Search

BACKGROUND Microbial pathogens, mainly bacteria, are a major cause of food spoilage resulting in several foodborne diseases. Food spoilage can be prevented by the application of chemical preservatives in the food industry but such process has harmful effects on human health and causes the introduction of chemicals in several food chains, leading to toxicity and long-term complications. Due to such adverse effects, the need to find natural preservatives that are safer to use, effective and less complicated is increasing. OBJECTIVES This study is based on plant extracts that play a major role in microbicidal action (the use of natural preservatives is preferred over chemical ones). Antimicrobial action of different plant extracts was assessed using Staphylococcus aureus and Escherichia coli as experimental bacterial strains. MATERIAL AND METHODS Ethanolic extracts of different plants like Punica granatum, Acacia catechu and Phyllanthus emblica were highly effective against the both analyzed bacterial strains at a dosage of 10 mg/mL, while the extracts of Ocimum bacilicum and Quercus infectoria were effective only against S. aureus and E. coli, respectively. RESULTS Punica granatum and Phyllanthus emblica extracts were found to be the most effective and exhibited bacteriostatic and bactericidal activities against the highly infectious strains of pathogenic bacteria causing food spoilage, with minimum inhibitory concentration (MIC) of 2.5 mg/mL and minimum bactericidal concentration (MBC) of 5 mg/mL. CONCLUSIONS The plant extracts used in the study were highly effective in reducing bacterial contamination and can be used as an alternative to chemical preservatives to avoid and control foodborne diseases and for preservation of food with no health-related hazards caused by chemicals.

Background Adhatoda vasica L. is a medicinal plant, known as Malabar nut in English, belonging to the family Acanthaceae. It has been used traditionally to treat respiratory disorders like severe coughs, colds, chronic bronchitis, asthma, tuberculosis, and other illnesses. The multifunctional range of bioactives found in it has piqued the interest of pharmaceutical companies, who are looking for more evidence-based ways to develop new formulations. Objective To analyse the A. vasica leaves by GC-MS technique and evaluation of its antioxidant activity. Method Methanolic extract of A. vasica L. (MEAV) leaves was analyzed by GC-MS for identification and characterization of its bioactives and traditional therapeutic claims. A widely anticipated 2,2-diphenyl-1-picrylhydrazyl (DPPH) method was used to determine the antioxidant activity of MEAV. Results The major compounds revealed in MEAV leaves are: 1,3,5-triazine-2,4,6-triamine (3.06%); 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (5.35%); 5-hydroxymethylfurfural (16.82%); 2-butylphenol (6.85%); 3,4-dihydroxy-5-methyl-dihydro-furan-2-on (2.5%); 2(OR 3)–(1,1-dimethylethyl)-4-methoxyphenol (3.52%); megastigmatrienone 3 (1.02%); tetradecanoic acid (1.52%); vomifoliol (0.58%); oxalic acid, cyclobutylhexyl ester (6.03%); hexadecanoic acid (6.06%); 4-ethyl-2-oxo-2,5,6,7-tetrahydro-1H-cyclopenta[B]pyridine-3-carbonitrile (10.08%); phytol (2.01%); and vitamin E (3.18%). A significant reduction in free radicals against DPPH was observed, which revealed the antioxidant potential of MEAV. Conclusion MEAV consists of both polar and nonpolar components. GC-MS analysis was used to identify these compounds. The current work validates that the antioxidant activity of MEAV is attributed to the presence of compounds such as vitamin E and terpenes. Highlights This work validates the antioxidant activity of methanolic extract of A. vasica attributed to the presence of compounds like vitamin E and terpenes.

To overcome problems associated with topical delivery of tacrolimus (TCS), a thermoresponsive in situ gel system containing pluronic F127 (PL), and chitosan (CS) was developed, to enhance the preco...

Background: Form last few decades, nanoparticles have witnessed breakthroughs in the treatment of neurological disorders due to their unique physiochemical properties, which make them an effective drug delivery system. However, there is not much information available on the toxicity of nanoparticles in neuronal disorders. The toxic effect of nanoparticles on brain disorders and their regulatory issues are the primary concerns of the healthcare industry. Methods: A strategical literature search was performed on various bibliographic databases such as Scopus, PubMed, SciFinder, Google Scholar, Medline, Google Patent, Derwent Innovation, and Orbit Intelligence for retrieval of peer-reviewed articles and patents on regulatory issues and toxicity of nanoparticles in neuronal disorders for last decade. The relevant hits of articles and patents were analyzed, and citation search for the relevant documents was carried out. Results:: The literature documents have been summarized regarding the existing regulatory issues and toxicity of nanoparticles on neuronal disorders with a focus on the detailed mechanism of the developmental toxicity of nanoparticles. The focus of this report is to emphasize the negative effects of nanoparticle on neuronal disorders, which may partially contribute to the management of toxicity of nanoparticles. Conclusion: Although nanoparticles have unique physical and chemical properties that explain the broad range of application for the central nervous system, they can also manifest neurotoxic effects due to cell necrosis, generation of free radicals, immune responses and neuroinflammation. Thus, this review highlights risk assessment, safety regulations and regulatory guidelines of nanoparticles, which may reduce adverse reactions in humans and animals.

Background Wrightia tinctoria R.Br. (Apocyanaceae) is known as a biologically effective plant for the treatment of jaundice in the Indian traditional system of medicine. It is a wild medicinal tree possessing anti-inflammatory, antidiabetic, antinociceptive, hepatoprotective, antibacterial, antifungal, antiviral, antipsoriatic, anticancerous, anthelmintic, aphrodisiac, analgesic, and antipyretic activities. Its constituents are of utmost interest to pharmaceutical industries owing to their many actions and biological activities. Method Methanolic extract of W. tinctoria (MEWT) was investigated by gas chromatography-mass spectroscopy and provided affirmative results assisting in the identification and characterization of therapeutic claims regarding this species in the traditional system. The antioxidant activity of MEWT was determined by the most suitable DPPH method. Results The basic compounds found in MEWT were β-caryophyllene (0.22%), mome inositol (12.02%), neophytadiene (1.61%), eicosanoic acid methyl ester (0.32%), 8,11,14-eicosatrienoic acid methyl ester (0.60%), phytol (0.94%), phytol palmitate (1.37%), squalene (1.57%), flavone 4-OH, 5-OH, 7-di-O-glucoside (29.34%), γ-tocopherol (0.49%), stigmast-5-en-3-ol (3.14%), methyl commate B (1.76%), methyl commate A (5.20%), and 24-norursa-3,12-diene (20.36%). The obtained results in the analysis of antioxidant activity of MEWT exhibited considerable free radical scavenging capacity against DPPH-generated free radicals. Conclusions This study expands the knowledge of MEWT chemical composition and provides evidence to substantiate ethno-medicinal use of the plant by exploring antioxidant activity. The substantial antioxidant activity of MEWT could be due to presence of terpenes, flavonoids, vitamin E, and other reported compounds. Highlights This study includes identification of phytochemicals and antioxidant potential of methanolic extract of Wrightia tinctoria, assisting in therapeutic claims regarding this species in the traditional system.

Cancer is among the most dreadful fatal diseases globally, and the efficacy of recent chemotherapeutic approaches is limited due to many related drawbacks. The major limitation associated with canc...

In the present work, a simple, rapid, reliable and accessible high-performance thin-layer chromatography (HPTLC) technique has been established for the concurrent quantification of plumbagin. The well-known medicinal plant, Plumbago zeylanica L., has been traditionally used to treat a variety of ailments in India and other countries. Chromatographic separation was conceded on pre-coated silica gel plates F254. The apposite mobile phase toluene‒acetic acid (9.0:0.5, V/V) was developed to expand the plates which separated components according to the marker compounds. Densitometric scanning was performed by CAMAG Scanner V and measured at wavelength 272 nm. The marker compounds were practically resolved with RF 0.44 ± 0.02 for plumbagin. Further, the antioxidant potential of the methanolic extract of P. zeylanica was also assessed with 1,1-diphenyl-2-picrylhydrazyl (DPPH) by using an ultraviolet (UV) spectrophotometer. The percentage inhibition of free radical was found to be 76.5%. The developed HPTLC method was validated for accuracy, linearity, precision and specificity. The extract has revealed considerable antioxidant activity. The reported existing phenolic and flavonoids compounds are responsible for the antioxidant activity of the plant extract as reported in the literature.

Rheumatoid arthritis is an inflammatory disorder, affecting around 1% of the world population. Antioxidant activity plays important role to overcome the inflammation associated with arthritis. Phoenix dactylifera (date) seeds, generally considered as a waste product or utilized as food for domestic farm animals, have been used as a source of antioxidants at different disease conditions. The aim of the present study was to enhance the release of date seed extract in order to achieve high antioxidant activity. Nanoemulsion of methanolic extract of date seed was prepared by aqueous titration method. The selected formulations were exposed to thermodynamic stability and dispersibility tests. The optimized nanoemulsions were evaluated on the basis of droplet size (23.14 ± 0.055nm), polydispersity index (0.166 ± 0.124), percent transmittance (99.12 ± 0.0163), refractive index (1.36 ± 0.046), viscosity (cP) (12.30 ± 0.75), conductivity (µS/cm) (347.46 ± 1.10), and drug content (%) (99.67 ± 0.11). The in vitro release studies revealed that final optimized formulation has cumulative release of drug (57.51% ± 2.65%), which was more significantly greater as compared to drug suspension (26.44% ± 1.15%). Further in vitro antioxidant activity studies revealed that the developed methanolic extract of date seed-loaded nanoemulsion has more antioxidant potential when compared with methanolic extract.

Omega-3 polyunsaturated fatty acids (ω-3-PUFAs) are dietary components that have been extensively recognized for their therapeutic value and have shown diverse therapeutic effects including anti-inflammatory, antiarrhythmic, antithrombotic, immunomodulatory and antineoplastic activities. Most of the ω-3-PUFAs are obtained through diet or supplements because the body does not synthesize them. The high instability of ω-3-PUFAs to oxidative deterioration, lower bioavailability at the target tissues and reduced bioactivity of ω-3-PUFAs is an impediment for achieving their therapeutic potential. The present review provides an overview of potential therapeutic activities of ω-3-PUFAs and different novel technical approaches based on nanotechnology, which have been emphasized to overcome instability problems as well as enhance the bioactivity of ω-3-PUFAs. Future prospects related to this area of research are also provided.

The aim of the present study was to develop and characterize karanjin-loaded ethosomes-based gel formulation for enhanced topical delivery and effective therapy of skin acne. Karanjin-loaded ethosomes (K-ETH) presented a nanometric size of 140.87 ± 2.35 nm, entrapment of 71.41 ± 2.74% and enhanced permeation with 1.9 times increase in the flux and 2.4 times higher skin deposition compared to the hydro-ethanolic solution of karanjin. The DSC analysis confirmed successful entrapment of the karanjin within the ethosomes. The developed ethosomes were incorporated in the carbopol gel for adequate application on the skin surface. The ethosomal gel (K-EGF) also exhibited greater penetration in the rat skin as revealed by CLSM. The optimized K-EGF formulation was non-irritant to the skin as evident by Draize score test and histopathological examination. The highest zone of inhibition, 30.0 ± 1.52 mm and 36.22 ± 0.57 mm was produced by the K-EGF against Propionibacterium acnes and Staphylococcus epidermidis, respectively, indicating substantial antibacterial properties of the K-EGF. DPPH assay indicated its potent antioxidant effects. Substantial anti-inflammatory effects in the carrageenan-induced edema in the rat paw were evident with inhibition of rat paw edema by 66.66% and 70.37% upon application of K-EGF and standard anti-inflammatory agent, respectively. Anti-acne effects were also evident with K-EGF treatment with significant decrease in number and size of sebaceous gland units in dermis. Overall, the above findings vouch for a therapeutic opportunity to improve topical delivery of karanjin in acne treatment employing ethosomal gels as the promising carrier system. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s13205-021-02978-3.

Nanoemulsions have gained enormous reputation in advanced drug delivery for their ease of formation, clarity and enhanced absorption rate leading to better bioavailability and therapeutic profiles. In spite of these advantages, nanoemulsions have a major flaw which is linked to their stability. Nanoemulsions are kinetically stable and thermodynamically unstable systems. Developing a robust nanoemulsion is of utmost importance as it ensures its safe and effective delivery in-vivo. Other important aspects of any formulation is about their biological fate. The fate of nanoemulsions within biological systems usually depends upon its physicochemical properties which include particle concentration, size, shape, electrical charge, and interfacial characteristics. The different environments of the gastro intestinal tract may cause significant changes in the physicochemical properties of nanoemulsions. This must be taken into consideration while designing an effective delivery system. The present chapter provides an insight about the fate of nanoemulsions in a biological system along with effects of the intestinal lymphatic system over the nanoemulsion carrier system.

The present work aimed to evaluate the efficacy of topical tacrolimus (0.01%) loaded propylene glycol (PG) modified nano-vesicles (Proglycosomes Nano-vesicles, PNVs) for the treatment of experimental dry eye syndrome (DES) in rabbits. DES was induced by topical application of atropine (1.0%) and benzalkonium chloride (0.1%) aqueous solution. PNVs treatment (PNV group) was compared with tacrolimus solution 0.01% (TAC group) and untreated group and healthy group were used as controls. PNV treated animals showed improved clinical performance with marked increase in tear production and tear break-up time (TBUT). Further, PNVs also subside ocular inflammation as evident from absence of matrix metalloprotenaise-9 and normal ocular surface temperature (32.3 ± 0.34 °C). Additionally, PNVs have positive effect on ocular and epithelial damage observed through low ocular surface staining score and improved globlet cell density. The PNV treatment was found to more effectively compared to TAC solution and most of the parameters were close to those of healthy animals. In conclusion, tacrolimus PNV formulation (0.01%) could be a potential therapy for treatment of dry eye syndrome.

Advancements in the field of cancer therapeutics have witnessed a recent surge in the use of liposomes. The physicochemical characteristics of the liposomes and their components, including the lipid phase transition temperature, vesicular size and size distribution, surface properties, and route of administration, play a significant role in the modulation of the immune response as an adjuvant and for loaded antigen (Ag). Cationic liposomes, concerning their potential ability to amplify the immunogenicity of the loaded Ag/adjuvant, have received enormous interest as a promising vaccine delivery platform for cancer immunotherapy. In the present review, the physicochemical considerations for the development of Ag/adjuvant-loaded liposomes and the cationic liposomes’ effectiveness for promoting cancer immunotherapy have been summarized.

Dendrites are polymeric hyper-branched 3D-nanoarchitecture with various surface functional groups that increase their functionality and make them versatile in drug delivery applications. They can be exploited as drug carriers for various therapeutics to minimise the drug toxicity and enhancement of their efficacy. The precise control throughout the dendritic design such as size and branching density as well as surface functionality offers this carrier more suitability for drug delivery. Various therapeutics with anticancer, anti-inflammatory, neuroprotective, cardio-protective and antimicrobial activity have been successfully associated with different types of dendrimers. More recently, dendrimers and another nanocarrier-based hybrid system (dendrimers–liposomes and dendrimers–carbon nanotube) are investigated for wider application in the field of drug delivery. The concept of such emerging hybrid nanosystems opens the way for the simultaneous delivery of therapeutics and diagnostics as a theranostic to assess the progression of therapy in better management of chronic disorders like cancer. The present book chapter provides a comprehensive discussion and contemporary research carried out to exploit dendrimer-based formulations for drug delivery application.

The aim of the present study was to develop, optimize brucine-loaded transliposomes (BRC-TL) formulation for dermal delivery of brucine for skin cancer. The BRC-TL formulations were evaluated for vesicle size, entrapment efficiency, and in vitro drug release. The optimized formulation was further evaluated for skin penetration by confocal laser microscopy and dermatokinetic study. The optimized BRC-TL formulation presented sealed lamellar shaped vesicles, with vesicles size, polydispersity index, entrapment efficiency, and in vitro drug release of 136.20 ± 2.87 nm, 0.354 ± 0.02, 86.01 ± 1.27%, and 83.09 ± 2.07%, respectively. Ex vivo permeation study showed that, developed BRC-TL formulation had a 2.4-fold increment in permeation as compared to BRC suspension. Texture analysis showed that the BRC-TL gel presented firmness of 158.91 g, consistency of 615.03 g/s, cohesiveness of − 115.26 g and a viscosity index of − 472.05 g/s. The confocal images of rat skin clearly showed the deeper penetration of rhodamine B-loaded TL formulation as compared to the Rhodamine B-hydro alcoholic solution. The optimized BRC-TL formulation demonstrated significantly higher cytotoxicity than placebo liposome and BRC suspension (P

Aim: The current study aimed to explore the feasibility of the nanoemulgel for the topical delivery of aceclofenac. Materials & methods: Solubility of drugs in the formulation systems was determined and aceclofenac nanoemulsion (NE) was prepared by high-pressure homogenization technique. Carbopol 940 was added as a gelling agent. Results & conclusion: The composition of optimized NE consist of labrafil along with triacetin as oil, tween 80 and cremophor EL in combination as a surfactant and transcutol HP along with PEG 400 and ethanol as cosurfactant. The droplet size of the NE was 141.1 ± 3.65 nm, with low polydispersity index and negative zeta potential. The aceclofenac–nanoemulgel was developed using carbopol 940 and exhibited excellent permeation in comparison to the marketed sample.

In the present study we investigated the protective role of intranasal rosuvastatin liquid crystalline nanoparticles (Ros-LCNPs) against pentylenetetrazole (PTZ) induced seizures, increasing current electroshock (ICES) induced seizures, and PTZ-induced status epilepticus. From the dose titration study, it was evident that intranasal rosuvastatin (ROS), at lower dose, was more effective than oral and intraperitoneal ROS. The Ros-LCNPs equivalent to 5 mg/kg ROS were developed by hydrotrope method using glyceryl monooleate (GMO) as lipid phase. The high resolution TEM revealed that the formed Ros-LCNPs were cubic shaped and multivesicular with mean size of 219.15 &plusmn, 8.14 nm. The Ros-LCNPs showed entrapment efficiency of 70.30 &plusmn, 1.84% and release was found to be biphasic following Korsmeyer&ndash, Peppas kinetics. Intranasal Ros-LCNPs (5 mg/kg) showed significant increase in latency to PTZ-induced seizures and ICES seizure threshold compared to control and intranasal ROS solution. Additionally, intranasal Ros-LCNPs provided effective protection against PTZ-induced status epilepticus. No impairment in cognitive functions was observed following intranasal Ros-LCNPs. The results suggested that Ros-LCNPs could be an effective and promising therapeutics for the epilepsy management.

The present study aimed at the development and evaluation of tacrolimus gellan gum nanoparticles (TGNPs) for the effective management of dry eye disease (DED) following topical application. TGNPs were developed by ionotropic gelation between gellan gum and aluminum chloride. Developed TGNPs were nanosized (274.46 ± 8.90 nm) with high % encapsulation efficiency (74.2 ± 2.4%) and loading capacity (36.14 ± 1.7%). The nanosize and spherical morphology of TGNPs was confirmed by transmission electron microscopy (TEM) and atomic force microscopy (AFM). Fourier transform infrared spectroscopy (FTIR) revealed no interaction between drug and GG. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirms the conversion of crystalline tacrolimus to amorphous post encapsulation in the nanoparticle. TGNPs showed prolonged drug release throughout 12 h and higher pre-corneal retention compared to tacrolimus solution. HET-CAM studies, histopathological evaluation, and Draize test confirmed the safety of the formulation for ocular use. Further, the pharmacodynamic studies using experimental DED in rabbits showed that TGNPs are effective in treating symptoms of DED. In conclusion, topical delivery of TGNPs could hold potential for efficient management of DED.

The study's purpose intended to develop and optimize an NLC formulation for topical berberine administration with increased skin acne efficacy. The “three-parameters, three-level Box-Behnken design” was employed to improve the formulation based on vesicle size, PDI, and encapsulation efficiency. In-vitro profile for drug release, skin penetration investigation using confocal microscopy, skin irritation, anti-inflammatory, and anti-acne studies were performed on the optimized formulation. The vesicles with a size of 132.5 ± 10.34 nm, PDI of 0.224 ± 5.12, and entrapment efficiency of 85.956 ± 5.78% were found in the optimized formulation. The optimized formulation had spherical vesicles, according to TEM imaging. In vitro release studies showed that final optimized NLC formulation has cumulative release of drug (72.675 ± 3.686%), which was significantly greater as compared to NLC gel formulation (48.354 ± 4.893%). Thermo-analytical studies of NLCs formulation determined smooth drug interaction via rat skin membrane. Confocal microscopy revealed that, rhodamine-NLC formulation was traceable up to 54.9 μm across skin of rats, while solution of rhodamine penetrated only up to 20.4 μm of rat skin. Skin irritation study further showed significantly lower irritation level of skin (erythema: 0.50.231 and edema: 0.50.320) by applying optimized NLC-gel formulation compared to the control irritant. Furthermore, in comparison to the positive control, the anti-acne study demonstrated a decrease in all acne parameters, in addition to higher effectiveness over the commercially available formulation. These findings suggest that developed berberine loaded NLC gel could be a promising vehicle for the safe and effective topical administration of drugs to treat acne vulgaris.

Medicinal plants have been used since ancient times for their various therapeutic activities and are safer compared to modern medicines, especially when properly identifying and preparing them and choosing an adequate dose administration. The phytochemical compounds present in plants are progressively yielding evidence in modern drug delivery systems by treating various diseases like cancers, coronary heart disease, diabetes, high blood pressure, inflammation, microbial, viral and parasitic infections, psychotic diseases, spasmodic conditions, ulcers, etc. The phytochemical requires a rational approach to deliver the compounds to enhance the efficacy and to improve patients’ compatibility. Nanotechnology is emerging as one of the most promising strategies in disease control. Nano-formulations could target certain parts of the body and control drug release. Different studies report that phytochemical-loaded nano-formulations have been tested successfully both in vitro and in vivo for healing of skin wounds. The use of nano systems as drug carriers may reduce the toxicity and enhance the bioavailability of the incorporated drug. In this review, we focus on various nano-phytomedicines that have been used in treating skin burn wounds, and how both nanotechnology and phytochemicals are effective for treating skin burns.

Present work aims to optimize and characterize orally administered, ubidecarenone (UDC)-loaded glycerylmonooleate-based cubosome (GCBMs) and phytantriol based cubosomes (PCBMs) for effective management of doxorubicin-induced cardiotoxicity and to enhance bioavailability of UDC. Formulations optimized using statistical hybrid-design approach exhibited particle size of 152.0 ± 1.78 and 248.8 ± 1.83 nm, polydispersity index of 0.183 ± 0.021 and 0.225 ± 0.018 with zeta potential of −26.8 ± 0.76 and −23.3 ± 0.22 mV and percentage entrapment efficiency (% EE) of 92.3 ± 4.99% and 94.7 ± 5.67%, for GCBMs and PCBMs, respectively. High-resolution transmission electron microscopy revealed agreement with the particle size and shows the discrete cubic geometry of particles, while small-angle X-ray scattering analysis confirmed the primitive (Im3m) and diamond (Pn3m) type crystalline cubic self-assemble structure of the particles. The comparative bioavailability profiles of UDC from GCBMs and PCBMs (AUC 0→∞ = 19,546.8 ± 512.88 ng·h/L for GCBMs and 27,961.99 ± 602.46 ng·h/L for PCBMs) were approximately 6.5- and 7.0-fold higher than that of UDC suspension (AUC 0→∞ = 3132.806 ± 405.44 ng·h/L). Cardioprotective assessment showed a significant increase in superoxide dismutase and β-glutathione peroxidase levels, while a decrease in the level of catalase, creatine kinase-MB isoenzyme, lactate dehydrogenase, and lipid peroxidation was observed in animals pre-treated with developed CBMs. Histopathology studies revealed no significant damage, infiltrated cells, and signs of fibrosis in the CBM-treated groups.

Background: A recently FDA approved 3D printed drug is paving a path for new pharmaceutical manufacturing era. The 3D printing is a novel approach of producing 3D pharmaceuticals from digital designs, in a layer-by-layer fashion. However, traditional manufacturing of drug products is being carried out from decades with well-established manufacturing processes and with well approved regulatory guidelines but these processes are too obsolete in concern of process aptitude and manufacturing flexibility. On the other hand, 3D printing provides a competitive flexibility in terms of personalized drug dosage forms with complex geometries that will be made on-demand with desired drug release kinetics, hence providing the formulator a substantial provision of improvising the safety and efficacy of the drugs. Furthermore, this novel 3D technology allows tailoring of composite tissue scaffolds and sample models for characterization that closely mimic in-vivo simulations. Nevertheless, certain limitations are there in terms of regulatory aspects hindering the launch of 3DP products in the market. Methods: Exhaustive search were made on Google Scholar and PubMed databases concerning 3-D printing methods, drug delivery applications, and past to present evolution of personalized medicine. Results: Although a high magnitude of progress have been made on 3-D printing techniques in a short span of time, still inkjet, nozzle-based deposition, stereolithography and selective laser sintering techniques are the most popular ones. Their application is adapted in the fabrication of tablets, implants, polypills and nanoparticles. Conclusion: 3D printing is revolutionizing the pharma expectations towards customized medicines but still there is a need to explore the aspects of cost, flexibility and bioequivalence. The present review provides a comprehensive account of various 3D printing technologies and highlights the opportunities and key challenges of 3D printing relevant to pharmaceuticals.

Thymoquinone (TQ) is a potent phytoconstituent from Nigella sativa and well recognized for its neuroactivity via antioxidant mechanisms, but its higher lipophilicity and plasma protein binding lowers its bioavailability negating any appreciable clinical outcome, thus losing the possibility to form any conventional dosage form. TQ's brain targeted drug delivery can result into an increased efficacy and bioavailability, thus, in a novel attempt, we aim to formulate brain targeted Polysorbate-80 coated thymoquinone PLGA nanoparticles (P-80-TQN) and evaluate their activity towards Alzheimer's disease. The modified single-emulsion solvent-evaporation technique was employed to formulate the TQN and further coated by Polysorbate-80 to obtain brain targeted P-80-TQN. The effectiveness of TQ released from P-80-TQN was evaluated in Alzheimer's (AD), biochemically by Super-Oxide Dismutase (SOD) enzymatic assay and behaviorally by Despair Test in Streptozotocin-(STZ)-induced Alzheimer's mice models at 5 mg/kg TQ-equivalent dose. AD markers: β-amyloid tangles were validated through histopathology of the brain's hippocampal tissues from euthanized mice. A Stable and homogenous targeted P-80-TQN (226.2 nm, ζ = −45.6 mV) formulation was prepared and characterized physiochemically and spectrally. It significantly reduced the IT (39.45 ± 3.32 s), and increased SOD functioning (8.33 ± 2.61 units/mg) after treating mice for 28 days at 5 mg/kg equivalent P-80-TQN. An invitro biphasic cumulative release of TQ (59.10 ± 2.10) from P-80-TQN was observed over 24 h, whereas invivo TQ release in brain from P-80-TQN was observed and explained in terms of AUC (0–600mins) and Cmax which were obtained 4.5 and 4.3 times respectively and Tmax was 3 times faster than normal TQ. A reduced and solvated protein aggregates (

Topical ocular delivery of therapeutics are always a challenging arena in order to achieve high ocular bioavailability with safe administration. Ideal ocular delivery of drug required 4 P's that is Patient compliance, Prolong retention, Penetration to cornea and Prolong release of drug. In an attempt to achieve desired characteristics for ocular delivery, Ketorolac loaded PLGA nanoparticles were fabricated by double emulsification solvent evaporation method and optimized by employing response surface methodology (RSM) followed by statistical analysis. Results obtained by RSM were further validated for fitness in model by different checkpoint formulations. Vitamin E TPGS was selected as emulsifier, which acquires high emulsifying capability and high permeability character. Zeta-size study revealed that optimized formulation has mean particle size 142.8 ± 11.7 nm, which was in agreement of TEM study and zeta potential was found −24.2 ± 1.2 mV. Encapsulation efficiency was achieved 63.5 ± 8.4%. Release profile was established by different mathematical modelling. It was observed that optimized formulation showed sustained release and followed by Korsmeyer-Peppas model. Corneal transport study showed enhanced drug permeation as compared to drug solution. HET-CAM test and histopathology studies revealed that optimized PLGA NPs was non-irritant and safe for ocular application.

Introduction: Ophthalmic formulations in terms of eye drops are more frequently used formulation for ocular disorders. But unfortunately this mode of drug instillation into the cul-de-sac of eye shows very poor ocular bioavailability (less than 5%). A large number of carrier systems have been investigated to overcome this problem. In the present study a novel nano-carrier system (Ketorolac loaded cubosomes) is developed and evaluated for the safe and enhance ocular bioavailability. Methods: Cubosomes were developed and optimized by utilizing glyceryl mono-oleate, poloxamer 407 and initial drug concentration. Finally developed formulation was evaluated for various in vitro characteristics i.e. particles size, size distribution, shape and morphology, in-vitro release profile, corneal permeation, corneal retention, and ocular tolerance study. Results: The optimized drug loaded cubosomal formulation showed mean particle size, polydispersity index, and entrapment efficiency 127.3±12.23 nm, 0.205±0.011, and 53.27±5.23 %, respectively. Transmission electron microscopic analysis revealed a cubic shape of developed formulation. Further, developed formulation exhibited biphasic release profile. Significant high transcorneal permeation (2.07 folds) and corneal retention (2.24 folds) of ketorolac was observed with cubosomal formulation correspond to Ketorolac solution (p

Introduction: Superiority of topical instillation of drug into the cul-de-sac for the treatment of various ophthalmic complications can be validated with commercial availability of a large number of conventional formulations even though this mode of instillation still elicits limitations owing to poor ocular bioavailability. To overcome the drawbacks of conventional formulations, a large number of novel carriers have been investigated. In this perspective, a new novel nanocarrier, chondroitin sulfate (ChS)-chitosan (CS)-nanoparticles (NPs) are being evaluated for improved delivery of bromfenac sodium. Materials and Methods: Formulation was developed and optimized for CS, chondroitin, and initial drug concentration. Optimized formulation was evaluated for various in vitro aspects i.e., particles’ size, size distribution, zeta potential, shape and morphology, in vitro release profile, corneal permeation, corneal retention, corneal uptake, and ocular tolerance test. Results: The mean particle size, polydispersity index, zeta potential, and entrapment efficiency of optimized formulation were found to be 245.6 ± 14.22 nm, 0.187 ± 0.016, +37.59 ± 4.05 mV, and 71.72 ± 4.43%, respectively. Transmission electron microscopic analysis revealed a spherical shape of developed formulation. Further, formulation exhibited biphasic release profile and Korsmeyer–Peppas model was found to be the best fit model. Significantly high transcorneal permeation (1.62-fold) and corneal retention (1.92-fold) of bromfenac was observed through ChS-CS-NPs when compared with marketed eyedrops (P < 0.01). Furthermore, high corneal uptake of CHSCS- NPs was confirmed by confocal laser scanning microscopy (CLSM). Safety profile of the developed formulation was established by hen’s egg test-chorioallantoic membrane test. Conclusion: Encouraging outcomes of in vitro and ex vivo studies indicated that CHS-CS-NPs could be a potential substitute for improved ocular delivery.

The biomedical applications of curcumin (CUR) are limited due to its poor oral bioavailability. In this work, CUR nanoparticles were successfully prepared by combining the supercritical anti-solvent (SAS) process with Tween 80 as a solubilizing agent and permeation enhancer. Different processing parameters that can govern the mean particle size and size distribution of nanoparticles were well investigated by manipulating the types of solvents, mixing vessel pressure, mixing vessel temperature, CO2 flow rate, solution flow rate and solution concentration. Solid state characterization was done by Fourier Transform infrared spectroscopy, differential scanning calorimetry, dynamic light scattering, scanning electron microscopy, and powder X-ray diffraction study. Solubility and dissolution profile of SAS-processed CUR were found to be significantly increased in comparison with native CUR. Further, a validated ultra-performance liquid chromatographic method with quadrupole-time of flight-mass spectrometry was developed to investigate the pharmacokinetic parameters after a single oral dose (100mg/kg) administration of CUR (before/after SAS-processed) in male Wistar rats. From the plasma concentration vs. time profile graph, oral bioavailability of SAS-processed CUR was found to be increased approximately 11.6-fold (p0.001) as compared to native CUR.

In the present study, we selected two potential herbal drugs (Smilax china and Salix alba) and developed nano lipidic carriers (NLC) gel for safe and effective topical therapy against psoriasis. Optimization of formulation of NLCs was performed using Box-Behnken design by selecting three input variables viz. lipid concentration, surfactant concentration and sonication time at three levels; and evaluated for the average particle size, polydispersity and %encapsulation as the response parameters. The outcomes of the present study showed that optimized dual drug-loaded NLCs had low average particle size (150.20 ± 3.57 nm) and polydispersity (0.301 ± 0.01) and high entrapment (86.32 ± 2.78% w/w). TEM imaging of the optimized formulation showed spherical vesicles. The drug release and dermal transport studies revealed sustained drug release (57.55 ± 5.38%) and enhanced dermal flux (3.88 μg/cm2/h), respectively. Thermo-analytical studies of NLCs showed fluidized state of the membrane of mice skin for smooth penetration of drugs. Confocal study revealed uniform distribution and deeper layer penetration of the optimized NLC gel system as compared to hydroalcoholic solution. Further, dermatokinetic study showed improved penetration of drug-loaded NLC gel in mice skin than the marketed formulation. The score obtained from skin irritation study revealed non-irritancy of the developed system. Further, in the developed psoriatic model, PASI score established decline in all the parameters as compared to the toxic control group, as well as better efficacy than the marketed formulation. Hence, the obtained results construe that developed NLCs as potential carriers for the effective and safe topical delivery of herbal drugs.

A novel, accurate, precise and economical stability indicating Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) method, was developed and validated for the quantitative determination of ubidecarenone (UDC) in bulk drug, UDC marketed formulation and UDC loaded cubosomes (CBMs) nanocarriers through Response surface methodology (RSM) design with three factors and three levels was performed to optimize the chromatographic variables followed by forced degradation studies of UDC were performed to detect degradation peak. RP-HPLC separation was achieved using mobile phase consisting of Acetonitrile:Tetrahydrofuran:Deionised water in the ratio 55:42:3 and a flow rate of 1.0 mL/min was optimized with a standard retention time (Rt) of 2.15 min, through experiment. The method was found linear in the concentration range of 5-100 µg/mL with a regression coefficient of 0.999. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 3.04 µg/mL and 9.11 µg/mL, respectively.