伊曲康唑
生物利用度
环糊精
聚乙烯醇
溶解度
材料科学
溶解
渗透
药物输送
药理学
药品
刺激
β-环糊精
体内
核化学
药代动力学
抗真菌
皮肤病科
色谱法
有机化学
医学
化学
生物化学
生物技术
膜
免疫学
生物
作者
Risky Arya Putri,Cindy Kristina Enggi,Sulistiawati Sulistiawati,Habiburrahim Burhanuddin,Israini Wiyulanda Iskandar,Rizki Rachmad Saputra,Latifah Rahman,Sartini Sartini,Yusnita Rifai,Muhammad Aswad,Andi Dian Permana
标识
DOI:10.1080/09205063.2024.2380129
摘要
Itraconazole (ITZ) is one of the broad-spectrum antifungal agents for treating fungal keratitis. In clinical use, ITZ has problems related to its poor solubility in water, which results in low bioavailability when administered orally. To resolve the issue, we formulated ITZ into the inclusion complex (ITZ-IC) system using β-cyclodextrin (β-CD), which can potentially increase the solubility and bioavailability of ITZ. The molecular docking study has confirmed that the binding energy of ITZ with the β-CD was −5.0 kcal/mol, indicating a stable conformation of the prepared inclusion complex. Moreover, this system demonstrated that the inclusion complex could significantly increase the solubility of ITZ up to 4-fold compared to the pure drug. Furthermore, an ocular drug delivery system was developed through dissolving microneedle (DMN) using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA) as polymeric substances. The evaluation results of DMN inclusion complexes (ITZ-IC-DMN) showed excellent mechanical strength and insertion ability. In addition, ITZ-IC-DMN can dissolve rapidly upon application. The ex vivo permeation study revealed that 75.71% (equivalent to 3.79 ± 0.21 mg) of ITZ was permeated through the porcine cornea after 24 h. Essentially, ITZ-IC-DMN exhibited no signs of irritation in the HET-CAM study, indicating its safety for application. In conclusion, this study has successfully developed an inclusion complex formulation containing ITZ using β-CD in the DMN system. This approach holds promise for enhancing the solubility and bioavailability of ITZ through ocular administration.
科研通智能强力驱动
Strongly Powered by AbleSci AI