期刊
NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
卷 13, 期 5, 页码 1703-1713出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.nano.2017.03.003
关键词
Nano-micelles; P-gp-inhibitors; Bioavailability; Apoptosis; DMBA-model
The nano-miceller drug delivery carriers of tamoxifen (TMX) having natural ingredients like polyunsaturated fatty acid (PUFA) with self-nanoemulsifying properties was developed with naringenin (NG) in a synergistic manner i.e. TMX-NG-SNEDDS. The optimized nano-formulation revealed complete drug release in 30 min and >80% permeation in 45 min. Superior cellular uptake potential (4.6-6.5-fold) of the TMX-NGSNEDDS using Caco-2 cells while cytotoxicity study on MCF-7 cells indicated significant results (P < 0.05) of TMX-NG-SNEDDS. The in vivo pharmacokinetic study also construed remarkable improvement (7.3 and 11.4-fold increase in C-max and AUC) in rate of drug absorption and 2-fold reduction in T-max by optimized TMX-NG-SNEDDS. In vivo DMBA model construed superior efficacy of the formulation by reducing tumor size, and improved survival rate of the animals justifies its safety aspect as well. (C) 2017 Elsevier Inc. All rights reserved.
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