β⁃胡萝卜素纳米乳的制备及处方工艺优化研究

Preparation and optimization ofβ⁃carotene nanoemulsion and its formulation technology

目的探讨聚唾液酸修饰的β⁃胡萝卜素纳米乳制剂的优缺点并使用星点设计效应面法探究最优化处方。方法以β⁃胡萝卜素的溶解度为指标筛选最优油相条件;然后以离心稳定常数、包封率与药物载药量等为考察指标,采用星点设计效应面法筛选出最优化处方以及制备工艺,采用马尔文电位仪测定粒径和电位,考察纳米乳制剂的释放度和热稳定性,并以此类指标对纳米乳制剂进行表征。结果得到聚唾液酸修饰的β⁃胡萝卜素纳米乳制剂最优化处方为:0.4%(w)β⁃胡萝卜素、25%(w)中链甘油三酸酯(MCT)、4%(w)聚唾液酸⁃十八胺(PSA⁃C18)、0.4%(w)司盘80(Span 80),该纳米乳制剂具有较小且均一的粒径,较高的Zeta电位,以及显著的缓释作用。研究初步证明聚唾液酸修饰的纳米乳能够高效装载β⁃胡萝卜素,并且能够有效提高β⁃胡萝卜素的热稳定性。结论通过对聚唾液酸修饰的β⁃胡萝卜素纳米乳的处方工艺进行优化研究,将为β⁃胡萝卜素纳米乳制剂的开发和应用提供理论依据和技术支持。

Objective To investigate the advantages and disadvantages ofβ⁃carotene nanoemulsion modified by polysialic acid,and to explore the optimal formulation ofβ⁃carotene nanoemulsion by the central point design response surface method.Methods Firstly,the solubility ofβ⁃carotene was used as an indicator to screen the optimal oil phase in this study;Then,the centrifugal stability constant,entrapment efficiency and drug loading were regarded as indicators,and the optimal prescription and preparation process were selected by using the central point design response surface method.The particle size and Zeta potential were measured by Zetasizer Nano ZS90,the release profiles in vitro and thermal stability of nanoemulsion were explored,and the physicochemical properties of nanoemulsion were characterized with these indexes.Results The optimal formulation ofβ⁃carotene nanoemulsion modified by polysialic acid was consist ofβ⁃carotene of 0.4%(w),medium chain triglyceride(MCT)of 25%(w),polysialic acid⁃octadecylamine derivative(PSA⁃C18)of 4%(w)and Span 80 of 0.4%(w).The nanoemulsion exhibited small and uniform particle size,relative high surface Zeta potential and significant slow release behavior in vitro.It was preliminarily demonstrated that nanoemulsion modified by polysialic acid could efficiently loadβ⁃carotene and improve thermal stability ofβ⁃carotene.Conclusion By optimizing the formulation and technology ofβ⁃carotene nanoemulsion modified by polysialic acid,it will provide theoretical basis and technical support for the development and application ofβ⁃carotene nanoemulsion.