Porous biodegradable microparticles for delivery of pentamidine.
The primary objective of this study was to develop a method for the preparation of porous biodegradable controlled release formulation of poly(lactide/glycolide) (PLGA). The model drug used for this study was pentamidine. Scanning electron microscopy pictures showed that these microparticles are highly porous and spherical in shape. A comparison of particle size reveals a similar median particle size (54-68 microm) in all six batches. The particles are all smaller than 90 microm. Differential scanning calorimetry thermograms revealed that pentamidine was mostly present in the crystalline form in the microparticles and did not dissolve in PLGA. The efficiency of encapsulation of pentamidine was higher than 58% in all six batches. The amount of drug released from these microparticles was at least 12% within the first 60 min. At least 50% of the total drug was released within the first 4 h. Drug release from these microparticles continued for up to 12 h. This faster drug dissolution was due to the highly porous surface. This highly porous surface will allow large molecules to release at a much faster rate than the regular microcapsules/microspheres.
Mandal
T K
TK
Division of Pharmaceutics, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Dr., New Orleans, LA 70125, USA. tmandal@xula.edu
Bostanian
L A
LA
Graves
R A
RA
Chapman
S R
SR
Idodo
T U
TU
D001673:Biodegradation, Environmental; D016503:Drug Delivery Systems; D019344:Lactic Acid / Q000008:administration & dosage*; D008863:Microspheres; D010419:Pentamidine / Q000008:administration & dosage* / Q000737:chemistry; D011100:Polyglycolic Acid / Q000008:administration & dosage*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000008:administration & dosage*; D012995:Solubility
D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D010419:Pentamidine