Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo

J Microencapsul. 2012;29(3):296-307. doi: 10.3109/02652048.2011.651495. Epub 2012 Jan 27.

Abstract

Objective: To formulate and evaluate solid-reversed-micellar-solution (SRMS)-based solid lipid microparticles (SLMs) for intramuscular administration of gentamicin.

Methods: SRMS formulated with Phospholipon® 90G and Softisan® 154 were used to prepare gentamicin-loaded SLMs. Characterizations based on size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release of gentamicin from the SLMs was performed in phosphate buffer while in vivo release studies were conducted in rats.

Results: Maximum EE% of 90.0, 91.6 and 83.0% were obtained for SLMs formed with SRMS 1:1, 1:2 and 2:1, respectively. Stable, spherical and smooth SLMs of size range 9.80 ± 1.46 µm to 33.30 ± 6.42 µm were produced. The release of gentamicin in phosphate buffer varied widely with the lipid contents. Moreover, significant (p < 0.05) amount of gentamicin was released in vivo from the SLMs.

Conclusion: SRMS-based SLMs would likely offer a reliable means of delivering gentamicin intramuscularly.

MeSH terms

  • Animals
  • Buffers
  • Calorimetry, Differential Scanning / methods
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers
  • Drug Compounding
  • Drug Delivery Systems
  • Gentamicins / administration & dosage*
  • Gentamicins / chemistry*
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Injections, Intramuscular / methods
  • Kinetics
  • Lipids / chemistry*
  • Micelles
  • Microspheres*
  • Particle Size
  • Phosphates / chemistry
  • Rats
  • Temperature

Substances

  • Buffers
  • Drug Carriers
  • Gentamicins
  • Lipids
  • Micelles
  • Phosphates