Tripodo Giuseppe, Pasut Gianfranco, Trapani Adriana, Mero Anna, Lasorsa Francesco Massimo, Chlapanidas Theodora, Trapani Giuseppe, Mandracchia Delia
Department of Drug Sciences, University of Pavia , Viale Taramelli 12, 27100 Pavia, Italy.
Biomacromolecules. 2015 Feb 9;16(2):550-7. doi: 10.1021/bm501616e. Epub 2015 Jan 14.
The aim of this work was to evaluate the potential of INVITE-based nanomicelles, an amphiphilic polymer constituted by inulin (INU) and vitamin E (VITE), as a platform for improving the biopharmaceutical properties of hydrophobic drugs. For this purpose, curcumin was selected as a model and curcumin-INVITE nanomicelles were prepared. This drug delivery system was characterized both in vitro for what concerns the physicochemical properties, blood compatibility, and cellular uptake, and in vivo for the evaluation of the pharmacokinetic profile. It was found that these nanomicelles released curcumin in a controlled manner, and they were able to penetrate cellular membrane. Moreover, they showed an improved pharmacokinetic profile after intravenous administration. In conclusion, INVITE micelles might constitute promising nanocarriers for improving the biopharmaceutical performance of hydrophobic drugs.
本研究的目的是评估基于菊粉（INU）和维生素E（VITE）构成的两亲性聚合物——基于INVITE的纳米胶束作为改善疏水药物生物药剂学性质平台的潜力。为此，选择姜黄素作为模型并制备了姜黄素-INVITE纳米胶束。该药物递送系统在体外针对其物理化学性质、血液相容性和细胞摄取进行了表征，在体内则用于评估药代动力学特征。结果发现，这些纳米胶束以可控方式释放姜黄素，并且能够穿透细胞膜。此外，静脉给药后它们显示出改善的药代动力学特征。总之，INVITE胶束可能构成用于改善疏水药物生物药剂学性能的有前景的纳米载体。
