Abstract
Clotrimazole (CLO) is a strong antifungal drug approved to treat vaginal candidiasis (VC). Nanosponges (NSs) were developed to maintain providing CLO in a steady pattern with amplified accumulation in the vaginal mucosa. The quasi-emulsion solvent diffusion method was utilized to prepare NSs. The optimized NSs selected by Design Expert® exhibited a production yield percent (PY%) of 60.10±0.39%, encapsulation efficiency percent (EE%) of 91.21±0.59%, particle size (PS) 275.50±0.97nm, polydispersity index (PDI) 0.425±0.01, and zeta potential (ZP) of -27.40±0.25mV. The morphological results confirmed a spongy, porous structure. Fourier Transform Infrared Spectroscopy ensured the drug encapsulation. Differential scanning calorimetric studies showed no interaction between the excipients and CLO. The prepared NSs-loaded gel of optimized CLO-NSs was evaluated, the mucoadhesive strength (6065.85±52.03 dyne/cm2) with spermicidal activity of (0% sperm motility/60s). The ex-vivo deposition depicted significantly increased vaginal retention of CLO by 2.44-fold compared to Candistan® 2% vaginal cream (the market product). Finally, the in-vivo study on rats demonstrated thesuperior efficacy of CLO-NSs gel relative to Candestan®, with significantly reduced inflammatory biomarkers and minimal histopathological alterations in the treatment of vaginal candidiasis with a high safety profile.
Published Version
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