DEVELOPMENT AND CHARACTERIZATION OF CRISABOROLE LOADED INVASOMAL GEL FOR EFFECTIVE TOPICAL ANTI-INFLAMMATORY EFFECT

Abstract

The present study aimed to develop and characterize a Crisaborole-loaded invasomal gel to enhance topical anti-inflammatory efficacy. Invasomes were prepared using phosphatidylcholine, ethanol, and terpenes by the thin-film hydration method and optimized based on vesicle size and entrapment efficiency. The optimized formulation (IN2) exhibited a vesicle size of 185.65 nm and an entrapment efficiency of 82.26 ± 0.36%, indicating uniform and stable vesicle formation. The optimized invasomes were incorporated into a Carbopol gel base to obtain an effective topical delivery system (IG-2). The invasomal gel displayed excellent viscosity (3425 cps), pH (5.8), drug content (99.12%), and good spreadability and extrudability properties, suitable for dermal application. In-vitro drug release studies revealed a sustained release pattern of 96.65% over 12 hours compared to the pure drug, demonstrating improved permeation and prolonged activity. Kinetic analysis showed that the drug release followed first-order kinetics with an R² value of 0.9702, suggesting a diffusion-controlled mechanism. Stability studies indicated that the formulation remained physically and chemically stable over 6 months under refrigerated and ambient conditions. The developed Crisaborole-loaded invasomal gel proved to be a promising, stable, and effective system for topical anti-inflammatory therapy, offering better penetration, sustained release, and patient compliance compared to conventional formulations.

KEYWORDS:

Crisaborole, Invasomes, Phosphatidylcholine, Topical gel, Anti-inflammatory, Entrapment efficiency, Sustained release, Stability study.