Design and optimization of liquisolid compact based vaginal sustained release tablet of antifungal agent for vaginal candidiasis

Abstract

Antifungal therapy is causing an alarming drug resistance problem during the treatment of Vaginal Candidiasis and also many of the antifungal vaginal marketed formulations have reported major side-effect of the irritation. Hence the quest for natural therapy is currently booming. Lawsone is having poor aqueous solubility and its antifungal activity is therefore hindered. Therefore, the present research work aimed to formulate the liquisolid compact based vaginal tablet of Lawsone to improve its solubility and dissolution rate. The tablet was optimized by 3² full factorial design. The independent factors selected were carrier (Neusilin US2): coating material (Aerosil 200) ratio (R) and concentration of the mucoadhesive polymer (HPMC K4M) while the dependent factors studied were in vitro release (6 h and 12 h) and mucoadhesive strength. The drug was dispersed in nonvolatile solvent (polyethylene glycol 400) to prepare the liquid medicament that was further used for liquisolid compact. The FTIR, DSC and XRD studies revealed no incompatibility between Lawsone and the excipients of the tablet and suggested that the drug was dispersed completely into the liquid medication and therefore transformed from crystalline to amorphous state. In vitro release study suggested sustained release with enhanced dissolution of optimized liquisolid compact tablet LT7 (94.92%) than the plain tablet (61.16%). The in vitro antifungal activity against C. albicans, C. glabrata and C. krusei for liquisolid tablet and the marketed tablet formulation showed insignificant difference.

Graphical Abstract

Keywords:

• Vaginal tablet
• Lawsone
• Neusilin US2
• liquisolid compact
• sustained release
• antifungal activity

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This research received funding in the form of senior research fellowship to the first author from the Council of Scientific and Industrial Research, Delhi (India).