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载有胆固醇和抗坏血酸的两亲性共聚物聚丙烯酸酯的生物纳米粒子用于药物传递。

Bionanoparticles of amphiphilic copolymers polyacrylate bearing cholesterol and ascorbate for drug delivery.

机构信息

State Key Laboratory of Chemical Resource, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China.

出版信息

J Colloid Interface Sci. 2012 Jul 1;377(1):197-206. doi: 10.1016/j.jcis.2012.04.004. Epub 2012 Apr 10.

Abstract

In this study, a series of amphiphilic polymers with poly(ascorbyl acrylate) (PAAA) as hydrophilic blocks and polyacrylate bearing side-chain cholesteryl mesogens (PCholDEGA) as hydrophobic blocks were prepared using a combination of four-step reactions consisting of two consecutive reversible addition-fragmentation chain transfer (RAFT), desulfurization, and hydrogenolysis under normal pressure. The thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) as well as wide-angle X-ray diffraction (WAXD) studies showed that the copolymers with PCholDEGA as major block had relatively high stability and clear isotropization temperature (T(i)). Small-angle X-ray diffraction (SAXD) investigation exhibited that the copolymers had bilayer smectic A structure. Their self-assembly behavior was monitored by turbidity change using UV-vis spectrometer, and the morphology and size of the nanoparticles via self-assembly were detected using transmission electron microscopy (TEM) and dynamic light scattering (DLS). The entrapment efficiency and loading capacity of these amphiphilic copolymers were investigated using nile red and drug molecule Ibuprofen. These polymeric micelles with PAAA shell extending into the aqueous solution and strong hydrophobic PCholDEGA core have potential abilities to act as promising nanovehicles with high loading and targeting delivery.

摘要

在这项研究中,通过四步反应(包括两次连续的可逆加成-断裂链转移(RAFT)、脱硫和常压下的氢解),制备了一系列具有聚(抗坏血酸丙烯酯)(PAAA)作为亲水嵌段和带有侧链胆甾醇介晶基元的聚丙烯酸酯(PCholDEGA)作为疏水嵌段的两亲聚合物。热重分析(TGA)和差示扫描量热法(DSC)以及广角 X 射线衍射(WAXD)研究表明,以 PCholDEGA 为主要嵌段的共聚物具有相对较高的稳定性和清晰的各向同性温度(T(i))。小角 X 射线衍射(SAXD)研究表明,共聚物具有双层近晶 A 结构。通过紫外-可见分光光度计监测浊度变化来监测它们的自组装行为,并通过透射电子显微镜(TEM)和动态光散射(DLS)检测自组装形成的纳米粒子的形态和尺寸。使用尼罗红和药物分子布洛芬(Ibuprofen)研究了这些两亲性共聚物的包封效率和载药量。这些具有 PAAA 壳延伸到水溶液中的聚合物胶束和具有强疏水性 PCholDEGA 核的聚合物胶束具有作为具有高载药量和靶向递送的有前途的纳米载体的潜在能力。

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