Department of Chemistry, Indian Institute of Technology Kharagpur, 721 302, India.
Department of Chemistry, Indian Institute of Technology Kharagpur, 721 302, India.
J Colloid Interface Sci. 2017 Sep 1;501:22-33. doi: 10.1016/j.jcis.2017.04.034. Epub 2017 Apr 12.
Stimuli-sensitive polymersomes are one of the important vehicles and have been extensively studied as smart drug delivery system. Polymersomes have added advantage over the micelles because of having the ability to carry not only hydrophobic but also hydrophilic guest in their aqueous core. Among various stimuli, the change of pH and redox reaction is very important for drug delivery purpose especially for anticancer drug. Therefore, in this work, two poly(ethylene glycol) methyl ether methacrylate (mPEG) containing hydrophilic random anionic copolymers, poly[(2-hydroxyethyl methacrylate-3,3'-dithiodipropanoic acid)-co-(poly(ethylene glycol) methyl ether methacrylate)], poly[(HEMA-DTDPA)-co-mPEG] with different copolymer ratios were designed and synthesized. The self-assembly behaviour of these copolymers were studied by use of various techniques, including fluorescence spectroscopy, light scattering, and electron and optical microscopy. Both the copolymers were observed to form negatively charged polymersomes spontaneously in aqueous media at pH 7. The polymersomes were shown to successfully encapsulate hydrophobic as well as hydrophilic guests. The polymersomes of both the polymers showed pH- and redox-sensitive release of encapsulated guest leading to a very good system for cytoplasmic delivery. The polymers were found to be nontoxic and hemocompatible up to a reasonably high concentration. Also the polymers did not show any denaturizing effect on the secondary structure of carrier protein, human serum albumin. It was concluded that these two dual stimuli-sensitive cytocompatible polymersomes can have potential use as drug delivery system in cancer chemotherapy.
刺激响应聚合物囊泡是一种重要的载体，已被广泛研究作为智能药物传递系统。聚合物囊泡比胶束具有更多的优势，因为它们不仅能够携带疏水性物质，还能够携带亲水性物质进入其水核。在各种刺激中，pH 值和氧化还原反应的变化对于药物传递目的非常重要，特别是对于抗癌药物。因此，在这项工作中，设计并合成了两种含有亲水性随机阴离子共聚物的聚（乙二醇）甲基醚甲基丙烯酸酯（mPEG），聚[（2-羟乙基甲基丙烯酸酯-3,3'-二硫代二丙酸）-共-（聚（乙二醇）甲基醚甲基丙烯酸酯）]，聚[（HEMA-DTDPA）-共-mPEG]，具有不同的共聚物比例。使用荧光光谱、光散射、电子和光学显微镜等多种技术研究了这些共聚物的自组装行为。两种共聚物在 pH 7 的水介质中均能自发形成带负电荷的聚合物囊泡。聚合物囊泡被证明能够成功地包封疏水性和亲水性客体。两种聚合物的聚合物囊泡均表现出 pH 和氧化还原敏感的包封客体释放，从而形成了一种非常好的细胞质传递系统。聚合物在相当高的浓度下被发现是非毒性和血液相容性的。此外，聚合物对载体蛋白人血清白蛋白的二级结构没有任何变性作用。研究结论认为，这两种双重刺激响应的细胞相容性聚合物囊泡可以作为癌症化疗中的药物传递系统具有潜在的应用价值。
