Abstract
In this work, poly(lactic-co-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.
Highlights
Infectious diseases are recognized as a public health challenge [1]
The results show that the use of these loaded LEV poly(lactic-co-glycolic acid) (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
The goal was to find the best nanoformulation with the highest EE, adequate size, and appropriate antibiotic release
Summary
Infectious diseases are recognized as a public health challenge [1]. The appearance of antibiotics, more than 70 years ago, has totally changed the treatment of infectious diseases, contributing to significantly diminish the associated mortality [2]. The use of nanocarriers as antibiotic delivery systems could help to improve the current limitations associated to antibiotic therapy. Antibiotics could be poorly soluble in water, sensitive to temperature, and degraded by proteolytic enzymes They will be protected (encapsulated) inside the nanocarriers. The use of nanocarriers can be considered as an excellent approach to avoid, at least partially, the limitations associated with antibiotic therapy. The selection of the nanoencapsulation method should take into account the drug nature, personnel safety, the nanoparticle requirements, etc. Methods such as emulsion–solvent evaporation/extraction, nanoprecipitation, salting out, emulsion solvent diffusion, ionic gelation, and many others have been used [2,17,18,19]
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