基于纳米乳—凝胶技术的雷公藤多苷纳米载体的制备及药效学研究(1)
[摘要]该研究采用“纳米乳-凝胶技术”制备雷公藤多苷纳米凝胶，并对其药效学进行考察。以油酸作为油相，聚氧乙烯蓖麻油为表面活性剂，1，2-丙二醇为助表面活性剂，通过绘制伪三元相图确定雷公藤多苷纳米乳的处方组成，制备雷公藤多苷纳米凝胶。以7%的2，4-二硝基氯苯丙酮溶液致敏，0.3%的2，4-二硝基氯苯溶液多次激发建立小鼠耳慢性皮炎湿疹模型，考察雷公藤多苷纳米凝胶对小鼠耳肿胀及皮肤红肿的影响;并采用ELISA法测定血清中IFN-γ，IL-4和IL-8等细胞因子的浓度，对雷公藤多苷纳米凝胶的药效学进行考察。结果表明，雷公藤多苷纳米凝胶可以显著抑制小鼠耳肿胀度(P<0.01)，并可以改善造模后小鼠耳部皮肤出现的水肿、红斑情况。雷公藤多苷纳米凝胶还可以显著降低模型小鼠血清中IFN-γ和IL-4的表达。该研究制备的雷公藤多苷纳米凝胶对小鼠皮炎湿疹模型具有良好的治疗效果，有望为临床皮炎湿疹的治疗提供一种新型外用长效制剂。
[关键词]雷公藤多苷;纳米凝胶;经皮给药;皮炎湿疹
, 百拇医药 [收稿日期]2014-10-04
[基金项目]国家自然科学基金项目(81373896);上海市科委基础研究项目(14JC1491300)
[通信作者]*刘继勇，博士，副主任药师，硕士生导师，Tel： (021)31162308，E-mail：liujiyong@gmail.com
Development of Tripterygium glycosides nano-carries based on
″nanoemulsion-gels″ and its pharmacodynamics
GU Qing1， YOU Ben-ming2， YANG Di-shun2， PAN Yong-hua2， SHU Wei1， LIU Ji-yong2*
, 百拇医药
(1.Department of Pharmacy， Central Hospital of Zhabei District， Shanghai 200070， China;
2.Department of Pharmacy， Changhai Hospital， Second Military Medical University， Shanghai 200433， China)
[Abstract]The aim of this study is to develop the Tripterygium glycosides nanoemulsion gels and investigate its pharmacodynamics. Oleic acid was used as oil phase， polyoxyethylene castor oil as surfaetant， and 1，2-propanediol as cosurfactant to screen the formula of Tripterygium glycoside nanoemulsion using the pseudo-temary phase diagrams.Then the nanoemulsion gels was prepared. The ICR mouse ears were sensitazated by 7% DNCB， and then were excited by 0.3% DNCB to stimulate the model of mouse chronic dermatitis and eczema.The concentrations of IFN-γ， IL-4 and IL-8 in mouse blood were determined by ELISA. The results showed that Tripterygium glycosides nanoemulsion gels could significantly inhibit the swelling of mouse ears(P<0.01)and ameliorate the edama and erythema of model mouse ears skin. Also it could significantly decrease the expression of IFN-γ and IL-4 in model mouse blood. Tripterygium glycosides nanoemulsion gels had a good therapeutic effect on mouse model of dermatitis and eczema. It was expected to provide a new and long-acting exterernal preparation for the treatment of dermatitis and eczema.
, 百拇医药
[Key words]Tripterygium glycosides; nanoemulsion gels; transdermal drug delivery; dermatitis eczema
doi：10.4268/cjcmm20150114
雷公藤多苷为卫茅科植物雷公藤Tripterygium wilfordii Hook.f的主要活性部位，包括雷公藤内酯甲、雷公藤内酯醇等萜类内酯化合物及少量的生物碱类成分，具有抗炎、镇痛、抗肿瘤等作用，常用于皮肤湿疹、类风湿性关节炎、免疫抑制、肾病综合症及恶性肿瘤等疾病的治疗，具有良好的效果。但由于雷公藤多苷口服存在着较大的毒性反应，其消化系统和泌尿生殖系统的不良反应发生率分别为35.8%，22.8%，严重限制了其临床应用[1]。, http://www.100md.com(顾清 尤本明 杨帝顺 潘勇华 舒薇 刘继勇)
[关键词]雷公藤多苷;纳米凝胶;经皮给药;皮炎湿疹
, 百拇医药 [收稿日期]2014-10-04
[基金项目]国家自然科学基金项目(81373896);上海市科委基础研究项目(14JC1491300)
[通信作者]*刘继勇，博士，副主任药师，硕士生导师，Tel： (021)31162308，E-mail：liujiyong@gmail.com
Development of Tripterygium glycosides nano-carries based on
″nanoemulsion-gels″ and its pharmacodynamics
GU Qing1， YOU Ben-ming2， YANG Di-shun2， PAN Yong-hua2， SHU Wei1， LIU Ji-yong2*
, 百拇医药
(1.Department of Pharmacy， Central Hospital of Zhabei District， Shanghai 200070， China;
2.Department of Pharmacy， Changhai Hospital， Second Military Medical University， Shanghai 200433， China)
[Abstract]The aim of this study is to develop the Tripterygium glycosides nanoemulsion gels and investigate its pharmacodynamics. Oleic acid was used as oil phase， polyoxyethylene castor oil as surfaetant， and 1，2-propanediol as cosurfactant to screen the formula of Tripterygium glycoside nanoemulsion using the pseudo-temary phase diagrams.Then the nanoemulsion gels was prepared. The ICR mouse ears were sensitazated by 7% DNCB， and then were excited by 0.3% DNCB to stimulate the model of mouse chronic dermatitis and eczema.The concentrations of IFN-γ， IL-4 and IL-8 in mouse blood were determined by ELISA. The results showed that Tripterygium glycosides nanoemulsion gels could significantly inhibit the swelling of mouse ears(P<0.01)and ameliorate the edama and erythema of model mouse ears skin. Also it could significantly decrease the expression of IFN-γ and IL-4 in model mouse blood. Tripterygium glycosides nanoemulsion gels had a good therapeutic effect on mouse model of dermatitis and eczema. It was expected to provide a new and long-acting exterernal preparation for the treatment of dermatitis and eczema.
, 百拇医药
[Key words]Tripterygium glycosides; nanoemulsion gels; transdermal drug delivery; dermatitis eczema
doi：10.4268/cjcmm20150114
雷公藤多苷为卫茅科植物雷公藤Tripterygium wilfordii Hook.f的主要活性部位，包括雷公藤内酯甲、雷公藤内酯醇等萜类内酯化合物及少量的生物碱类成分，具有抗炎、镇痛、抗肿瘤等作用，常用于皮肤湿疹、类风湿性关节炎、免疫抑制、肾病综合症及恶性肿瘤等疾病的治疗，具有良好的效果。但由于雷公藤多苷口服存在着较大的毒性反应，其消化系统和泌尿生殖系统的不良反应发生率分别为35.8%，22.8%，严重限制了其临床应用[1]。, http://www.100md.com(顾清 尤本明 杨帝顺 潘勇华 舒薇 刘继勇)