神经酰胺ⅢB磷脂复合物的制备及其评价

Preparation and evaluation of ceramideⅢB phospholipid complex

以神经酰胺ⅢB(CeramideⅢB,CerⅢB)和大豆卵磷脂(Phospholipid,PC)为原料,无水乙醇为反应溶剂,通过蒸发溶剂法制备CerⅢB-磷脂复合物(Ceramide phospholipid complex,CerPC)。通过正交实验优化工艺后,利用傅立叶变换红外光谱(FT IR)、差示扫描量热法(DSC)和扫描电镜(SEM)确定了CerPC的形成机制。采用Franz扩散池的Strat-M^(?)膜进行体外扩散试验,分析渗透性和保留性。采用鸡胚尿囊膜(CAM)试验对刺激性进行了分析。采用COX-2抑制剂筛选试剂盒测定神经酰胺ⅢB磷脂复合物对炎症因子COX-2的抑制率。结果表明,研究中设计的磷脂复合物制备方式安全有效,可以作为CerⅢB的载药系统以提高CerⅢB的生物利用度并扩大其应用领域。

Using ceramideⅢB(CerⅢB)and lecithin as raw materials and anhydrous ethanol as reaction solvent,ceramideⅢB phospholipid complex(CerPC)was prepared by evaporative solvent method.By orthogonal experiment,CerPC was prepared and confirmed according to the following method.CerⅢB(20.0 mg/mL)and phospholipids was added in anhydrous ethanol in a molar ratio of 1∶6 and stirred for 1.0 h at 60℃.The formation of CerPC was confirmed by using Fourier transform infrared(FT IR)spectroscopy,differential scanning calorimetry(DSC),and scanning electron microscopy(SEM).Permeability and retention were analyzed by an in vitro diffusion test in a Franz diffusion cell with a Strat-M^(?)membrane.Safety and irritation were analyzed by a chick embryo chorioallantois membrane(CAM)assay.The inhibition rate of CerPC on inflammatory factor COX-2 was determined by using a COX-2 inhibitor screening kit.The results show that the preparation method of the phospholipid complex designed in this study is safe and effective,and thus can be used as a drug delivery system for CerⅢB to improve its bioavailability and expand its application field.