Formulation and evaluation of fluvastatin sodium drug-in-adhesive transdermal system

Abstract

Current investigation is aimed at designing a fluvastatin sodium loaded drug-in-adhesive patch (DIA Patch) to overcome the problems associated with the daily oral administration of the drug. The patches were prepared by solvent casting method using acrylate emulsion polymers like covinax 525-78, mowinyl 461 and novacryl PSR32 which served as sustained release matrix polymer and adhesive. Methocel K-15M was added as a solubilizer whereas transcutol, oleic acid and isopropyl myristate were tried as permeation enhancers for the drug-in-adhesive patch. The combination of mowinyl-isopropyl myristate patch was further optimized by 3 2 factorial design to study the effect of two independent variables i.e. concentration of solubilizer and permeation enhancer on responses i.e.% drug release, tensile strength and peel adhesion strength. The formulation was further evaluated for its lipid lowering activity and skin irritation index. The % cumulative release of drug at the end of 24 h was found to be 87.74%. The formulation shows tensile strength of 12.75 kg/cm 2 and peel adhesion strength of 32.44 N/25 mm. The Primary irritation index (PII) for DIA patch was found to be 0.22. The fluvastatin sodium loaded DIA patch significantly inhibits serum cholesterol and triglyceride levels as compared to oral control (p<0.01) in triton WR 1339 induced hyperlipidemic rat. Hence the developed transdermal patch could be acceptable for transdermal use.

A review on transdermal drug delivery system

“…For instance, Atorvastatin provides a bio-availability not more than 14% and only about 5% of Simvastatin enters into the general circulation. This is due to the first-pass metabolism in the liver and the clearance by the digestive system (9) . Transdermal delivery systems are currently available containing Scopolamine (Hyoscine) for motion sickness, Clonidine and Nitro-glycerine for cardiovascular disease, Fentanyl for chronic pain, Nicotine to aid smoking cessation, Estradiol (alone or in combination with Levonorgestrel or Norethisterone) for hormone replacement and testosterone for hypogonadism.…”

Development and Characterisation of a Topical Methyl Salicylate Patch: Effect of Solvents on Adhesion and Skin Permeation

“…Percutaneous absorption can deliver drugs to the body or the skin, and this has become a popular route due to its convenience and user-friendly administration [1][2][3][4]. Given such advantages, topical administration can allow for better patient compliance and reduced dosing frequency, with the possibility of withdrawing immediately [5][6][7][8][9][10].…”

“…A total of six solvents were chosen based on the different solvent groups and their physicochemical properties, including propylene glycol (PG), Transcutol ® P (TRC), isopropyl myristate (IPM), Labrasol ® (LA) or caprylocapropyl macrogol-8 glycerides, Plurol ® oleique CC 497 (PLU) or polyglyceryl-3 dioleate and Maisine ® CC (MAI) or glycerol monolinoleate. These solvents are also generally regarded as safe and have been previously used for skin patch formulations [4,[33][34][35][36][37][38][39][40][41][42].…”