富含天然脂质的自微乳给药系统用于有效共递送他莫昔芬和柚皮素：改善乳腺癌治疗的系统方法。
Natural lipids enriched self-nano-emulsifying systems for effective co-delivery of tamoxifen and naringenin: Systematic approach for improved breast cancer therapeutics.
机构信息
UGC Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh, India 160 014; University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies Panjab University, Chandigarh, India 160 014.
UGC Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh, India 160 014.
出版信息
Nanomedicine. 2017 Jul;13(5):1703-1713. doi: 10.1016/j.nano.2017.03.003. Epub 2017 Mar 23.
The nano-miceller drug delivery carriers of tamoxifen (TMX) having natural ingredients like polyunsaturated fatty acid (PUFA) with self-nano-emulsifying 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-NG-SNEDDS 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 and AUC) in rate of drug absorption and 2-fold reduction in T 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.
载有天然成分（如多不饱和脂肪酸）的他莫昔芬纳米胶束药物传递载体具有自乳化特性，并用柚皮素（NG）以协同方式开发，即 TMX-NG-SNEDDS。优化的纳米制剂在 30 分钟内完全释放药物，在 45 分钟内渗透超过 80%。TMX-NG-SNEDDS 对 Caco-2 细胞具有更高的细胞摄取潜力（4.6-6.5 倍），而 MCF-7 细胞的细胞毒性研究表明 TMX-NG-SNEDDS 具有显著的效果（P<0.05）。体内药代动力学研究也表明，优化的 TMX-NG-SNEDDS 使药物吸收速度显著提高（C 和 AUC 分别增加 7.3 和 11.4 倍），T 降低 2 倍。DMBA 体内模型通过降低肿瘤体积来证明该制剂的优异疗效，提高动物的存活率也证明了其安全性。
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