摘要
维生素C是一种水溶性维生素,具有美白祛斑、延缓衰老的美容功效,但是容易氧化变质,且不易被皮肤吸收。脂质体作为一种新兴药物载体,对包封的药物具有保护作用,从而提高其作用时间。
本课题以水溶性物质维生素C为模型材料,采用动态高压微射流(DHPM)作为核心技术,结合传统脂质体制备方法,通过工艺优化,制备了维生素C脂质体和维生素C纳米脂质体,并研究了这两种脂质体的物理化学性质(粒径、包封率、外观形貌、稳定性、缓释性)和生物利用率(抗氧化能力和皮肤渗透性)。
本课题建立了测定维生素C脂质体包封率的分析方法：采用透析法分离游离维生素C、甲醇破乳、紫外分光光度法测定包封率。
制备了维生素C脂质体和维生素C纳米脂质体,考察了工艺配方因素的影响。结果表明,维生素C脂质体的最优制备条件为：制备温度为65℃,维生素C浓度为2 mg/ml,维生素C和总脂材质量比为1：25,卵磷脂和胆固醇质量比为5：1,表面活性剂和总脂材质量比为2：10,卵磷脂和无水乙醇质量体积比为2.5：100。制备维生素C纳米脂质体的最优条件为：制备温度60℃,维生素C浓度5 mg/ml,维生素C和总脂材质量比为1：10,卵磷脂和胆固醇质量比为4：1,表面活性剂和总脂材质量比为4：10,卵磷脂：无水乙醇=10：100,处理压力为140 MPa,处理2次。
对维生素C脂质体和维生素C纳米脂质体的理化性质、缓释性和稳定性进行评价,结果表明：维生素C纳米脂质体较好,包封率为(47.16±6.28)%,平均粒度为(73.9±4.4)nm,微观形貌呈实体球状,贮藏稳定性、体内稳定性良好,缓释作用明显。
对比研究了维生素C脂质体和维生素C纳米脂质体的抗氧化功能和皮肤穿透能力,结果表明,两种脂质体的维生素C抗氧化功能和游离维生素C基本一致；皮肤渗透能力的排列顺序为：维生素C纳米脂质体>维生素C脂质体>游离维生素C。
Vitamin C is water soluble,it has the effect of skin lightening and anti-aging,but it is easy to oxidative deterioration, and not easily penetrate through the skin. As a new drug carrier,liposomes has the effect of protecting the core material encapsulated and improving the bioavailability of drugs.
As the core material, Vitamin C was prepared to Vitamin C liposomes and Vitam in C nanoliposomes using dynamic high-pressure microfluidization (DHPM) as a core technology which combined with the traditional method of liposomal preparation. In addition, both the physical and chemical properties of liposomes (mean particle size, encapsulation efficiency, morphology, stability, time-controlled releasing,) and bioavailability (antioxidant capacity and skin permeability.) were characterized.
The analysis method of determinating entrapment efficiency of vitamin C liposomes was established:separated free vitamin C by dialysis, breaken the liposomes by methanol emulsion, determinated Vitamin C content by UV spectrophotometry.
The traditional liposomal preparation methods and DHPM combined with the traditional method of liposomal preparation were developed to prepare vitamin C liposomes and vitamin C nanoliposomes, respectively. Each factor was analyzed and the orthogonal test was taken to optimize the formula.The optimized formula of vitamin C liposomes as follows:the preparation temperature was 65℃,the concentration of vitamin C was 2 mg/ml, the mass ratio of vitamin C and lipids was 1:25, the mass ratio of phospholipid and cholesterol was 5:1, the mass ratio of Tween-80 and lipids was 2:10,the mass volume ratio of phospholipid and ethanol was 2.5:100. The optimized formula of vitamin C nanoliposomes as follows:the preparation temperature was 60℃,the concentration of vitamin C was 5 mg/ml, the mass ratio of vitamin C and lipids was 1:10, the mass ratio of phospholipid and cholesterol was 4:1, the mass ratio of Tween-80 and lipids was 4:10,the mass volume ratio of phospholipid and ethanol was 10:100,the treatment pressure and times were 120 MPa and 4.
The physicochemical properties of both vitamin C liposomes and vitamin C nanoliposomes were evaluated.Vitamin C nanoliposomes had advantages over vitamin C liposomes with the encapsulation efficiency(47.16±6.28%),the mean particle size(73.9±4.4 nm),showed a solid spherical morphology,good storage and vivo stability,significantly slow release.
Compared the antioxidant capacity and the skin penetration of vitamin C liposomes and vitamin C nanoliposomes, results showed that, compared to free vitamin C,the antioxidant capacity of two types of liposomes was not affected; he order of skin penetration was:Vitamin C nanoliposomes> Vitamin C liposomes> Free Vitamin C.
引文
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