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Preparation, evaluation and metabolites study in rats of novel amentoflavone-loaded TPGS/soluplus mixed nanomicelles.
Drug Delivery ( IF 6 ) Pub Date : 2020-01-08 , DOI: 10.1080/10717544.2019.1709920
Xue Feng 1 , Yuting Chen 1 , Luya Li 1 , Yuqian Zhang 2 , Lantong Zhang 1 , Zhiqing Zhang 2
Affiliation  

Amentoflavone (AMF) is a kind of biflavonoids existing in Ginkgo biloba leaves. It has many biological activities, such as antioxidant, anti-inflammatory, anti-bacterial, antiviral, hypoglycemic, anti-tumor and inducing apoptosis. However, its solubility and bioavailability are poor and there are a few studies on it in vivo. In this study, to improve its solubility and bioavailability, the nanomicelles were prepared with TPGS and soluplus as carriers for the first time. The particle size, Zeta potential, encapsulation efficiency, drug loading, stability, cytotoxicity, cellular uptake, and metabolites in rats were studied. Cytotoxicity, cellular uptake, and metabolites in rats of AMF-loaded TPGS/soluplus mixed micelles were compared with those of AMF. As a result, AMF-loaded TPGS/soluplus mixed micelles with a particle size of 67.33 ± 2.01 nm and Zeta potential of -0.84133 ± 0.041405 mV were successfully prepared. The encapsulation efficiency and drug loading of the mixed nanomicelles were 99.18 ± 0.76% and 2.47 ± 0.01%, respectively. The physical and chemical properties of the mixed micelles were stable within 60 d, and the cytotoxicity of the mixed micelles was much greater than that of AMF monomers. Thirty-four kinds of metabolites of AMF were identified in rats. The metabolites were mainly distributed in rat feces. No metabolites were detected in bile and plasma. 14 kinds of metabolites of the mixed micelles in rats were detected, including 11 in feces, 6 in urine, and 3 in plasma, which indicated that the bioavailability of AMF has been improved. And the toxicity to cancer cells was enhanced, which laid a foundation for the development of new drugs.

中文翻译:

新型载有黄酮的TPGS / soluplus混合纳米胶束在大鼠中的制备,评价和代谢物研究。

黄酮(AMF)是银杏叶片中存在的一种双黄酮类化合物。它具有许多生物活性,例如抗氧化剂,抗炎,抗菌,抗病毒,降血糖,抗肿瘤和诱导细胞凋亡。但是,它的溶解度和生物利用度很差,并且在体内有一些研究。在这项研究中,为提高其溶解度和生物利用度,首次以TPGS和soluplus为载体制备了纳米胶束。研究了大鼠的粒径,Zeta电位,包封效率,载药量,稳定性,细胞毒性,细胞摄取和代谢产物。比较了AMF负载的TPGS / soluplus混合胶束对大鼠的细胞毒性,细胞摄取和代谢产物的影响。结果,AMF负载的TPGS / soluplus混合胶束的粒径为67.33±2。成功制备了01 nm和-0.84133±0.041405 mV的Zeta电位。混合纳米胶束的包封效率和载药量分别为99.18±0.76%和2.47±0.01%。混合胶束的理化性质在60 d内稳定,并且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。成功制备了84133±0.041405 mV。混合纳米胶束的包封效率和载药量分别为99.18±0.76%和2.47±0.01%。混合胶束的理化性质在60 d内稳定,且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。成功制备了84133±0.041405 mV。混合纳米胶束的包封效率和载药量分别为99.18±0.76%和2.47±0.01%。混合胶束的理化性质在60 d内稳定,且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。混合纳米胶束的包封效率和载药量分别为99.18±0.76%和2.47±0.01%。混合胶束的理化性质在60 d内稳定,并且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。混合纳米胶束的包封效率和载药量分别为99.18±0.76%和2.47±0.01%。混合胶束的理化性质在60 d内稳定,并且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。混合胶束的理化性质在60 d内稳定,且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。混合胶束的理化性质在60 d内稳定,且混合胶束的细胞毒性远大于AMF单体。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。在大鼠中鉴定出34种AMF代谢产物。代谢物主要分布在大鼠粪便中。在胆汁和血浆中未检测到代谢物。共检测到14种混合胶束代谢产物,其中粪便11种,尿液6种,血浆3种,表明AMF的生物利用度得到提高。增强了对癌细胞的毒性,为新药的开发奠定了基础。
更新日期:2020-04-20
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