Development and Optimization of Mucoadhesive Microspheres of Miconazole Nitrate

Abstract

Vulvovaginal candidiasis (vaginal thrush) is common fungal infection caused by candida albicans in vaginal canal.
The physiology mechanism of vaginal cavity offers problem of draining out of formulations with vaginal irrigation.
The currently available formulation also shows problem of shorter resident time in the vaginal lumen and have
feeling of uncomfort and uneasiness due to size and shape of dosage forms. Miconazole nitrate is choice of drug for
the treatment of vulvovaginal candidiasis. The objective of present research work was to formulate controlled
release mucoadhesive microspheres of miconazole nitrate by spray drying technique and compressing it to tablet
dosage form which should disintegrate into microspheres at the site and adhere to the vaginal lumen, hence releasing
the drug for longer duration of time. Formulation variables were optimized using three factor, three level BoxBehnken design composed of HPMC K100M (X1), Eudragit RSPO (X2), Ethyl cellulose 100CP (X3) as
independent variables. The response surface methodology was employed and was optimized for the response
variables, viz., entrapment efficiency and cumulative % drug release at different time intervals. The %
mucoadhesion of optimized microspheres formulation was found to be 90 % after 8 hours of microspheres
application. The tablet will disperse after contacted with vaginal fluid in the form of mucoadhesive microspheres
and adhere with mucosal surface and consistently release the drug upto 12 hr.