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紫杉醇纳米晶体的体外和体内评价

Evaluation of Paclitaxel Nanocrystals In Vitro and In Vivo.

作者信息

Li Wanqing, Li Zhiguo, Wei Lisha, Zheng Aiping

机构信息

School of Basic Medicine, Beijing University of Chinese Medicine, Beijing, P.R.China.

State Key Laboratory of Toxicology and Medical Countermeasures Department of Pharmaceutics, Beijing Institute of Pharmacology and Toxicology, Beijing, P.R.China.

出版信息

Drug Res (Stuttg). 2018 Apr;68(4):205-212. doi: 10.1055/s-0043-119461. Epub 2017 Nov 30.

Abstract

We created a novel paclitaxel (PTX) nanoparticle drug delivery system and compared this to acommercial injection preparation to evaluate the antitumor effects for both formulations in vivo and in vitro.PTXnanocrystals were 194.9 nm with potential of -29.6 mV. Cytotoxicity tests indicated that both formulations had similar effects and cytotoxicity was dose- and time-dependent.Pharmacodynamics indicated that the drug concentration at the tumor was greater with PTX nanocrystals compared to commercial injection (P<0.01) and that drug accumulated more and for a longer duration. In vivo antitumor evaluation indicated significant antitumor effects and low toxicity of PTX nanocrystals. Moreover, bioimaging indicated that the PTX retention time in MCF-7-bearing mice was longer, especially at the tumor site, and this high drug concentration was maintained for a long time.Overall, PTX nanocrystalsare feasible and superior to traditional injection formulation chemotherapy.

摘要

我们创建了一种新型紫杉醇(PTX)纳米颗粒药物递送系统,并将其与市售注射制剂进行比较,以评估两种制剂在体内和体外的抗肿瘤效果。PTX纳米晶体的粒径为194.9nm,电位为-29.6mV。细胞毒性试验表明,两种制剂具有相似的效果,且细胞毒性呈剂量和时间依赖性。药效学表明,与市售注射剂相比,PTX纳米晶体在肿瘤部位的药物浓度更高(P<0.01),且药物积累更多、持续时间更长。体内抗肿瘤评估表明,PTX纳米晶体具有显著的抗肿瘤作用且毒性较低。此外,生物成像表明,PTX在荷MCF-7小鼠体内的保留时间更长,尤其是在肿瘤部位,且这种高药物浓度能长时间维持。总体而言,PTX纳米晶体是可行的,且优于传统注射制剂化疗。

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