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Encapsulation of nor-β-lapachone into poly(D,L)-lactide-co-glycolide (PLGA) microcapsules: full characterization, computational details and cytotoxic activity against human cancer cell lines
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-09-07 00:00:00 , DOI: 10.1039/c7md00196g
Marcília P. Costa 1, 2, 3, 4 , Anderson C. S. Feitosa 4, 5, 6, 7 , Fátima C. E. Oliveira 4, 5, 6, 7 , Bruno C. Cavalcanti 4, 5, 6, 7 , Gleiston G. Dias 4, 8, 9, 10, 11 , Ewerton W. S. Caetano 4, 12, 13, 13, 14 , Francisco A. M. Sales 4, 12, 13, 13, 14 , Valder N. Freire 4, 6, 15, 16 , Stefano Di Fiore 17, 18, 19 , Rainer Fischer 17, 18, 19, 20, 21 , Luiz O. Ladeira 4, 8, 10, 11, 15 , Eufrânio N. da Silva Júnior 4, 8, 9, 10, 11 , Claudia Pessoa 4, 5, 6, 7, 22
Affiliation  

In this work, we characterize nor-β-lapachone-loaded (NβL-loaded) microcapsules prepared using an emulsification/solvent extraction technique. Features such as surface morphology, particle size distribution, zeta potential, optical absorption, Raman and Fourier transform infrared spectra, thermal analysis data, drug encapsulation efficiency, drug release kinetics and in vitro cytotoxicity were studied. Spherical microcapsules with a size of 1.03 ± 0.46 μm were produced with an encapsulation efficiency of approximately 19%. Quantum DFT calculations were also performed to estimate typical interaction energies between a single nor-β-lapachone molecule and the surface of the microparticles. The NβL-loaded PLGA microcapsules exhibited a pronounced initial burst release. After the in vitro treatment with NβL-loaded microcapsules, a clear phagocytosis of the spheres was observed in a few minutes. The cytotoxic activity against a set of cancer cell lines was investigated.

中文翻译:

也不-β拉帕醌的封装入聚(d大号)-lactide--glycolide(PLGA)微胶囊:充分表征,计算细节和针对人癌细胞系的细胞毒活性

在这项工作中,我们表征了使用乳化/溶剂萃取技术制备的无β-拉帕酮负载(NβL负载)微胶囊的特性。研究了诸如表面形态,粒度分布,ζ电势,光吸收,拉曼和傅立叶变换红外光谱,热分析数据,药物包封效率,药物释放动力学和体外细胞毒性等特征。球形微胶囊的大小为1.03±0.46μm,封装效率约为19%。还进行了量子DFT计算以估计单个nor-β-拉帕酮分子与微粒表面之间的典型相互作用能。装载NβL的PLGA微胶囊表现出明显的初始爆发释放。经过体外用负载NβL的微胶囊处理后,在几分钟内观察到了球体的明显吞噬作用。研究了针对一组癌细胞系的细胞毒性活性。
更新日期:2017-10-18
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