Transport of Zidovudine-and Lamivudine-Loaded Polybutylcyanoacrylate and Methylmethacrylate-Sulfopropylmethacrylate Nanoparticles across the In Vitro Blood-Brain Barrier: Characteristics of the Drug-D

Zidovudine和Lamivudine負載於Polybutylcyanoacrylate和Methylmethacrylate-Sulfopropylmethacrylate奈米粒子上的生體外血腦屏障穿透：藥物釋放系統的特性

郭勇志(Yung-Chih Kuo) ； 鍾秋燕(Chiu-Yen Chung)

《Journal of the Chinese Institute of Chemical Engineers》 36卷6期 (2005/11) Pp. 627-638

https://doi.org/10.6967/JCICE.200511.0627

摘要

本文探討負載於polybutylcyanoacrylate (PBCA)和methylmethacrylate-sulfopropylmethacrylate (MMA-SPM)上的zidovudine (AZT)和lamivudine (3TC)對生體外血腦屏障的穿透行為。牛腦微血管內皮細胞(BBMEC)緻密單層膜可由初代分離與培養的技術獲得，而由免疫細胞化學螢光法，可證實BBMEC的同質均一性和單層膜的緊密細胞間接合。此外，對膠體藥物載體系統而言，PBCA和MMA-SPM奈米粒子的平均粒徑分別為92nm和78nm，且幾乎為單一粒徑分佈。在對BBMEC單層膜的穿透研究中，AZT和3TC結合奈米粒子載體的穿透量遠高於非載體系統的穿透量，這說明了奈米粒子載體可有效改善藥物的腦部標的釋放。由比較此二奈米粒子扮演AZT和3TC載體的功能，可知負載於PBCA上的穿透量超過負載於MMA-SPM上的一倍半。

並列摘要

Transport study of zidovudine (AZT) and lamivudine (3TC) loaded on polybutylcyanoacrylate (PBCA) and methylmethacrylate-sulfopropylmethacrylate (MMA-SPM) nanoparticles (NPs) across the in vitro blood-brain barrier (BBB) model system was presented. Through primary culture, confluent monolayer of bovine brain-microvascular endothelial cells (BBMECs) with the feature of cellular homogeneity and tight intercellular junction was demonstrated by immunocytochemical fluorescent method. Besides, for the colloidal drug-carrier system, average diameters of the two nearly monodispersed PBCA and MMA-SPM nanospheres were, respectively, about 92 nm and 78 nm. The amount of AZT and 3TC across the current BBMEC monolayer in carrier-incorporated system was much higher than that in non-carrier system, suggesting sufficient amelioration in drug transport by employing the NP carriers for brain-targeting delivery. Comparing PBCA NPs with MMA-SPM NPs, the amount of drug (AZT and 3TC) across the in vitro BBB system for the former was in excess of 1.5 times that for the latter.

並列關鍵字

Blood-brain barrier ； Zidovudine ； Lamivudine ； Polybutylcyanoacrylate ； Methylmethacrylate-sulfopropylmethacrylate ； Nanoparticle