İzokonazol nitratın farklı siklodesktrin türevleri ile gerçekleştirilen kompleksleri üzerine çalışmalar

Isoconazole nitrate (ISN) is an anti-fungal active agent within azole family with superior anti-mycotic and antibacterial features. ISN has a wide variety of antimicrobial action against pathogenic yeasts, filamentous spores, dermatophytes, moulds and some Gram-positive bacteria. Many antifungal agents, even ISN, have lower aqueous solubility with variable dissolution kinetics. Literature review recommended the use of inclusion complexes of antifungal drugs-different cyclodextrin derivatives to enhance aqueous solubility and stability of active agents. ISN/β-CD, ISN/HP-β-CD and ISN/M-β-CD inclusion complexes were formulated by using two different techniques such as spraydrying and lyophilization method. The characterization of the prepared complexes were studied and according to the results of the characterization tests, a decision was taken to use spray-dried complexes in the following studies. In situ gel formulations containing spray-dried complexes were prepared by using Pluronic® F127 and HPMC based on their improved solubility, gelling features, stability, antimicrobial efficiency, rheological behavior and in vitro release characteristics. As a result, ISN/M-β-CD and ISN/HP-β-CD inclusion complexes included in situ gel formulations were considered as effective drug delivery systems to the vaginal therapy, owing to their prolonged-release behavior, stability and in vitro efficacy.