树枝状聚合物PAMAM包覆葛根素脂质体角膜渗透性研究
投稿时间:2009-10-02    责任编辑:  点此下载全文
引用本文:刘毅,孙考祥,姚文军,梁娜,慕宏杰,梁荣才,姚晨.树枝状聚合物PAMAM包覆葛根素脂质体角膜渗透性研究[J].中国中药杂志,2010,35(1):30.
DOI:10.4268/cjcmm20100106
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作者中文名作者英文名单位中文名单位英文名E-Mail
刘毅 LIU Yi 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
孙考祥 SUN Kaoxiang 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China sunkx@ytu.edu.cn 
姚文军 YAO Wenjun 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
梁娜 LIANG Na 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
慕宏杰 MU Hongjie 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
梁荣才 LIANG Rongcai 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
姚晨 YAO Chen 烟台大学 药学院药剂教研室, 山东 烟台 264005 School of Pharmacy, Yantai University, Yantai 264005, China  
基金项目:国家自然科学基金项目(30873447)
中文摘要:目的: 研究树枝状聚合物PAMAM包覆葛根素(puerarin,PUE)脂质体的角膜渗透特性。 方法 :制备PAMAM G2和PAMAM G3包覆的葛根素脂质体,以葛根素水溶液和未包覆葛根素脂质体为对照,进行兔离体角膜渗透试验,同时考察包覆脂质体中,不同的摩尔投料比(PAMAM/磷脂=0.1%,0.5%,1.0%,2.0%),PAMAM对角膜渗透性的影响,计算渗透参数。 结果 :PAMAM/磷脂摩尔比为1.0%(PAMAM G2)和0.5% (PAMAM G3)的包覆脂质体的Papp(表观渗透系数),Jss(稳态流量)均明显高于葛根素水溶液和未包覆脂质体(P<0.01),且PAMAM/磷脂摩尔比为1.0%(PAMAM G2)和0.5% (PAMAM G3)包覆脂质体的促角膜渗透性高于其他比例包覆的脂质体(P<0.01)。 结论 :PAMAM包覆葛根素脂质体可以显著改善葛根素在兔眼部的角膜渗透性,作为眼用载体有希望增加药物的眼部吸收和生物利用度。
中文关键词:PAMAM  树枝状聚合物  葛根素  包覆脂质体  角膜渗透性
 
Corneal penetration of PAMAM dendrimers-coated puerarin liposomes
Abstract:Objective : To study the corneal penetration of PAMAM dendrimers-coated puerarin liposomes in rabbits. Method : Evaluated PAMAM(G2,G3)dendrimers-coated puerarin liposomes were prepared and the in vitro transcorneal penetration were compared to puerarin drop solution and uncoated liposomes. The effect of different proportion of PAMAM to phospholipids in formulation on corneal penetration and the penetration parameters were investigated. Result : The steady state fluxes and permeability coefficients of puerarin by PAMAM G2(1.0%)and PAMAM G3(0.5%)coated puerarin liposomes were greater than that by puerarin drop solution and uncoated liposomess(P<0.01),meanwhile the PAMAM G2(1.0%) and PAMAM G3(0.5%)coated liposomes were better than other ratios of coated liposomes for improvement of corneal penetration(P<0.01). Conclusion : The PAMAM coated liposomes is able to enhance the corneal penetration of puerarin and promising as an ocular drug carriers.
keywords:PAMAM  dendrimer  puerarin  coated liposomes  transcorneal penetration
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