聚合物囊泡与传统脂质体相比提高抗癌药物氟他胺口服生物利用度的研究进展。
Elaboration of polymersomes versus conventional liposomes for improving oral bioavailability of the anticancer flutamide.
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
出版信息
Nanomedicine (Lond). 2018 Dec;13(23):3025-3036. doi: 10.2217/nnm-2018-0238. Epub 2018 Dec 3.
AIM
Flutamide is an outstanding anticancer drug with poor oral bioavailability. This is the first work to investigate the potential of polymersomes versus conventional liposomes to improve flutamide bioavailability.
MATERIALS & METHODS: Polymersomes were prepared by solvent-switching technique and successfully optimized with excellent nanometric size (143 nm) and ζ-potential (-33.4 mV). Physicochemical characterization, stability in gastrointestinal tract and in vivo oral pharmacokinetics in male Sprague-Dawely rats were performed.
RESULTS
A significantly higher stability in simulated intestinal fluid was demonstrated by polymersomes compared with liposomes. Great improvement in flutamide oral bioavailability in polymersomes compared with both liposomes and drug suspension was obtained.
CONCLUSION
Polymersomes are promising nanoplatforms to overcome stability problems of liposomes and to improve flutamide oral bioavailability.
目的
氟他胺是一种具有较差口服生物利用度的优秀抗癌药物。这是首次研究聚合物囊泡相对于传统脂质体来提高氟他胺生物利用度的潜力。
材料与方法
采用溶剂转换技术制备聚合物囊泡，并成功进行了优化，得到了具有优异纳米尺寸（143nm）和 ζ-电位（-33.4mV）的聚合物囊泡。对其进行了理化特性表征、在胃肠道中的稳定性以及雄性 Sprague-Dawely 大鼠体内的口服药代动力学研究。
结果
聚合物囊泡在模拟肠液中的稳定性明显优于脂质体。与脂质体和药物混悬剂相比，聚合物囊泡可显著提高氟他胺的口服生物利用度。
结论
聚合物囊泡是一种有前途的纳米平台，可以克服脂质体的稳定性问题，并提高氟他胺的口服生物利用度。
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