Lotfipour F, Abdollahi S, Jelvehgari M, Valizadeh H, Hassan M, Milani M
Hematology and Oncology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Res (Stuttg). 2014 Jul;64(7):348-52. doi: 10.1055/s-0033-1358747. Epub 2013 Dec 4.
Researchers have demonstrated that antimicrobial agents in nanoparticle (NP) forms have better activities. Vancomycin (VCM), as a glycopeptide antibiotic with antimicrobial activity against gram positive bacteria, is poorly absorbed from the intestinal tract. Enterococcus is a genus of bacteria that became resistant to a wide range of antibiotics in last decades, and cause severe infections in hospitalized patients. This paper describes preparation of VCM--loaded poly (lactic-co-glycolic acid) (PLGA) NPs and compares the antimicrobial effects with drug solution against clinical Enterococcus isolates. VCM-loaded PLGA NPs were fabricated by W1/O/W2 solvent evaporation method. The comparison of obtained Minimum Inhibitory Concentration (MIC) values showed a significant decrease in the antimicrobial effect of VCM -loaded NPs. Results also indicated that the potency of the NPs against VCM resistant isolates of Enterococcus was less than VCM susceptible isolates. The reduced antimicrobial effect of formulated NPs in invitro condition is perhaps related to the strong electrostatic linkage between hydrophilic drug (VCM) and hydrophobic polymer (PLGA) that lead to the slow release of the antibiotic from polymeric NPs.
研究人员已证明纳米颗粒（NP）形式的抗菌剂具有更好的活性。万古霉素（VCM）作为一种对革兰氏阳性菌具有抗菌活性的糖肽类抗生素，在肠道中的吸收较差。肠球菌是一类细菌，在过去几十年中对多种抗生素产生了耐药性，并在住院患者中引起严重感染。本文描述了负载万古霉素的聚乳酸-羟基乙酸共聚物（PLGA）纳米颗粒的制备，并将其与药物溶液对临床分离的肠球菌的抗菌效果进行了比较。通过W1/O/W2溶剂蒸发法制备了负载VCM的PLGA纳米颗粒。对获得的最低抑菌浓度（MIC）值的比较表明，负载VCM的纳米颗粒的抗菌效果显著降低。结果还表明，纳米颗粒对万古霉素耐药的肠球菌分离株的效力低于对万古霉素敏感的分离株。在体外条件下，配制的纳米颗粒抗菌效果降低可能与亲水性药物（VCM）和疏水性聚合物（PLGA）之间的强静电连接有关，这导致抗生素从聚合物纳米颗粒中缓慢释放。
