Hill Marcus, Cunningham Richard N, Hathout Rania M, Johnston Christopher, Hardy John G, Migaud Marie E
School of Pharmacy, Queen's University Belfast, Belfast BT7 1NN, UK.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt.
J Funct Biomater. 2019 Jun 13;10(2):26. doi: 10.3390/jfb10020026.
Tobramycin is a potent antimicrobial aminoglycoside and its effective delivery by encapsulation within nanoparticle carriers could increase its activity against infections through a combination of sustained release and enhanced uptake. Effective antimicrobial therapy against a clinically relevant model bacteria () requires sufficient levels of therapeutic drug to maintain a drug concentration above the microbial inhibitory concentration (MIC) of the bacteria. Previous studies have shown that loading of aminoglycoside drugs in poly(lactic-co-glycolic) acid (PLGA)-based delivery systems is generally poor due to weak interactions between the drug and the polymer. The formation of complexes of tobramycin with dioctylsulfosuccinate (AOT) allows the effective loading of the drug in PLGA-nanoparticles and such nanoparticles can effectively deliver the antimicrobial aminoglycoside with retention of tobramycin antibacterial function.
妥布霉素是一种强效抗菌氨基糖苷类药物，通过包裹在纳米颗粒载体中实现有效递送，可通过缓释和增强摄取的组合提高其抗感染活性。针对临床相关模型细菌进行有效的抗菌治疗需要足够水平的治疗药物，以维持药物浓度高于细菌的微生物抑制浓度（MIC）。先前的研究表明，由于药物与聚合物之间的相互作用较弱，氨基糖苷类药物在聚乳酸-乙醇酸共聚物（PLGA）基递送系统中的负载通常较差。妥布霉素与二辛基磺基琥珀酸酯（AOT）形成复合物，可使药物有效负载于PLGA纳米颗粒中，此类纳米颗粒可有效递送抗菌氨基糖苷类药物，并保留妥布霉素的抗菌功能。
