作者
Andi Dian Permana, Emilia Utomo, Muhammad Rezky Pratama, Muh Nur Amir, Qonita Kurnia Anjani, Sandra Aulia Mardikasari, Sumarheni Sumarheni, Achmad Himawan, Andi Arjuna, Usmanengsi Usmanengsi, Ryan F Donnelly
发表日期
2021/4/12
期刊
ACS Applied Materials & Interfaces
卷号
13
期号
15
页码范围
18128-18141
出版商
American Chemical Society
简介
The poor solubility of itraconazole (ITZ) has limited its efficacy in the treatment of vaginal candidiasis. Accordingly, the improvement of ITZ solubility using a solid dispersion technique was important to enhance its antifungal activity. Besides, as the purpose of this research was to develop local-targeting formulations, bioadhesive-thermosensitive in situ vaginal gel combined with the gel-flake system was found to be the most suitable choice. To obtain optimum solubility, entrapment efficiency, and drug-loading capacity, optimization of solid dispersion (SD) and gel-flake formulations of ITZ was performed using a composite central design. The results showed that the optimized formulation of SD-ITZ was able to significantly enhance its solubility in both water and simulated vaginal fluid to reach the values of 4.211 ± 0.23 and 4.291 ± 0.21 mg/mL, respectively. Additionally, the optimized formulation of SD-ITZ gel flakes …
引用总数