Development of targeting liposomal drugs using functional coating a folate-polymer conjugate

使用叶酸-聚合物缀合物功能涂层开发靶向脂质体药物

• 批准号: 23590054
• 负责人: MAITANI Yoshie
• 金额: $ 3.24万
• 依托单位: Keio University (2013)Hoshi University (2011-2012)
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2011
• 资助国家: 日本
• 起止时间: 2011 至 2013
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-23590054/
• 关键词: ターゲティング; ナノ製剤; リポソーム; リガンド; がん治療; 葉酸; 葉酸高分子

The tumor targeting of anticancer drugs is important in chemotherapy to reduce serious side-effect for patients. Folate-polymer-coated liposomes were developed for targeted chemotherapy using doxorubicin (DXR) as a model drug. Folate-poly(L-lysine) (F-PLL) conjugates were synthesized. DXR-loaded anionic liposomes were coated with F-PLL, using Layer-by layer method. In KB cells overexpressing folate receptors, F-PLL-coated liposomal DXR increased the cellular association and cytotoxicity compared with that of PLL-coated liposomes. Differently in folate-PEG modified liposome, higher folate conjugated PLL-coated liposome showed higher KB cellular uptake, suggesting different distribution of folate at the surface of liposomes.Folate-targeted liposomes were prepared successfully by coating the folate-polymer-conjugate F-PLL.

抗癌药物的肿瘤靶向性是减少化疗严重副作用的重要手段。叶酸聚合物包被脂质体被开发用于靶向化疗，以阿霉素（DXR）为模型药物。合成叶酸-聚l -赖氨酸（F-PLL）偶联物。用F-PLL包被负载dxr的阴离子脂质体，采用逐层方法。在过表达叶酸受体的KB细胞中，f - pll包被脂质体DXR与pll包被脂质体相比增加了细胞关联和细胞毒性。不同于叶酸- peg修饰的脂质体，高叶酸共轭pll包被的脂质体表现出更高的KB细胞摄取，表明叶酸在脂质体表面的分布不同。通过包被叶酸聚合物偶联的F-PLL成功制备了叶酸靶向脂质体。

项目成果

Folate receptor-mediated therapeutics: folate receptor-mediated particle systems for drug and gene delivery in cancer therapy, Vitamin-Binding Proteins-Their Functional Consequences

叶酸受体介导的治疗：叶酸受体介导的粒子系统用于癌症治疗中的药物和基因递送，维生素结合蛋白-其功能后果

• 发表时间: 2013
• 作者: 長井雅子;小林智香;長井幸史;今井清博;根矢三郎;Y. Maitani
• 通讯作者: Y. Maitani

ヒアルロン酸コーティングpH感受性リポソームのCD44ターゲティング能と薬物放出性

透明质酸包被的pH敏感脂质体的CD44靶向能力和药物释放特性

• 发表时间: 2013
• 作者: 伊東賢之介;野村優;服部喜之;米谷芳枝
• 通讯作者: 米谷芳枝

Dual functional octreotide-modified liposomal irinotecan leads to high therapeutic efficacy for medullary thyroid carcinoma xenografts

• DOI: 10.1111/j.1349-7006.2011.02128.x
• 发表时间: 2012-02-01
• 期刊: CANCER SCIENCE
• 影响因子: 5.7
• 作者: Iwase, Yuko;Maitani, Yoshie
• 通讯作者: Maitani, Yoshie

葉酸結合ポリマーコーティングリポソームの開発

叶酸结合聚合物包被脂质体的开发

• 发表时间: 2012
• 作者: 金子洵;渡辺和男;米谷芳枝
• 通讯作者: 米谷芳枝

Folate receptor-mediated therapeutics : Vitamin-Binding Proteins : Functional Consequences, edited by K. Dakshinamurti

叶酸受体介导的疗法：维生素结合蛋白：功能性后果，K. Dakshinamurti 编辑

• 发表时间: 2013
• 作者: 大嶋英津子;林祥弘;今西祐;西口純也;綛田長生;西村順二;高山幸三;Y. Maitani
• 通讯作者: Y. Maitani