Chitosan-palmitic acid based polymeric micelles as promising carrier for circumventing pharmacokinetic and drug delivery concerns of tamoxifen

被引:39
|
作者
Thotakura, Nagarani [1 ]
Dadarwal, Mukesh [1 ]
Kumar, Rajendra [2 ]
Singh, Bhupinder [2 ,3 ]
Sharma, Gajanand [2 ]
Kumar, Pramod [1 ]
Katare, Om Prakash [2 ]
Raza, Kaisar [1 ]
机构
[1] Cent Univ Rajasthan, Sch Chem Sci & Pharm, Dept Pharm, Bandar Sindri 305817, Rajasthan, India
[2] Panjab Univ, UGC Ctr Excellence Applicat Nanomat Nanoparticles, Chandigarh 160014, India
[3] Panjab Univ, Univ Inst Pharmaceut Sci, Div Pharmaceut, Chandigarh 160014, India
关键词
Controlled release; MCF-7 cell line; Biocompatability; Bioadhesion; MTT assay; IN-VITRO EVALUATION; GRAFTED CHITOSAN; CONTROLLED-RELEASE; BREAST-CANCER; NANOPARTICLES; CYTOTOXICITY; PARAMETERS; DOCETAXEL; PROFILE; PACLITAXEL;
D O I
10.1016/j.ijbiomac.2017.05.016
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Being a BCS class II drug and a good substrate for microsomal enzymes, tamoxifen (TAM) offers a scope for research owing to poor aqueous solubility and compromised bioavailability. The present study designs a novel copolymer derived from palmitic acid and chitosan, and evaluate the derived TAM-loaded micelles for various delivery attributes. The nanometric micellar carriers not only substantially loaded the drug, but also controlled the rate of release of TAM. The designed nanocarrier significantly enhanced the cytotoxicity of TAM on MCF-7 cancer cells. The developed system was designed for intravenous route and was observed to be substantially haemo-compatible with an enhancement of approx. 5 times in AUC vis-a-vis plain drug. The findings employing new polymer-based carrier are promising in nature for the better delivery of similar drugs. (C) 2017 Elsevier B.V. All rights reserved.
引用
收藏
页码:1220 / 1225
页数:6
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