Fabrication of a new composite scaffold material for delivering rifampicin and its sustained drug release in rats

MA Xueming; LIN Zhen; ZHANG Jiawei; SANG Chaohui; QU Dongbin; JIANG Jianming

doi:10.3969/j.issn.1673-4254.2016.03.03

Abstract：Objective To fabricate a new composite scaffold material as an implant for sustained delivery of rifampicin and evaluate its performance of sustained drug release and biocompatibility. Methods The composite scaffold material was prepared by loading poly(lactic-co-glycolic) acid (PLGA) microspheres that encapsulated rifampicin in a biphasic calcium composite material with a negative surface charge. The in vitro drug release characteristics of the microspheres and the composite scaffold material were evaluated;the in vivo drug release profile of the composite scaffold material implanted in a rat muscle pouch was evaluated using high-performance liquid chromatography. The biochemical parameters of the serum and liver histopathologies of the rats receiving the transplantation were observed to assess the biocompatibility of the composite scaffold material. Results The encapsulation efficiency and drug loading efficiency of microspheres were (56.05 ± 5.33)% and (29.80 ± 2.88)%, respectively. The cumulative drug release rate of the microspheres in vitro was (94.19 ± 5.4)% at 28 days, as compared with the rate of (82.23±6.28)%of composite scaffold material. The drug-loaded composite scaffold material showed a good performance of in vivo drug release in rats, and the local drug concentration still reached 16.18±0.35μg/g at 28 days after implantation. Implantation of the composite scaffold material resulted in transient and reversible liver injury, which was fully reparred at 28 days after the implantation. Conclusion The composite scaffold material possesses a good sustained drug release capacity and a good biocompatibility, and can serve as an alternative approach to conventional antituberculous chemotherapy.