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聚合物胶束作为多功能药物载体。

Polymeric micelle as multifunctional pharmaceutical carriers.

作者信息

Kore Girish, Kolate Atul, Nej Ajanta, Misra Ambikanandan

出版信息

J Nanosci Nanotechnol. 2014 Jan;14(1):288-307. doi: 10.1166/jnn.2014.9021.

Abstract

A number of formulations have been developed and reported in literature as a carrier for drug, gene, and diagnostic agents. Amphiphilic block copolymers have achieved increasing attention due to their high stability both in vitro and in vivo and their good biocompatibility. In comparison to other long-circulating nanocarriers, micelles possess a number of advantages such as tissue penetrability, reduced toxicity, and controlled drug release. The characteristic features of micelle as carriers, such as particle size, shape, drug loading, cellular internalization, stability, and release kinetics of drugs can be improved by altering the physicochemical properties of the constituent block copolymers and method of preparation. Polymeric micelles formed from amphiphilic blocks have been successfully used for delivery of drugs that lack water solubility. Chelation or incorporation of a diagnostic agent in ligand conjugated micelle may help in tracing in vivo biodistribution. We review a number of research articles demonstrating that micelle formulations can be used efficiently in clinical situations by taking care of the toxicity of surfactants, and the interaction between polymer and drug, to prepare a formulation carrying a more therapeutic agent with a minimum amount of polymer.

摘要

文献中已开发并报道了多种作为药物、基因和诊断剂载体的制剂。两亲性嵌段共聚物因其在体外和体内的高稳定性以及良好的生物相容性而受到越来越多的关注。与其他长循环纳米载体相比,胶束具有许多优点,如组织穿透性、降低毒性和可控药物释放。通过改变组成嵌段共聚物的物理化学性质和制备方法,可以改善胶束作为载体的特征,如粒径、形状、载药量、细胞内化、稳定性和药物释放动力学。由两亲性嵌段形成的聚合物胶束已成功用于递送水溶性差的药物。在配体共轭胶束中螯合或掺入诊断剂可能有助于追踪体内生物分布。我们综述了一些研究文章,这些文章表明,通过关注表面活性剂的毒性以及聚合物与药物之间的相互作用,胶束制剂可以在临床情况下有效使用,从而制备出携带更多治疗剂且聚合物用量最少的制剂。

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