ABSTRACT:
Tretinoin (TRT) is a metabolite of vitamin A, which is indicated primarily in the topical treatment of comedonal and papulopustular Acne vulgaris. TRT suffers several disadvantages which can strongly limit its utility. To overcome problems associated with topical delivery of TRA in the plain form, microsphere based sustained delivery formulation were studied in present research. Topical microspheres of tretinoin were prepared using different methods (double emulsification and solvent evaporazation) and compared. Microspheres of tretinoin prepared in this study were nearly spherical. SEM pictures indicated spherical particles with smooth surface and free of surface irregularities. The particle size range of microspheres was between 20-150 micrometer, which is suitable enough for the preparation of topical gel formulations. The drug entrapment efficiency by both method of preparation was admirable. Nearly 90% of the drug content of microspheres was released in 12 hrs. In vitro drug release from microspheres indicated Zero and Higuchi kinetics of drug release pattern. Prepared microsphere based formulation helps in molecular tretinoin movement at the skin surface l rather than the crystalline form of tretinoin, which may cause irritation and other skin disorders. Side effects of tretinoin are reduced dramatically when it is applied as microbased formulation which also adds in faster absorprion of drug via skin surface. Microsperes also helps in protecting Tretinoin against photo-degradation.