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新型紫杉醇制剂:聚乙烯吡咯烷酮纳米颗粒包裹的紫杉醇用于癌症治疗中的药物递送。

Novel Taxol formulation: polyvinylpyrrolidone nanoparticle-encapsulated Taxol for drug delivery in cancer therapy.

作者信息

Sharma D, Chelvi T P, Kaur J, Chakravorty K, De T K, Maitra A, Ralhan R

机构信息

Department of Biochemistry, All India Institute of Medical Sciences, New Delhi, India.

出版信息

Oncol Res. 1996;8(7-8):281-6.

PMID:8938791
Abstract

Taxol is a novel antitumor alkaloid that has shown clinical activity against several tumors. However, due to its low aqueous solubility, Cremophor EL (polyoxyethylated castor oil) and ethanol are used as excipients in the pharmaceutical drug formulations. These agents are implicated in hypersensitivity reactions. Hence the goal of this work was to design a novel Taxol formulation using polymeric nanoparticles to eliminate the Cremophor EL vehicle for drug delivery. Polyvinylpyrrolidone nanoparticles containing Taxol were prepared by a reverse microemulsion method. The size of the nanoparticles as determined by quasielastic light scattering was found to be between 50 and 60 nm. The antitumor effect of Taxol encapsulated nanoparticles was evaluated in B16F10 murine melanoma transplanted in C57B1/6 mice. The in vivo efficacy of Taxol-containing nanoparticles as measured by reduction in tumor volume and increased survival time was significantly greater than that of an equivalent concentration of free Taxol. These results suggest that encapsulation of Taxol in polymeric nanoparticles could be useful in improving its therapeutic efficacy in treatment of solid tumors.

摘要

紫杉醇是一种新型抗肿瘤生物碱,已显示出对多种肿瘤的临床活性。然而,由于其水溶性低,在药物制剂中使用聚氧乙烯蓖麻油(Cremophor EL)和乙醇作为辅料。这些试剂与过敏反应有关。因此,这项工作的目标是设计一种使用聚合物纳米颗粒的新型紫杉醇制剂,以消除用于药物递送的聚氧乙烯蓖麻油载体。通过反向微乳液法制备了含紫杉醇的聚乙烯吡咯烷酮纳米颗粒。通过准弹性光散射测定的纳米颗粒尺寸在50至60纳米之间。在移植于C57B1/6小鼠的B16F10小鼠黑色素瘤中评估了紫杉醇包封纳米颗粒的抗肿瘤作用。通过肿瘤体积减小和存活时间延长来衡量,含紫杉醇纳米颗粒的体内疗效明显高于同等浓度的游离紫杉醇。这些结果表明,将紫杉醇包封在聚合物纳米颗粒中可能有助于提高其在实体瘤治疗中的疗效。

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