López-López Manuel, Fernández-Delgado Angela, Moyá María Luisa, Blanco-Arévalo Daniel, Carrera Cecilio, de la Haba Rafael R, Ventosa Antonio, Bernal Eva, López-Cornejo Pilar
Department of Chemical Engineering, Physical Chemistry and Materials Science, Faculty of Experimental Sciences, University of Huelva, Campus de El Carmen, Avda. de las Fuerzas Armadas s/n, 21071 Huelva, Spain.
Department of Physical Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain.
Pharmaceutics. 2019 Jan 30;11(2):57. doi: 10.3390/pharmaceutics11020057.
In this work, poly(lactic--glycolic acid) (PLGA) and chitosan (CS) nanoparticles were synthesized with the purpose of encapsulating levofloxacin (LEV). A thorough study has been carried out in order to optimize the preparation of LEV-loaded polymeric nanoparticles (NPs) suitable for parenteral administration. Changes in the preparation method, in the organic solvent nature, in the pH of the aqueous phase, or in the temperature were investigated. To the authors´ knowledge, a systematic study in order to improve the LEV nanocarrier characteristics and the yield of drug encapsulation has not been carried out to date. The physicochemical characterization of the NPs, their encapsulation efficiency (EE), and the in vitro release of LEV revealed that the best formulation was the emulsion-solvent evaporation method using dichloromethane as organic solvent, which renders suitable LEV loaded PLGA NPs. The morphology of these NPs was investigated using TEM. Their antimicrobial activities against several microorganisms were determined in vitro measuring the minimum inhibitory concentration (MIC). The results show that the use of these loaded LEV PLGA nanoparticles has the advantage of the slow release of the antibiotic, which would permit an increase in the time period between administrations as well as to decrease the side effects of the drug.
在本研究中，合成了聚乳酸-乙醇酸共聚物（PLGA）和壳聚糖（CS）纳米颗粒，用于包裹左氧氟沙星（LEV）。为了优化适合肠胃外给药的载LEV聚合物纳米颗粒（NPs）的制备，进行了深入研究。研究了制备方法、有机溶剂性质、水相pH值或温度的变化。据作者所知，迄今为止尚未开展旨在改善LEV纳米载体特性和药物包封率的系统研究。NPs的物理化学表征、其包封效率（EE）以及LEV的体外释放表明，最佳配方是使用二氯甲烷作为有机溶剂的乳化溶剂蒸发法，该方法可制备出合适的载LEV的PLGA NPs。使用透射电子显微镜（TEM）研究了这些NPs的形态。通过测量最小抑菌浓度（MIC）在体外测定了它们对几种微生物的抗菌活性。结果表明，使用这些载LEV的PLGA纳米颗粒具有抗生素缓释的优势，这将增加给药间隔时间并减少药物的副作用。
