The alkaline milieu of chronic wounds severely impairs the therapeutic effect of antibiotics, such as rifampicin; as such, the development of new drugs, or the smart delivery of existing drugs, is required. Herein, two innovative polyelectrolyte nanoparticles (PENs), composed of an amphiphilic chitosan core and a polycationic shell, were synthesized at alkaline pH, and in vitro performances were assessed by 1H NMR, elemental analysis, FT-IR, XRD, DSC, DLS, SEM, TEM, UV/Vis spectrophotometry, and HPLC. According to the results, the nanostructures exhibited different morphologies but similar physicochemical properties and release profiles. It was also hypothesized that the simultaneous use of the nanosystem and an antioxidant could be therapeutically beneficial. Therefore, the simultaneous effects of ascorbic acid and PENs were evaluated on the release profile and degradation of rifampicin, in which the results confirmed their synergistic protective effect at pH 8.5, as opposed to pH 7.4. Overall, this study highlighted the benefits of nanoparticulate development in the presence of antioxidants, at alkaline pH, as an efficient approach for decreasing rifampicin degradation.
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.
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