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Hydrophilic drug release from bioerodible polyanhydride microspheres
Author(s) -
VasheghaniFarahani Ebrahim,
Khorram Mohammad
Publication year - 2001
Publication title -
journal of applied polymer science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.575
H-Index - 166
eISSN - 1097-4628
pISSN - 0021-8995
DOI - 10.1002/app.10007
Subject(s) - prepolymer , copolymer , solubility , condensation polymer , theophylline , monomer , materials science , polymer chemistry , chloroform , solvent , dosage form , chemistry , nuclear chemistry , organic chemistry , chromatography , polymer , polyurethane , medicine , endocrinology
Abstract The present investigation was carried out to develop bioerodible drug delivery systems. Copolymers of fumaric anhydride and isophthalic anhydride were synthesized by melt polycondensation. To synthesize a copolymer with known composition, soluble in common organic solvents, a prepolymer of each monomer was first prepared. Copolymers were synthesized by mixing two prepolymers followed by melt polycondensation of the resulting mixture with a specific ratio of each prepolymer. Microspheres loaded with theophylline and diltiazem hydrochloride (DHC) were obtained using the solvent removal method in an oil‐in ‐oil (O/O) emulsion system. The size of the drug loaded microspheres was less than 75 μm, which is suitable for subcutaneous or intramuscular injection. DHC was incorporated in a polymeric carrier better than theophylline because of its solubility in chloroform and dichloromethane. In vitro release of two drugs in the phosphate buffer solution indicated that the release profile of DHC was closer to a zero‐order kinetic profile compared with theophylline. Finally, drug release data was compared with three semiempirical models. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 83: 1457–1464, 2002