Factors affecting on in vitro release of miconazole from in situ ocular gel

Abstract

The reason for conducting this study is to prolong release of miconazole in the ocular site of action by ocular-based gels (OBGs) formulations. The formulation factors affecting on the release from OBG should be studied using various gelling agents in various concentrations to achieve the improvement in retention and residence time in response to prolonged release. In this study, the formulations were prepared using carbopol 940, pectin, sodium alginate, poloxamer 407, and poly(methacrylic acid) at 0.5%, 1%, and 1.5% w/v, respectively. Hydroxypropyl methylcellulose E5 (HPMC E5) 1% was added as thickening agent/viscosity builder. The formulation containing carbopol 940, pectin and sodium alginate at 1.5% w/v, displayed a noticable improvement in viscosity, gelling capacity, and extended release for 7 h in comparison with the reference drug. Overall, the release showed that the sodium alginate with HPMC E5 form in situ gel which had longer time of release reach to 12 h compared with other polymers. the release of miconazole from the OBGs affected significantly by two factors includes gelling capacity and viscosity builder. The novelty of this study is supporting the delivery of ocular drugs through a cornea as an important key of the eye instead of dependence on an internal blood supply using an oral or a parental administration.

Keywords

• gelling capacity
• in situ gels and sodium alginate
• miconazole
• ocular
• poloxamer 407