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一种基于硬脂酸修饰的裂褶多糖的新型自组装胶束,用于高效递送紫杉醇。

A novel self-assembled micelles based on stearic acid modified schizophyllan for efficient delivery of paclitaxel.

机构信息

Biotechnology Group, Chemical Engineering Faculty, Tarbiat Modares University, P.O.Box:14115-114, Tehran, Iran.

Biotechnology Group, Chemical Engineering Faculty, Tarbiat Modares University, P.O.Box:14115-114, Tehran, Iran.

出版信息

Colloids Surf B Biointerfaces. 2021 Mar;199:111524. doi: 10.1016/j.colsurfb.2020.111524. Epub 2020 Dec 13.

Abstract

This study was aimed to design a novel amphiphilic carrier based on schizophyllan (SPG) exopolysacharide for drug delivery. Stearic acid (SA) was used for the esterification of SPG with two degrees of substitutions (SA-SPG0.5 and SA-SPG1). The H NMR and FTIR spectroscopies verified the succesfull esterification of SPG. The polymeric micelles easily self-assembled into nanomicelles by ultrasound method. Fluorescence spectroscopy showed that the critical micelle concentrations (CMCs) of SA-SPG0.5 and SA-SPG1 micelles were 0.068 mg/mL and 0.027 mg/mL, respectively. DLS analyses showed that nanomicelles were ranged from 156 to 175 nm. SEM and TEM images showed that nanomicelles were mostly spherical. Paclitaxel (PTX) as a drug model was successfully loaded into SA-SPG nanomicelles with three different drug/polymer weight ratios of 0.1, 0.2 and 0.3. The highest encapsulation efficiency (75 %) was obtained when the PTX/SA-SPG weight ratio was 0.1. The in vitro release of PTX from SA-SPG micelles represented the sustained release profile over 144 h. MTT assay showed that the PTX-loaded SA-SPG nanomicelles had the higher cytotoxicity against MCF-7 cells than free PTX. These results revealed that the synthesized SA-SPG nanomicelles had a promising potential as a new carrier for efficient delivery of hydrophobic drugs.

摘要

本研究旨在设计一种基于裂褶多糖(SPG)的新型两亲性载体用于药物传递。硬脂酸(SA)用于 SPG 的酯化,取代度为 2(SA-SPG0.5 和 SA-SPG1)。1H NMR 和 FTIR 光谱验证了 SPG 的成功酯化。聚合物胶束通过超声方法容易自组装成纳米胶束。荧光光谱表明,SA-SPG0.5 和 SA-SPG1 胶束的临界胶束浓度(CMC)分别为 0.068mg/mL 和 0.027mg/mL。DLS 分析表明纳米胶束的粒径范围为 156 至 175nm。SEM 和 TEM 图像表明纳米胶束大多为球形。紫杉醇(PTX)作为药物模型,成功地负载于 SA-SPG 纳米胶束中,药物/聚合物的重量比为 0.1、0.2 和 0.3。当 PTX/SA-SPG 的重量比为 0.1 时,包封效率最高(75%)。SA-SPG 胶束中 PTX 的体外释放表现出超过 144 小时的持续释放特征。MTT 测定表明,载有 PTX 的 SA-SPG 纳米胶束对 MCF-7 细胞的细胞毒性高于游离 PTX。这些结果表明,合成的 SA-SPG 纳米胶束具有作为高效传递疏水性药物的新型载体的潜力。

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