Preparation, characterization and in vitro release properties of ibuprofen-loaded microspheres based on polylactide, poly(epsilon-caprolactone) and their copolymers.
In this paper, ibuprofen was encapsulated into microspheres by oil-in-water (o/w) emulsion solvent evaporation method. Biodegradable polymers with certain compositions and characteristics such as polylactide (PLA), poly(epsilon-caprolactone) (PCL) and their block copolymer were used to prepare the microspheres. The results indicate that, under the same processing conditions, the drug entrapment efficiency was similar (approximately 80%) for microspheres prepared with PLA and P(LA-b-CL) (78.7/21.3 by mole), but it was only 25.4% for PCL microspheres. The in vitro drug release rate decreased in the order of PCL, P(LA-b-CL) (78.7/21.3 by mole) and PLA microspheres. PCL microspheres showed more serious burst release during the first day (almost 80%) than P(LA-b-CL) (50%) and PLA microspheres (18%). The complete ibuprofen release duration from the last two kinds of microspheres exceeded 1 month. Characterization of the microspheres by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and polarized optical microscope (POM) revealed that ibuprofen was amorphous in PCL microspheres and partially crystalline in P(LA-b-CL) and PLA microspheres. The different release behaviour of ibuprofen from the three kinds of microspheres could be attributed to the different crystallinity of the studied polymers and drug dispersion state in polymer matrices. All the above results suggest that the copolymer with a certain ratio of lactide to -caprolactone could have potential applications for long-term ibuprofen release.
Zhu
K J
KJ
Zhejiang University, Hangzhou, PR China. kjzhu@ipsm.zju.edu.cn
Li
Y
Y
Jiang
H L
HL
Yasuda
H
H
Ichimaru
A
A
Yamamoto
K
K
Lecomte
P
P
Jerome
R
R
D000042:Absorption; D002152:Calorimetry, Differential Scanning / Q000379:methods; D003460:Crystallization; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods*; D007052:Ibuprofen / Q000493:pharmacokinetics; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008859:Microscopy, Polarization / Q000379:methods; D008863:Microspheres; D010316:Particle Size; D011091:Polyesters; D013499:Surface Properties
D003692:Delayed-Action Preparations; D011091:Polyesters; C016240:polycaprolactone; C033616:poly(lactide); D007052:Ibuprofen