Kalinova Radostina, Dimitrov Ivaylo
Institute of Polymers, Bulgarian Academy of Sciences, Akad. G. Bonchev St., bl. 103-A, 1113 Sofia, Bulgaria.
Nanomaterials (Basel). 2022 Jan 27;12(3):434. doi: 10.3390/nano12030434.
Polymeric micelles have gained increasing interest as efficient drug delivery systems for cancer treatment and diagnosis. The aim of the present study was to construct and to evaluate novel polymeric nanosized drug carriers with tunable surface charges. Initially, amphiphilic triblock copolymers with predetermined molar mass characteristics were synthesized by applying controlled polymerization techniques. The copolymers self-assembled in aqueous media into core-shell spherical micelles, comprising a biodegradable hydrophobic poly(D,L-lactide) core, positively charged middle layer of poly((2-dimethylamino)ethyl methacrylate), and an outer shell of neutral hydrophilic poly(oligo(ethylene glycol) methyl ether methacrylate), with various densities of the short polyether side chains. The block copolymer micelles with average diameters of about 70 nm and surface charges varying from strongly positive to neutral were characterized and loaded with the model, natural, hydrophobic drug curcumin. Characteristics such as drug loading efficiency, in-vitro drug release profiles, and stability under physiological conditions were evaluated and discussed in terms of nanocarriers' composition. As a result, the most promising candidates for potential application in nanomedicine were identified.
聚合物胶束作为用于癌症治疗和诊断的高效药物递送系统越来越受到关注。本研究的目的是构建并评估具有可调节表面电荷的新型聚合物纳米药物载体。首先,通过应用可控聚合技术合成具有预定摩尔质量特征的两亲性三嵌段共聚物。这些共聚物在水性介质中自组装成核壳球形胶束,其包含可生物降解的疏水性聚(D,L-丙交酯)核、带正电荷的聚(甲基丙烯酸(2-二甲基氨基)乙酯)中间层以及具有不同密度短聚醚侧链的中性亲水性聚(寡聚(乙二醇)甲基醚甲基丙烯酸酯)外壳。对平均直径约为70nm且表面电荷从强正电到中性变化的嵌段共聚物胶束进行了表征,并负载了模型天然疏水性药物姜黄素。根据纳米载体的组成,评估并讨论了诸如载药效率、体外药物释放曲线和生理条件下的稳定性等特性。结果,确定了在纳米医学中潜在应用最有前景的候选物。