茶多酚醇质体的制备和体外透皮吸收研究
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摘要
目的:制备茶多酚醇质体,并对其进行皮肤渗透性评价。方法:采用注入法制备醇质体,马尔文Zeta电位仪测定其粒径及电位,紫外分光光度法测定包封率;采用改良Franz扩散池装置,以ICR小鼠背部皮肤作为渗透屏障,进行体外经皮渗透试验。结果:成功制备了茶多酚醇质体,平均粒径(162.2±7.1)nm,Zeta电位-(34.3±3.9)mV,包封率(37.43±1.90)%。体外试验中,茶多酚醇质体的稳态渗透速率是97.27μg.cm-2.h-1,分别是茶多酚30%乙醇溶液、脂质体、水溶液的2.86,7.47,11.98倍,24 h累积渗透量排序为:茶多酚醇质体>30%乙醇溶液>脂质体>水溶液。结论:醇质体的制备方法可行,醇质体能够促进茶多酚的皮肤渗透。
Objective:To prepare tea polyphenols(TP)ethosomes,and investigate their percutaneous permeation in vitro.Methods:TP ethosomes were prepared by ethanol infusion method,and the encapsulation efficiency was determined by UV-spectrometry.The transdermal penetration of different TP dosage forms was evaluated in vitro using modified Franz diffusion cells method,with the back skin of ICR male rats as percutaneous permeation barrier.Results:TP ethosomes were successfully prepared with encapsulation efficiency of(37.43±1.90)%,average particle size of(162.2±7.1) nm,and Zeta potential of-(34.3±3.9) mV.The steady state flux In vitro of TP from ethosome was 97.27 μg·cm-2·h-1,which was 2.86,7.47 and 11.98 times as that from 30% enthanol TP solution,TP liposomes and aqueous TP solution,respectively.The accumulated permeation amount in 24 h of different TP dosage forms was in the following order: ethosomes>30% ethanol solution>liposomes>aqueous solution.Conclusions:The preparation technique of ethosomes is feasible,and it can enhance the penetration of TP through skin effectively.
Objective:To prepare tea polyphenols(TP)ethosomes,and investigate their percutaneous permeation in vitro.Methods:TP ethosomes were prepared by ethanol infusion method,and the encapsulation efficiency was determined by UV-spectrometry.The transdermal penetration of different TP dosage forms was evaluated in vitro using modified Franz diffusion cells method,with the back skin of ICR male rats as percutaneous permeation barrier.Results:TP ethosomes were successfully prepared with encapsulation efficiency of(37.43±1.90)%,average particle size of(162.2±7.1) nm,and Zeta potential of-(34.3±3.9) mV.The steady state flux In vitro of TP from ethosome was 97.27 μg·cm-2·h-1,which was 2.86,7.47 and 11.98 times as that from 30% enthanol TP solution,TP liposomes and aqueous TP solution,respectively.The accumulated permeation amount in 24 h of different TP dosage forms was in the following order: ethosomes>30% ethanol solution>liposomes>aqueous solution.Conclusions:The preparation technique of ethosomes is feasible,and it can enhance the penetration of TP through skin effectively.
引文
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[14]FRANZ TJ.Percutaneous absorption on the relevance of in vitrodata[J].J Invest Dermatol,1975,64(3):190-195.
[15]ELSAYED MM,ABDALLAH OY,NAGGAR VF,et al.Deform-able liposomes and ethosomes:Mechanism of enhanced skin deliv-ery[J].Int J Pharm,2006,322(1-2):60-66.
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[17]杨飞,李芳,焦海胜,等.秋水仙碱醇质体的制备及体外经皮渗透研究[J].中国药学杂志,2009,44(5):349-352.
[18]刘星言,刘宏,张阳德.苦参碱醇质体的制备及其体外透皮性能[J].中国组织工程研究与临床康复,2009,13(25):4857-4860.
[2]JHOO JW.Antioxidant measurement and applications[M].A-merican Chemical Society,2007.
[3]HU G,HAN C,CHEN J.Inhibition of oncogene expression bygreen tea and(-)-epigallocatechin gallate in mice[J].NutrCancer,1995,24(2):203-209.
[4]王聪慧,张星星,孙莉颖,等.茶多酚药理作用研究进展[J].中国药业,2010,(4):62-63.
[5]KIRJAVAINEN M,URTTI A,JAASKELAINEN I,et al.Interac-tion of liposomes with human skin in vitro-the influence of lipidcomposition and structure[J].Biochim Biophys Acta,1996,1304(3):179-189.
[6]TOUITOU E,DAYAN N,BERGELSON L,et al.Ethosomes-novelvesicular carriers for enhanced delivery:characterization and skinpenetration properties[J].J Control Release,2000,65(3):403-418.
[7]PAOLINO D,LUCANIA G,MARDENTE D,et al.Ethosomes forskin delivery of ammonium glycyrrhizinate:in vitro percuteneouspermeation through human skin and in vivo anti-inflammatory ac-tivity on human volunteers[J].J Control Release,2005,106(1-2):99-110.
[8]TOUITOU E,GODIN B,DAYAN N,et al.Intracellular deliverymediated by an ethosomal carrier[J].Biomaterials,2001,22(22):3053-3059.
[9]MANOSROI A,JANTRAWUT P,MANOSROI J.Anti-inflamma-tory activity of gel containing novel elastic niosomes entrappedwith diclofenac diethylammonium[J].Int J Pharm,2008,360(1-2):156-163.
[10]STEMBERG B.Freeze-fracture electron microscopy of liposomes[M].Boca Raton:CRC Press,1993:363-383.
[11]DVORAKOVA K,DORR RT,VALCIC S,et al.Pharmacokinetiesof the green tea derivative,EGCG,by thepical route of administra-tion in mouse and human skin[J].Cancer Chemother Pharma-col,1999,43(3):331-335.
[12]CHEN L,LEE MJ,LI H,et al.Absorption,distribution,and elim-ination of tea polyphenols in rats[J].Drug Metab Dispos,1997,25(9):1045-1050.
[13]CAI Y,ANAVY ND,CHOW HH.Contribution of presystemic he-patic extraction to the low oral bioavailability of green tea cate-chins in rats[J].Drug Metab Dispos,2002,30(11):1246-1249.
[14]FRANZ TJ.Percutaneous absorption on the relevance of in vitrodata[J].J Invest Dermatol,1975,64(3):190-195.
[15]ELSAYED MM,ABDALLAH OY,NAGGAR VF,et al.Deform-able liposomes and ethosomes:Mechanism of enhanced skin deliv-ery[J].Int J Pharm,2006,322(1-2):60-66.
[16]HE R,CUI DX,GAO F.Preparation of fluorescence ethosomesbased on quantum dots and their skin scar penetration properties[J].Materials Letters,2009,63(20):1662-1664.
[17]杨飞,李芳,焦海胜,等.秋水仙碱醇质体的制备及体外经皮渗透研究[J].中国药学杂志,2009,44(5):349-352.
[18]刘星言,刘宏,张阳德.苦参碱醇质体的制备及其体外透皮性能[J].中国组织工程研究与临床康复,2009,13(25):4857-4860.