A novel preparation method for PLGA microspheres using non-halogenated solvents.
We investigated a new preparation method for microspheres based on an Oil/Water type emulsion solvent evaporation method using non-halogenated solvents. This method is based on phase separation between acetone and aqueous glycerol. For the preparation of microspheres by this method, a solution of poly(DL-lactic-co-glycolic acid) (PLGA) in acetone and aqueous glycerol containing poly(vinyl alcohol) were used asthe dispersed and continuous phases in the emulsification process, respectively. Vitamin B12 was used as the model drug. The formation of PLGA microspheres was observed above 60% glycerol in the continuous phase. The yield and encapsulation efficiency of the PLGA microspheres was about 80%, which was the maximum yield obtained with 70% glycerol. The release of vitamin B12 lasted for three weeks.
Matsumoto
Akihiro
A
Tanabe Seiyaku Co. Ltd., 2-10, Dosho-machi 3-chome, Chuo-ku, Osaka 541-8505, Japan. matsumoto.akihiro@mf.mt-pharma.co.jp
Kitazawa
Takeo
T
Murata
Junichi
J
Horikiri
Yuji
Y
Yamahara
Hiroshi
H
D000096:Acetone / Q000737:chemistry*; D004655:Emulsions; D005990:Glycerol / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D008863:Microspheres; D008970:Molecular Weight; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011142:Polyvinyl Alcohol / Q000737:chemistry; D012997:Solvents / Q000737:chemistry*; D014805:Vitamin B 12 / Q000493:pharmacokinetics / Q000494:pharmacology; D014867:Water / Q000737:chemistry
D004655:Emulsions; D009821:Oils; D012997:Solvents; D014867:Water; D000096:Acetone; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011142:Polyvinyl Alcohol; D014805:Vitamin B 12; D005990:Glycerol