苍艾油传递体的制备工艺及体外释药研究

Study on Preparation Technology and Release in vitro of Cangai Oil Transfersomes

  • 摘要: 目的 制备苍艾油传递体,并对其体外释药行为进行考察。方法 采用薄膜-超声法制备以胆酸钠及丙二醇为膜软化材料的苍艾油传递体,通过石油醚萃取-UV法测定其包封率;并通过HPLC检测指标性成分丁香酚,研究其体外释放及经皮渗透行为。结果 通过优选处方制得的苍艾油传递体的平均粒径为(149±4.37)nm,多分散指数为0.189±0.024,包封率为(89±2.50)%,Zeta电位为(-42.95±1.78)mV。体外释放结果显示苍艾油体外释放在6 h基本达到稳态,而苍艾油传递体及苍艾油脂质体到12 h仍呈持续释放趋势;体外经皮渗透结果显示从6 h开始苍艾油传递体较苍艾油脂质体及苍艾油均具有更高的累积渗透量(P<0.05)。结论 通过优选工艺制备的苍艾油传递体外观圆整、粒径分布较窄,在增加苍艾油溶解度的同时,还能起到一定的缓释效果,且将其通过体外经皮给药后还能显著增加苍艾油的透皮效率,是一个有较好潜力的经皮给药载体。

     

    Abstract: OBJECTIVE To study the preparation of Cangai oil transfersomes and investigate its release behavior in vitro. METHODS Cangai oil transfersomes was prepared by using the thin-film ultrasonic method and taking sodium cholate and propanediol as membrane softeners. The encapsulation rate was determined by petroleum-ether-extraction and UV method. The release and transdermal penetration behavior of Cangai oil transfersomes in vitro were investigated by HPLC while eugenol was detected as the index component. RESULTS The average particle size of Cangai oil transfersomes prepared by the preferred formulation was (149±4.37) nm, and the polydispersity index was 0.189±0.024, encapsulation rate was (89±2.50)%, and the zeta potential value was (-42.95±1.78)mV. The results of release in vitro showed that the release of Cangai oil reached a steady state at about 6 hours, while Cangai oil transfersomes and Cangai oil liposomes continued to release for 12 hours. The results of percutaneous permeation in vitro showed that Cangai oil transfersomes had higher cumulative permeation than Cangai oil liposome and Cangai oil from 6 hours (P<0.05). CONCLUSION Cangai oil transfersomes prepared by optimized prescription has an integrated appearance and narrow particle size distribution. It not only increases the solubility of Cangai oil, but also has a certain slow-release effect, which is a potential transdermal drug delivery carrier. It can also significantly increase the transdermal efficiency of Cangai oil after transdermal administration in vitro, and it is a transdermal drug carrier with good potential.

     

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