagonists & inhibitors, Injections, Intraperitoneal, Lipids administration & dosage, Male, Mice, Nanostructures administration & dosage, Particle Size, Central Nervous System drug effects, Curcumin administration & dosage, Curcumin chemistry, Drug Carriers chemistry, Histones metabolism, Lipids chemistry, Nanostructures chemistry
- Abstract
The natural p300-specific histone acetyltransferase (HAT) inhibitor, curcumin (CUR), has been widely investigated for its potential therapeutic effect as an anticancer and anti-inflammatory agent. Notwithstanding this interesting pharmacological profile, CUR shows some drawbacks, such as poor absorption and a very fast metabolism and elimination, that limit its clinical use. Aim of the present study was to formulate CUR loaded nanostructured lipid carriers (NLC-CUR) in order to improve the bioavailability and stability of this compound after systemic administration with increased effects in the central nervous system (CNS). NLC-CUR were prepared and characterized on their physicochemical properties by PCS and DSC analyses. Thus, NLC-CUR were systemically injected and the effects in the CNS were compared with a CUR control formulation containing 0.05% DMSO (DMSO-CUR). Our results demonstrate that CUR is able to decrease histone acetylation in the CNS when included in NLCs. Western blot analysis shows that intraperitoneal injection of NLC-CUR (100mg/kg) in mice induces a marked hypoacetylation of histone 4 (H4) at lysine 12 (K12) in the spinal cord compared with control group. Notably, DMSO-CUR (100mg/kg) did not change the H4K12 acetylation level in the CNS. Our study suggests a novel approach to ameliorate the pharmacokinetics of CUR that allows a better permeation in the CNS., (Copyright © 2012 Elsevier B.V. All rights reserved.)
- Published
- 2012
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198. On the assessment of photostability of sunscreens exposed to UVA irradiation: from glass plates to pig/human skin, which is best?
- Author
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Crovara Pescia A, Astolfi P, Puglia C, Bonina F, Perrotta R, Herzog B, and Damiani E
- Subjects
- Adult, Animals, Chemistry, Pharmaceutical methods, Drug Stability, Ear, Epidermis chemistry, Epidermis radiation effects, Female, Glass, Humans, In Vitro Techniques, Kinetics, Lipid Peroxidation, Swine, Thiobarbituric Acid Reactive Substances analysis, Skin chemistry, Sunscreening Agents chemistry, Sunscreening Agents radiation effects, Ultraviolet Rays
- Abstract
Photostability of suncare products is a great area of interest since several sunscreens on the market are photounstable, and this is primarily a problem concerning the UVA region (320-400 nm). Here we report a comparative study on the photostability assessment of two commercial sunscreens with same SPF, spread onto glass plates or onto full thickness pig ear skin or human/pig SCE membranes, and exposed to 183 kJ/m(2) UVA. Absorbance spectra and lipid peroxidation (measured by TBARS production) were determined. The results indicate: (a) sunscreen performance consequent to UVA exposure is independent of whether it is spread onto a non-biological and chemically inert substrate such as glass, or on biological substrates such as skin/SCE membranes; (b) despite the same SPF, sunscreen performance and photostability can be very different; (c) the data on human SCE membranes are similar to those on pig SCE membranes, indicating the suitability of the latter as a model for human skin. However, since the results obtained using skin membranes, akin to the more realistic conditions of use in vivo, do not substantially differ from those obtained on glass plates, the method proposed here using the latter may be applied for rapid, inexpensive, efficacy screening of photostability of sunscreens. Photostability testing should be a mandatory requirement for safer sunscreen protection products, since the results clearly show that some are still far from perfect., (Copyright © 2012 Elsevier B.V. All rights reserved.)
- Published
- 2012
- Full Text
- View/download PDF
199. Lipid nanoparticles as novel delivery systems for cosmetics and dermal pharmaceuticals.
- Author
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Puglia C and Bonina F
- Subjects
- Acne Vulgaris drug therapy, Administration, Cutaneous, Administration, Topical, Anti-Inflammatory Agents, Non-Steroidal administration & dosage, Antifungal Agents administration & dosage, Cosmetics chemistry, Cosmetics radiation effects, Dermatitis, Atopic drug therapy, Dermatologic Agents chemistry, Dermatologic Agents pharmacokinetics, Dermatologic Agents radiation effects, Drug Stability, Emulsions, Excipients, Humans, Light, Lipids chemistry, Lipids pharmacokinetics, Lipids radiation effects, Mycoses drug therapy, Nanoparticles chemistry, Nanoparticles radiation effects, Psoriasis drug therapy, Skin metabolism, Cosmetics administration & dosage, Dermatologic Agents administration & dosage, Drug Carriers chemistry, Lipids administration & dosage, Nanoparticles administration & dosage, Skin Diseases drug therapy
- Abstract
Introduction: Lipid nanoparticles are innovative carrier systems developed as an alternative to traditional vehicles such as emulsions, liposomes and polymeric nanoparticles. Solid lipid nanoparticles (SLN) and the newest nanostructured lipid carriers (NLC) show important advantages for dermal application of cosmetics and pharmaceuticals., Area Covered: This article focuses on the main features of lipid nanoparticles, in terms of their preparation and recent advancements. A detailed review of the literature is presented, introducing the importance of these systems in the topical delivery of drugs and active substances., Expert Opinion: Lipid nanoparticles are able to enhance drug penetration into the skin, allowing increased targeting to the epidermis and consequently increasing treatment efficiency and reducing the systemic absorption of drugs and cosmetic actives. The complete biodegradation of lipid nanoparticles and their biocompatible chemical nature have secured them the title of 'nanosafe carriers.' SLN and NLC represent a new technological era, which has been taken over by the cosmetic and pharmaceutical industry, which will open new channels for effective topical delivery of substances.
- Published
- 2012
- Full Text
- View/download PDF
200. Lipid nanoparticles as carrier for octyl-methoxycinnamate: in vitro percutaneous absorption and photostability studies.
- Author
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Puglia C, Bonina F, Rizza L, Blasi P, Schoubben A, Perrotta R, Tarico MS, and Damiani E
- Subjects
- Adult, Calorimetry, Differential Scanning methods, Chemistry, Pharmaceutical methods, Drug Stability, Emulsions chemistry, Humans, Oils chemistry, Particle Size, Permeability, Photochemical Processes, Skin drug effects, Skin Absorption, Cinnamates chemistry, Drug Carriers chemistry, Lipids chemistry, Nanoparticles chemistry, Nanostructures chemistry
- Abstract
The aim of the present study was the evaluation of lipid nanoparticles (solid lipid nanoparticles, SLN, and nanostructured lipid carriers, NLC) as potential carriers for octyl-methoxycinnamate (OMC). The release pattern of OMC from SLN and NLC was evaluated in vitro, determining its percutaneous absorption through excised human skin. Additional in vitro studies were performed in order to evaluate, after UVA radiation treatment, the spectral stability of OMC-loaded lipid nanoparticles. From the obtained results, ultrasonication method yielded both SLN and NLC in the nanometer range with a high active loading and a particle shape close to spherical. Differential scanning calorimetry data pointed out the key role of the inner oil phase of NLC in stabilizing the particle architecture and in increasing the solubility of OMC as compared with SLN. In vitro results showed that OMC, when incorporated in viscosized NLC dispersions (OMC-NLC), exhibited a lower flux with respect to viscosized SLN dispersions (OMC-SLN) and two reference formulations: a microemulsion (OMC-ME) and a hydroalcoholic gel (OMC-GEL). Photostability studies revealed that viscosized NLC dispersions were the most efficient at preserving OMC from ultraviolet-mediated photodegradation., (Copyright © 2011 Wiley-Liss, Inc.)
- Published
- 2012
- Full Text
- View/download PDF
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