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首页> 外文会议>PMSE Symposia >Dichloro(1,2-diaminocyclohexane) Platinum(II) (DACHPt) Loaded Polymer Micelles with Cross-Linked Core: Preparation and Characterization
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Dichloro(1,2-diaminocyclohexane) Platinum(II) (DACHPt) Loaded Polymer Micelles with Cross-Linked Core: Preparation and Characterization

机译：二氯（1,2-二氨基环己烷）铂（II）（分别）具有交联核心的加载聚合物胶束：制备和表征

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摘要

The platinum (II) analog, dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt), the oxaliplatin parent complex, is a potent chemotherapeutic with a wide spectrum of anticancer activity, low toxicity and lack of cross resistance in many cisplatin-resistant cancers. However, its clinical use is restrained by its poor solubility, unfavorable pharmacokinetics and various non-target side effects such as, cumulative peripheral distal neurotoxicity and acute dysesthesias. Polymer micelles with intramicellar cross-linking for structural reinforcement and polyanionic core for platinum (II) encapsulation offer a novel macromolecular platform for carrier based delivery of such compounds. These drug-carrier conjugates acquire new physicochemical, biochemical and pharmacological characteristics, thereby offering the possibly of reducing side effects, increasing drug bioavailability at the target sites and minimizing development of drug resistance. In this study block ionomer complexes (BIC) of poly(ethylene oxide)-b-poly(methacrylic acid) (PEO-b-PMA) and divalent metal cations (Ca~(2+)) were utilized as templates for the synthesis of cross-linked (cl)-micelles. DACHPt was loaded into the cross-linked core of the polymeric micelles. The physicochemical properties, loading efficacy, drug release from the polymer micelles and in vitro cytotoxicity of the formulation were investigated.
机译：铂（II）类似物，二氯（1,2-二氨基环己烷）铂（II）（1ACHT），奥沙利铂母体复合物是一种有效的化学治疗，具有广泛的抗癌活性，低毒性和许多顺铂缺乏抗抗抗抗抗抗抗-Resistant癌症。然而，其临床用途受其贫化性，不利的药代动力学和各种非目标副作用，例如累积外周端神经毒性和急性脱粘性的临床用途。具有用于铂（II）包封的结构增强和聚阴离子核的肌内胶束与肌醇交联，为这些化合物的载体提供了一种新的大分子平台。这些药物载体缀合物获得了新的物理化学，生化和药理学特征，从而提供可能降低副作用，增加靶位点的药物生物利用度，并最大限度地减少耐药性的发展。在该研究嵌段聚合物复合物（BIC）的聚（环氧乙烷）-B-聚（甲基丙烯酸）（PEO-B-PMA）和二价金属阳离子（Ca〜（2+））作为合成的模板使用交联（CL）-Micelles。用聚合物胶束的交联芯装入分量。研究了物理化学性质，加载功效，来自聚合物胶束的药物释放和制剂的体外细胞毒性。

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