Effects of amphiphilic diblock copolymer on drug nanoparticle formation and stability.
Effects of amphiphilic diblock copolymer on drug nanoparticle formation and stability.
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DOI：
10.1016/j.biomaterials.2013.09.015
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发表时间：
2013-12
期刊：
影响因子：
14
通讯作者：
Zhu, Zhengxi
中科院分区：
文献类型：
--
作者：
Zhu, Zhengxi
关键词：
本研究系统地比较了两亲性嵌段共聚物（di-BCP）对快速纳米沉淀法（FNP）制备的疏水性药物纳米粒的稳定作用，为选择合适的di-BCP提供了指导。四种广泛使用的二BCP，即，使用聚苯乙烯-嵌段-聚（乙二醇）（PS-b-PEG）、聚己内酯-嵌段-聚（乙二醇）（PCL-b-PEG）、聚丙交酯-嵌段-聚（乙二醇）（PLA-b-PEG）和聚（乳酸-共-乙醇酸）（PLGA-b-PEG），和β-胡萝卜素作为模型药物。结果表明，PLGA-b-PEG具有较高的玻璃化转变温度（Tg）和合适的溶解度参数（δ），疏水嵌段具有生物可降解性和非结晶性，是最合适的共聚物。PLGA嵌段的分子量在5 k至15 k的范围内对控制粒径显示出不显著的效果。可以获得具有超过83wt%的高载药量的无定形药物颗粒。许多显著的证据支持的纳米粒子的动力学冻结和非平衡堆积结构的聚合物链，而不是胶束或胶束纳米粒子的两个良好的隔离的聚合物嵌段。利用溶解度参数讨论了药物和嵌段共聚物对微粒稳定性、尺寸和结构的热力学影响。
This study systematically compares the effects of amphiphilic diblock copolymer (di-BCP) on stabilizing hydrophobic drug nanoparticles formed by flash nanoprecipitation (FNP), and provides a guideline on choosing suitable di-BCPs. Four widely used di-BCPs, i.e., polystyrene-block-poly(ethylene glycol) (PS-b-PEG), polycaprolactone-block-poly(ethylene glycol) (PCL-b-PEG), polylactide-block-poly(ethylene glycol) (PLA-b-PEG), and poly(lactic-co-glycolic acid) (PLGA-b-PEG), and β-carotene as a model drug were used. The study showed that PLGA-b-PEG was the most suitable one, whose hydrophobic block was biodegradable and noncrystallizable as well as had relatively high glass transition temperature (Tg) and a right solubility parameter (δ). The molecular weight of PLGA block over the range from 5k to 15k showed an insignificant effect on controlling the particle size. Amorphous drug particles with a high drug loading of over 83 wt% can be achieved. Much remarkable evidence supported the nanoparticles with kinetically frozen and nonequilibrium packing structures of polymer chains rather than either the micelles or micellar nanoparticles with two well segregated polymer blocks. The thermodynamic effects of the drug and BCP on the particle stability, size and structures were discussed by using solubility parameters.
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