Loveymi Badir Delf, Jelvehgari Mitra, Zakeri-Milani Parvin, Valizadeh Hadi
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. ; Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Adv Pharm Bull. 2012;2(1):43-56. doi: 10.5681/apb.2012.007. Epub 2012 Feb 15.
The purpose of this work was to preparation of vancomycin (VCM) biodegradable nanoparticles to improve the intestinal permeability, using water-in-oil-in-water (W/O/W) multiple emulsion method.
The vancomycin-loaded nanoparticles were created using double-emulsion solvent evaporation method. Using Eudragit RS100 as a coating material. The prepared nanoparticles were identifyed for their micromeritic and crystallographic properties, drug loading, particle size, drug release, Zeta potential, effective permeability (Peff) and oral fractional absorption. Intestinal permeability of VCM nanoparticles was figured out, in different concentrations using SPIP technique in rats.
Particle sizes were between 362 and 499 nm for different compositions of VCM-RS-100 nanoparticles. Entrapment efficiency expansed between 63%-94.76%. The highest entrapment efficiency 94.76% was obtained when the ratio of drug to polymer was 1:3. The in vitro release studies were accomplished in pH 7.4. The results showed that physicochemical properties were impressed by drug to polymer ratio. The FT-IR, XRPD and DSC results ruled out any chemical interaction betweenthe drug and RS-100. Effective intestinal permeability values of VCM nanoparticles in concentrations of 200, 300 and 400 μg/ml were higher than that of solutions at the same concentrations. Oral fractional absorption was achieved between 0.419-0.767.
Our findings suggest that RS-100 nanoparticles could provide a delivery system for VCM, with enhanced intestinal permeability.
本研究旨在采用水包油包水（W/O/W）多重乳液法制备万古霉素（VCM）可生物降解纳米颗粒，以提高其肠道通透性。
采用双乳液溶剂蒸发法制备载万古霉素纳米颗粒，以Eudragit RS100作为包衣材料。对制备的纳米颗粒进行微粉学和晶体学性质、载药量、粒径、药物释放、Zeta电位、有效渗透率（Peff）和口服分数吸收的鉴定。采用SPIP技术在大鼠体内测定不同浓度万古霉素纳米颗粒的肠道通透性。
不同组成的VCM-RS-100纳米颗粒粒径在362至499nm之间。包封率在63%-94.76%之间。当药物与聚合物的比例为1:3时，包封率最高，为94.76%。体外释放研究在pH 7.4条件下完成。结果表明，药物与聚合物的比例对其理化性质有影响。FT-IR、XRPD和DSC结果排除了药物与RS-100之间的任何化学相互作用。浓度为200、300和400μg/ml的万古霉素纳米颗粒的有效肠道渗透率值高于相同浓度的溶液。口服分数吸收在0.419-0.767之间。
我们的研究结果表明，RS-100纳米颗粒可为万古霉素提供一种递送系统，增强其肠道通透性。
