In vitro characterization of polyorthoester microparticles containing bupivacaine.
Laboratory-scale spray-congealing equipment was utilized to fabricate injectable microparticles consisting of polyorthoester and bupivacaine. Operating conditions for the spray-congealing process were optimized to produce microparticles with the desired shape and particle size to yield acceptable syringeability and injectability. Characterizations were performed to determine the chemico-physical properties of polyorthoester before and after microparticle fabrication. Microparticles with different drug loadings and comparable particle sizes were produced, and their in vitro drug-release profiles were determined. The in vitro drug release of microparticles with a high drug loading was markedly faster than those with a low drug loading. This is partially attributed to a more significant initial burst-drug release of the microparticles with a high drug loading. The microparticles have demonstrated the potential to be used for long-acting postsurgery pain management by local injection.
Deng
Jone-Shin
JS
Advanced Drug Delivery, Hospital Products Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA. dengjs@hpd.abbott.com
Li
Luk
L
Tian
Youqin
Y
Ginsburg
Eric
E
Widman
Matthew
M
Myers
Alecia
A
D002045:Bupivacaine / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D008863:Microspheres; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*
D011091:Polyesters; D002045:Bupivacaine