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Updated: Jan 2, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Synthesis and evaluation of polymeric micelle containing piperacillin/tazobactam for enhanced antibacterial activity
Milani Morteza1,2, Salehi Roya3,2, Hamishehkar Hamed3
1Infectious and Tropical Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Abstract:
Infections caused by multidrug-resistant bacteria such as P. aeruginosa are important therapeutic complications. Piperacillin/Tazobactam is considered a safe antimicrobial agent. But we should not ignore the prevalence of resistant strains to this drug. In this work, a new polymeric micelle composed of Piperacillin/Tazobactam-loaded Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (PLGA-PEG) was developed to improve the antimicrobial performance of P/T. The SEM and TEM studies of PLGA-PEG micelle showed, semi-spherical morphology with a mean diameter of below 30 nm. Zeta potential results indicated that the surface charge of PLGA-PEG micelle was -2.98 mV, while after encapsulation of P/T, the surface charge decreases to -4.13 mV. Clinical strains of P. aeruginosa were isolated and their resistance pattern against different antibiotics was evaluated. The MIC of free and P/T -Loaded PLGA-PEG micelles was determined. Also, the effect of free or P/T micelle against minimal biofilm eradication concentration and motility inhibition was evaluated. The bacterial isolates were resistant to most common antibiotics. The MIC of the free drug form and micelle form ranged from 4 to 512 µg/ml and 2 to 256 µg/ml, respectively. Generally, micelle showed more effective antibiofilm activities, inhibition of bacterial motility and reducing the MIC than that free drug form.
Insights
A novel polymeric micelle encapsulating Piperacillin/Tazobactam (P/T) enhances antimicrobial activity against multidrug-resistant Pseudomonas aeruginosa. This P/T-loaded micelle formulation demonstrates improved efficacy in reducing minimal inhibitory concentration and inhibiting biofilm formation.
Area of Science:
- Microbiology
- Materials Science
- Nanotechnology
Background:
- Multidrug-resistant bacteria, particularly Pseudomonas aeruginosa, pose significant therapeutic challenges.
- Piperacillin/Tazobactam (P/T) is a crucial antibiotic, but resistance to it is emerging.
- Developing novel drug delivery systems is essential to overcome antimicrobial resistance.
Purpose of the Study:
- To develop and characterize a new polymeric micelle system for Piperacillin/Tazobactam (P/T).
- To evaluate the enhanced antimicrobial performance of P/T-loaded micelles against resistant Pseudomonas aeruginosa.
- To assess the impact of the micelle formulation on biofilm eradication and bacterial motility.
Main Methods:
- Synthesis and characterization of Piperacillin/Tazobactam-loaded Poly(ethylene glycol) methyl ether-block-poly(lactide-co-glycolide) (PLGA-PEG) micelles using SEM, TEM, and zeta potential measurements.
- Isolation and antibiotic resistance profiling of clinical Pseudomonas aeruginosa strains.
- Determination of Minimum Inhibitory Concentration (MIC), Minimal Biofilm Eradication Concentration (MBEC), and motility inhibition assays for free P/T and P/T-loaded micelles.
Main Results:
- PLGA-PEG micelles exhibited a semi-spherical morphology with a mean diameter below 30 nm.
- Encapsulation of P/T into PLGA-PEG micelles resulted in a more negative surface charge (-4.13 mV) compared to blank micelles (-2.98 mV).
- P/T-loaded micelles showed a reduced MIC (2-256 µg/ml) compared to free P/T (4-512 µg/ml) against resistant P. aeruginosa strains.
- The micelle formulation demonstrated superior antibiofilm activity and bacterial motility inhibition compared to the free drug.
Conclusions:
- The developed PLGA-PEG polymeric micelle system effectively encapsulates Piperacillin/Tazobactam.
- This novel formulation significantly enhances the antimicrobial efficacy against multidrug-resistant Pseudomonas aeruginosa.
- The P/T-loaded micelles offer a promising strategy for combating antibiotic resistance by improving drug delivery and activity.
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