運(yùn)載輔酶Q10的納米結(jié)構(gòu)脂質(zhì)載體的制備及應(yīng)用
發(fā)布時(shí)間：2018-07-14 18:57
【摘要】：納米結(jié)構(gòu)脂質(zhì)載體(Nanostructured lipid carriers,NLC)作為20世紀(jì)末發(fā)展起來的一種新型膠體運(yùn)載系統(tǒng),能夠有效解決水溶性和生物相容性差的活性成分的穩(wěn)定及運(yùn)輸問題,是一種在化妝品中具有很大應(yīng)用潛力的功能性成分載體系統(tǒng)。輔酶Q10(Coenzyme Q10,CoQ10)作為一種脂溶性抗氧化劑,常被用于抗衰老化妝品中,但由于分子結(jié)構(gòu)中具有不飽和雙鍵,化學(xué)穩(wěn)定性差,限制了其在化妝品中的添加和應(yīng)用。本課題擬采用以辛基/癸基葡萄糖苷(APG)穩(wěn)定的NLC作為輔酶Q10的運(yùn)輸載體,提高其儲藏穩(wěn)定性和經(jīng)皮滲透吸收效果。并在此基礎(chǔ)上,采用季銨鹽殼聚糖(QCS)對CoQ10-NLC進(jìn)行表面修飾,進(jìn)一步提高載體的經(jīng)皮滲透量,并將載體添加到護(hù)膚乳霜中,對其應(yīng)用品質(zhì)進(jìn)行測試。首先,采用單因素實(shí)驗(yàn)的方法,制備運(yùn)載CoQ10的NLC,考察了固態(tài)和液態(tài)脂質(zhì)的質(zhì)量比、表面活性劑的質(zhì)量分?jǐn)?shù)以及高壓均質(zhì)的壓力和循環(huán)次數(shù)對CoQ10-NLC粒徑、Zeta電位及包封率的影響,確定了最佳制備條件:固態(tài)脂質(zhì)和液態(tài)脂質(zhì)的質(zhì)量比為1:1,表面活性劑的質(zhì)量分?jǐn)?shù)為1.5%,高壓均質(zhì)壓力為1000 bar,循環(huán)次數(shù)為7次。貯藏實(shí)驗(yàn)表明,溫度對CoQ10-NLC的影響較大,光照影響較小,在低溫條件下貯藏一個(gè)月后,CoQ10保留率達(dá)到80%以上,但在高溫條件下,CoQ10保留率直線下降。此外,CoQ10-NLC的體外透皮實(shí)驗(yàn)表明,CoQ10-NLC能夠有效地提高Co Q10在皮膚中的滲透。其次,為了增強(qiáng)CoQ10-NLC的體外透皮效果,采用促滲劑QCS對CoQ10-NLC進(jìn)行表面修飾,并結(jié)合QCS的自聚集行為以及與APG在溶液中的相互作用,比較了兩種添加方式:方式1(先制備CoQ10-NLC,再將QCS與其混合)和方式2(將QCS與APG先在水相中混合,再與油相乳化均質(zhì))所制備得到的乳液粒徑,結(jié)果顯示,方式2制備得到的QCS-CoQ10-NLC粒徑較小,在250~300 nm。進(jìn)一步通過體外透皮實(shí)驗(yàn)和激光共聚焦顯微鏡的觀測,考察了QCS-CoQ10-NLC的透皮吸收效果,顯示加入0.5%質(zhì)量分?jǐn)?shù)的QCS,可以增加CoQ10在皮膚中的滲透量,且增加量主要集中于表皮中;通過全反射傅立葉紅外光譜儀(FTIR)對QCS的促滲機(jī)理進(jìn)行了研究,結(jié)果表明QCS是通過改變角質(zhì)層中角蛋白的二級結(jié)構(gòu),導(dǎo)致角蛋白結(jié)構(gòu)疏松,從而達(dá)到促進(jìn)滲透效果。此外,通過儲藏穩(wěn)定性實(shí)驗(yàn)發(fā)現(xiàn),經(jīng)QCS修飾后的載體中CoQ10的保留率顯著提高。最后,將制備得到的QCS-CoQ10-NLC應(yīng)用于護(hù)膚乳霜,并與未添加NLC載體、添加了CoQ10和空白NLC的兩種護(hù)膚乳霜進(jìn)行對比。通過測試三種乳霜的理化性質(zhì),表明三種乳霜的耐熱、耐寒及離心穩(wěn)定性均很好;通過在不同溫度和光照條件下的貯藏穩(wěn)定性實(shí)驗(yàn)結(jié)果表明:與未包埋CoQ10的護(hù)膚乳霜相比,添加QCS-CoQ10-NLC護(hù)膚乳霜能夠有效地保護(hù)CoQ10,減少其在乳霜中的降解和泄露。此外,保濕性測試和感官評價(jià)結(jié)果顯示QCS-CoQ10-NLC的添加能夠提高乳霜的保濕性、堅(jiān)實(shí)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.
【學(xué)位授予單位】：江南大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2016
【分類號】：TQ658;TB383.1
本文編號：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.
【學(xué)位授予單位】：江南大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2016
【分類號】：TQ658;TB383.1
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1 吳麗娜;運(yùn)載輔酶Q10的納米結(jié)構(gòu)脂質(zhì)載體的制備及應(yīng)用[D];江南大學(xué);2016年
，本文編號：2122642
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