Sustained delivery of statistically optimized transfersomal gel of miconazole nitrate for vaginal candidiasis

Miconazole nitrate (MN), an antifungal drug with poor solubility, is used in the treatment of vaginal candidiasis. Conventional vaginal formulations have lower residence time and poor drug penetration resulting in the recurrence of the infection. Hence, transfersomes were formulated that would alleviate fungal infection by improving drug solubility and allowing effective permeation through the vaginal mucus and epithelium. MN-loaded transfersomes (MN-TF) were prepared by the thin film method. The optimization of the MN-TF was done by using 3(2) full factorial design. The Lipoid S100 (R) and Tween 80 (R) were selected as the phospholipid and edge activator, respectively. The responses, such as particle size, PDI, and entrapment efficiency were studied and found to be 180.70 +/- 2.11 nm, 0.293 +/- 0.012, and -13.2 +/- 1.3 mV, respectively. The optimized MN-TF was incorporated into the thermosensitive gel. The morphological study through TEM confirmed the nano size of the formulation. The FTIR study showed compatibility between the drug and excipients. The microbiological screening was performed against Candida albicans which showed a higher zone of inhibition for MN-TF than the marketed gel. The ex vivo transvaginal permeation study was done for MN-TF gel and compared with the marketed gel Daktarin (R). The permeability of the MN-TF was increased by 5.8-folds as compared to the marketed gel. The HET-CAM assay for the MN-TF gel demonstrated no irritation and hence was nontoxic and safe for vaginal administration. Therefore, the MN-TF gel had sustained drug release.