丹皮酚非离子表面活性剂囊泡的制备及其体外释放研究

Preparation of Paeonol Non-ionic Surfactant Vesicles and In Vitro Release of Paeonol

目的研究非离子表面活性囊泡对丹皮酚的包封作用及其体外释放行为的影响,为丹皮酚体内给药提供一种新的剂型,以期改善丹皮酚水溶性差、稳定性低等缺陷。方法采用改进的乙醇注入法,利用非离子表面活性剂Span60、胆固醇、PEG-SA为囊材,以丹皮酚为模型药物,制备非离子表面活性剂载药囊泡,通过包封率、粒径和电位的测定等优化出最佳的工艺,采用正交试验确定最佳处方,研究表面活性剂囊泡在模拟体液中的释放行为。结果表面活性剂囊泡的最佳处方为:Span60 80mg,胆固醇30mg,PEG15-SA 30mg,丹皮酚30mg,水合介质磷酸盐缓冲液(pH值=7.4)60mL。体外释放行为表明,表面活性剂囊泡具有明显的缓释作用。结论该方法制备的PEG化丹皮酚非离子表面活性剂囊泡具有较高的包封率以及很高的稳定性,PEG化泡囊作为丹皮酚载体有着潜在的应用价值。

Objective To investigate the effects of non-ionic surfactant vesicle encapsulation on paeonol （Pae） and its in vitro release behavior, and to provide a new formulation for in vivo administration of Pae to improve its aqueous solubility and stability. Methods The PEGylated non-ionic surfactant vesicles （NISVs） drug delivery systems were prepared from biocompatible non-ionic surfactant of Span60, choles- terol, and polyethylene glycol monostearate 15 （PEG15-SA） by the improved ethanol injection method, and Pae was used as a model drug. The optimized preparing process of PEG-Pae-NISVs （P-Pae-NISVs） was determined by encapsulation efficiency, particle size, and Zeta potential of the P-Pae-NISVs. The or- thogonal test was used to investigate the release behavior of surfactant vesicles in simulated body fluid to determine the optimal formulation of P-Pae-NISVs. Results The optimal formulation of P-Pae-NISVs was 80 mg Span60 ＋ 30 mg cholesterol ＋ 30 mg PEG15-SA ＋ 30 mg Pae ＋ 60 mL phosphate buffer saline （pH =7.4）. The release studies of Pae from P-Pae-NISVs in vitro exhibited a prolonged release profile as studied over 360 min. Conclusion The P-Pae-NISVs prepared in this way have high encapsulation efficiency and colloidal stability. The PEGylated niosome holds a promising application value as the carrier of Pae.