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Synthesis and characterization of TPGS-gemcitabine prodrug micelles for pancreatic cancer therapy

机译：TPGS-吉西他滨前药胶束对胰腺癌疗法的合成与表征

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摘要

The therapeutic potential of a nucleoside analog, gemcitabine, is severely compromised due to its rapid clearance from systemic circulation by enzymatic degradation into an inactive metabolite. In the present investigation, micelles based on polymer-drug conjugate were developed for gemcitabine and investigated for their potential to improve cancer chemotherapy. The tocopherol poly(ethylene glycol) succinate 1000 (TPGS)-gemcitabine prodrug was synthesized via an amide linkage and characterised by analytical methods, including FT-IR, H-1 NMR, and MALDI-TOF. The micellar formulation of TPGS-gemcitabine prodrug was developed by a self-assembly technique and evaluated for various physicochemical parameters including particle size, polydispersity, morphology, critical micelle concentration and release profile. It was observed that gemcitabine present in TPGS-gemcitabine micelles was resistant to deamination by crude cytidine deaminase. The improved cytotoxicity of the micellar formulation was observed using TPGS-gemcitabine micelles against pancreatic cancer cells. Further, it was found that, unlike native gemcitabine, nucleoside transporters were not required for TPGS-Gem micelles to demonstrate their anticancer potential. These findings revealed that TPGS-gemcitabine micelles may serve as a promising platform for gemcitabine in order to improve its anticancer efficacy.
机译：核苷类似物，吉西他滨的治疗潜力，严重由于折衷，以从系统循环通过酶促降解其快速清除成非活性代谢物。在本研究中，基于聚合物 - 药物缀合物的胶束用于吉西他滨开发，并研究了它们改善癌症化疗的潜力。通过酰胺键合成生育酚聚（乙二醇）琥珀酸盐1000（TPGS）-Gemcitabine前药，并通过分析方法表征，包括FT-IR，H-1 NMR和MALDI-TOF。通过自组装技术开发TPGS-Gemcitabine前药的胶束制剂，并评估各种物理化学参数，包括粒度，多分散性，形态，临界胶束浓度和释放曲线。观察到，在TPGS-吉西他滨胶束中存在的吉西他滨与粗胞苷脱氨酰酶耐脱胺。使用TPGS-吉西他滨胶束对胰腺癌细胞进行改善的胶束制剂的改进细胞毒性。此外，发现与本地吉西他滨不同，TPGS-宝石胶束不需要核苷转运蛋白，以证明它们的抗癌潜力。这些发现表明，TPGS-吉西他滨胶束可以作为吉西他滨的有希望的平台，以改善其抗癌效果。

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  • 来源
    《RSC Advances》 |2016年第65期|共12页
  • 作者

    Khare Vaibhav; Al Sakarchi Wejdan; Gupta Prem N.; Curtis Anthony D. M.; Hoskins Clare;

  • 作者单位

    Keele Univ Inst Sci &

    Technol Med Keele ST55BJ Staffs England;

    Keele Univ Inst Sci &

    Technol Med Keele ST55BJ Staffs England;

    CSIR Indian Inst Integrat Med Formulat &

    Drug Delivery Div Jammu 180001 India;

    Keele Univ Inst Sci &

    Technol Med Keele ST55BJ Staffs England;

    Keele Univ Inst Sci &

    Technol Med Keele ST55BJ Staffs England;

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  • 正文语种 eng
  • 中图分类 化学;
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