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目的制备关节腔注射用盐酸青藤碱固体脂质纳米粒(盐酸青藤碱-SLN)温敏凝胶并考察其体外释放特征。方法以泊洛沙姆407(P-407)和泊洛沙姆188(P-188)为凝胶基质,以凝胶胶凝温度为考察对象对处方进行优化;微乳液法制备盐酸青藤碱-SLN,冷溶法制备盐酸青藤碱-SLN温敏凝胶;用HPLC法测定盐酸青藤碱的量,透析法研究盐酸青藤碱-SLN温敏凝胶的体外释放特性。结果最佳处方为18%P-407、5%P-188和0.6%羟丙基甲基纤维素(HPMC),所制盐酸青藤碱-SLN温敏凝胶胶凝温度为(34.5±0.2)℃。体外释放结果显示盐酸青藤碱-SLN温敏凝胶24 h内累积释放率为(57.79±0.36)%,48 h内累积释放率为(75.16±0.12)%,具有明显的缓释作用。结论所制盐酸青藤碱-SLN温敏凝胶具有温敏特性和明显的缓释作用,纳米载体和温度敏感凝胶的组合有望成为新的关节腔给药传递系统。
Objective To prepare sinomenine solid lipid nanoparticles (Sinomenine Hydrochloride - SLN) thermo - sensitive gel for intraarticular injection and investigate its in vitro release characteristics. Methods Poloxamer 407 (P-407) and poloxamer 188 (P-188) were used as the gel matrix to optimize the formulation with the gelling temperature as the study object. The microemulsion method was used to prepare sinomenine hydrochloride- SLN and cold-dissolving method were used to prepare sinomenine-SLN thermosensitive gel. The amount of sinomenine hydrochloride was determined by HPLC. The in vitro release characteristics of sinomenine-SLN thermo-sensitive gel were investigated by dialysis. Results The best prescription was 18% P-407, 5% P-188 and 0.6% hydroxypropyl methylcellulose (HPMC). Sinomenine -SLN thermosensitive gel gelation temperature was 34.5 ± 0.2 ℃ . The in vitro release results showed that sinomenine-SLN thermo-sensitive gel accumulated within 24 h and the cumulative release rate within 48 h was (57.79 ± 0.36)% and (75.16 ± 0.12)%, respectively. CONCLUSION Sinomenine-SLN thermosensitive gels have thermo-sensitive properties and obvious sustained-release effects. The combination of nanocarriers and temperature-sensitive gels is expected to be a new delivery system for joint cavity delivery.