Indomethacin microencapsulation in polymeric blends of PLGA502 and PEOT-PBT multiblock copolymer

Abstract

Indomethacin (IND) is a non-selective nonsteroidal anti-inflammatory drug (NSAIDs) with high anti-inflammatory, antipyretic and analgesic activity. It has been widely used in the therapeutical management of moderate to severe rheumatic disorders, including rheumatoid arthritis, osteoarthritis and gouty arthritis. Nonetheless, its use as a first-line and long-term therapy is limited by its dose-dependent severe gastrointestinal, renal and hematologic adverse effects. Local administration via intraarticular (I.A.) injection can be an alternative to achieve high drug concentrations into the joint, but the high clearance rate of most drugs limits its use as a long-term administration route. Microencapsulation seems to be an excellent approach to overcome those limitations, allowing us to increase the retention time of the drug into the joint and to achieve a controlled drug delivery profile. Nonetheless, IND microencapsulation in PLGA was previously reported, showing a high drug delivery rate. This work aims to prepare and characterize INDloaded microspheres made of a polymeric blend of PEOT-PBT and PLGA502 with convenient features to achieve an intra-articular long-term delivery profile