通过喷雾干燥法提高包裹在聚（ε-己内酯）纳米颗粒中的抗逆转录病毒药物依非韦伦的口服生物利用度。
Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method.
作者信息
Tshweu Lesego, Katata Lebogang, Kalombo Lonji, Chiappetta Diego A, Hocht Christian, Sosnik Alejandro, Swai Hulda
机构信息
Polymers & Composites, Council for Scientific & Industrial Research Materials Science & Manufacturing, Council for Scientific & Industrial Research, Pretoria, South Africa.
出版信息
Nanomedicine (Lond). 2014;9(12):1821-33. doi: 10.2217/nnm.13.167. Epub 2013 Dec 23.
AIM
To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs.
MATERIALS & METHODS: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method.
RESULTS
NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability.
CONCLUSION
EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance. Original submitted 2 May 2013; Revised submitted 4 September 2013.
目的
将依法韦仑（EFV）包裹于聚己内酯（PCL）纳米粒（NPs）中，并将其口服药代动力学与载有EFV的胶束及纯EFV NPs进行比较。
材料与方法
采用复乳/喷雾干燥法制备载有EFV的PCL NPs。
结果
NPs的流体动力学直径为200 - 250 nm。包封率为86 - 93%，质量回收率高于60%。X射线衍射表明，在喷雾干燥过程中药物和PCL发生了非晶化。包裹于NPs中显著提高了血浆中的最大浓度及生物利用度。
结论
载有EFV的PCL NPs是开发具有改善（生物）药学性能的可扩展药物的一个有前景的平台。原始稿件于2013年5月2日提交；修订稿件于2013年9月4日提交。
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