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两亲性羧基化纤维素-g-聚(L-丙交酯)共聚物纳米粒用于熊果酸给药。

Amphiphilic carboxylated cellulose-g-poly(l-lactide) copolymer nanoparticles for oleanolic acid delivery.

机构信息

Beijing Key Laboratory of Lignocellulosic Chemistry, MOE Engineering Research Center of Forestry Biomass Materials and Bioenergy, Beijing Forestry University, Beijing 100083, China.

Beijing Key Laboratory of Lignocellulosic Chemistry, MOE Engineering Research Center of Forestry Biomass Materials and Bioenergy, Beijing Forestry University, Beijing 100083, China.

出版信息

Carbohydr Polym. 2019 Jun 15;214:100-109. doi: 10.1016/j.carbpol.2019.03.033. Epub 2019 Mar 14.

Abstract

Carboxylated cellulose nanocrystals (CCNs), as one of nanocellulose are promising hydrophilic biomass materials for drug delivery. In this work, a series of amphiphilic carboxylated cellulose-graft-Poly(L-lactide) (CC-g-PLLA) copolymers were synthesized via ring-opening polymerization (ROP) method. The copolymers were characterized by H-NMR, FT-IR, WXRD and TGA, and their solubility in organic solvents was improved. Then, these amphiphilic copolymers were self-assembled into nanoparticles for delivery of anticancer drug oleanolic acid (OA). The copolymer (DS 2.03) nanoparticles displayed the smallest size (196.82 ± 9.14 nm) and the highest drug loading efficiency (24.76 ± 0.58%). The nanoparticles exhibited a spherical shape, well water solubility of OA (16.9 mg/mL) and a prolonged drug release (120 h). In vitro and In vivo study indicated that the nanoparticles maintained cytotoxicity to 4T1 cells and MCF-7 cells and displayed high antitumor efficiency. The amphiphilic CC-g-PLLA copolymer nanoparticles provide a novel platform for drug delivery.

摘要

羧基化纤维素纳米晶体(CCNs)作为一种有前途的亲水性生物量材料,可用于药物传递。在这项工作中,通过开环聚合(ROP)方法合成了一系列两亲性羧基化纤维素接枝聚(L-丙交酯)(CC-g-PLLA)共聚物。通过 1 H-NMR、FT-IR、WXRD 和 TGA 对共聚物进行了表征,并且提高了其在有机溶剂中的溶解度。然后,这些两亲共聚物自组装成纳米颗粒以输送抗癌药物齐墩果酸(OA)。共聚物(DS 2.03)纳米颗粒显示出最小的尺寸(196.82±9.14nm)和最高的药物载药效率(24.76±0.58%)。纳米颗粒呈现球形,具有良好的水溶性(OA 为 16.9mg/mL)和延长的药物释放(120h)。体外和体内研究表明,纳米颗粒保持了对 4T1 细胞和 MCF-7 细胞的细胞毒性,并显示出高的抗肿瘤效率。两亲性 CC-g-PLLA 共聚物纳米颗粒为药物传递提供了一个新的平台。

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