科研之友
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摘要
It was aimed to develop albumin decorated phospholipid nanoemulsion of rapamycin for improved specificity at spinal cord injury site after systemic administration. Nanoemulsion was prepared by hot homogenization and ultrasonic emulsification of phospholipids. Interface of nanoemulsion was stabilized using cholesterol and functionalized by albumin. Nanoemulsion was optimized on the basis of particle size and zeta potential with the help of on one variable at time concept. Finally optimized nanoemulsion (RN7) was conjugated with albumin (ARN7) and both were evaluated for drug content, entrapment efficiency, morphology, in vitro release, in vitro cytotoxicity (MTT assay), in vitro anti-inflammatory potential (LPS induced model) and in vivo potential (post SCI like conditions in rat). Nano sized droplets with spherical shape, smooth surface and positive charge showed controlled release of rapamycin when compared with rapamycin solution (RS). RN7 and ARN7 kept astrocytes viable when compared with RS at the same dose. This may be due to avoidance of instant availability of rapamycin inside astrocytes. ARN7 showed significantly higher potential in reducing LPS induced pro-inflammatory cytokines when compared with RN7. Rapamycin delivery through ARN7 was found to be more effective in treating in vivo post SCI like conditions (behavioral and histopathological changes) when compared with RN7 due to the presence of albumin over the surface. In conclusion, albumin functionalized, cholesterol stabilized, phospholipid nanoemulsion was developed successfully with controlled release of rapamycin, improved cytokine inhibition and improved in vivo efficacy that may offer safe and effective mean for the treatment of post SCI like conditions.
- 出版日期2016
- 单位天津市中医药研究院附属医院; 中国人民解放军第二军医大学
