Formulation Consideration and Skin Retention-Permeation Study of Insitu Nanogel Containing Dimethylfumarate for Treatment of Psoriasis

Aims and Objective: to develop and evaluate an insitu nanogel formulation containing dimethylfumarate for targeted topical delivery therapy of psoriasis. Study Design: 32 full factorial design Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2016 to 2019. Methodology: Nanogel were formulated by chemical cross linked gel method using Polyvinyl alcohol and Hyaluronic acid (1:5) ratio using Glutaraldehyde (GA) (25 %w/v) and Hydrochloric acid (HCl) (6%v/v) as a crosslinking agent and catalyst. Dimethylfumarate loaded nanogel were clear and showed physicochemical parameters desired for topical delivery and stability. Results: The Permeation profile of dimethylfumarate through rat skin from selected nanogel formulation exhibited highest skin uptake. The Micoscopic observations indicated that the optimized nanogel had n significant effect on the microscopic structure of the sin and epithelial cells appered mostly unchanged. The surface epithelium lining and the granular cellular structure of the skin were totally intact. The developed Nanogel may be a potential drug delivery vehicle for targeted topical delivery of dimethylfumarate in the treatment of psoriasis. Conclusion: As per drug retention study the highest amount of drug retained on the skin and lowest amount of drug permeate to the skin. Hence it was observed that there was no significant correlation between skin retention and skin permeation study.

Chitosan (Poly-(D) glucosamine) based solid lipid nanoparticles of dexibuprofen for topical delivery: Formulation development and characterizations

Chitosan a poly-(D) glucosamine is a polysaccharide made by treating shrimp and other crustacean shells with the alkali sodium hydroxide. It is a hydrophilic polymer that helps to retain the drug inside the solid lipid nanoparticles (SLN’s) and prolongs the release of drug from the carrier system. The purpose of the study was to formulate Chitosan decorated SLN’s for the topical delivery of dexibuprofen by hot pressure homogenization technique. Blank SLN’s, drug loaded SLN’s and Chitosan decorated SLN’s were prepared. Particle size, zeta potential and PDI were determined. FTIR study was conducted to evaluate the compatibility of excipients with the active drug. Surface morphology of SLN’s was determined by field emission scanning electron microscope. Drug content and entrapment efficiency of SLN’s were determined using indirect method. In vitro release and ex vivo permeation study of SLN’s were carried out using Franz diffusion cell. The droplet size fell into the nano range i.e. 132±7 to 424±2 nm which is effective for topical drug delivery system. The PDI of formulations range from 0.21 to 0.42 which depicts the homogeneity of all the SLN’s formulations. Vibrational analysis indicates that there is no interaction between active drug and excipient used in the formulation. The surface morphology revealed the spherical shape of Chitosan decorated SLN’s. The in vitro release of formulations showed 79.91±1.07 to 89.94±1.8 % drug release. The drug permeation study showed high permeation of drug into the skin. The percent drug permeation ranges from 64.15±0.93 to 71.80±0.88% indicating good permeation of drug across the skin. Overall, SLN’s are an effective carrier for topical delivery of dexibuprofen and thus bypasses side effects associated with oral delivery.

Formulation of Piperine–Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

Development, optimization and characterization of flurbiprofen matrix transdermal drug delivery system using Box–Behnken statistical design

Background Present investigation for research was to develop matrix-type transdermal drug delivery system of flurbiprofen (FBP) with the various ratio of matrix polymers (hydrophilic and hydrophobic), the concentration of plasticizer and natural penetration enhancer by Box–Behnken statistical design to investigate the combined outcome of selected independent variables for effective management of rheumatoid arthritis. The influence of a binary mixture of polymers, plasticizer and penetration enhancer on physicochemical considerations including thickness, tensile strength, percent elongation, weight variation, percent moisture content, percent moisture uptake, water vapour transmission rate, folding endurance, drug content, in vitro drug dissolution study and then ex vivo drug permeation study was evaluated. Results The study demonstrated that the tensile strength of films improved by matrix polymer ratio and to a slighter gradation in the rise of plasticizer and natural penetration enhancer. Ex vivo drug permeation study was accompanied via excised porcine skin as a permeation barrier in Franz diffusion cell. Ex vivo drug permeation study indicated that matrix polymer ratio (HPMC K15M:ERL100) at 3:1 and natural penetration enhancer (d-limonene) at highest concentration 7.5% w/w containing formulation FBPT7 delivered maximum flux and supplementary improved the permeation of drug. The result of the skin irritation test revealed that the developed formulation is free from any type of skin irritation effects like erythema and oedema. Conclusion Based on the findings of this research, it can be established that a well-controlled release and very effective skin penetration of the drug was accomplished by the film FBPT7 in the existence of permeation enhancers for prolonged periods.

A Comparative Formulation Development and Evaluation of Tazarotene Ethosomal and Transfersomal Gel for Effective Management of Acne

Acne vulgaris is the most prevalent disorder in the period before puberty when increased adrenal androgen level causes enlargement of the sebaceous glands and it increased the production of sebum on the face, chest, and back. This disease is caused due to interaction between many causative agents or pathogenic components which lead to formation of the acne and those are seborrhea, follicular hyper keratinization, microbial formation of pilosebaceous unit by Propionibacterium acne and arrival of inflammatory mediators. Tazarotene is a well-known retinoid related to vitamin A that belongs to an acetylenic class of retinoid, used in the management of acne. Oral administration of Tazarotene causes changes in bone morphology after prolonged exposure to high doses, which also exhibit teratogenicity but this does not occur with topical delivery. Ethosomes are non-invasive delivery carriers enabling drugs to reach to the bottom of the skin layers and/or the system and transfersomes are the self-adaptable ultra-deformable flexible elastic bilayer vesicles composed of phospholipids able to penetrate through the pores of skin even smaller than its size. Present research aims the comparative evaluation of ethosomal and transfersomal gels loaded with Tazarotene in the treatment of acne. In the present study, ethosomes and transfersomes were formulated by the cold method and hand-shaking method, respectively, followed by loading of Tazarotene and development into gel formulation. The formulated gel samples were evaluated for in vitro release study, in vitro permeation study, in vitro anti-acne study, in vivo percutaneous permeation study by CLSM, and in vivo anti-acne study. The results proved that both the formulated ethosomal and transfersomal gels have better permeation through the skin but ethosomal gel showed better release in comparison to transfersomal gel, also final gels exhibited the anti-acne potentiality.

Exploration of neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex based film for transdermal delivery of protein/peptide

Present investigation is continuation of author’s previously published work. In the present investigation, the author has prepared neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex transdermal film for the delivery of protein/peptide drug. Concentration of gum (neem gum and kheri gum) and chitosan was varied in each concentration while drug concentration kept constant. Albumin was used as a model protein drug. Transdermal films were fabricated using a solvent casting method without using any plasticizer and evaluated for various parameters viz. folding endurance, surface pH, weight variation, drug content, percentage moisture content, surface morphology, in vitro drug release and ex vivo drug permeation study. The study showed that films were successfully fabricated with good acceptable physical properties. In vitro drug release study and ex vivo drug permeation study showed that polyelectrolyte films were able to extend drug delivery up to 9 days. It can be easily concluded from the findings of the results that neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex films can be easily prepared without using any plasticizer and able to deliver protein/peptide therapeutic agents for an extended period of time.