FORMULATION AND OPTIMIZATION OF LOVASTATIN MICROSPONGIC GEL FOR THE TREATMENT OF TOPICAL SUPERFICIAL ACTINIC POROKERATOSIS
Patel Shreya, Dr. Chainesh Shah, Patel Aarti, Patel Darshi, Dr. Umesh Upadhyay
Sigma Institute of Pharmacy, Sigma University, Bakrol, Vadodara-390019ABSTRACT: Microsponges are microscopic spheres with pores, known for their inert nature. These spheres typically range in size from 10 to 25 micrometers and are synthesized using the Quasi-emulsion solvent diffusion method, a specialized technique for controlled release formulations. Their unique structure allows for the controlled release of active drug ingredients, making them particularly valuable in topical drug products. By delivering drugs directly to the skin in a controlled manner, microsponges help minimize systemic exposure and reduce local skin reactions to active drugs. Lovastatin belongs to the class of drugs called statins, which are used to lower blood cholesterol levels being BCS class II drug, having low solubility and high permeability considered as suitable candidate for formulating as Microsponges to overcome the problem like side effect, short half-life and low bioavailability. Lovastatin is a cholesterol bringing down specialist and it is quickly hydrolyzed to beta- hydroxyacid which is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. It prevents the rate-limiting step in cholesterol biosynthesis, the conversion of HMG-CoA to mevalonate. Mutations in the mevalonate pathway gene are linked to porokeratosis. Remedial choices are not many and frequently restricted in viability. Porokeratosis might be alleviated by topical treatment that aims to replenish cholesterol, an essential end- product of the mevalonate pathway, and prevent the accumulation of toxic mevalonate pathway metabolites, we hypothesized. Lovastatin Microsponges have potential applications in topical drug delivery systems. Topically applied Lovastatin Microsponges can increase the residence time of drugs in epidermis, while reducing the systemic absorption of the drug.
KEY WORDS: Microsponges, Quasi Emulsion Solvent Diffusion Method, Porous Particles, HMG-Coa, Porokeratosis, Mutations