含液晶结构的固体脂质纳米粒包覆苯乙间苯二酚的表征及应用性能研究
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- 英文论文题名：Nanostructured lipid carriers with liquid crystal structure encapsulating Phenylethyl Resorcinol:characterization and in vitro study
- 论文作者：贾方雅 ; 高鸿建 ; 贾红娇 ; 张婉萍
- 英文论文作者：Fangya Jia ; Hongjian Gao ; Hongjiao Jia ; Wanping Zhang ; School of Perfume and Aroma Technology ; Shanghai Institute of Technology ; Electron Microscpy Core Labratory ; Shanghai Medical College ; Fudan University
- 年：2016
- 作者机构：上海应用技术学院;复旦大学上海医学院电子显微镜实验室;
- 论文关键词：固体脂质纳米粒 ; 液晶结构 ; 苯乙基间苯二酚 ; 体外缓释 ; 体外渗透
- 英文论文关键词：nanostructured lipid carriers ; liquid crystal ; Phenylethyl Resorcinol ; in vitro drug release ; in vitro penetration
- 会议召开时间：2016-06-15
- 会议录名称：第十一届中国化妆品学术研讨会论文集
- 英文会议录名称：The Proceedings of the 11th Seminar on Cosmetic China
- 语种：中文
- 分类号：TQ658
- 学会代码：ZGXE
- 会议名称：第十一届中国化妆品学术研讨会
- 会议地点：中国上海
- 主办单位：中国香料香精化妆品工业协会
- 学会名称：中国香料香精化妆品工业协会
- 页数：9
- 文件大小：848k
- 原文格式：O
- 会议级别：全国
摘要
本文主要描述了含有液晶结构的固体脂质纳米粒包覆苯乙基间苯二酚的性能表征及体外研究。制备方法采用了熔融超声法。实验表明,样品在透射电镜的观察下呈球形。粒径和PDI分别为153.9±8.3 nm和0.23±0.01。Zeta电位为-38.8±0.6mv。在9周的存储时间内,粒径分布在157.4nm到169.3nm之间,且PDI均小于0.3。通过高效液相色谱法测得包覆率为98.7%。小角X射线散射和卡尔费休水分测试证明了液晶结构的存在并对其进行了表征。体外缓释和渗透试验则张明了其作为液晶结构和固体脂质微粒结合体在化妆品应用方面的优势。
This study described the characterization and in vitro evaluation of the nanostructured lipid carriers with liquid crystal structure encapsulating Phenylethyl Resorcinol(PR-LC-NLC).It was prepared by melt and ultrasonication method.The results showed that the nanostructured lipid carriers with liquid crystal structure were spherical under transmission electron microscope.The particle size and PDI were 153.9±8.3 nm and0.23±0.01.The absolute value of the zeta potential was 38.8±0.6mv.In 9 weeks of storage,the mean particle size were in the range of 157.4 nm tol69.3 nm and PDI values were lower than 0.3.The entrapment efficiencies determined by ultrafiltration and High Performance Liquid Chromatography was 98.70%.Small Angle X-ray Scattering and Karl Fischer titration identified and characterized the liquid crystal structure of the PR-LC-NLC.In vitro drug release studies revealed a sustained drug release,and in vitro penetration studies showed an increase of retention amount of PR in the skin.Therefore,the combining of liquid crystal structure and NLC might eventually be a promising delivery vehicle in cosmetic dermal products.
This study described the characterization and in vitro evaluation of the nanostructured lipid carriers with liquid crystal structure encapsulating Phenylethyl Resorcinol(PR-LC-NLC).It was prepared by melt and ultrasonication method.The results showed that the nanostructured lipid carriers with liquid crystal structure were spherical under transmission electron microscope.The particle size and PDI were 153.9±8.3 nm and0.23±0.01.The absolute value of the zeta potential was 38.8±0.6mv.In 9 weeks of storage,the mean particle size were in the range of 157.4 nm tol69.3 nm and PDI values were lower than 0.3.The entrapment efficiencies determined by ultrafiltration and High Performance Liquid Chromatography was 98.70%.Small Angle X-ray Scattering and Karl Fischer titration identified and characterized the liquid crystal structure of the PR-LC-NLC.In vitro drug release studies revealed a sustained drug release,and in vitro penetration studies showed an increase of retention amount of PR in the skin.Therefore,the combining of liquid crystal structure and NLC might eventually be a promising delivery vehicle in cosmetic dermal products.
引文
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[4]X.Chen,S.Efrima,O.Reger,W.Wang,L.Nm,Z.M.Sui,B.L.Zhu,X.B.Yuan,K.Z.Yang.Doping silver nanoparticles in AOT lyotropic lamellar phases.Sci China Ser B-Chem,2001,44(5):492-499
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[6]H.F.Fan,G.Q.Liu,Y.Q.Huang,Y.Li,Q.Xia,Development of a nanostructured lipid carrier formulation for increasing photo-stability and water solubility of Phenylethyl Resorcinol,Applied Surface Science 288(2014)193-200
[7]R.Guo,Q.H.Fu.Polymer in the lyotropic lamellar liquid crystal of sodium oleate system.Acta Chimical Sinica(in Chinese),2000,58(10):1196-1201
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[12]M.Boy,H.Voss.Biocatalysis in microstructured lyotropic liquid crystals.J Mol Catal B-Enzym,1998,5:355-359
[13]R.G.Sun,J.Zhang,Y C.Wang.Conformation of liquid crystalline state in interaction between chemical materials and biomembrane in terms of modern physics.Sci China Ser B-Chem,1998,41(1):1-13
[14]E.Esposito,M.Fantin,M.Marti,M.Drechsler,L.Paccamiccio,P.Mariani,E.Sivieri,F.Lain,E.Menegatti,M.Morari,R.Cortesi,Solid lipid nanoparticles as delivery systems for bromocriptine,Pharm.Res.25(2008)1521-1530
[15]P.F.Yue,X.Y Lu,Z.Z.Zhang,H.L.Yuan,W.F.Zhu,Q.Zheng,M.Yang,The study on the entrapment efficiency and in vitro release of puerarin submicron emulsion,AAPS Pharm SciTech 10(2009)376-383
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[18]Electronic Resources:X.Kong,Y.Zhao,P.Quan,L.Fang(2015).Development of a topical ointment of betamethasone dipropionate loaded nanostructured lipid carrier.Asian Journal of Pharmaceutical Sciences[Online]Available at:http://www.sciencedirect.com/science/article/pii/S1818087615000719.
[19]M.Uner,Preparation,characterization and physico-chemical properties of Solid Lipid Nanoparticles(SLN)and Nanostructured Lipid Carriers(NLC):their benefits as colloidal drug carrier systems,Pharmazie 61(2006)375-386
[20]S.Das,W.K.Ng,R.B.H.Tan,Are nanostructured lipid carriers(NLCs)better than solid lipid nanoparticles(SLNs):development,characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?European Journal of Pharmaceutical Sciences 47(2012)139-151
[21]J.Miao,Y.Z.Du,H.Yuan,X.G.Zhang,Q.Li,Y F.Rao,M.D.Zhao,F.Q.Hu(2015).Improved cytotoxicity of paclitaxel loaded in nanosized lipid carriers by intracellular delivery.J Nanopart Res17:10(2015)9-21.
[22]S.A.Wissing,R.H.Muller,Solid lipid nanoparticles as carrier for sunscreens:in vitro release and in vivo skin penetration,Journal of Controlled Release 81(2002)225-233
[23]L.Y.Wang,S.S.Liao,Liquid Crystal Chemistry(in Chinese).Beijing:Science Press,1988.132-168
[24]G.Z.Li,J.C.Hao,L.Q.Zheng,F.Li,S.X.Hao,H.Q.Wang.Studies on lyotropic liquid crystal for the system of CPDB/w-butanol/w-octane/watersystem by means of~2HNMR and DSC methods.Chem J Chin Uni(in Chinese),1995,16:595-598
[25]G.N.Brown.Liquid Crystals and Biological Structures.New York:Academic Press,1979
[26]W.M.Obeidat,K.Schwabe,R.H.Muller,CM.Keck.Preservation of nano-structured lipid carriers(NLC),European Journal of Pharmaceutics and Biopharmaceutics 76(2010)56-67
[27]T.H.Tran,T.Ramasamy,D.H.Truong,H.G.Choi,C.S.Yong,J.O.Kim.Preperation and characterization of Fenofibrate-load nanostructured lipid carriers for oral bioavailability enhancement.AAPS PharmSciTech,2014,15:1509-151
[2]G.Vielhaber,G.Schmaus,K.Jacobs.4-(1-Phenylethyl)-1,3-benzenediol:a new,highly efficient lightening agent.IFSCC Mag 2006:9:2-9
[3]I.Meyer,M.Knupfer,H.Joppe,A.Kohler,B.Holscher,M.Mansfeld,A cosmetic composition for lightening skin and/or hair,European Patent:EP2853254,2015
[4]X.Chen,S.Efrima,O.Reger,W.Wang,L.Nm,Z.M.Sui,B.L.Zhu,X.B.Yuan,K.Z.Yang.Doping silver nanoparticles in AOT lyotropic lamellar phases.Sci China Ser B-Chem,2001,44(5):492-499
[5]V.Teeranachaideekul,R.H.Muller,V.B.Junyaprasert.Encapsulation of ascorbyl palmitate in nanostructured lipid carriers(NLC)—effects of formulation parameters on physicochemical stability.International Journal of Pharmaceutics340(2007)198-206
[6]H.F.Fan,G.Q.Liu,Y.Q.Huang,Y.Li,Q.Xia,Development of a nanostructured lipid carrier formulation for increasing photo-stability and water solubility of Phenylethyl Resorcinol,Applied Surface Science 288(2014)193-200
[7]R.Guo,Q.H.Fu.Polymer in the lyotropic lamellar liquid crystal of sodium oleate system.Acta Chimical Sinica(in Chinese),2000,58(10):1196-1201
[8]M.Makai,E.Csányi,Z.Németh,J.Pálinkás,I.Eros.Structure and drug release of lamellar liquid crystals containing glycerol.Inter J Pharm,2003,256:95-107
[9]V.Vill,R.Hashim.Carbohydrate liquid crystals:Structure-property relationship of thermotropic and lyotropic glycolipids.Curr Opin Colloid In Sci,2002,7:395-409
[10]J.H.Mu,G.Z.Li,G.Z.Liao,L.Huang,K.S.Zhao.Phase behavior and structure analysis of the middle mixed.Sci China Ser B-Chem,2002,45(2):184-190
[11]G.Z.Li,H.D.Xiao,Y Li,J.H.Mu,L.W.Wang.A study of lyotropic liquid crystal system and its research at enhanced oil recovery.Chem J Chin Uni(in Chinese),2001,22:108-111
[12]M.Boy,H.Voss.Biocatalysis in microstructured lyotropic liquid crystals.J Mol Catal B-Enzym,1998,5:355-359
[13]R.G.Sun,J.Zhang,Y C.Wang.Conformation of liquid crystalline state in interaction between chemical materials and biomembrane in terms of modern physics.Sci China Ser B-Chem,1998,41(1):1-13
[14]E.Esposito,M.Fantin,M.Marti,M.Drechsler,L.Paccamiccio,P.Mariani,E.Sivieri,F.Lain,E.Menegatti,M.Morari,R.Cortesi,Solid lipid nanoparticles as delivery systems for bromocriptine,Pharm.Res.25(2008)1521-1530
[15]P.F.Yue,X.Y Lu,Z.Z.Zhang,H.L.Yuan,W.F.Zhu,Q.Zheng,M.Yang,The study on the entrapment efficiency and in vitro release of puerarin submicron emulsion,AAPS Pharm SciTech 10(2009)376-383
[16]Electronic Resources:A Beloqui,M.A'.Solin'is,A.R.Gasco'n,A.J.Almeida,V.Pr'eat(2015).Nanostructured Lipid Carriers promising drug delivery systems for future clinics.Nanomedicine:Nanotechnology,Biology,and Medicine[Online]Available at:http://www.sciencedirect.com/science/article/pii/S1549963415001781.
[17]J.Vandervoort and A.Ludwig.Biocompatible stabilizers in the preparation of PLGA nanoparticles:a factorial design study.Int.J.Pharm.238:77Y92(2002).
[18]Electronic Resources:X.Kong,Y.Zhao,P.Quan,L.Fang(2015).Development of a topical ointment of betamethasone dipropionate loaded nanostructured lipid carrier.Asian Journal of Pharmaceutical Sciences[Online]Available at:http://www.sciencedirect.com/science/article/pii/S1818087615000719.
[19]M.Uner,Preparation,characterization and physico-chemical properties of Solid Lipid Nanoparticles(SLN)and Nanostructured Lipid Carriers(NLC):their benefits as colloidal drug carrier systems,Pharmazie 61(2006)375-386
[20]S.Das,W.K.Ng,R.B.H.Tan,Are nanostructured lipid carriers(NLCs)better than solid lipid nanoparticles(SLNs):development,characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?European Journal of Pharmaceutical Sciences 47(2012)139-151
[21]J.Miao,Y.Z.Du,H.Yuan,X.G.Zhang,Q.Li,Y F.Rao,M.D.Zhao,F.Q.Hu(2015).Improved cytotoxicity of paclitaxel loaded in nanosized lipid carriers by intracellular delivery.J Nanopart Res17:10(2015)9-21.
[22]S.A.Wissing,R.H.Muller,Solid lipid nanoparticles as carrier for sunscreens:in vitro release and in vivo skin penetration,Journal of Controlled Release 81(2002)225-233
[23]L.Y.Wang,S.S.Liao,Liquid Crystal Chemistry(in Chinese).Beijing:Science Press,1988.132-168
[24]G.Z.Li,J.C.Hao,L.Q.Zheng,F.Li,S.X.Hao,H.Q.Wang.Studies on lyotropic liquid crystal for the system of CPDB/w-butanol/w-octane/watersystem by means of~2HNMR and DSC methods.Chem J Chin Uni(in Chinese),1995,16:595-598
[25]G.N.Brown.Liquid Crystals and Biological Structures.New York:Academic Press,1979
[26]W.M.Obeidat,K.Schwabe,R.H.Muller,CM.Keck.Preservation of nano-structured lipid carriers(NLC),European Journal of Pharmaceutics and Biopharmaceutics 76(2010)56-67
[27]T.H.Tran,T.Ramasamy,D.H.Truong,H.G.Choi,C.S.Yong,J.O.Kim.Preperation and characterization of Fenofibrate-load nanostructured lipid carriers for oral bioavailability enhancement.AAPS PharmSciTech,2014,15:1509-151