纳米结构脂质载体制备方法及在化妆品中的应用研究进展

doi:10.3969/j.issn.1001-1803.2019.10.009

摘要/Abstract

摘要：

综述了纳米结构脂质载体的结构特点、制备工艺,概括了纳米结构脂质载体（NLC）用于化妆品的作用和添加形式,介绍了NLC在化妆品中作为防晒剂载体、活性物质载体、缓释载体的研究情况,展望了该技术在化妆品领域的发展前景。

Abstract:

The structural features and preparation technology of nanostructured lipid carrier（NLC）were reviewed. The role and adding forms of NLC in cosmetics were summarized. The research status of NLC as sunscreen carrier, active substance carrier and sustained release carrier in cosmetics was introduced. Furthermore, development outlook of NLC was prospected．

Key words: nanostructured lipid carriers, preparation techniques, cosmetics, application

中图分类号:

TQ658

刘清霞,徐梦漪,温子敏,朱永闯,龚盛昭,张勇. 纳米结构脂质载体制备方法及在化妆品中的应用研究进展[J]. 日用化学工业, 2019, 49(10): 681-687.

LIU Qing-xia,XU Meng-yi,WEN Zi-min,ZHU Yong-chuang,GONG Sheng-zhao,ZHANG Yong. Progress in preparation of nanostructured lipid carriersand its application in cosmetics[J]. China Surfactant Detergent & Cosmetics, 2019, 49(10): 681-687.

图/表 2

图 1

表 1

NLC技术的研究情况"

方法	活性成分	功效	脂质和乳化剂	粒径	主要研究结果	参考文献
热高压均质法	α-硫辛酸（LA）（辅酶）	抗氧化	Apifil、Miglyol^?812（辛酸/癸酸三甘油酯）、pluronic^?F68（泊洛沙姆）	（103±9）nm	制备得到可负载水溶性差的α-硫辛酸的胶态载体	[17]
热高压均质法	辅酶Q10	抗氧化	Miglyol^?812、Precifac^?ATO、癸酸聚乙二醇甘油酯、Tegocare 450	（195.9±3.6）nm	物理稳定性好,可实现双重释放模式,即初期快速释放至皮肤饱和,然后长效缓释以维持Q10在皮肤中的浓度	[18]
热高压均质法	番茄红素	抗氧化	橙蜡、米糠油、Eumulgin^?SG	150~160 nm	包封率高,前6 h快速释放,后18 h匀速释放,抗氧化性能提升	[19]
高压均质法	白藜芦醇	细胞内抗氧活性、抗菌	山嵛酸甘油酯、Comprotol^?888 ATO Miglyol	（287.2±5.1）, （110±1.3）nm	与SLN相比,NLC粒子具有更小粒径,更高的负载量和更强的抗氧化活性	[20]
高压均质法	四氢姜黄素和苯乙基间苯二酚复合	美白功效和抗衰老	辛酸癸酸甘油酯、乙酰化单甘酯和单硬脂酸甘油酯、鲸蜡硬脂醇橄榄油酸酯、山梨坦橄榄油酸酯和PEG-40硬脂酸酯	（351±2）nm	负载量高、稳定性好、美白性能优异等优点	[21]
高压均质法	苯酮-3（BP-3）、对甲氧基肉桂酸辛酯（OMC）	防晒剂	固体脂质（CP、棕榈蜡或蜂蜡）、GTCC	（138.7±0.5）nm	紫外吸收能力提高,被包覆的防晒剂光异构化程度降低	[22]
高压均质法	乙基己基三嗪酮、氧化锌	复合防晒剂	ODO、乙酰化单甘酯、Olivem^?800和Olivem^?1000	（314±4）nm	具有良好的稳定性	[23]
热高压均质法	二苯酮-3和对甲氧基肉桂酸辛酯	防晒剂	辛酸癸酸甘油三酯、鲸蜡醇棕榈酸酯、单硬脂酸甘油酯（A165）、泊洛沙姆 188、大豆卵磷脂	192.4 nm	复合乳化剂可增加防晒剂的包封率	[24]
乳化超声法	rhEGF	重组人表皮生长因子	Precirol^?ATO5、Miglyol^?182、泊洛沙姆、吐温80	（330.7±3.59）nm	提高皮肤愈合效果	[25]
乳化超声法	苯乙基间苯二酚	美白	二十二醇、辛酸癸酸三甘油酯、鲸蜡硬脂基葡糖苷、甲基葡糖苷倍半硬脂酸酯、EG-20甲基葡糖苷倍半硬脂酸酯	（153.9±8.3）nm	粒径小、包覆率高和稳定性良好,缓释。可增加皮肤滞留量,减少渗透,有利于活性成分作用于皮肤而不会渗入机体对机体造成不良影响	[11]
乳化超声法	甲氧基肉桂酸辛酯（3%）、丁基甲氧基二苯甲酰甲烷（2%）	防晒剂	鲸蜡硬酯基酸-20（5%）、氢化蓖麻油（2%）、辛酸癸酸三甘油酯（6%）	305 nm	防晒剂的稳定性提高,并且起到了协同防晒的作用	[26]
乳化超声法	摩洛哥坚果油	保湿,抗衰老	Precifac^?ATO5、Softisan 142、摩洛哥坚果油、吐温80	（137.70±0.70）nm	与空白样相比,NLC使皮肤保湿性提高	[27]
乳化蒸发-低温固化法	槲皮素	抗炎	单硬脂酸甘油酯、中链甘油三酯（MCT）	215.2 nm	增加活性物表皮保留率	[28]
乳化超声法	维生素E	保湿、润肤	Precifac^?ATO 5、维生素E、吐温80	105 nm	生物相容性好,无刺激	[29]
溶剂扩散法	羟苯甲酮	防晒剂	单硬脂酸甘油酯、Miglyol^?812、油酸、聚乙烯醇（PVA）、Carbopol^?934P（卡波姆934P）	（327±30）~（797±100）nm	提高体外防晒因子和UVA防护值超过6倍和8倍,减少副作用	[30]

表 1

参考文献 53

[1]	Bangham A D . A correlation between surface charge and coagulant action of phospholipids[J]. Nature, 1961,192:1197-1198.
[2]	Md Asif Iqbal, Shadab Md, Jasjeet Kaur Sahni , et al. Nanostructured lipid carriers system: Recent advances in drug delivery[J]. Journal of Drug Targeting, 2012,20(10) , 813-830.
[3]	Basavaraj K H . Nanotechnology in medicine and relevance to dermatology: Present concepts[J]. Indian J Dermatol, 2012,57(3):169-174.
[4]	Ren Huili, Wang Hongyan . Research progress on the preparation and application of nanostructured lipid carriers[J]. Cereal and Food Industry, 2015,22(5):51-56.
[5]	Sagar R M, Amol B D, Sachin P , et al. Nanoparticles: Emerging carriers for drug delivery[J]. Saudi Pharmaceutical Journal, 2011,19(3):129-141.
[6]	Wang Gang, Wang Junjie, Wu Wei , et al. Advances in lipid-based drug delivery: enhancing efficiency for hydrophobic drugs[J]. Expert Opinion on Drug Delivery, 2015,12(9):1475-1499.
[7]	Puri A, Loomis K, Smith B , et al. Lipid-based nanoparticles as pharmaceutical drug carriers: from concepts to clinic[J]. Crit Rev Ther Drug Carrier Syst, 2009,26(6):523-580.
[8]	Doktorovova S, Kovacevic A B, Garcia M L , et al. Preclinical safety of solid lipid nanoparticles and nanostructured lipid carriers: Current evidence from in vitro and in vivo evaluation[J]. Eur J Pharm Biopharm, 2016,108:235-252.
[9]	Müller R H, Radtke M, Wissing S A . Nanostructured lipid matrices for improved microencapsulation of drugs[J]. Int J Pharm, 2002,242(1/2):121-128.
[10]	Schafer-korting M, Mehnert W, Korting H C . Lipid nanoparticles for improved topical application of drugs for skin diseases[J]. Adv Drug Deliver Rev, 2007,59(6):427-443.
[11]	Jia Fangya . Nanostructured lipid carriers with liquid crystal structure encapsulating: preparation and characterization[D]. Shanghai: Shanghai Institute of Technology, 2016.
[12]	Domingo C, Saurina J . An overview of the analytical characterization of nanostructured drug delivery systems: towards green and sustainable pharmaceuticals: a review[J]. Anal Chim Acta, 2012,744:8-22.
[13]	Pardeshi C, Rajput P, Belgamwar V , et al. Solid lipid based nanocarriers: an overview[J]. Acta Pharm, 2012,62(4):433-472.
[14]	Gaba B, Fazil M, Ali A , et al. Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration[J]. Drug Del, 2015,22:691-700.
[15]	Jenning V, Thunemann A F, Gohla S H . Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids[J]. Int J Pharm, 2000,199:167-177.
[16]	Jenning V, Schafer-Korting M, Gohla S . Vitamin A-loaded solid lipid NPs for topical use: drug release properties[J]. J Control Release, 2000,66:115-126.
[17]	Ruktanonchai U, Bejrapha P, Sakulkhu U , et al. Physicochemical characteristics, cy-totoxicity, and antioxidant activity of three lipid nanoparticulate formulations of alpha-lipoic acid[J]. Aaps Pharmscitech, 2009,10:227-234.
[18]	Obeidat W M, Schwabe K, Müller R H , et al. Preservation of nanostructured lipid carriers (NLC)[J]. Eur J Pharm Biopharm, 2010,76:56-67.
[19]	Okonogi S, Riangjanapatee B . Physicochemical characterization of lycopene-loaded nanostructured lipid carrier formulations for topical administration[J]. International Journal of Pharmaceutics, 2015,478(2):726-735.
[20]	Gokce E H, Korkmaz E, Dellera E , et al. Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: evaluation of antioxidant potential for dermal applications[J]. Int J Nanomed, 2012 (7):1841-1850.
[21]	Zhao Shizhi . Preparation and evaluation of compound whitening nano carriers[D]. Jiangsu: Southeast University, 2017.
[22]	Ling Hui, Zheng Cheng, Mao Taoyan , et al. Encapsulation of OMC and BP-3 with biocompatible lipid nanoparticles via high pressure homogenization[J]. Journal of Chemical Engineering of Chinese Universities, 2018,32(2):377-385.
[23]	Chen Yanling, Xia Qiang . Preparation and characteration of organic and inorganic sunscreens loaded nanostructured lipid carriers (NLC)[J]. Detergent ＆ Cosmetics, 2013,36(2):25-32.
[24]	Wei Yuan, Ling Hui, Zheng Cheng , et al. Preparation and aggregation kinetics of nanostructured lipid carrier[J]. Journal of Chemical Industry and Engineering (China) , 2018,69(10):4427-4437.
[25]	Gainza G, Bonafonte D C . The topical administration of rhEGF-loaded nanostructured lipid carriers (rhEGF-NLC) improves healing in a porcine full-thickness excisional wound model[J]. J Control Release, 2015,490(1):404-411.
[26]	Liu Xiaohui . Preparation and characterization of the nanostructured lipid carriers loaded UVA/UVB sunscreens[D]. Shanghai: Shanghai Institute of Technology, 2016.
[27]	Tichota D M, Silva A C, Sousa Lobo M S , et al. Design, characterization, and clinical evaluation of argan oil nanostructured lipid carriers to improve skin hydration[J]. Int J Nanomedicine, 2014 (9):3855-3864.
[28]	Guo Chenyu, Yang Chunfen, Li Qilu , et al. Development of a quercetin-loaded nanostructured lipid carrier formulation for to-pical delivery[J]. Int J Pharm, 2012,430:292-298.
[29]	Eiras F, Amaral M H, Silva R , et al. Characterization and biocompatibility evaluation of cutaneous formulations containing lipid nanoparticles[J]. Int J Pharm, 2017,519(1/2):373-380.
[30]	Sanad R A, Abdelmalak N S, Badawi A A . Formulation of a novel oxybenzone-loaded nanostructured lipid carriers (NLCs)[J]. Aaps Pharmscitech, 2010,11:1684-1694.
[31]	Lippacher A, Müller R, Mäder K . Investigation on the viscoelastic properties of lipid based colloidal drug carriers[J]. Int J Pharm, 2000,196(2):227-230.
[32]	Mehnert W, Mäder K . Solid lipid nanoparticles: production, characterization and applications[J]. Adv Drug Delivery Rev, 2001,47(2/3):165-196.
[33]	Liu Xiaohui, Li Qiong, Chen Lianghong , et al. Progress in research work with respect to preparation of nanostructured solid liposome and its application in cosmetics[J]. China Surfactant Detergent ＆ Cosmetics, 2013,43(6):469-473.
[34]	Gasco M R . Method for producing solid lipid microspheres having a narrow size distribution: US5250236[P]. 1991-08-05.
[35]	Liu Kai, Sun Jin, He Zhonggui . Development on novel nanostructured lipid carriers[J]. Journal of Shenyang Pharmaceutical University, 2008,25(3):236-242.
[36]	Müller R h, Radtke M, Wissing S A . Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations[J]. Adv Rev, 2002,54(1):131-155.
[37]	Beloqui A, Solinis M A, Rodriguez-Gascon A , et al. Nanostructured lipid carriers: promising drug delivery systems for future clinics[J]. Nanomedicine, 2016,12(1):143-161.
[38]	Kim H, Kim J T, Barua S , et al. Seeking better topical delivery technologies of moisturizing agents for enhanced skin moisturization[J]. Expert Opin Drug Deliv, 2017: 1-15.
[39]	Sala M, Diab R, Elaissari A , et al. Lipid nanocarriers as skin drug delivery systems: properties, mechanisms of skin interactions and medical applications[J]. Int J Pharm, 2018,535(1):1-17.
[40]	Liang Rong, Wu Lina, Yang Cheng , et al. Application of co-enzyme Q10-loaded nanostructured lipid carriers in cosmetics[J]. China Surfactant Detergent ＆ Cosmetics, 2016,46(9):524-529.
[41]	Pardeike J, Hommosee A, Muller R H . Lipid nanoparticles (SLN and NLC) in cosmetic and pharmaceutical dermal products[J]. Int J Pharm, 2009,366(1/2):170-184.
[42]	Silva A C, Santos D, Ferreira D C , et al. Minoxidil-loaded nanostructured lipid carriers (NLC): characterization and rheological behavior of topical formulations[J]. Pharmazie, 2009,64(3):177-182.
[43]	Silva A C, Amaral M H, Gonzalez-Mira E , et al. Solid lipid nanoparticles (SLN) -based hydrogels as potential carriers for oral transmucosal delivery of risperidone: prepatation and characterization studies[J]. Colloids Surf B: Biointerfaces, 2012,93:241-248.
[44]	Eiras F, Amaral M H, Silva R , et al. Characterization and biocompatibility evaluation of cutaneous formulations containing lipid nanoparticles[J]. Int J Pharm, 2017,519(112):373-380.
[45]	Sachin S Salunkhe, Neela M Bhatia, Varsha B Pokharkar , et al. Topical delivery of Idebenone using nanostructured lipid carriers: evaluations of sun-protection and anti-oxidant effects[J]. Journal of Pharmaceutical Investigation, 2013,43(4) , 287-303.
[46]	Hou Dongzhi, Xie Changsheng, Ping Qineng . Characteristics of solid lipid nanoparticles as carrier system for sunscreen agent[J]. Journal of China Pharmaceutical University, 2007,38(2):177-180.
[47]	Xia Q, Saupe A, Müller R H , et al. Nanostructured lipid carriers as novel carrier for sunscreen formulations[J]. International Journal of Cosmetic Science, 2007,29(6):473-482.
[48]	Li Miaomiao . Study on encapsulation and stability of nature active products[D]. Beijing: Beijing University of Chemical Technology, 2015.
[49]	Mitri K, Shegokar R, Gohla S , et al. Lipid nanocarriers for dermal delivery of lutein: preparation, characterization, stability and performance[J]. International Journal of Pharmaceutics, 2011,414(1):267-275.
[50]	Fatime Pinto, Drangana P C, de Barros , et al. Design of multifunctional nanostructured lipid carriers enriched with α-tocopherol using vegetable oils[J]. Industrial Crops & Products, 2018,118:149-159.
[51]	Veerawat Teeranachaideekul, Eliana B Souto, Varaporn B Junyaprasert , et al. Cetyl palmitate-based NLC for topical delivery of co-enzyme Q10-development, physicochemucal characterization and in vitro release studies[J]. European Journal of Pharmaceutics and Biopharamceutics, 2007,67:141-148.
[52]	Wissing S A, Mader K C, Müller R H . Solid lipid nanoparticles (SLN) as a novel carrier system offering prolonged release of the perfume allure (Chanel)[J]. Proc Int Syrup Control Rel Bioact Mater, 2000,27:311-312.
[53]	Lason E, Sikora E, Ogonowski J , et al. Release study of selected terpenes from nanostructured lipid carriers[J]. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2016,510:87-92.