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Effects of antibiotic physicochemical properties on their release kinetics from biodegradable polymer microparticles

Sarita R Shah1, Allan M Henslee, Patrick P Spicer

  • 1Department of Bioengineering, Rice University, MS-142, 6100 Main St., Houston, Texas, 77005, USA.

Pharmaceutical Research
|May 31, 2014
PubMed
Abstract

Insights

Antibiotic properties like molecular weight and charge significantly impact drug loading and release from poly(DL-lactic-co-glycolic acid) (PLGA) microparticles (MPs). This allows for predicting drug delivery behavior for improved antibiotic therapies.

Area of Science:

  • Biomaterials Science
  • Pharmaceutical Sciences
  • Drug Delivery

Background:

  • Poly(DL-lactic-co-glycolic acid) (PLGA) microparticles (MPs) are widely used for controlled drug release.
  • Understanding how antibiotic physicochemical properties influence PLGA MP performance is crucial for optimizing drug delivery systems.

Purpose of the Study:

  • To investigate the impact of antibiotic physicochemical properties on the characteristics of PLGA microparticles.
  • To analyze the effects on morphology, loading efficiency, size, release kinetics, and efficacy of antibiotics within PLGA MPs.

Main Methods:

  • Six antibiotics (cefazolin, ciprofloxacin, clindamycin, colistin, doxycycline, vancomycin) were loaded into PLGA MPs at 10% and 20% wt% using a double emulsion method.
  • Characterization included assessment of microparticle morphology, size, loading efficiency, in vitro release kinetics, and antibiotic efficacy.

Main Results:

  • Antibiotic molecular weight and charge significantly influenced loading efficiency and release kinetics from PLGA MPs.
  • Lower molecular weight (<600 Da) antibiotics showed biphasic release, while higher molecular weight (>1000 Da) antibiotics exhibited triphasic release.
  • All released antibiotics retained efficacy against susceptible strains, with release durations ranging from 17 to 49 days.

Conclusions:

  • The chemical nature of antibiotics is a key determinant of their behavior within PLGA microparticles.
  • These findings enable prediction of loading and release kinetics for antibiotic-loaded PLGA MPs, guiding formulation development.

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