响应面法优化西兰花种子萝卜硫素前体脂质体的制备工艺  

Optimization of preparation of sulforaphane proliposome in broccoli seeds by response surface method

作　　者：徐焕普 裴朝阳 孙仕杰 武迎雪 许路路 韩静[1] 徐慧[2] Huanpu XU;Zhaoyang PEI;Shijie SUN;Yingxue WU;Lulu XU;Jing HAN;Hui XU(Shenyang Pharmaceutical University School of Pharmaceutical Engineering,Shenyang,Liaoning 110000,China;Shenyang Institute of Applied Ecology,Chinese Academy of Sciences,Shenyang,Liaoning 110000,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110000 [2]中国科学院沈阳应用生态研究所,辽宁沈阳110000

出　　处：《过程工程学报》2021年第3期305-313,共9页The Chinese Journal of Process Engineering

基　　金：辽宁省科技攻关计划(编号:萝卜硫素纳米自微乳递送系统的研究与开发)。

摘　　要：将萝卜硫素制成前体脂质体以提高萝卜硫素的稳定性,改善其水溶性和生物利用度。以包封率和粒径为指标,分别考察了载体材料、表面活性剂种类和用量及脂药比的影响,响应面法优化得前体脂质体的最优处方。通过常温稳定性实验考察了脂质体和前体脂质体的稳定性。结果表明,最优处方为脂药比为6.5:1,NaCl与萝卜硫素质量比为105:1,泊洛沙姆-188与药物质量比为1.5:1。得最大平均包封率为77.43%,平均粒径为160.5 nm。稳定性实验表明,以药物保留率为指标时,脂质体与前体脂质体在60天内稳定性好且萝卜硫素的保留率高。以包封率为指标时,脂质体混悬液产生沉淀,包封率降低,前体脂质体在60天内包封率无明显降低。前体脂质体可解决萝卜硫素的氧化变质和脂质体因沉淀、絮凝等原因而造成的包封率降低。前体脂质体包封率高,制备简单,不仅提高了萝卜硫素的稳定性,且可提高萝卜硫素的水溶性,应用前景广阔。Sulforaphane is made into proliposomes to improve the stability of liposomes,while improving the water solubility and bioavailability of sulforaphane.Taking the encapsulation efficiency and particle size as indicators,the carrier materials,the type and amount of surfactants and the effects of lipid-drug ratios were investigated respectively.The optimal formulation of proliposome was optimized by response surface method.The stability of liposomes and proliposomes was investigated through room temperature stability experiments.The results showed that the optimal prescription was that the mass ratio of lipid phase to sulforaphane was 6.5:1,the mass ratio of Na Cl to sulforaphane was 105:1,and the mass ratio of poloxamer-188 to sulforaphane was 1.5:1.The maximum average encapsulation rate was 77.43%,and the average particle size was 160.5 nm.Stability experiment results showed that when the drug retention rate was used as an indicator,liposomes and proliposomes had good stability within 60 days and a high retention rate of sulforaphane.When the encapsulation rate was used as an indicator,the liposome suspension produced precipitated,the encapsulation rate decreased,and the encapsulation rate of the proliposome did not decrease significantly within 60 days.This indicated that the proliposome can solve the oxidative deterioration of sulforaphane and the decrease of the encapsulation rate of the liposome due to precipitation,flocculation and other reasons.The proliposome has high encapsulation efficiency and simple preparation.It not only improves the stability of sulforaphane,but also improves the water solubility of sulforaphane and has broad application prospects.

关 键 词：萝卜硫素 前体脂质体 脂质体 西兰花种子 响应面 

分 类 号：R94[医药卫生—药剂学]