万古霉素 PLGA 纳米粒作为胶体药物递送系统的特性和改善的肠道通透性。
The characteristics and improved intestinal permeability of vancomycin PLGA-nanoparticles as colloidal drug delivery system.
机构信息
Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Colloids Surf B Biointerfaces. 2013 Mar 1;103:174-81. doi: 10.1016/j.colsurfb.2012.10.021. Epub 2012 Oct 23.
AIM
In the present investigation, vancomycin (VCM) biodegradable nanoparticles were developed for oral administration, with the aim of improving its intestinal permeability.
METHODS
The vancomycin-loaded nanoparticles were prepared using double-emulsion solvent evaporation method. The prepared nanoparticles were characterized for their micromeritic and crystallographic properties, particle size, zeta potential, drug loading and release. Intestinal permeability of VCM nanoparticles was determined in different concentrations using SPIP technique in rats.
RESULTS
Particle sizes were between 450 nm and 466 nm for different compositions of VCM-PLGA nanoparticles. Entrapment efficiency ranged between 38.38% and 78.6% with negative zeta (ζ) potential. The FT-IR, XRPD and DSC results ruled out any chemical interaction between the drug and PLGA. Effective intestinal permeability values of VCM nanoparticles in concentrations of 200, 300 and 400 μg/ml were significantly higher than that of solutions at the same concentrations.
CONCLUSION
Our findings suggest that PLGA nanoparticles could provide a delivery system for VCM, with enhanced intestinal permeability.
目的
本研究旨在开发可口服的万古霉素（VCM）可生物降解纳米粒，以提高其肠道通透性。
方法
采用复乳溶剂蒸发法制备载万古霉素纳米粒。对所制备的纳米粒进行微粉学和结晶学性质、粒径、Zeta 电位、载药量和释放度的表征。采用 SPIP 技术在大鼠体内测定不同浓度下 VCM 纳米粒的肠道通透性。
结果
不同组成的 VCM-PLGA 纳米粒的粒径在 450nm 到 466nm 之间。包封效率在 38.38%到 78.6%之间，Zeta（ζ）电位为负。FT-IR、XRPD 和 DSC 结果排除了药物与 PLGA 之间的任何化学相互作用。浓度为 200、300 和 400μg/ml 的 VCM 纳米粒的有效肠道通透性值明显高于相同浓度的溶液。
结论
我们的研究结果表明，PLGA 纳米粒可为 VCM 提供一种给药系统，可增强其肠道通透性。
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