Effect of polymer terminal groups on the drug release and experimental characterization of an electrospun naringin-loaded microsphere/sucrose acetate isobutyrate (SAIB) depot

摘要

The study was designed to develop an improved in situ injection drug delivery system by preparing naringin (Ng) loaded electrospray microspheres with different terminal groups PLGA and studying their effect on drug release and related properties of naringin-loaded electrospray microspheres/sucrose acetate isobutyrate (Ng-m-SAIB) depot. The electrospray technique was used to prepare microspheres, that were characterized for their shapes and size distribution, as well as the related properties of the Ng-m-SAIB depot were tested. The initial drug release rate of hydroxyl-terminated microspheres (OH-Ng-m) was lower than that of carboxyl-terminated microspheres (COOH-Ng-m) and ester-terminated microspheres (COOR-Ng-m). The burst release, on the first day after preparing the mixed depots of OH-/COOH/COOR-Ng-m-SAIB, was significantly decreased from 43.9%, 47.4%, and 56.1% to 1.6%, 2.4%, and 3.9%, respectively. During the 88-day release profile, OH-Ng-m-SAIB had a low drug release (1.39% per day) in the early stage, yet maintained a relatively stable drug release. These findings suggest that by modifying the PLGA terminal groups in electrospray microspheres, the drug release profile of Ng-m-SAIB depot can be effectively tailored.