Development of liver surface application formulation of anticancer drugs and gene medicine for clinical application

临床应用的抗癌药物和基因药物肝表面应用制剂的开发

• 批准号: 21590042
• 负责人: NISHIDA Koyo
• 金额: $ 3.08万
• 依托单位: Nagasaki University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2009
• 资助国家: 日本
• 起止时间: 2009 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21590042/
• 关键词: 製剤学; コントロールドリリース; 薬剤学; 薬理学; 遺伝子; 臨床応用; 癌; 薬物送達システム; 粘性添加剤; 吸収速度

The aim of the present study was to analyze the ideal pharmaceutical formulation conditions for the appropriate absorption rate from the liver surface. It was shown clearly that the rate of drug absorption from the liver surface in case of viscous additive agents carboxymethyl cellulose and polyvinyl alcohol can be predicted by the permeability of a dialysis membrane. Furthermore, we examined the effect of lipophilicity on the rate of drug absorption from the liver surface by utilizing paraben derivatives. The rate of absorption increased with lipophilicity, but too lipophilic substances were poorly absorbed. Fundamental knowledge concerning pharmaceutical formulation was obtained as the first stage of the application to cancer chemotherapy.

本研究的目的是分析理想的药物制剂条件，以获得肝脏表面的适当吸收率。它清楚地表明，在粘性添加剂羧甲基纤维素和聚乙烯醇的情况下，药物从肝表面的吸收速率可以通过透析膜的渗透性来预测。此外，我们研究了亲脂性对药物从肝脏表面吸收的速率的影响，通过利用对羟基苯甲酸酯衍生物。吸收率随着亲脂性的增加而增加，但亲脂性太强的物质吸收较差。作为应用于癌症化疗的第一阶段，获得了关于药物制剂的基础知识。

项目成果

Liver- and Lobe-Specific Gene Transfer Following the Continuous Microinstillation of Plasmid DNA onto the Liver Surface in Mice : Effect of In stillation Speed

将质粒 DNA 连续微量滴注到小鼠肝脏表面后进行肝脏和肝叶特异性基因转移：静止速度的影响

• 发表时间: 2009
• 期刊: Biological & Pharmaceutical Bulletin 32
• 作者: 戸早太一;加藤潤也;片桐幸輔;桝飛雄真;富永昌英;東屋功;K. Nakashima;Shintaro Fumoto
• 通讯作者: Shintaro Fumoto

Rac-Mediated Macropinocytosis Is a Critical Route for Naked Plasmid DNA Transfer in Mice

• DOI: 10.1021/mp900042p
• 发表时间: 2009-07-01
• 期刊: MOLECULAR PHARMACEUTICS
• 影响因子: 4.9
• 作者: Fumoto, Shintaro;Nishi, Junya;Nishida, Koyo
• 通讯作者: Nishida, Koyo

Multiple components in serum contribute to hepatic transgene expression by lipoplex in mice

血清中的多种成分有助于脂质复合物在小鼠体内表达肝脏转基因

• DOI: 10.1002/jgm.1618
• 发表时间: 2011
• 期刊: J Gene Med
• 影响因子: 3.5
• 作者: 藁谷美香;東顕二郎;森部久仁一;山本恵司;Naoki Yoshikawa
• 通讯作者: Naoki Yoshikawa

研磨剤を含有する核酸導入剤

含有磨料的核酸转移剂

• 发表时间: 2011

Relationship between lipophilicity and absorption from the liver surface of paraben derivatives and antipyrine in rats

对羟基苯甲酸酯衍生物和安替比林的亲脂性与大鼠肝表面吸收的关系

• 发表时间: 2011
• 期刊: J. Pharm. Pharmacol.
• 作者: Nishida K;Kobayashi M;Miyamoto H;Yoshikawa N;Fumoto S;Sasaki H;Nakamura J
• 通讯作者: Nakamura J