Effect of polyethylene glycol on preparation of rifampicin-loaded PLGA microspheres with membrane emulsification

Fuminori Ito1, Hiroyuki Fujimori, Hiroyuki Honnami

  • 1Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan. fuminoito@spice.ocn.ne.jp

Insights

Poly(lactide-co-glycolide) (PLGA) microspheres loaded with the anti-tubercle drug rifampicin (RFP) were prepared using membrane emulsification. Polyethylene glycol (PEG) addition improved microsphere uniformity and suppressed initial drug release.

Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Poly(lactide-co-glycolide) (PLGA) is a biodegradable polymer widely used for drug delivery.
  • Rifampicin (RFP) is a crucial anti-tubercle drug requiring effective delivery systems.
  • Controlling microsphere size and drug release is essential for therapeutic efficacy.

Purpose of the Study:

  • To prepare monodisperse poly(lactide-co-glycolide) (PLGA) microspheres loaded with rifampicin (RFP).
  • To investigate the effect of polyethylene glycol (PEG) on microsphere characteristics and drug release.
  • To optimize the preparation of RFP-loaded PLGA microspheres using Shirasu Porous Glass (SPG) membranes.

Main Methods:

  • Microsphere preparation via solvent evaporation and Shirasu Porous Glass (SPG) membrane emulsification.
  • Tuning microsphere size by altering SPG membrane pore size.
  • Evaluating the impact of polyethylene glycol (PEG) molecular weight and concentration on microsphere monodispersity and stability.

Main Results:

  • Monodisperse RFP-loaded PLGA microspheres were successfully prepared with varying sizes.
  • Polyethylene glycol (PEG) with a molecular weight of 20,000 significantly enhanced microsphere monodispersity.
  • The addition of PEG reduced the initial burst release of RFP from the PLGA microspheres.
  • A 100% yield of RFP-loaded PLGA microspheres was achieved.

Conclusions:

  • Membrane emulsification using SPG membranes is an effective method for producing monodisperse RFP-loaded PLGA microspheres.
  • Polyethylene glycol (PEG) acts as a crucial stabilizer, improving uniformity and controlling drug release kinetics.
  • Optimized PEG addition can lead to enhanced drug delivery systems with suppressed initial burst release.