Abstract
In this study, bioadhesive mini-matrices of natamycin were prepared for vaginal application by hot-melt extrusion. In addition, melt viscosity measurements, thermogravimetric analysis, in vitro drug release studies and in vitro mucoadhesion test were performed. High molecular weight grades of KlucelTM hydroxypropylcellulose were used as a thermoplastic polymer. TEC and PEG 400 were chosen as plasticizer. According to the obtained results of melt viscosity measurements, the maximum torque of extrudates prepared using PEG 400 increased with increasing drug loading. The thermo-gravimetric analyses showed that natamycin is stable up to 198℃ and this result gives the opportunity to hot melt extrussion process at 90℃. In vitro drug release results showed that the release was extended up to 72 hours and drug release rate increased with increasing drug loading. In respect to the in vitro mucoadhesion test results, the values of work of mucoadhesion were found high as 771,977 mN.mm, 753,199 mN.mm, 686,356 mN.mm for the prepared hot melt extruded mini-matrices. Our results showed that the developed formulations were found worthy of further studies.
Highlights
Vaginal candidiasis (VC) often referred to as vulvovaginal candidiasis, is a common mucosal infection of vagina, mainly caused by Candida species
Bioadhesive mini-matrices of natamycin were prepared for vaginal application by hot-melt extrusion
In vitro drug release results showed that the release was extended up to 72 hours and drug release rate increased with increasing drug loading
Summary
Vaginal candidiasis (VC) often referred to as vulvovaginal candidiasis, is a common mucosal infection of vagina, mainly caused by Candida species. Apart from prolongation of drug release at the site of absorption, drug targeting to the affected site can be realized [11] [12] Fundamental thermodynamic quantities, such as surface free energies of both adhesive and substrate, determine the magnitude of the adhesive forces. An objective of the present study was to develop and produce vaginal mini matrices containing natamycin utilizing hot-melt extrusion technique to optimize drug delivery. Özgüney ing and evaluating this antifungal treatment modality using analytical, bioadhesion, dissolution, and thermal studies
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