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

Monodisperse poly(lactide-co-glycolide) (PLGA) microspheres containing rifampicin (RFP), anti-tubercle drug, as hydrophobic model drug were prepared by solvent evaporation method with a membrane emulsification technique using Shirasu Porous Glass (SPG) membranes. Five kinds of rifampicin-loaded PLGA (RFP/PLGA) microspheres with different sizes were prepared by changing pore size of the membranes. Effect of polyethylene glycol (PEG) added to polyvinyl alcohol (PVA) solution (continuous phase) upon the monodispersity of microspheres was studied. PEG was used as a stabilizer for microspheres dispersing in PVA solution. The most suitable molecular weight of PEG as a stabilizer was 20,000. RFP/PLGA microspheres prepared with PEG20000 were apparently more uniform than those prepared without PEG. The yield of RFP/PLGA microspheres was 100%. The initial burst observed in the release of RFP from RFP/PLGA microspheres was suppressed by the addition of PEG.

[1]  S. Kasturi,et al.  Covalent conjugation of polyethyleneimine on biodegradable microparticles for delivery of plasmid DNA vaccines. , 2005, Biomaterials.

[2]  S. Omi.  Preparation of monodisperse microspheres using the Shirasu porous glass emulsification technique , 1996 .

[3]  D W Pack,et al.  Fabrication of PLG microspheres with precisely controlled and monodisperse size distributions. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[4]  T Yashiki,et al.  A new technique to efficiently entrap leuprolide acetate into microcapsules of polylactic acid or copoly(lactic/glycolic) acid. , 1988, Chemical & pharmaceutical bulletin.

[5]  O'donnell,et al.  Preparation of microspheres by the solvent evaporation technique. , 1997, Advanced drug delivery reviews.

[6]  M Dunne,et al.  Influence of particle size and dissolution conditions on the degradation properties of polylactide-co-glycolide particles. , 2000, Biomaterials.

[7]  G. G. Stokes.  "J." , 1890, The New Yale Book of Quotations.

[8]  G. Soma,et al.  Efficient intracellular delivery of rifampicin to alveolar macrophages using rifampicin-loaded PLGA microspheres: effects of molecular weight and composition of PLGA on release of rifampicin. , 2004, Colloids and surfaces. B, Biointerfaces.

[9]  M. Shimizu,et al.  Particle control of emulsion by membrane emulsification and its applications. , 2000, Advanced drug delivery reviews.

[10]  K. Makino,et al.  Preparation and properties of monodispersed rifampicin-loaded poly(lactide-co-glycolide) microspheres. , 2004, Colloids and surfaces. B, Biointerfaces.

[11]  T. Kondo,et al.  Preparation of Poly(D,L‐lactide) and Copoly(lactide‐glycolide) Microspheres of Uniform Size , 1996, The Journal of pharmacy and pharmacology.

[12]  H. Okada,et al.  Controlled-release of leuprolide acetate from polylactic acid or copoly(lactic/glycolic) acid microcapsules: influence of molecular weight and copolymer ratio of polymer. , 1988, Chemical & pharmaceutical bulletin.

[13]  M. Iso,et al.  Synthesis of polymeric microspheres employing SPG emulsification technique , 1994 .

[14]  Jayanth Panyam,et al.  Rapid endo‐lysosomal escape of poly(DL‐lactide‐coglycolide) nanoparticles: implications for drug and gene delivery , 2002, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.