3-溴丙酮酸脂质立方液晶的处方筛选及制备工艺优化

侯方燕; 王海蓉; 田勇; 刘浩; 赵军军; 李见春

doi:10.13898/j.cnki.issn.1000-2200.2020.05.023

3-溴丙酮酸脂质立方液晶的处方筛选及制备工艺优化

Formulation screening and preparation process optimization of 3-bromopyruvate liquid crystalline nanoparticles

摘要

摘要:
目的筛选3-溴丙酮酸脂质立方液晶纳米粒（3-BP-LCNP）处方并优化制备工艺。
方法通过注入法联合高压均质法制备3-BP-LCNP，以粒径、包封率和载药量为评价指标，采用正交设计和单因素分析进行处方筛选及制备工艺优化；使用马尔文粒度仪进行粒径和电位测定，采用透析法对包封率及载药量进行考察。
结果3-BP-LCNP最优处方及制备工艺为甘油单油酸酯：泊洛沙姆407为8:1（总质量保持在1g），分散相用量为25 mL，3-BP投入量为26.67 mg，14900 psi下循环9次，测得平均粒径为192.7 nm，平均包封率为72.53%，载药量为2.71%。
结论采用注入法联合高压均质法制备的3-BP-LCNP，制备方法简单及工艺稳定可行。

Abstract:
ObjectiveTo screen the formulation and preparation process optimization of 3-bromopyruvate liquid crystalline nanoparticles(3-BP-LCNP).
Methods3-BP-LCNP were prepared by injection method combined with high pressure homogenization.The particle size, encapsulation rate and drug loading were set as the evaluation index, the orthogonal design and single factor analysis were used to optimize the prescription screening and preparation process.The particle size and potential were measured using Malvern particle size meter and the encapsulation rate and drug loading were investigated by dialysis method.
ResultsThe optimal formulation and preparation process of 3-BP-LCNP was monooleate:poloxamer 407 at 8:1(the total mass kept at 1 g), the dispersed phase was 25 mL, the 3-BP input was 26.67 mg, and the cycle was 9 times at 14 900 psi.The results showed that the average particle diameter was 192.7 nm, the average encapsulation efficiency was 72.53%, and the drug loading was 2.71%.
ConclusionThe preparation method and process of 3-BP-LCNP are stable and feasible by using the injection method combined with high pressure homogenization.

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