Fabrication and characterization of chitosan-carbopol-71G polyelectrolyte complex-based mucoadhesive pellets of miconazole nitrate for vaginal candidiasis

Devegowda Vishakante Gowda*, A

Abstract

Various approaches have been used in the past to overcome the problems associated with the delivery of antifungal drugs, for effective treatment of vaginal candidiasis. In the present investigation, mucoadhesive polyelectrolyte complex pellets (MPECP) loaded with Miconazole nitrate (MN) were prepared using chitosan/carbopol-71G interpolymer complex (IPC) by Fluid Bed Process (FBP) method. IPC was prepared by precipitation method, followed by characterization with Fourier transform infrared spectroscopy (FT-IR) and Differential scanning calorimeter (DSC). The prepared MPECP were tested for physicochemical properties, in vitro drug release behavior, swelling studies and mucoadhesive strength. The possibility of chemical interaction between drug and excipients was ruled out in the prepared pellets as confirmed by FT-IR and DSC studies. SEM photomicrographs showed that pellets had rough surface and were spherical. The dissolution behavior of MN from MPECP into the simulated vaginal fluid (SVF) pH 4.2 was controlled and followed non-fickian release mechanism. Moreover, in vitro mucoadhesive study confirmed that complex MP3 showed pH independent controlled releases of MN without an initial burst release, with highest mucoadhesive property and satisfactory residence in vaginal cavity (8h) of rat. The adherence of swelled pellets (MP3), for over 8 hrs, to the vaginal mucous membrane was confirmed by in vivo X-ray studies. The results showed no significant change in the pellet properties and drug content. Thus, the formulated MPECP seems to be a potential candidate for controlled release of MN in vaginal pH with optimum swelling behavior and zero order release.

Relevant Publications in Journal of Chemical and Pharmaceutical Research