Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)

Abstract

The aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid- co -polyethylene glycol) (PLA–PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro release study, it was proven that the MPs (both PLA/PVA- and PLA–PEG/PVA-based) demonstrated long-term AMI release (2 months), the kinetics of which adhered to the Korsmeyer–Peppas model. The loading efficiencies of AMI in the study were determined at the followings levels: 36.5 ± 1.5 μg/mg for the PLA-based MPs and 106 ± 32 μg/mg for the PLA–PEG-based MPs. These values were relatively high and draw parallels with studies published on the encapsulation of aminoglycosides. The MPs provided antimicrobial action against the Staphylococcus aureus , Escherichia coli , Pseudomonas aeruginosa , and Klebsiella pneumoniae bacterial strains. The materials were also comprehensively characterized by the following methods: differential scanning calorimetry; gel permeation chromatography; scanning electron microscopy; Fourier transform infrared spectroscopy–attenuated total reflectance; energy-dispersive X-ray fluorescence; and Brunauer–Emmett–Teller surface area analysis. The findings of this study contribute toward discerning new means for conducting targeted therapy with polar, broad spectrum antibiotics.

Amikacin-loaded niosome nanoparticles improve amikacin activity against antibiotic-resistant Klebsiella pneumoniae strains

“…The different amikacin- nanoparticles with different structures have been reported. The encapsulating of amikacin by using low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA-PEG), both supplemented with poly(vinyl alcohol) (PVA), was reported that the particle size was < 30 μm for long term release the MBC, MIC and, cytotoxicity was not determined (Glinka et al 2021 ). Another amikacin- nanoparticle is the combination of gold nanostars (GNS) and amikacin, in which it is the minimum inhibitory concentration (MIC), and minimal bactericidal concentration (MBC) were 80 and 160 µM of GNS for all strains, respectively (Aguilera-Correa et al 2022 ).…”

Antibacterial Porous Systems Based on Polylactide Loaded with Amikacin

“…Combining PLA with PVA also enhances the hydrophilicity and ductility of the resulting product [ 10 , 14 ]. Another finding is that PVA acts as an emulsifier when preparing materials from PLA and hydrophilic modifiers, e.g., hydrophilic drugs (W/O emulsion system) [ 15 ].…”

“…A few materials modified with AMI for wound healing have appeared in published papers; however, these concerned fabricated materials originating from natural polymers, e.g., chitosan-based porous matrices [ 31 ], alginate-based hydrogel membranes [ 32 , 33 ] and collagen [ 34 ]. In a previous work by the authors [ 15 ], a novel PLA-based material (microparticles) with encapsulated AMI was proposed. A description was given of the difficulties encountered when preparing the AMI-modified polymeric materials founded on hydrophobic synthetic polymers, in this case PLA [ 15 , 34 ].…”

“…In a previous work by the authors [ 15 ], a novel PLA-based material (microparticles) with encapsulated AMI was proposed. A description was given of the difficulties encountered when preparing the AMI-modified polymeric materials founded on hydrophobic synthetic polymers, in this case PLA [ 15 , 34 ]. In brief, the main issue related to the hydrophilicity of AMI, therein exceeding that of other aminoglycosides employed in medication (gentamicin, tobramycin, and especially neomycin).…”

Preparation and Characterization of Aminoglycoside-Loaded Chitosan/Tripolyphosphate/Alginate Microspheres against E. coli

“…However, their clinical use has been compromised by widespread instances of resistance [ 32 ] or adverse side effects such as ototoxicity and nephrotoxicity at high antibiotic doses [ 33 ], being the preparation of new aminoglycoside formulations that allow on-demand drug delivery a plausible solution to this sticky issue. Poly (lactic acid) or poly (lactic-co-glycolic acid)-based systems have been commonly employed for AGA encapsulation [ 34 , 35 , 36 ]; however, the formation of PLGA and PLA particles requires the use of organic solvents. This is a major drawback since, among other effects, the use of organic solvents can produce relevant toxicological effects and, moreover, can reduce the scalability and practical industrial application of these systems.…”