异补骨脂素纳米结构脂质载体的制备及其体外透皮研究
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摘要
为增加异补骨脂素的皮肤透过量及滞留量,提高其生物利用度。该文采用高压均质法制备异补骨脂素纳米结构脂质载体(IPRN-NLC),以包封率、载药量及平均粒径为评价指标,运用正交实验优化最佳处方。采用Franze扩散池法考察IPRN-NLC的体外透皮。结果表明,最优处方固液脂质比为7∶3,药脂比1∶30,表面活性剂1%,制备的IPRN-NLC平均包封率为(90.25±0.73)%,平均载药量为(1.56±0.27)%,平均粒径为(305±1.57)nm;体外透皮实验显示IPRN-NLC提高了IPRN的皮肤透过量,且皮肤滞留量是IPRN(水)溶液的3倍。采用高压均质法制备的IPRN-NLC提高了IPRN的皮肤透过量及滞留量,在经皮给药领域具有广阔的应用前景。
To increase the permeation and retention of isopsoralen in skin,and improve its bioavailability. Isopsoralen loaded nanostructure liquid carrier( IPRN-NLC) was prepared by high pressure homogenization andoptimized by orthogonal experiment with the encapsulation efficiency,drug loading and average particle size as the evaluation indexes. The in vitro transdermal permeation of IPRNNLC was evaluated by Franze diffusion cells. The results showed that solid-liquid lipid ratio of optimum IPRN-NLC formulation was 7∶3,drug-lipid ratio of 1∶ 30,1% surfactant. Under these conditions,IPRN-NLC had an average encapsulation of(90. 25 ± 0. 73) %,drug loading of(1. 56 ± 0. 27) % and an average particle size of(305 ± 1. 57) nm. The in vitro transdermal permeation results showed that IPRN-NLC could increase the amount of IPRN permeated though skin,with 3 times of the epidermal retention as compared with IPRN solution. From the results we can know that the IPRN-NLC prepared by high pressure homogenization can improve the permeation andaccumulation of IPRN in the skin,with wide application prospects in the field of transdermal administration.
To increase the permeation and retention of isopsoralen in skin,and improve its bioavailability. Isopsoralen loaded nanostructure liquid carrier( IPRN-NLC) was prepared by high pressure homogenization andoptimized by orthogonal experiment with the encapsulation efficiency,drug loading and average particle size as the evaluation indexes. The in vitro transdermal permeation of IPRNNLC was evaluated by Franze diffusion cells. The results showed that solid-liquid lipid ratio of optimum IPRN-NLC formulation was 7∶3,drug-lipid ratio of 1∶ 30,1% surfactant. Under these conditions,IPRN-NLC had an average encapsulation of(90. 25 ± 0. 73) %,drug loading of(1. 56 ± 0. 27) % and an average particle size of(305 ± 1. 57) nm. The in vitro transdermal permeation results showed that IPRN-NLC could increase the amount of IPRN permeated though skin,with 3 times of the epidermal retention as compared with IPRN solution. From the results we can know that the IPRN-NLC prepared by high pressure homogenization can improve the permeation andaccumulation of IPRN in the skin,with wide application prospects in the field of transdermal administration.
引文
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[2]Zhou J,Shi W,Li L H,et al.Detection of misdistribution of tyrosinase from melanosomes to lysosomes and its upregulation under psoralen/ultraviolet A with a melanosome-targeting tyrosinase fluorescent probe[J].Anal Chem,2016,88(8):4557.
[3]中国药典.一部[S].2015:187.
[4]白鸽,曹学丽,谭莉,等.补骨脂素和异补骨脂素的分离纯化研究[J].北京工商大学学报:自然科学版,2009,27(5):1.
[5]陈小川,李紫微,唐慧娴,等.基于UHPLC技术的补骨脂指纹图谱研究[J].世界科学技术——中医药现代化,2014(4):865.
[6]Conforti F,Marrelli M,Menichini F,et al.Natural and synthetic furanocoumarins as treatment for vitiligo and psoriasis[J].Curr Drug Ther,2009,4(1):38.
[7]郑娟,沈成英,庞建云,等.丹参酮ⅡA纳米结构脂质载体的处方优化及其体外透皮研究[J].中国中药杂志,2016,41(17):3232.
[8]Rhythm A,Sameer S,Katiyar,et al.Solid lipid nanoparticles and nanostructured lipid carrier-based nanotherapeutics in treatment of psoriasia:a comparative study[J].Expert Opin Drug Deliv,2017,14(2):165.
[9]Pardeike Jana,Hommoss Aiman,Muller R H.Lipid nanoparticles(SLN,NLC)in cosmetic and pharmaceutical dermal products[J].Int J Pharm,2009,366(1/2):170.
[10]Lav K,Kamla P.Development of thermodynamically stable nanostructured lipid carrier system using central composition design for zero order permeation of econazole nitrate though epidermis[J].Pharm Dev Technol,2013,18(3):634.
[11]Pardeike J,Schwabe K,Muller R H.Influence of nanostructured lipid carriers(NLC)on the properties of the Cutanova Nanorepari Q10 cream and the in vivo skin hydration effect[J].Int J Pharm,2010,396(1/2):166.
[12]Jia L J,Zhang D R,Li Z Y,et al.Nanostructured Lipid carriers for parenteral delivery of silybin:biodistribution and pharmacokinetic studies[J].Colloids Surface B,2010,80(2):213.
[13]杜广胜.TPGS乳化的尼美舒利纳米结构脂质载体的研究[D].天津:天津大学,2013.