运载辅酶Q10的纳米结构脂质载体的制备及应用
发布时间：2018-07-14 18:57
【摘要】：纳米结构脂质载体(Nanostructured lipid carriers,NLC)作为20世纪末发展起来的一种新型胶体运载系统,能够有效解决水溶性和生物相容性差的活性成分的稳定及运输问题,是一种在化妆品中具有很大应用潜力的功能性成分载体系统。辅酶Q10(Coenzyme Q10,CoQ10)作为一种脂溶性抗氧化剂,常被用于抗衰老化妆品中,但由于分子结构中具有不饱和双键,化学稳定性差,限制了其在化妆品中的添加和应用。本课题拟采用以辛基/癸基葡萄糖苷(APG)稳定的NLC作为辅酶Q10的运输载体,提高其储藏稳定性和经皮渗透吸收效果。并在此基础上,采用季铵盐壳聚糖(QCS)对CoQ10-NLC进行表面修饰,进一步提高载体的经皮渗透量,并将载体添加到护肤乳霜中,对其应用品质进行测试。首先,采用单因素实验的方法,制备运载CoQ10的NLC,考察了固态和液态脂质的质量比、表面活性剂的质量分数以及高压均质的压力和循环次数对CoQ10-NLC粒径、Zeta电位及包封率的影响,确定了最佳制备条件:固态脂质和液态脂质的质量比为1:1,表面活性剂的质量分数为1.5%,高压均质压力为1000 bar,循环次数为7次。贮藏实验表明,温度对CoQ10-NLC的影响较大,光照影响较小,在低温条件下贮藏一个月后,CoQ10保留率达到80%以上,但在高温条件下,CoQ10保留率直线下降。此外,CoQ10-NLC的体外透皮实验表明,CoQ10-NLC能够有效地提高Co Q10在皮肤中的渗透。其次,为了增强CoQ10-NLC的体外透皮效果,采用促渗剂QCS对CoQ10-NLC进行表面修饰,并结合QCS的自聚集行为以及与APG在溶液中的相互作用,比较了两种添加方式:方式1(先制备CoQ10-NLC,再将QCS与其混合)和方式2(将QCS与APG先在水相中混合,再与油相乳化均质)所制备得到的乳液粒径,结果显示,方式2制备得到的QCS-CoQ10-NLC粒径较小,在250~300 nm。进一步通过体外透皮实验和激光共聚焦显微镜的观测,考察了QCS-CoQ10-NLC的透皮吸收效果,显示加入0.5%质量分数的QCS,可以增加CoQ10在皮肤中的渗透量,且增加量主要集中于表皮中;通过全反射傅立叶红外光谱仪(FTIR)对QCS的促渗机理进行了研究,结果表明QCS是通过改变角质层中角蛋白的二级结构,导致角蛋白结构疏松,从而达到促进渗透效果。此外,通过储藏稳定性实验发现,经QCS修饰后的载体中CoQ10的保留率显著提高。最后,将制备得到的QCS-CoQ10-NLC应用于护肤乳霜,并与未添加NLC载体、添加了CoQ10和空白NLC的两种护肤乳霜进行对比。通过测试三种乳霜的理化性质,表明三种乳霜的耐热、耐寒及离心稳定性均很好;通过在不同温度和光照条件下的贮藏稳定性实验结果表明:与未包埋CoQ10的护肤乳霜相比,添加QCS-CoQ10-NLC护肤乳霜能够有效地保护CoQ10,减少其在乳霜中的降解和泄露。此外,保湿性测试和感官评价结果显示QCS-CoQ10-NLC的添加能够提高乳霜的保湿性、坚实感、吸收性和保持度。
[Abstract]:Nanostructured lipid carriers (NLC), as a new colloidal delivery system developed at the end of the 20th century, can effectively solve the problem of stability and transport of water-soluble and biocompatible active components. It is a functional component carrier system with great application potential in cosmetics. Coenzyme Q10 (Coenzyme Q10 CoQ10), as a liposoluble antioxidant, is often used in anti-aging cosmetics. However, the addition and application of CoQ10 in cosmetics are limited because of its unsaturated double bonds in molecular structure and poor chemical stability. In this study, octyl / decyl glucoside (APG) -stabilized NLC was used as the carrier of coenzyme Q10 to improve its storage stability and percutaneous osmotic absorption. On this basis, the surface of CoQ10-NLC was modified with quaternary ammonium chitosan (QCS) to further improve the transdermal permeation of the carrier, and the carrier was added to the cream and its application quality was tested. First of all, NLCs carrying CoQ10 were prepared by single factor experiment. The effects of mass ratio of solid and liquid lipids, mass fraction of surfactants, pressure of high pressure homogenization and cycle times on Zeta potential and encapsulation efficiency of CoQ10-NLC were investigated. The optimum preparation conditions were determined as follows: the mass ratio of solid lipid to liquid lipid was 1: 1, the mass fraction of surfactant was 1.5, the pressure of high pressure homogenization was 1000 bar. the number of cycles was 7 times. The storage experiment showed that the effect of temperature on CoQ10-NLC was greater than that of light. The retention rate of CoQ10 was more than 80% after one month storage at low temperature, but the retention rate of CoQ10 decreased linearly at high temperature. In addition, in vitro transdermal experiments of CoQ10-NLC showed that CoQ10-NLC could effectively enhance the penetration of CoQ10 in skin. Secondly, in order to enhance the transdermal effect of CoQ10-NLC in vitro, the surface of CoQ10-NLC was modified with QCS, which combined with the self-aggregation behavior of QCS and the interaction between QCS and APG in solution. The particle size of the emulsion prepared by two ways of adding CoQ10-NLC1 (preparing CoQ10-NLCL, then mixing QCS with QCS) and mode 2 (mixing QCS and APG in water first, then emulsifying and homogenizing with oil phase) was compared. The particle size of QCS-CoQ10-NLC prepared in mode 2 was smaller, and the size of QCS-CoQ10-NLC was at 250 ~ 300 nm. Furthermore, the transdermal absorption of QCS-CoQ10-NLC was investigated by in vitro transdermal experiments and laser confocal microscopy. The results showed that the penetration of CoQ10 in skin could be increased by adding 0.5% QCS-CoQ10-NLC, and the increase was mainly concentrated in the epidermis. The mechanism of promoting infiltration of QCS was studied by FTIR. The results show that QCS can promote infiltration by changing the secondary structure of keratin in the stratum corneum and resulting in loose structure of keratin. In addition, the retention rate of CoQ10 in QCS modified carrier was significantly increased by storage stability experiment. Finally, the prepared QCS-CoQ10-NLC was applied to skin care cream, and compared with that without NLC carrier, CoQ10 and blank NLC cream. The physicochemical properties of the three creams were tested, the results showed that the three creams had good heat resistance, cold tolerance and centrifugal stability, and the results of storage stability at different temperatures and under different light conditions showed that: compared with the unburied CoQ10 skin care cream, the stability of the three creams was better than that of the unburied CoQ10 cream. The addition of QCS-CoQ10-NLC cream can effectively protect CoQ10 and reduce its degradation and leakage. In addition, the results of moisture retention test and sensory evaluation showed that the addition of QCS-CoQ10-NLC could improve the moisturizing, firmness, absorbability and retention of creams.
【学位授予单位】：江南大学
【学位级别】：硕士
【学位授予年份】：2016
【分类号】：TQ658;TB383.1
本文编号：2122642
[Abstract]:Nanostructured lipid carriers (NLC), as a new colloidal delivery system developed at the end of the 20th century, can effectively solve the problem of stability and transport of water-soluble and biocompatible active components. It is a functional component carrier system with great application potential in cosmetics. Coenzyme Q10 (Coenzyme Q10 CoQ10), as a liposoluble antioxidant, is often used in anti-aging cosmetics. However, the addition and application of CoQ10 in cosmetics are limited because of its unsaturated double bonds in molecular structure and poor chemical stability. In this study, octyl / decyl glucoside (APG) -stabilized NLC was used as the carrier of coenzyme Q10 to improve its storage stability and percutaneous osmotic absorption. On this basis, the surface of CoQ10-NLC was modified with quaternary ammonium chitosan (QCS) to further improve the transdermal permeation of the carrier, and the carrier was added to the cream and its application quality was tested. First of all, NLCs carrying CoQ10 were prepared by single factor experiment. The effects of mass ratio of solid and liquid lipids, mass fraction of surfactants, pressure of high pressure homogenization and cycle times on Zeta potential and encapsulation efficiency of CoQ10-NLC were investigated. The optimum preparation conditions were determined as follows: the mass ratio of solid lipid to liquid lipid was 1: 1, the mass fraction of surfactant was 1.5, the pressure of high pressure homogenization was 1000 bar. the number of cycles was 7 times. The storage experiment showed that the effect of temperature on CoQ10-NLC was greater than that of light. The retention rate of CoQ10 was more than 80% after one month storage at low temperature, but the retention rate of CoQ10 decreased linearly at high temperature. In addition, in vitro transdermal experiments of CoQ10-NLC showed that CoQ10-NLC could effectively enhance the penetration of CoQ10 in skin. Secondly, in order to enhance the transdermal effect of CoQ10-NLC in vitro, the surface of CoQ10-NLC was modified with QCS, which combined with the self-aggregation behavior of QCS and the interaction between QCS and APG in solution. The particle size of the emulsion prepared by two ways of adding CoQ10-NLC1 (preparing CoQ10-NLCL, then mixing QCS with QCS) and mode 2 (mixing QCS and APG in water first, then emulsifying and homogenizing with oil phase) was compared. The particle size of QCS-CoQ10-NLC prepared in mode 2 was smaller, and the size of QCS-CoQ10-NLC was at 250 ~ 300 nm. Furthermore, the transdermal absorption of QCS-CoQ10-NLC was investigated by in vitro transdermal experiments and laser confocal microscopy. The results showed that the penetration of CoQ10 in skin could be increased by adding 0.5% QCS-CoQ10-NLC, and the increase was mainly concentrated in the epidermis. The mechanism of promoting infiltration of QCS was studied by FTIR. The results show that QCS can promote infiltration by changing the secondary structure of keratin in the stratum corneum and resulting in loose structure of keratin. In addition, the retention rate of CoQ10 in QCS modified carrier was significantly increased by storage stability experiment. Finally, the prepared QCS-CoQ10-NLC was applied to skin care cream, and compared with that without NLC carrier, CoQ10 and blank NLC cream. The physicochemical properties of the three creams were tested, the results showed that the three creams had good heat resistance, cold tolerance and centrifugal stability, and the results of storage stability at different temperatures and under different light conditions showed that: compared with the unburied CoQ10 skin care cream, the stability of the three creams was better than that of the unburied CoQ10 cream. The addition of QCS-CoQ10-NLC cream can effectively protect CoQ10 and reduce its degradation and leakage. In addition, the results of moisture retention test and sensory evaluation showed that the addition of QCS-CoQ10-NLC could improve the moisturizing, firmness, absorbability and retention of creams.
【学位授予单位】：江南大学
【学位级别】：硕士
【学位授予年份】：2016
【分类号】：TQ658;TB383.1
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1 吴丽娜;运载辅酶Q10的纳米结构脂质载体的制备及应用[D];江南大学;2016年
，本文编号：2122642
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