紫杉醇-明胶纳米颗粒的药代动力学和生物分布

A. Verma, A. Chanchal, R. Pandey, R. Vohra, N. Islam, A. Misra
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引用次数: 3

摘要

纳米尺度的药物传递系统(dds)特性控制提供了相对于游离药物更好的药代动力学和药效学控制。本文综述了紫杉醇-明胶纳米颗粒(B型,75 Bloom)的制备及其在治疗中的应用,通过动态光散射(DLS)和透射电子显微镜(TEM)证实,其粒径范围为~ 150 ~ 200 nm,包封效率为~ 45%。PGN在肝癌HepG2细胞系中的剂量依赖性抗肿瘤可塑性可达72小时,且药物本身在24小时内显示65%的毒性(<1 (g))。在正常和荷瘤近交系Balb-c小鼠中进行的药代动力学和生物分布研究(终点为2、6、24和48小时)显示,PGN在肝脏和肿瘤中积累。观察到紫杉醇在肾脏中的蓄积增强。体内抗肿瘤研究表明,PGN可使肿瘤减少约三倍。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacokinetics and Biodistribution of Paclitaxel–Gelatin Nanoparticles
ABSTRACT Nanoscale manipulation of properties of drug delivery systems (DDSs) provides improved control over the pharmacokinetics and pharmacodynamics of encapsulated drugs relative to free drugs. This article summarizes the preparation and therapeutic applications of paclitaxel–gelatin nanoparticles (PGNs) (Type B, 75 Bloom) in the size range ∼150 to 200 nm as confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM), with ∼45% entrapment efficiency. Dose-dependent antineoplasticity in hepatocarcinoma, HepG2 cell line, was observed up to 72 h of incubation with PGN and the drug per se (<1 (g) showed 65% toxicity within 24 h). A pharmacokinetics and biodistribution study with endpoints at 2, 6, 24, and 48 h performed in normal and tumor-bearing, inbred Balb-c mice showed accumulation in liver and tumor with PGN. Enhanced paclitaxel accumulation in kidney was observed. In vivo antineoplastic studies showed an approximately threefold reduction of tumor with PGN.
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