含游离蛋黄卵磷脂的姜黄素自纳米乳的制备及体外质量评价

Preparation of curcumin self-nanoemulsifying drug delivery system containing free egg phospholipid and in vitro quality evaluation

目的制备含游离蛋黄卵磷脂的姜黄素自纳米乳(EP-CUR-SNEDDS),并对其进行体外质量评价。方法先将姜黄素(CUR)制备成姜黄素自纳米乳(CUR-SNEDDS),采用星点设计-响应曲面法确定最佳处方。再加入蛋黄卵磷脂(EP)使体系稳定,制备成EP-CURSNEDDS,以粒径与Zeta电位为评价指标确定最优处方,并以溶出度和稳定性为指标进行体外评价。结果制备的CUR-SNEDDS、EP-CUR-SNEDDS均为澄清透明均一的油状液,乳滴呈类球形且分布均匀,粒径均小于30 nm,Zeta电位分别为(-0.97±1.43)mV、(-35.63±0.81)mV。室温长期放置下,CUR-SNEDDS颜色略有加深、药物少量析出,处于不稳定状态;而EP-CURSNEDDS稳定性良好,乳化后粒径无明显变化。EP-CUR-SNEDDS相较于CUR-SNEDDS,在显著提高姜黄素的体外溶出速率及程度的同时制剂更加稳定。结论成功制备了粒径均一、载药量较高和稳定性好的EP-CUR-SNEDDS,在提高药物的生物利用度方面更具潜力。

Objective To prepare the curcumin self-nanoemulsifying drug delivery system containing free egg phospholipid(EP-CUR-SNEDDS)and evaluate its in vitro quality.Methods First,curcumin was prepared into curcumin self-nanoemulsifying drug delivery system(CUR-SNEDDS).The optimal formulation was evaluated by central composite design-response surface methodology.EP was added to stabilize the system.The particle size and Zeta potential were used as evaluation indexes to determine the optimal prescription.The dissolution rate and stability in vitro were used as the indexes for the in vitro evaluation.Results The prepared CUR-SNEDDS,and EP-CUR-SNEDDS were all transparent with uniform oily liquids,with emulsion droplets being spherical and uniformly distributed.The particle diameters were all less than 30 nm,and the Zeta potentials were(-0.97±1.43)mV,and(-35.63±0.81)mV respectively.After long-term storage at room temperature,the color of CURSNEDDS was slightly deepened and a small amount was precipitated,indicating an unstable state.The EP-CUR-SNEDDS was stable,and the particle size had no obvious change after the emulsification.Compared with CUR-SNEDDS,EP-CUR-SNEDDS had higher dissolution rate and degree of curcumin in vitro,and were more stable preparation.Conclusion EP-CUR-SNEDDS with uniform particle size,high drug loading and good stability has been prepared,with better potential in bioavailability.