Iranian journal of basic medical sciences · 2026
Preparation, characterization, and comparison of the release of antibacterial peptide CM11 from PLGA nanoparticles and microparticles.
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Eshaghi Mohammadmahdi, Moosazadeh Moghaddam Mehrdad, Dehghani Marzieh, Jonaidi-Jafari Nematollah, Hesarikia Hamid, Taheri Ramezan Ali
Аннотация
OBJECTIVES: Pseudomonas aeruginosa (P. aeruginosa) is a Gram-negative bacterium capable of causing acute and chronic infections. Treating these infections is increasingly challenging as this bacterium develops antibiotic resistance. Antimicrobial peptides (AMPs) have emerged as promising therapeutic candidates due to their broad-spectrum activity. Cecropin-Melittin-11 (CM11), a cationic AMP, has shown antimicrobial activity against various pathogens. However, the progression of AMPs from preclinical research to clinical application is hindered by enzymatic degradation, short systemic half-life, and cytotoxicity. To overcome these challenges, poly(lactic-co-glycolic acid)(PLGA) particles for peptide delivery have gained attention.
MATERIALS AND METHODS: CM11-loaded PLGA nanoparticles (NPCM11) and microparticles (MPCM11) were prepared using a double-emulsion solvent evaporation (W1/O/W2) method and characterized for particle size, morphology, encapsulation efficiency, and in vitro release. Their antibacterial activity against planktonic and biofilm-forming P. aeruginosa was evaluated using broth microdilution assay. Their cytocompatibility was evaluated using 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT) assay.
RESULTS: Optimum formulations of NPCM11 and MPCM11 were synthesized, exhibiting spherical morphology with average sizes of 281 nm and 7.63 µm, respectively. The encapsulation efficiency (EE%) of NPCM11 and MPCM11 was 63.5% and 60.3%, respectively, while the in vitro CM11 release was 82% and 58%. According to broth microdilution and biofilm inhibition assays, NPCM11 outperformed free CM11 and MPCM11 against planktonic bacteria, whereas both NPCM11 and MPCM11 were superior to free CM11 in biofilm inhibition. MTT assay revealed that NPCM11 and MPCM11 significantly reduced CM11 cytotoxicity.
CONCLUSION: Overall, NPCM11 and MPCM11 were promising formulations of CM11 for treating P. aeruginosa infections.
MATERIALS AND METHODS: CM11-loaded PLGA nanoparticles (NPCM11) and microparticles (MPCM11) were prepared using a double-emulsion solvent evaporation (W1/O/W2) method and characterized for particle size, morphology, encapsulation efficiency, and in vitro release. Their antibacterial activity against planktonic and biofilm-forming P. aeruginosa was evaluated using broth microdilution assay. Their cytocompatibility was evaluated using 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT) assay.
RESULTS: Optimum formulations of NPCM11 and MPCM11 were synthesized, exhibiting spherical morphology with average sizes of 281 nm and 7.63 µm, respectively. The encapsulation efficiency (EE%) of NPCM11 and MPCM11 was 63.5% and 60.3%, respectively, while the in vitro CM11 release was 82% and 58%. According to broth microdilution and biofilm inhibition assays, NPCM11 outperformed free CM11 and MPCM11 against planktonic bacteria, whereas both NPCM11 and MPCM11 were superior to free CM11 in biofilm inhibition. MTT assay revealed that NPCM11 and MPCM11 significantly reduced CM11 cytotoxicity.
CONCLUSION: Overall, NPCM11 and MPCM11 were promising formulations of CM11 for treating P. aeruginosa infections.