Copolymers of pharmaceutical grade lactic acid and sebacic acid: drug release behavior and biocompatibility.
Pharmaceutical grade D,L-lactic acid, which is rather an economic source in comparison to lactide monomer, was utilized for synthesis of a series of copolymers with sebacic acid. Polymers were characterized by GPC, FTIR, NMR and DSC techniques, and formulated into blank and methotrexate (MTX) loaded microspheres by emulsion-solvent evaporation method. In vitro degradation of blank microspheres was studied by FTIR, GPC and SEM analysis. MTX loaded microspheres showed the encapsulation efficiency of 44-64% and were in the size range of 40-60 microm. These were used to study the release profile of the encapsulated drug. The release was found to be affected by the pH and buffer concentration of the release medium which was in turn revealed by solubility studies of MTX. The overall study demonstrates significance of drug as well as polymer properties on release. Biocompatibility of polymer was evaluated by injecting microspheres subcutaneously into Sprague-Dawley (SD) rat and no local histopathological abnormalities were found.
Modi
Sweta
S
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Mohali, India.
Jain
Jay Prakash
JP
Domb
A J
AJ
Kumar
Neeraj
N
D000818:Animals; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000009:adverse effects / Q000138:chemical synthesis*; D002021:Buffers; D002626:Chemistry, Pharmaceutical; D003652:Decanoic Acids / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D003998:Dicarboxylic Acids / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D005260:Female; D006863:Hydrogen-Ion Concentration; D007249:Inflammation / Q000139:chemically induced / Q000473:pathology; D007279:Injections, Subcutaneous; D007700:Kinetics; D019344:Lactic Acid / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D008727:Methotrexate / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D011108:Polymers / Q000008:administration & dosage / Q000009:adverse effects / Q000138:chemical synthesis*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013997:Time Factors
D001672:Biocompatible Materials; D002021:Buffers; D003652:Decanoic Acids; D003998:Dicarboxylic Acids; D004337:Drug Carriers; D011108:Polymers; D019344:Lactic Acid; C011107:sebacic acid; D008727:Methotrexate