New Oral Formulation and in Vitro Evaluation of Docetaxel-Loaded Nanomicelles.
New Oral Formulation and in Vitro Evaluation of Docetaxel-Loaded Nanomicelles.
复制标题
DOI：
10.3390/molecules21091265
复制
发表时间：
2016-09-21
期刊：
影响因子：
--
通讯作者：
Jaafari MR
中科院分区：
文献类型：
--
作者：
Hekmat A;Attar H;Seyf Kordi AA;Iman M;Jaafari MR
Taxotere®（多西他赛的一种商业形式，DTX）的静脉内施用导致许多问题，例如超敏反应、溶血、皮肤过敏和由于其长时间注射而导致的患者拒绝。由于其疏水性，DTX的口服吸收非常低。本研究的目的是制备并进行用于口服给药的DTX负载纳米胶束的体外评价，以增加DTX的口服递送。用两种表面活性剂Tween 20和Tween 80制备所研究的制剂，并对其粒度、zeta电位、稳定性、包封率、在胃液和肠液中的稳定性研究、在C26结肠癌细胞系中的毒性研究和细胞摄取进行表征。制备的纳米胶束粒径约为14 nm，包封率为99%，在胃液和肠液中稳定至少6 h，与泰索帝®相比，暴露72 h后IC 50显著降低。纳米胶束使DTX的水溶性增加了1500倍以上（在纳米胶束中为10 mg/mL，而在水中为6 µg/mL）。本研究结果表明，新的DTX制剂可用于口服给药的DTX和值得进一步研究。
Intravenous administration of Taxotere® (a commercial form of docetaxel, DTX) leads to many problems such as hypersensitivity, hemolysis, cutaneous allergy, and patient refusal due to its prolonged injection. The oral absorption of DTX is very low due to its hydrophobic nature. The purpose of this study was to prepare and carry out an in vitro evaluation of DTX-loaded nanomicelles for oral administration in order to increase the oral delivery of DTX. Studied formulations were prepared with the two surfactants Tween 20 and Tween 80 and were characterized for their particle size, zeta potential, stability, encapsulation efficiency, stability studies in gastric fluid and intestinal fluid, toxicity studies in C26 colon carcinoma cell line, and cellular uptake. The prepared nanomicelles with particle size of around 14 nm and encapsulation efficiency of 99% were stable in gastric fluid and intestinal fluid for at least 6 h and IC50 decreased significantly after 72 h exposure compared to that of Taxotere®. Nanomicelles increased the water solubility of DTX more than 1500 times (10 mg/mL in nanomicelles compared to 6 µg/mL in water). Results of this study reveal that the new formulation of DTX could be used for the oral delivery of DTX and merits further investigation.
登录
查看更多内容
影响因子：
8
作者：
Hu K;Cao S;Hu F;Feng J
通讯作者：
Feng J
影响因子：
6.6
作者：
Pridgen EM;Alexis F;Farokhzad OC
通讯作者：
Farokhzad OC
DOI：
10.1016/j.ejpb.2011.03.022
发表时间：
2011-09-01
影响因子：
4.9
作者：
Petersen, Silvia;Steiniger, Frank;Bunjes, Heike
通讯作者：
Bunjes, Heike
影响因子：
5.8
作者：
Liu, Donghua;Liu, Zhihong;Zhang, Na
通讯作者：
Zhang, Na
影响因子：
5.8
作者：
Anton, Nicolas;Mojzisova, Halina;Saulnier, Patrick
通讯作者：
Saulnier, Patrick