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首页> 外文期刊>Regulatory Toxicology and Pharmacology: RTP >Safety against nephrotoxicity in paclitaxel treatment: Oral nanocarrier as an effective tool in preclinical evaluation with marked in vivo antitumor activity
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Safety against nephrotoxicity in paclitaxel treatment: Oral nanocarrier as an effective tool in preclinical evaluation with marked in vivo antitumor activity

机译:对紫杉醇治疗中肾毒性的安全性:口腔纳米载波作为临床前评价的有效工具,标记为体内抗肿瘤活性

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Abstract Oral paclitaxel (PTXL) formulations freed from cremophor ? EL (CrEL) is always in utmost demand by the cancerous patients due to toxicities associated with the currently marketed formulation. In our previous investigation [ Int. J. Pharm. 2014; 460:131], we have developed an oral oil based nanocarrier for the lipophilic drug, PTXL to target bioavailability issue and patient compliance. Here, we report in vivo antitumor activity and 28-day sub-chronic toxicity of the developed PTXL nanoemulsion. It was observed that the apoptotic potential of oral PTXL nanoemulsion significantly inhibited the growth of solid tumor (59.2?±?7.17%; p ? ? ) was found to be comparatively more toxic to the experimental animals. Taxol ? treatment resulted glomerulonephritis in histopathological examination, which could be correlated with increased level of creatinine and associated nephrotoxicity. This investigations conclude that the developed oral nanoemulsion presents a viable therapeutics bio-system to step towards clinical application as well as substitute CrEL based PTXL formulations. Graphical abstract Display Omitted Highlights ? Pronounced in vivo antitumor efficacy of oral paclitaxel nanoemulsion in solid tumor bearing model. ? The 28-day toxicity study of the nanoemulsion proved to be a viable media to deliver paclitaxel. ? Overall, devoid of Cremophor ? EL in paclitaxel formulation has proved its safety against nephrotoxicity. ? The developed nanosystem pose higher potential to step towards its clinical application.
机译:摘要口腔紫杉醇(PTXL)配方来自Cremophor吗? EL(CREL)由于与目前销售的配方相关的毒性,癌症患者始终处于最大的需求。在我们之前的调查中[int。 J. Pharm。 2014; 460:131],我们已经开发了一种用于亲脂性药物的口腔油纳米载体,PTX1靶向生物利用度问题和患者依从性。在这里,我们报告了发育的PTX1纳米乳液的体内抗肿瘤活性和28天的亚慢性毒性。观察到口服PTX1纳米乳液的凋亡电位显着抑制了固体瘤的生长(59.2?±7.17%;p≤α)对实验动物的毒性相对较多。紫杉醇?治疗导致肾小球肾炎在组织病理学检查中,这与肌酸酐和相关肾毒性的水平增加有关。该研究得出结论,发育的口服纳米乳液呈现可行的治疗生物系统,迈向临床应用以及基于替代的基于旋风的PTXL制剂。图形抽象显示省略了亮点?在实体瘤轴承模型中的口腔紫杉醇纳米乳液的体内抗肿瘤效果。还纳米乳液的28天毒性研究证明是一种可行的培养基,可提供紫杉醇。还总的来说,没有特克菲尔?紫杉醇配方在紫杉醇配方中证明了其对肾毒性的安全性。还开发的纳米系统呈迈向其临床应用的潜力较高。

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