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Updated: Jun 25, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Preparation of ciprofloxacin-encapsulated poly(DL-lactide-co-glycolide) microspheres and its antibacterial activity
Young-Il Jeong1, Hee-Sam Na, Jae-Woon Nah
1Department of Polymer Science and Engineering, Sunchon, Jeonnam 540-742, Republic of Korea.
Abstract:
In this study, we created ciprofloxacin.HCl (CIP)-encapsulated poly(DL-lactide-co-glycolide) (PLGA) microspheres by the solvent evaporation method. Their antibacterial activity was evaluated with pathogenic microorganisms in vitro and in vivo. Since the half-life of CIP in the blood stream is short, sustained-release properties of microspheres may provide enhanced antibacterial activity. CIP-encapsulated microspheres of PLGA were prepared by the O/O method. CIP-encapsulated PLGA microspheres showed spherical shapes under a scanning electron microscope (SEM), and their particle sizes ranged from 10 to 50 microm. In an in vitro drug release study, CIP was continuously released over 3 weeks from the microspheres, and a burst effect was observed for the first 3 days. In the in vitro antibacterial activity test, CIP-microspheres showed lower antibacterial activity compared to free CIP because of their sustained-release properties, while empty microspheres did not affect the growth of microorganisms. In the in vivo antibacterial activity test, the number of microorganisms following treatment with CIP-encapsulated microspheres was significantly lower than after treatment with free CIP at 5 days postinjection. These results suggest that encapsulated CIP keeps its antibacterial activity after microencapsulation.
Insights
This study developed ciprofloxacin hydrochloride (CIP)-encapsulated poly(DL-lactide-co-glycolide) (PLGA) microspheres. The sustained-release formulation demonstrated effective antibacterial activity in vivo, suggesting preserved efficacy after encapsulation.
Area of Science:
- Biomaterials Science
- Pharmaceutical Sciences
- Microbiology
Background:
- Ciprofloxacin hydrochloride (CIP) has a short bloodstream half-life, limiting its therapeutic efficacy.
- Developing sustained-release drug delivery systems can improve antibiotic pharmacokinetics and therapeutic outcomes.
- Poly(DL-lactide-co-glycolide) (PLGA) microspheres are a promising platform for controlled drug delivery.
Purpose of the Study:
- To create and characterize CIP-encapsulated PLGA microspheres using the solvent evaporation method.
- To evaluate the in vitro and in vivo antibacterial activity of the developed microspheres.
- To assess the sustained-release properties and antibacterial efficacy of encapsulated CIP.
Main Methods:
- CIP-encapsulated PLGA microspheres were prepared via the O/O solvent evaporation method.
- Microsphere morphology and particle size (10-50 microm) were analyzed using scanning electron microscopy (SEM).
- In vitro drug release studies were conducted over 3 weeks, and in vitro/in vivo antibacterial activity was tested against pathogenic microorganisms.
Main Results:
- CIP-PLGA microspheres exhibited spherical morphology and sustained CIP release over 3 weeks, with an initial burst effect.
- In vitro tests showed reduced antibacterial activity for CIP-microspheres compared to free CIP due to sustained release.
- In vivo studies demonstrated significantly lower microorganism counts with CIP-microspheres compared to free CIP at 5 days post-injection.
Conclusions:
- CIP-encapsulated PLGA microspheres maintain their antibacterial activity after the encapsulation process.
- The sustained-release properties of PLGA microspheres enhance the in vivo antibacterial efficacy of ciprofloxacin.
- This formulation holds potential for improved therapeutic strategies against bacterial infections.
