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Transdermal insulin delivery is an alternative route to deliver insulin through the body skin with the challenges to overcome the low drug skin permeability and high molecular weight. Polyaniline doped with poly(4-styrenesulfonic acid) (PANI:PSS), a conductive polymer with the high electrical conductivity, was synthesized and utilized as a drug carrier to improve the drug delivery capability from a porous thermoplastic polyurethane (TPU) matrix. The insulin was electrostatically attached to PANI:PSS based on the ion exchange between insulin and PSS. For the in vitro drug release of insulin loaded PANI:PSS relative to the pristine insulin alone, the amount of insulin released was improved to 84.70% with the time to equilibrium of 2 h under the electrical field of 6 V. For the ex vivo release-skin permeation, the amount insulin released and permeated became lower at 57.02% with time to equilibrium of 2 h, due to the pig skin acting as a barrier for insulin permeation. The modified insulin transdermal delivery, with PANI:PSS as the drug carrier and drug enhancer relative to without, is shown here to influence the insulin release rate, amount, and duration, suitable to treat diabetes patients. [ABSTRACT FROM AUTHOR]

The objective of this study is to investigate the dose-response relationship between various concentrations of permeation enhancers (PEs) and their ability to enhance drug release from a polymer matrix, utilizing an innovative parameter known as release enhancement efficiency (K). Additionally, the molecular mechanism underlying dynamic enhancement was also examined. Isopropyl myristate (IPM) was used as model enhancer and zolmitriptan (ZOL) was used as model drug to investigate dose-effect relationship in pressure sensitive adhesives (PSA). The release behavior of the PEs was determined by LC-MS/MS and verified by confocal laser scanning microscopy (CLSM). The enhancing effect of the PE on ZOL release was evaluated through in vitro release experiments and further validated by pharmacokinetics study. And the molecular mechanism was characterized with thermal analysis (DSC), Fourier transform infrared spectroscopy (FT-IR) and molecular dynamics simulation. K was 0.156, 0.286 and 0.279 at 3%, 6% and 9% IPM concentrations, indicating that the enhancement efficiency reached the maximum when the 6% IPM was applied. According to the mechanism research results, the fluidity of PSA increased linearly with the increase of IPM concentrations, but the interaction between IPM and ZOL reached its strongest point at 6%. In summary, the increase of K value (from 0 to 6% IPM content) was caused by the synergy of increased mobility of PSA and interaction (dipole-dipole and hydrogen-bond) among three components, and when the above two actions were in antagonistic, K no longer increased (6–9% IPM content). [ABSTRACT FROM AUTHOR]

Heart valve disorders (HVD) caused by medical complications like calcification, thrombosis and infective endocarditis are a reason for cardiac dysfunctionality. The main aim of the present study was to develop a 3D polymeric antibacterial heart valve to prevent endocarditis and infection at the surgical site, through heart valve tissue engineering (HVTE), as a novel approach for the treatment of HVD. In this regard, using a 3D printed designed mold, a scaffold of poly glycerol sebacate: polycaprolactone: gelatin (50:40:10) containing ciprofloxacin, a broad-spectrum antibacterial drug, was made using melt molding method (D1 scaffold). Then, a layer of PGS-gelatin was coated on the optimized scaffold using a dip coating and EDC-NHS cross-linking agent (D2 scaffold). Based on the results, the D1 presented a 21.17 ± 0.8° contact angle while in D2 it was 37.49 ± 1.3°. The calcification rate also showed a lower amount of calcium and phosphorus deposition on the cross-linked surface of D2 (6.12 ± 0.35 µg mg−1) compared with D1 (14.2 ± 1.27 µg mg−1). D2 also demonstrated a remarkable antibacterial activity which was effective against Gram-negative and Gram-positive bacteria. The in vitro release profile showed that D2 can release ciprofloxacin gradually and continuously for over 140 h. The D2 showed a non-thrombogenic interface based on blood compatibility testing. Cell study results assessed by the Alamar Blue, Calcein-AM, and Hoechst stain assay, revealed that the human cardiac fibroblasts grew well on D2 compared to D1. The results of the present study support the main idea of ​​creating an antibacterial and biocompatible 3D biomimetic heart valve for HVTE. [ABSTRACT FROM AUTHOR]

Objectives: This study aims to prepare a topical cubosomal formulation that contains 5-Fluorouracil (5-FU), a hydrophilic anti-cancer drug, that belongs to the Biopharmaceutics Classification System (BCS-III) i.e., high solubility and low permeability. Materials and Methods: The 5-FU loaded cubosomes were prepared using Glyceryl Monooleate (GMO) as a lipid polymer, in the presence of Poloxamer 407 (Polox-407) and Tween 80 (T80) as stabilizers. Four formulations of cubosomes were formulated by varying concentrations of Polox-407 and GMO while keeping the concentration of T80 constant. A melting, followed by homogenization technique has been used for the preparation of 5-FU cubosomes. Several In vitro characterization experiments, chemical compatibility studies, pH, viscosity, Scanning Electron Microscopy (SEM), particle size analysis, zeta potential, in vitro drug release studies, in vitro permeation study, and stability studies were performed. Results: The compatibility studies have confirmed the chemical compatibility of the drug and ingredients, while stability analysis has assured that the prepared formulations were stable. Particle size analysis and surface morphology showed that particles were nano-sized with suitable cubical shapes, well segregated from each other. The zeta potential was -0.6 mV and viscosity has been recorded as 18 cP. The drug release and permeation studies revealed that the cumulative amount of the drug was 95% and 94% respectively. Conclusion: Altogether, these findings suggested that upon further optimization, this formulation may have the potential to be translated as an effective therapy for the clinical management of superficial cancers. [ABSTRACT FROM AUTHOR]

Copyright of China Plastics / Zhongguo Suliao is the property of Journal Office of CHINA PLASTICS and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Hydrogels are three‐dimensional polymeric materials with applications in various areas such as biomedicine, tissue engineering, pollutant capture systems, and so forth. However, its application is limited due to the reproducibility of its properties. Factors such as the composition of the constituents, the type of union between the polymer chains, and the crosslinking time play a crucial role in ensuring its reproducibility. In this study, the objective is to prepare a matrix with well‐defined properties that ensure controlled release processes. Treatment of Himantothallus grandifolius with Na2CO3 aqueous solution afforded in 18.9% yield alkaline extract. Hydrogels were prepared by ionic complexation of alginate from H. grandifolius, and polyguluronate enriched alginate from Desmarestia ligulata with chitosan stabilized by immersion in 0.1 M CaCl2 solution; better swelling ratio in water was found for hydrogels with low molecular weight chitosan (MW 125,000 g/mol) than those with medium molecular weight chitosan (MW450,000–500,000 g/mol). Liberation of the model drug metformin hydrochloride from alginates: chitosan complexes (3:1) at pH 1.5 was especially low for hydrogel from H. grandifolius during the first 2 h; 70% of metformin was released at pH 6.5 after 24 h. This polyelectrolyte complex constitutes a good material for potential application in biomedicine considering its cationic and anionic characteristics. [ABSTRACT FROM AUTHOR]

An object of the present study was the development of liposomes loaded with the medicine Veklury® (remdesivir) stabilized by electrostatic adsorption of polysaccharide film formed from chitosans with different physicochemical characteristics and hyaluronic acid. The functionalization of the structures was achieved through the inclusion of an aptamer (oligonucleotide sequence) with specific affinity to the spike protein of the human coronavirus HCoV-OC43. The hydrodynamic size, electrokinetic potential and stability of the structures were evaluated at each step in the procedure. The encapsulation efficiency and loaded amount of remdesivir (99% and 299 µg/mL) were estimated by UV–vis spectroscopy. Our investigations showed manifestation of promising tendencies for prolonged periods of the drug release and increased effectiveness of its antiviral action. Among all studied versions of the delivery system, the most distinguished and suitable in a model coronavirus therapy are the liposomes formed from chitosan oligosaccharides. The cytotoxicity of the liposomes was determined against the HCT-8 cell line. A cytopathic effect inhibition test was used for the assessment of the antiviral activity of the compounds. The virucidal activity and the effect on the viral adsorption of the samples were reported by the end-point dilution method, and the alteration in viral titer was determined as Δlgs compared to untreated controls. The redox-modulating properties of the nanoparticles were studied in vitro in certain/several/a few chemical model systems. Our investigations showed a manifestation of promising tendencies for a prolonged effect of the drug release and increased effectiveness of its antiviral action. [ABSTRACT FROM AUTHOR]

Type 2 diabetes mellitus (T2DM) is a long-term metabolic disease that is commonly characterized by insulin deficiency or resistance, and prevalence has been increasing gradually all over the world. The aim of this study is to produce Metformin-loaded 3D printed scaffolds for an alternative drug delivery application in the treatment of Type 2 DM with two different biopolymers. Sodium Alginate (SA)/Polyethylene glycol (PEG) scaffolds loaded with varying concentrations of Metformin (0.5 and 2 wt.%) were prepared by adding 9 wt.% of SA to 3 wt.% of PEG. The physical analyses of the solutions were examined after the production process, and as a result, no significant changes were observed in the viscosity, density, and surface tension of the solutions with the addition of Metformin. Morphological (SEM), molecular interaction (FTIR), thermal analysis (DSC), tensile strength analyses were done. SEM images and histograms showed that the desired pore structure was obtained in the scaffolds produced by the 3D printing method, and the average pore sizes were 236.14±18.999, 255.28±14.168, and 318.83±13.038 µm for SA/PEG, 0.5% and 2% Metformin-loaded scaffolds, respectively. A drug release test was performed by UV spectroscopy. Metformin from both 0.5% and 2% scaffolds showed a burst release in 30 minutes because of the high solubility of SA and PEG in water. More than 97% of the drug was released from both scaffolds. However, they displayed sustained release up to 24 hours. Therefore, Metformin-loaded 3D-printed scaffolds have promising potential for the treatment of T2DM as they are an alternative to the oral administration of the drug. [ABSTRACT FROM AUTHOR]

With biocompatibility and biodegradability, self-healing hydrogels prepared from biopolymers show great advantages in bioengineering and bioscience as drug delivery carrier. In this research, the biodegradable hydrogel was constructed based on poly(amino acid) of poly(aspartic acid) (PAsp) and pectin for in vivo antitumor applications as DOX release carrier. The PAsp bearing hydrazide groups and isopropyl groups (PAPH) was synthesized by ring opening of polysuccinimide (PSI) by isopropylamine and hydrazine, and used to fabricate fully biodegradable hydrogel with oxidized pectin (OPec) through dynamic acylhydrazone bond cross-linking. The regulatable mechanical strength of the hydrogel could adapt its bioapplication, and the excellent biocompatibility ensured biosafety in biomedical areas. Furthermore, the pectin backbone and the PAsp endowed the hydrogel with biodegradability both by enzyme and in vivo. The PAPH/Opec hydrogel as DOX carrier inhibited the tumor growth with the tumor weight 80% lower than the control group and reduced the in vivo toxicity of the DOX. As a result, this biodegradable PAPH/Opec hydrogel could find show great potential as sustained drug delivery vehicle in biomedical areas. [ABSTRACT FROM AUTHOR]

Supramolecular hydrogels as biomaterials have been widely investigated for medical applications. However, the inadequate strength and stability of supramolecular hydrogels limit their applications in dressings, stents and drug carriers. In order to improve the mechanical properties of supramolecular hydrogels, a graphene oxide-hyaluronic acid-polyethylene glycol supramolecular hydrogel (GHCAP)is successfully prepared by the host-guest interaction of cyclodextrin and adamantane functional groups, with hyaluronic acid grafted cyclodextrin and graphene oxide (GO)as the main polymers and four-arm polyethylene glycol grafted adamantane as guest polymers. The elastic modulus of GHCAP-functionalized hydrogel is significantly increased compared with that of hyaluronic acid-polyethylene glycol supramolecular hydrogel (HCAP)without graphene oxide, and the loading rate of GHCAP-functionalized hydrogel for cichoric acid drugs reached 43. 38% under the same conditions. Hence, the supramolecular hydrogels of GHCAP are expected to have wide application in the fields of medical biomaterials such as tissue dressings and drug carriers. [ABSTRACT FROM AUTHOR]

Currently, bone infections caused by diseases or injuries are a major health issue. In addition, the conventional therapeutic approaches used to treat bone diseases or injuries present several drawbacks. In the area of tissue engineering, researchers have been developing new alternative therapeutic approaches, such as scaffolds, to promote the regeneration of injured tissues. Despite the advantages of these materials, most of them require an invasive surgical procedure. To overcome these problems, the main focus of this work was to develop scaffolds for bone regeneration, which can be applied using injectable hydrogels that circumvent the use of invasive procedures, while allowing for bone regeneration. Throughout this work, injectable hydrogels were developed based on a natural polymer, dextran, along with the use of two inorganic compounds, calcium β-triphosphate and nanohydroxyapatite, that aimed to reinforce the mechanical properties of the 3D mesh. The materials were chemically characterized considering the requirements for the intended application: the swelling capacity was evaluated, the degradation rate in a simulated physiological environment was assessed, and compression tests were performed. Furthermore, vancomycin was incorporated into the polymeric matrices to obtain scaffolds with antibacterial performance, and their drug release profile was assessed. The cytotoxic profile of the hydrogels was assessed by an MTS assay, using osteoblasts as model cells. The data obtained demonstrated that dextran-based hydrogels were successfully synthesized, with a drug release profile with an initial burst between 50 and 80% of the drug. The hydrogels possess fair biocompatibility. The swelling capacity showed that the stability of the samples and their degradation profile is compatible with the average time period required for bone regeneration (usually about one month) and have a favorable Young's modulus (200–300 kPa). The obtained hydrogels are well-suited for bone regeneration applications such as infections that occur during implantation or bone graft substitutes with antibiotics. [ABSTRACT FROM AUTHOR]

Drug nanofibers play a crucial role in ameliorating therapeutic effects, reducing toxicity, and increasing the bioavailability of drugs. This study was aimed at the fabrication of isotretinoin-loaded MMT-reinforced bi-polymeric (PAN/PU) nanofibers with varying concentrations of isotretinoin. In this study, montmorillonite (MMT)-reinforced cross-linked polyacrylonitrile and pullulan nanofibers combined with varying amounts of isotretinoin were fabricated through an electrospinning approach and investigated for their drug permeation potential. PAN-PU nanofibers were successfully integrated with the isotretinoin. The incorporation of isotretinoin into the nanofibrous structure was confirmed by FTIR and XRD. TGA study indicated the stability of the fabricated nanoparticles. The SEM results showed the beaded and smooth morphology of nanofibers. Formulation with a higher drug concentration had a non-significantly (p > 0.05) higher swelling ratio. Drug-loaded polymeric nanofiber erodes at a slower rate as compared to drug-free nanofibers. The ex-vivo permeation study of nanofibers revealed that the drug was not released all at once, but rather gradually and consistently over the period of 24 h, indicating a controlled release of the drug. In addition, the drug concentration in the nanofibers affected the permeation of the drug. According to the findings, isotretinoin-loaded MMT-reinforced bi-polymeric (PAN/PU) nanofibers with varying concentrations of isotretinoin were successfully fabricated. The fabricated nanofibers (PAN/PU) showed a promising potential for controlled permeation of drugs through rabbit skin. [ABSTRACT FROM AUTHOR]

This study presents a comprehensive evaluation of novel composite biomaterials designed for dental applications, aiming to potentially address the prevalent challenge of dental and periodontal tissue loss. The composites consisted of biomimetic hydroxyapatite (mHA) enriched with Mg2+, CO32−, and Zn2+ ions, type I collagen, alginate, and, additionally, chitosan and sericin. The granules were loaded with ibuprofen sodium salt. The investigation encompassed a morphology characterization, a porosity analysis, a chemical structure assessment, and an examination of the swelling behavior, drug release kinetics (ibuprofen), and release profiles of zinc and magnesium ions. The granules exhibited irregular surfaces with an enhanced homogeneity in the chitosan-coated granules and well-developed mesoporous structures. The FT-IR spectra confirmed the presence of ibuprofen sodium, despite overlapping bands for the polymers. The granules demonstrated a high water-absorption capacity, with delayed swelling observed in the chitosan-coated granules. Ibuprofen displayed burst-release profiles, especially in the G1 and G3 samples. In the case of the chitosan-coated granules (G2 and G4), lower amounts of ibuprofen were released. In turn, there was a significant difference in the released amount of magnesium and zinc ions from the granules, which was most likely caused by their different location in the hydroxyapatite crystals. The cytotoxicity assays confirmed the non-cytotoxic behavior of the biomaterial. These findings suggest the potential applicability of these biomaterials in dental scenarios, emphasizing their multifunctional and biocompatible nature. [ABSTRACT FROM AUTHOR]

Liposomes are considered among the most versatile and advanced nanoparticle delivery systems used to target drugs to specific cells and tissues. Structurally, liposomes are sphere-like vesicles of phospholipid molecules that are surrounded by equal number of aqueous compartments. The spherical shell encapsulates an aqueous interior which contains substances such as peptides and proteins, hormones, enzymes, antibiotics, antifungal and anticancer agents. This structural property of liposomes makes it an important nano-carrier for drug delivery. Extrusion is one of the most frequently used technique for preparing monodisperse uni-lamellar liposomes as the technique is used to control vesicle size. The process involves passage of lipid suspension through polycarbonate membrane with a fixed pore size to produce vesicles with a diameter near the pore size of the membrane used in preparing them. An advantage of this technique is that there is no need to remove the organic solvent or detergent from the final preparation. This review focuses on composition of liposome formulation with special emphasis on factors affecting drug release and drug-loading. [ABSTRACT FROM AUTHOR]

Today, the disease treatment aims to increase the patient's quality of life, reduce the dose of drugs used, extend the dosing interval, and purify the patient from the side and harmful effects. Controlled drug release systems are the systems that respond best in this respect. In this study, the evaluation of the in vitro release of 5-fluorouracil for the transdermal delivery system of NaAlg/HPMC/TiO2 biocompatible membranes was investigated. The nanocomposite membrane was prepared by adding TiO2 nanoparticles to a mixture of sodium alginate and hydroxypropyl methylcellulose polymers. Membranes were analyzed by Fourier Transform Infrared, Scanning Electron Microscopy, Differential Scanning Calorimetry, X-Ray Diffraction, and Thermogravimetric analyses. In addition, water contact angles and mechanical tests of the membranes were carried out. The degree of swelling of the prepared membranes was examined; the highest swelling degree was obtained as 304.9% in pH 5.0 buffer. The effects of crosslinking time, nanoparticle amount, and temperature were investigated in the release studies of 5-FU. The highest drug release was found to be 65.3% at the end of 24 h in membranes containing 5% TiO2 and crosslinked for 1 h. The release kinetics of 5-FU were evaluated according to four kinetic models, and the release from NaAlg/HPMC/TiO2 membranes showed conformity with the Korsmeyer–Pappes model. [ABSTRACT FROM AUTHOR]

[Display omitted] • Minor structural differences of hydrophobic porphyrins can distinctly influence their release properties from liposomes. • mTHPP (meta OH) redistributes much slower than pTHPP (para OH) from liposomal membranes. • Reversed-phase HPLC experiments indicate a higher partition coefficient for mTHPP. • In MD simulations, mTHPP has a higher tendency for hydrogen bonding, a larger tilt angle and locates deeper in the membrane. • Both HPLC and MD simulation results support the observed differences in release and redistribution of mTHPP and pTHPP from liposomal membranes. The release of hydrophobic compounds from liposomal membranes occurs by partitioning and is thus determined by the physicochemical properties (e.g. logP and water solubility) of the drug. We postulate that even minor structural differences, e.g. the position of the phenolic OH-group of the hydrophobic porphyrins mTHPP and pTHPP (meta vs. para substitution), distinctly affect their partitioning and release behavior from liposomes. The release and redistribution of mTHPP and pTHPP from lecithin or POPC/POPG liposomes to different acceptor particles (DSPE-mPEG micelles and liposomes) was studied by asymmetrical flow field-flow fractionation to separate donor and acceptor particles. Reversed phase HPLC was applied to detect differences in partitioning. Molecular dynamics (MD) simulations were carried out to obtain molecular insight in the different behavior of the two compounds inside a lipid bilayer. Despite the minor differences in chemical structure, mTHPP is more hydrophobic and redistributes much slower to both acceptor phases than pTHPP. MD simulations indicate that compared to pTHPP, mTHPP makes stronger hydrogen bonds with the lipid head groups, is oriented more parallel to the lipid tails and is embedded slightly deeper in the membrane. [ABSTRACT FROM AUTHOR]

DC Beads and CalliSpheres are commonly used microspheres in clinical transcatheter arterial chemoembolization, but these microspheres cannot be visualized by themselves. Therefore, in our previous study, we developed multimodal imaging nano-assembled microspheres (NAMs), which are visualized under CT/MR and the location of embolic microspheres can be determined during postoperative review, facilitating the evaluation of embolic areas and guiding subsequent treatment. Moreover, the NAMs can be carried with positively and negatively charged drugs, increasing the choice of drugs. Systematic comparative analysis of the pharmacokinetics of NAMs with commercially available DC Bead and CalliSpheres microspheres is important for evaluating the clinical application of NAMs. In our study, we compared the similarities and differences between NAMs and two drug-eluting beads (DEBs) in respect to drug loading capacity, drug release profiles, diameter variation and morphological characteristics. The results indicate that NAMs had good drug delivery and release characteristics as well as DC Bead and CalliSpheres in vitro experimental stage. Therefore, NAMs have a good application prospect in transcatheter arterial chemoembolization treatment of hepatocellular carcinoma. [ABSTRACT FROM AUTHOR]

In order to get more effective results from natural and synthetic drugs used in cancer treatment, studies on solutions that will increase the bioavailability of these drugs in the cancerous region are very important. Mesoporous organosilica nanoparticles are one of the prominent among these solutions. Especially if mesoporous organosilica structures are designed in accordance with the drug to be transported, they can provide very important advantages. In this study, the synthesis and characterization of pH-responsive mesoporous organosilica nanocarrier functionalized with 2-aminothiophenol (MON-B) was carried out for more efficient transport and controlled release of natural hydrophobic curcumin. Characterization of monosilyl organic compound 1 was performed 1H and 13C NMR, FT-IR and MS while TGA, BET, XRD, FT-IR and SEM–EDS analyses were used to characterize mesoporous organosilica nanocarrier MON-B. The amount of curcumin loaded into the nanocarrier MON-B was calculated as 22% (EE) according to the measurements in UV–Vis spectrophotometer. In vitro drug release studies of curcumin-loaded MON-B at pH 7.4 resulted in 1% curcumin release after 368 h while the release of curcumin was recorded as 33% at pH 4.5 in the same period. These results show that MON-B can transport hydrophobic curcumin at physiological pH without leakage and provide pH-controlled and prolonged release of curcumin through its acid-labile C=N bond. [ABSTRACT FROM AUTHOR]

This study focuses on the covalent functionalization of the carboxylated graphene oxide layers with human serum albumin for developing new nanoplatforms capable of efficient drug loading and release for antitumor therapy. Thus, new GO-HSA conjugates have been developed and their interactions with methotrexate (MTX) molecules were evidenced through FT-IR, UV-Vis and Raman spectroscopy. The cumulative in vitro release profiles of MTX drug from GO-HSA-MTX nanoplatforms were analyzed through UV-Vis spectroscopy showing a more controlled release behavior of MTX drug under acidic conditions that simulate the tumor microenvironment demonstrating the potential use of GO-HSA-MTX as antitumoral nanocarriers. [ABSTRACT FROM AUTHOR]

Copyright of Die Orthopädie is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Die Orthopädie is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Purpose: Many current drug delivery technologies are ineffective and require high concentrations of active drugs for effective therapy. Novel drug delivery systems (NDDS) are increasingly being investigated to achieve targeted and controlled drug release. This study uses a microsponge-loaded drug delivery system to overcome the problem associated with traditional therapy for diaper dermatitis. Therefore, we aimed to formulate and characterize luliconazole microsponge-loaded gel for anti-fungal activity. Methods: Quasi-emulsion solvent diffusion method was used for developing luliconazole microsponge. The characterization of drug-loaded microsponge was investigated. Optimization of formulation carried out through in vitro release studies and entrapment efficacy. The formulation of microsponge-loaded gel was carried out and evaluated using physicochemical studies. The effectiveness of optimized formulations was examined for anti-fungal activity against Candida albicans. Results: The prepared microsponge was found to have a particle size between 20 and 50 µm, an entrapment efficiency of 53 ± 0.3–92.7 ± 0.1% and a drug release of 71.8 ± 0.2–88.5 ± 0.02%. The pH was in the range of 6.8–7.4, and the viscosity of the prepared formulation was 265.5 cPs. In vitro, the release of luliconazole microsponge-loaded gel showed that formulation F6 has the highest percentage (%) of cumulative drug release (CDR) compared to other formulations. The anti-fungal activity of the microsponge-loaded gel against Candida albicans showed a clear zone of inhibition in the F6 formulation. Conclusion: Our study results demonstrate that the F6 formulation has the highest % of CDR and shows better anti-fungal activity. Therefore, luliconazole microsponge-loaded gel formulation can improve drug delivery in diaper rash caused by fungal infection. [ABSTRACT FROM AUTHOR]

Exceptionally fast temperature-responsive, mechanically strong, tough and extensible monolithic non-porous hydrogels were synthesized. They are based on divinyl-crosslinked poly(N-isopropyl-acrylamide) (PNIPAm) intercalated by hydroxypropyl methylcellulose (HPMC). HPMC was largely extracted after polymerization, thus yielding a 'template-modified' PNIPAm network intercalated with a modest residue of HPMC. High contents of divinyl crosslinker and of HPMC caused a varying degree of micro-phase-separation in some products, but without detriment to mechanical or tensile properties. After extraction of non-fixed HPMC, the micro-phase-separated products combine superior mechanical properties with ultra-fast T-response (in 30 s). Their PNIPAm network was highly regular and extensible (intercalation effect), toughened by hydrogen bonds to HPMC, and interpenetrated by a network of nano-channels (left behind by extracted HPMC), which ensured the water transport rates needed for ultra-fast deswelling. Moreover, the T-response rate could be widely tuned by the degree of heterogeneity during synthesis. The fastest-responsive among our hydrogels could be of practical interest as soft actuators with very good mechanical properties (soft robotics), while the slower ones offer applications in drug delivery systems (as tested on the example of Theophylline), or in related biomedical engineering applications. [ABSTRACT FROM AUTHOR]

The physics of tablets mixtures has gained much attention lately. The purpose of this work is to evaluate the compaction properties of Kollidon® SR (KSR) in the presence of different excipients such as Microcrystalline cellulose (MCC), Monohydrous lactose (MH Lactose), Poly (vinyl acetate) (PVA100), and a water-soluble drug Diclofenac sodium (DNa) to prepare once daily formulation. Tablets were prepared using direct compression and were compressed into flat-faced tablets using hydraulic press at various pressures. The combination of MCC and KSR in the tablets showed reduced porosity, and almost constant low Py values as KSR levels increased; also, KSR-DNa tablets had higher percentage porosity and crushing strength values than KSR-MH Lactose tablets. The crushing strengths of KSR-MCC tablets were larger than those of KSR-DNa tablets. Ternary mixture tablets comprised of KSR-MCC-DNa showed decreased porosities and low Py values as the percentage of KSR increased especially at high compression pressures but had higher crushing strengths compared to KSR-DNa or MCC-DNa binary tablets. KSR-MH Lactose-DNa ternary tablets experienced lower porosities and crushing strengths compared to KSR-MCC-DNa tablets. Quaternary tablets of KSR-PVA100-MCC-DNa showed lower porosity and Py values than quaternary tablets obtained using similar proportion of MH Lactose instead of MCC. In conclusion, optimum quaternary tablets were obtained with optimum crushing strengths, relatively low Py, and moderate percentage porosities among all prepared quaternary tablets. The drug release of the optimum quaternary tablets demonstrated similar in vitro release profile compared to that of the marketed product with a mechanism of release that follows Korsmeyer-Peppas model. [ABSTRACT FROM AUTHOR]

This study reports on the synthesis of Mn1 − xZnxFe2O4 (Mn, Zn ferrite) magnetic nanoparticles (MNPs) as drug delivery carriers for effective therapeutic outcomes. The MNPs were prepared using the coprecipitation method, and their magnetic properties were investigated based on their composition. Among the compositions tested, Mn0.8Zn0.2Fe2O4 MNPs exhibited superparamagnetic properties with a saturation magnetization moment of 34.6 emu/g at room temperature (25°C). To enhance the water solubility of curcumin (Cur), known for its hydrophobic nature, it was successfully loaded onto alginate (Alg)/chitosan (Chit)@Mn0.8Zn0.2Fe2O4 nanoparticles (NPs). The nanocomposite was characterized by field emission scanning electron microscopy (FE-SEM) which revealed a particle size of approximately 20 nm. The crystalline structure of the NPs was analyzed using X-ray diffraction, while Fourier-transform infrared (FTIR), energy-dispersive X-ray, and map analysis techniques were employed for further characterization. In terms of drug release, there was an initial burst release of Cur (around 18%) within the first hour, followed by a slower release (approximately 61%) over the next 36 h. The anti-tumor properties of the Cur-loaded NPs were evaluated using the Methyl Thiazol Tetrazolium (MTT) assay and quantitative real-time polymerase chain reaction. The MTT assay confirmed a higher cytotoxic effect of Cur-loaded Alg/Chit@Mn0.8Zn0.2Fe2O4 NPs on the MCF-7 breast cancer cell line compared to free Cur, highlighting the significance of incorporating Cur into nano-sized carrier systems. [ABSTRACT FROM AUTHOR]

Hydrogels are possible materials that could be useful in medication delivery systems. Diverse release mechanisms are used when drug molecules embedded in the hydrogel structure need to be released. Both case I and case II of transport refer to the release of the medication during the intermolecular arrangement because of swelling. Numerous mathematical models have been proposed that only include one form of transport; nevertheless, both transport pathways are required for the entire release of a drug from a gel matrix. The case I transport during swelling and the case II transport during the fully swollen condition are both displayed by crosslinked hyaluronic acid hydrogel systems. The methodology put out in this paper enables for the selection of suitable gel compositions while attempting to account for both transit instances. In the Data Envelopment Analysis coupled with principal component analysis approaches are enable the optimization and selection of gel compositions that account for both transport situations. [ABSTRACT FROM AUTHOR]

The main objective of this research is to investigate how curcumin liposomal nanocarriers influence the drug release behaviour of PVA/PEG hydrogels in relation to physico-mechanical properties. For this purpose, optimal nanoliposomes from drug loading and release viewpoints, prepared by the thin-film hydration method, were incorporated into the hydrogel composition. Hydrogel samples were physically crosslinked using the freeze–thaw procedure. According to the dynamic laser scattering, atomic force microscopy and field-emission scanning electron microscopy observations, negative nanoliposomes with negative surface charges showed a spherical morphology with an average particle size of about 100 nm and narrow size distribution. The X-ray diffraction results revealed that adding nanoliposomes to the hydrogel increases the degree of PVA chains crystallinity, enhances tensile modulus and tensile strength of the hydrogel, while decreasing swelling and dehydration rates. SEM micrographs observation displayed that the porosity in the hydrogel structure in the presence of nanoliposomes increases. Nevertheless, in agreement with physical properties, drug release from nanoliposome-in-hydrogel is slower and more controlled as compared to that from free curcumin hydrogel, especially in the early stages. The MTT assay results indicated that although all hydrogel samples are non-toxic, human foreskin fibroblast cell proliferation on hydrogel in the presence of curcumin-loaded nanoliposomes has improved somewhat. [ABSTRACT FROM AUTHOR]

This research study focuses on the formulation and evaluation of an ACNE gel using Metronidazole (1%) and Doxycycline (0.5%) as active ingredients. Three types of polymers, Hydroxypropyl Methylcellulose (HPMC), Carbopol 940, and Carbopol 934 were used for gel formation. The formulated gels were evaluated for their physical characteristics, in vitro drug release, and drug-polymer compatibility. The calibration curves for both Metronidazole and Doxycycline displayed strong linearity within the concentration range of 5 to 25 μg/mL, facilitating accurate drug quantification. The gel formulations exhibited pH values of 6.0 (HPMC), 5.8 (Carbopol 940), and 5.7 (Carbopol 934), which are within the skin's natural pH range. The mean viscosity values were recorded as 205 cP (HPMC), 220 cP (Carbopol 940), and 231 cP (Carbopol 934). Spreadability and extrudability tests also yielded favorable results, suggesting ease of application. The in vitro drug release study showed a time-dependent increase in drug release, with the highest cumulative release observed from the HPMC formulation (90% at 8 hours), followed by Carbopol 940 (80% at 8 hours), and Carbopol 934 (64% at 8 hours). Fourier Transform Infrared Spectroscopy (FTIR) analysis revealed no significant interaction between the drugs and the polymers, indicating their compatibility. This study offers a promising approach to the development of effective ACNE gel formulations with Metronidazole and Doxycycline, while emphasizing the influence of the type of polymer on the drug release profile. [ABSTRACT FROM AUTHOR]

The current study presents research about electrodeposition in relation to electrospinning PCL wires on a Zr substrate and loading the coating with vancomycin. The structural composition of the coatings was investigated via FT-IR analysis. The morphology evaluated using scanning electron microscopy coupled with energy-dispersive X-ray spectroscopy, for the composition (SEM-EDS), evidenced the presence of the polymer wires, with and without drug vancomycin loading. The wettability of the coatings was evaluated from the hydrophobic–hydrophilic point of view, and the characterization was completed with mechanical and electrochemical tests. All the electrochemical tests performed in simulated body fluid highlighted that PCL represents a barrier against corrosion processes. The quantitative method to evaluate the loading efficiency shows that almost 80% of the total loaded vancomycin is released within 144 h; after the initial burst at 24 h, a steady release of vancomycin is observed over 7 days. A kinetic model of the drug release was also constructed. [ABSTRACT FROM AUTHOR]

α-mangostin (AM) is a promising natural anticancer agent that can be used in cancer research. However, its effectiveness can be limited by poor solubility and bioavailability. To address this issue, chitosan-based nanoparticles (CSNPs) have been investigated as a potential delivery system to enhance the cytotoxicity to cancer cells and improve selectivity against normal cells. In this study, we developed folate-conjugated chitosan nanoparticles (F-CS-NPs) using a carbodiimide-based conjugation method to attach folate to chitosan (CS), which have different molecular weights. The NPs were crosslinked using tripolyphosphate (TPP) via ionic gelation. To characterize the F-CS-NPs, we utilized various analytical techniques, including transmission electron microscopy (TEM) to evaluate the particle size and morphology, Fourier-transform infrared spectroscopy (FTIR) to confirm the presence of functional groups, and ultraviolet-visible spectroscopy (UV-Vis) to measure the absorption spectrum and confirm the presence of folate. The particle size of AM-F-CS-NPs ranged from 180 nm to 250 nm, with many having favorable charges ranging from +40.33 ± 3.4 to 10.69 ± 1.3 mV. All NPs exhibited the same spherical morphology. The use of F-CS-NPs increased drug release, followed by a sustained release pattern. We evaluated the cytotoxicity of AM, AM-F-CS-HMW, and AM-F-CS-LMW NPs against MCF-7 cells and found IC50 values of 8.47 ± 0.49, 5.3 ± 0.01, and 4.70 ± 0.11 µg/mL, respectively. These results confirm the improved cytotoxicity of AM in MCF-7 cells when delivered via F-CS-NPs. Overall, our in vitro study demonstrated that the properties of F-CS-NPs greatly influence the cytotoxicity of AM in MCF-7 breast cancer cells (significantly different (p < 0.05)). The use of F-CS-NPs as a drug-delivery system for AM may have the potential to develop novel therapies for breast cancer. [ABSTRACT FROM AUTHOR]

Spinal cord injury (SCI) has a high disability rate and poor treatment efficacy and severely affects the health and daily life of patients. Improving the local microenvironment after SCI is crucial for restoring the normal physiological function of the spinal cord. In this study, the injectable near-infrared (NIR) photothermal responsive drug-loaded multiwalled carbon nanotubes (DMWCNTs) containing hydrogel microspheres were prepared by microfluidic technology for SCI treatment. Specifically, paclitaxel (PTX) and vascular endothelial growth factor (VEGF) were loaded into dopamine-modified DMWCNTs, which were then further compounded into gellan gum (GG) by using microfluidic technology to obtain [PTX/VEGF]@DMWCNTs/GG microspheres. The physicochemical properties of the microspheres were characterized using various methods, including transmission electron microscopy (TEM), energy-dispersive X-ray (EDX) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, optical microscopy, and scanning electron microscopy (SEM). Results showed that microspheres with good injectability and controllable drug release were successfully prepared by using microfluidic technology. The presence of MWCNTs endowed the microspheres with photothermal responsiveness, which led to more drug release under NIR irradiation. The cytotoxicity test results showed that the microspheres had no obvious cytotoxicity and the drug-loaded MWCNTs containing hydrogel microspheres could promote the differentiation of neural stem cells (NSCs). Immunofluorescence results in rats with hemisectioned SCI showed that the microspheres promoted the differentiation of NSCs and the growth of neurons and inhibited the formation of astrocytes and glial scars at the lesion site. In conclusion, the injectable near-infrared photothermal responsive drug-loaded multiwalled carbon nanotube hydrogel microspheres prepared in this study exhibit a promoting effect on SCI repair and provide a strategy for developing transplantation materials for SCI treatment. [ABSTRACT FROM AUTHOR]

Hybrid crosslinked hydrogel-based drug delivery systems can deliver therapeutically beneficial drug release effects through controlled release on a temporal and spatial scale. Due to their tuneable physicochemical properties and the ability to prevent drug degradation, these systems facilitate different physicochemical interactions that control drug release. This research aims to synthesize a potent pH-sensitive crosslinked chitosan/polyvinylpyrrolidone hydrogel using different ratios of both the polymers and varying the glutaraldehyde crosslinking agent amount by the solution casting technique for controlled amoxicillin-release properties to mitigate gastrointestinal tract bacterial infection. The effect of polymer ratios and glutaraldehyde amount is investigated by the developing porosity, gel fraction, and extent of swelling in simulated physiological fluids of pH 1.2, 6.8, and 7.4 and in vitro biodegradation at pH 7.4. Interaction between the polymers with the formation of crosslinked structures, good stability, amorphous phase nature, and honeycomb-like structures of the hydrogels is revealed by Fourier-transform infrared spectroscopy, thermogravimetric analysis, X-ray diffraction, and scanning electron microscopy. Based on these properties, a chitosan/polyvinylpyrrolidone hydrogel (ratio of 60:40) crosslinked with 600 μL glutaraldehyde in 8 g of the polymers displaying adequate swelling in acidic to basic pH and in vitro biodegradation at pH 7.4 is chosen for the in situ loading of 200 mg of the drug amoxicillin. The cumulative drug release in simulated physiological fluids and the drug release kinetics using different models show that the best-fit Korsmeyer-Peppas model suggests amoxicillin release from the matrix follows diffusion and swelling-controlled time-dependent non-Fickian transport related to hydrogel erosion. This composition displays excellent antimicrobial activity against Streptococcus pyogenes and Escherichia coli. Graphical Abstract [ABSTRACT FROM AUTHOR]

The use of drug-loaded microbubbles for targeted drug delivery, particularly in cancer treatment, has been extensively studied in recent years. However, the loading capacity of microbubbles has been limited due to their surface area. Typically, drug molecules are loaded on or within the shell, or drug-loaded nanoparticles are coated on the surfaces of microbubbles. To address this significant limitation, we have introduced a novel approach. For the first time, we employed a transmembrane ammonium sulfate and pH gradient to load doxorubicin in a crystallized form in the core of polymeric microcapsules. Subsequently, we created remotely loaded microbubbles (RLMBs) through the sublimation of the liquid core of the microcapsules. Remotely loaded microcapsules exhibited an 18-fold increase in drug payload compared with physically loaded microcapsules. Furthermore, we investigated the drug release of RLMBs when exposed to an ultrasound field. After 120 s, an impressive 82.4 ± 5.5% of the loaded doxorubicin was released, demonstrating the remarkable capability of remotely loaded microbubbles for on-demand drug release. This study is the first to report such microbubbles that enable rapid drug release from the core. This innovative technique holds great promise in enhancing drug loading capacity and advancing targeted drug delivery. [ABSTRACT FROM AUTHOR]

In recent years, the 3D printing of personalized drug formulations has attracted the attention of medical practitioners and academics. However, there is a lack of data-based analyses on the hotspots and trends of research in this field. Therefore, in this study, we performed a bibliometric analysis to summarize the 3D printing research in the field of personalized drug formulation from 2012 to 2022. This study was based on the Web of Science Core Collection Database, and a total of 442 eligible publications were screened. Using VOSviewer and online websites for bibliometric analysis and scientific mapping, it was observed that annual publications have shown a significant growth trend over the last decade. The United Kingdom and the United States, which account for 45.5% of the total number of publications, are the main drivers of this field. The International Journal of Pharmaceutics and University College London are the most prolific and cited journals and institutions. The researchers with the most contributions are Basit, Abdul W. and Goyanes Alvaro. The keyword analysis concluded that the current research hotspots are "drug release" and "drug dosage forms". In conclusion, 3D printing has broad application prospects in the field of personalized drugs, which will bring the pharmaceutical industry into a new era of innovation. [ABSTRACT FROM AUTHOR]

In this study, PVA/p(HEMA-co-MAPTAC) hydrogels were synthesized by redox polymerization using polyvinyl alcohol (PVA), 2-hydroxyethyl methacrylate (HEMA) and [3-(Methacryloylamino)propyl]trimethylammonium chloride (MAPTAC). In order to increase the antimicrobial activities of synthesized PVA/p(HEMA-co-MAPTAC) hydrogels, they were modified with Au nanoparticles. The swelling behavior of the synthesized hydrogels was investigated. Hydrogels were characterized by various techniques. The drug release studies of PVA/p(HEMA-co-MAPTAC) and PVA/p(HEMA-co-MAPTAC)@Au hydrogels were performed in PBS medium using Ribonucleic acid (RNA) as genetic material and sodium diclofenac (NaDc) as drug. It was determined that PVA/p(HEMA-co-MAPTAC) hydrogel held 91.5 mg/g RNA and 97.48 mg/g NaDc and released 28.32 mg/g RNA and 71.12 mg/g NaDc in PBS medium. Subsequently, PVA/p(HEMA-co-MAPTAC)@Au hydrogel adsorbed 87.46 mg/g RNA and 119.44 mg/g NaDc and released 18.96 mg/g RNA, 104.99 mg/g NaDc drug in PBS medium. Using the data obtained at the end of the release studies, the drug release kinetics of the hydrogels were examined. According to the Korsmeyer Peppas model, RNA release from hydrogels showed Fickian diffusion, while NaDc release showed non-Fickian diffusion behavior. The antibacterial and antifungal activities of the hydrogels were tested using gram-negative bacteria E. coli, gram-positive bacteria B. subtilis and a fungus species C. albicans. [ABSTRACT FROM AUTHOR]

Background: Antibiotic beads are used to treat local bacterial infections by delivering high drug concentrations to infected tissue. Objectives: This study examined the elution characteristics of metronidazole from metronidazole-calcium sulfate (MCa) and metronidazole-calcium-potassium sulfate (MCaK) beads over 20 days and the antibacterial efficacy of the beads after storage. Methods: The MCa and MCaK beads were prepared by mixing 250 mg of metronidazole and 10 g of calcium sulfate hemihydrate with water and a 3% potassium sulfate solution, respectively. The beads were placed in phosphate-buffered saline for the elution study. The metronidazole eluents were determined using high-performance liquid chromatography. The microstructures were examined by scanning electron microscopy (SEM), and the antimicrobial activity was evaluated by a microbioassay. Results: For the 20-day study, the total amount of metronidazole released was greater in the MCa beads than in the MCaK beads by 6.61 ± 0.48 mg (89.11% ± 3.04%) and 4.65 ± 0.36 mg (73.11% ± 4.38%), respectively. The amounts of eluted drugs from the MCa and MCaK beads were higher than the minimum inhibitory concentration at 0.5 µg/mL against anaerobic bacteria at both 20 days and 14 days. SEM showed that calcium crystals on the outer surface had dissolved after elution, and thinner calcium crystals were prominent in the MCaK beads. The MCa and MCaK beads exhibited antibacterial activity after setting, followed by storage at room temperature or 4°C for 21 days. Conclusions: The MCa beads could release more drug than the MCaK beads, but all eluted metronidazole amounts were effective in controlling bacterial infections. Both metronidazole beads could be stored at ambient temperature or in a refrigerator. [ABSTRACT FROM AUTHOR]

The present study aimed to prepare hydrogel based on polyvinyl alcohol (PVA) and gelatin (Ge) and characterization of PVA/Ge hydrogel for their potential use as a sustained drug delivery system. Polyvinyl Alcohol (PVA) and-Gelatin (Ge) were cross-linked using glutaraldehyde (GA) as a crosslinking agent and hydrochloric acid (HCl) as a catalyst. Different feed polymer ratio and crosslinking agent concentration were used to prepare a series of PVA/Ge hydrogels. The obtained PVA/Ge hydrogels were investigated for dynamic and equilibrium swelling studies. The effect of polymers ratio, degree of crosslinking and pH of the medium on swelling of PVA/Ge hydrogels was investigated. Furthermore, the values of diffusion coefficient (D), volume fraction, polymer-solvent interaction parameter, molecular weight between crosslink and crosslink density were calculated. For swelling studies, 0.05M USP phosphate buffer solutions of different pH (1.2, 5.5, 6.5 and 7.5) were used. For the drug release study, ciprofloxacin HCl was loaded into selected samples as a model drug. The release of drug from these samples was performed for 12 hours in USP phosphate buffers of pH 1.2, 5.5 and 7.5. The release data from these samples were fitted into various kinetic models like zero order, first order, Higuchi and Peppas models to investigate the release mechanism. It was found that by varying the composition of PVA/Ge hydrogel and GA concentration, a significant difference was observed in drug release kinetics. FTIR spectroscopy and X-ray diffraction were used for the characterization of hydrogels. PVA/Ge hydrogel showed sustained release of the model drug at various pH values suggesting its potential use as a sustained drug delivery system.

Gemcitabine is a widely used antimetabolite drug of pyrimidine structure, which can exist as a free-base molecular form (Gem). The encapsulated forms of medicinal drugs are of interest for delayed and local drug release. We utilized, for the first time, a novel approach of mechano-chemistry by liquid-assisted grinding (LAG) to encapsulate Gem on a “matrix” of porphyrin aluminum metal-organic framework Al-MOF-TCPPH2 (compound 2). The chemical bonding of Gem to compound 2 was studied by ATR-FTIR spectroscopy and powder XRD. The interaction involves the C=O group of Gem molecules, which indicates the formation of the encapsulation complex in the obtained composite. Further, the delayed release of Gem from the composite was studied to phosphate buffered saline (PBS) at 37 °C using an automated drug dissolution apparatus equipped with an autosampler. The concentration of the released drug was determined by HPLC-UV analysis. The composite shows delayed release of Gem due to the bonded form and constant concentration thereafter, while pure Gem shows quick dissolution in less than 45 min. Delayed release of Gem drug from the composite follows the kinetic pseudo-first-order rate law. Further, for the first time, the mechanism of delayed release of Gem was assessed by the variable stirring speed of drug release media, and kinetic rate constant k was found to decrease when stirring speed is decreased (diffusion control). Finally, the prolonged time scale of toxicity of Gem to pancreatic cancer PANC-1 cells was studied by continuous measurements of proliferation (growth) for 6 days, using the xCELLigence real-time cell analyzer (RTCA), for the composite vs. pure drug, and their differences indicate delayed drug release. Aluminum metal-organic frameworks are new and promising materials for the encapsulation of gemcitabine and related small-molecule antimetabolites for controlled delayed drug release and potential use in drug-eluting implants.