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. 2022 Nov 2;11(11):1530.
doi: 10.3390/antibiotics11111530.

Gentamicin-Ascorbic Acid Encapsulated in Chitosan Nanoparticles Improved In Vitro Antimicrobial Activity and Minimized Cytotoxicity

Mohamed A Abdel-Hakeem  1 , Ahmed I Abdel Maksoud  1   2 , Mohammed Abdullah Aladhadh  3 , Khalid Abdulrahman Almuryif  4 , Rafaat M Elsanhoty  2 , Dalia Elebeedy  1
Affiliations

Gentamicin-Ascorbic Acid Encapsulated in Chitosan Nanoparticles Improved In Vitro Antimicrobial Activity and Minimized Cytotoxicity

Mohamed A Abdel-Hakeem et al. Antibiotics (Basel). .

Abstract

Nano-drug delivery is a promising tactic to enhance the activity and minimize the cytotoxicity of antimicrobial drugs. In the current study, chitosan nanoparticles (CSNPs) were used as a carrier for the delivery of gentamicin sulfate (GM) and ascorbic acid (AA). The particles were synthesized by ionotropic gelation method and characterized by FT-IR, Zeta potential, and transmission electron microscope imaging. The obtained particles were evaluated for their in vitro antimicrobial activity and cytotoxicity. The prepared particles (GM-AA-CSNPs) under the optimal condition of 4:1:1 of chitosan to drug ratio showed encapsulation efficiency and loading capacities of 89% and 22%, respectively. Regarding biological activities, GM-AA-CSNPs showed a lower minimum inhibitory concentration (MIC) than free gentamicin sulfate and GMCSNPs mixture without presenting cytotoxicity against normal cells (HSF). Moreover, the GM-AA-CSNPs did not exhibit hemolytic activity. These results highlight that the GM-AA-CSNPs are confirmed as a hopeful formula for future investigations on the development of antimicrobial preparations.

Keywords: FTIR; antimicrobial drugs; chitosan nanoparticles (CSNPs); gentamicin sulfate (GM); nano-drug delivery.

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Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

Figure 1
Figure 1
EE% and LC% of GM (A) and AA (B) in GM–AA–CSNPs. CS:GM:AA ratio F1 (1:1:1)–F2 (2:1:1)–F3 (4:1:1).
Figure 2
Figure 2
In vitro release profile of GM (A) and AA (B) from CSNPs at different pH values.
Figure 3
Figure 3
Characterization of GM–AA–CSNPs. (A): TEM image; (B,C): Zeta potential.
Figure 4
Figure 4
FTIR spectra of CS (A) showed 3426 cm−1 (–OH and –NH2), 2922 cm−1, 2872 cm−1 (–CH), 1601 cm−1 (–NH2), and 1076 cm−1 (C–O–C). GM (B) showed characteristic peaks at 3150 cm−1 (–OH and –NH2 stretching) and 1526 cm−1 (C=N). AA (C) showed characteristic peaks at 3360 cm−1 (–COOH), 1700 cm−1, and 1650 cm−1 (C=O). GM–AA–CSNPs (D).
Figure 5
Figure 5
MICs and MBCs of free and loaded drugs for S. aureus (A) and P. aeruginosa (B). (*) represents the significant difference at p < 0.05 from the control and GM group.
Figure 6
Figure 6
Cell viability % of HSF cells after exposure to CSNPs, GM, AA, GM–AA–CSNPs, and GMCSNPs/AA mixture at different times. (*, a, b) represents the significant difference at p < 0.05 from the control, GM, and GMCSNPs groups, respectively.
Figure 7
Figure 7
Hemolysis assay of GMCSNPs and GM–AA–CSNPs against the positive and negative controls.
See this image and copyright information in PMC

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