a Department of Pharmaceutical Engineering , School of Biological Science and Technology, University of Jinan , Jinan , Shandong Province , PR China.
b School of Basic Medical Sciences, Dali University , Dali , Yunnan , PR China.
J Biomater Sci Polym Ed. 2018 Dec;29(18):2299-2311. doi: 10.1080/09205063.2018.1544457. Epub 2018 Dec 31.
A copolymeric micelle formulation of itraconazole (ITR-M) was prepared using linear-dendritic monoallyloxy poly (ethylene glycol)-b-poly (ε-caprolactone) (APEG-PCL) as drug carrier materials. DL and EE values of ITR-M were 5.70 ± 0.12% and 91.30 ± 1.90%, respectively. The micelle formulation enhanced the ITR solubility up to 30.42 μg/mL. In vitro release of ITR from the ITR-M was mainly drug diffusion process followed by the copolymer's degradation. ITR-M showed similar anti-Candida albicans activity to that of crude ITR although its release of ITR was slow and continuous. The in vivo pharmacokinetic study demonstrated that the ITR-M could improve tissue distribution of ITR. In conclusion, APEG-PCL could be a potential carrier in the development of antifungal drug delivery system.
采用线性树枝状单烯丙氧基聚（乙二醇）-b-聚（ε-己内酯）（APEG-PCL）作为药物载体材料，制备了伊曲康唑（ITR）的共聚胶束制剂。ITR-M 的 DL 和 EE 值分别为 5.70±0.12%和 91.30±1.90%。胶束制剂将 ITR 的溶解度提高到 30.42μg/mL。ITR 从 ITR-M 的体外释放主要是药物扩散过程，随后是共聚物的降解。尽管 ITR-M 释放 ITR 缓慢且持续，但它对白色念珠菌的抗真菌活性与粗 ITR 相似。体内药代动力学研究表明，ITR-M 可以改善 ITR 在组织中的分布。总之，APEG-PCL 可以成为开发抗真菌药物传递系统的潜在载体。
