National Research Center "Kurchatov Institute", 123182 Moscow, Russia.
Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, 119333 Moscow, Russia.
Molecules. 2021 Jan 24;26(3):602. doi: 10.3390/molecules26030602.
Nanoparticles based on biocompatible methoxy poly(ethylene glycol)--poly(D,L-lactide) (mPEG--P(D,L)LA) copolymers as potential vehicles for the anticancer agent oxaliplatin were prepared by a nanoprecipitation technique. It was demonstrated that an increase in the hydrophobic PLA block length from 62 to 173 monomer units leads to an increase of the size of nanoparticles from 32 to 56 nm. Small-angle X-ray scattering studies confirmed the "core-corona" structure of mPEG--P(D,L)LA nanoparticles and oxaliplatin loading. It was suggested that hydrophilic oxaliplatin is adsorbed on the core-corona interface of the nanoparticles during the nanoprecipitation process. The oxaliplatin loading content decreased from 3.8 to 1.5% wt./wt. (with initial loading of 5% wt./wt.) with increasing PLA block length. Thus, the highest loading content of the anticancer drug oxaliplatin with its encapsulation efficiency of 76% in mPEG--P(D,L)LA nanoparticles can be achieved for block copolymer with short hydrophobic block.
基于生物相容性甲氧基聚乙二醇-聚（D，L-丙交酯）（mPEG-P（D，L）LA）共聚物的纳米粒子被制备为抗癌剂奥沙利铂的潜在载体，采用纳米沉淀技术。结果表明，疏水性 PLA 嵌段长度从 62 个单体单元增加到 173 个单体单元会导致纳米粒子的尺寸从 32nm 增加到 56nm。小角 X 射线散射研究证实了 mPEG-P（D，L）LA 纳米粒子和奥沙利铂负载的“核-壳”结构。在纳米沉淀过程中，亲水性奥沙利铂被吸附在纳米粒子的核-壳界面上。随着 PLA 嵌段长度的增加，奥沙利铂的负载量从 3.8%wt./wt.（初始负载量为 5%wt./wt.）降低至 1.5%wt./wt.。因此，对于具有短疏水性嵌段的嵌段共聚物，可以实现抗癌药物奥沙利铂的最高负载量 3.8%wt./wt.，包封效率为 76%。
