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首页> 外文期刊>Advanced Functional Materials >Dendron-Based Micelles for Topical Delivery of Endoxifen: A Potential Chemo-Preventive Medicine for Breast Cancer
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Dendron-Based Micelles for Topical Delivery of Endoxifen: A Potential Chemo-Preventive Medicine for Breast Cancer

机译：基于Dendron的胶束可局部递送Endoxifen：乳腺癌的一种潜在的化学预防药物

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摘要

Endoxifen (EDX) is an active metabolite of tamoxifen that has been proven effective in the prevention and treatment of estrogen-positive breast cancer; however, oral administration of tamoxifen often causes severe side effects. Here, the topical delivery of EDX is explored using polymeric micelles to achieve localized drug delivery with potentially minimal side effects. EDX is encapsulated into dendron micelles (DM) with various surface groups (-NH_2, -COOH, or -Ac) and into cationic liposomes as a control. End-group modification significantly affects the drug loading, where the DM-COOH micelles allow the most efficient encapsulation. Furthermore, unlike the burst release from the liposomes, all DMs show sustained release of EDX over 6 days. Each formulation is evaluated for its potential to deliver EDX across the skin layers. DMs substantially enhance the permeation of EDX through both mouse (up to 20-fold) and human (up to 4-fold) skin samples relative to ethanol, a chemical penetration enhancer. Franz diffusion cell experiments reveal that DM-COOH induces the highest flux of EDX among all groups. The enhanced drug loading, controlled release profiles, and enhanced skin permeation all demonstrate that DMs are a useful platform for the topical delivery of EDX, offering a potential alternative administration route for chemoprevention.
机译：Endoxifen（EDX）是他莫昔芬的活性代谢产物，已被证明可有效预防和治疗雌激素阳性乳腺癌。但是，他莫昔芬的口服给药经常引起严重的副作用。在这里，使用聚合物胶束探索EDX的局部递送，以实现具有潜在最小副作用的局部药物递送。 EDX被封装到具有各种表面基团（-NH_2，-COOH或-Ac）的树枝状胶束（DM）中，并封装在阳离子脂质体中作为对照。端基修饰会显着影响载药量，其中DM-COOH胶束可实现最有效的封装。此外，与从脂质体中突然释放不同，所有DM在6天内显示出EDX的持续释放。评估每种制剂在皮肤层上传递EDX的潜力。相对于乙醇（一种化学渗透促进剂），DM可以大大增强EDX通过小鼠（最多20倍）和人（最多4倍）皮肤样品的渗透。 Franz扩散池实验表明，DM-COOH诱导了所有组中最高的EDX通量。增强的药物载量，控释特性和增强的皮肤渗透性均表明DMs是EDX局部给药的有用平台，为化学预防提供了潜在的替代给药途径。

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  • 来源
    《Advanced Functional Materials》 |2014年第17期|2442-2449|共8页
  • 作者

    Yang Yang; Ryan M. Pearson; Oukseub Lee; Chan-Woo Lee; Robert T. Chatterton Jr.; Seema A. Khan; Seungpyo Hong;

  • 作者单位

    Department of Biopharmaceutical Sciences College of Pharmacy University of Illinois Chicago, IL, 60612, USA;

    Department of Biopharmaceutical Sciences College of Pharmacy University of Illinois Chicago, IL, 60612, USA;

    Department of Surgery Robert H. Lurie Comprehensive Cancer Center Feinberg School of Medicine Northwestern University Chicago, IL, 60611, USA;

    Research and Development Center Durae Co., Gunpo, Gyeonggi-do, Republic of Korea;

    Department of Obstetrics/Gynecology Robert H. Lurie Comprehensive Cancer Center Feinberg School of Medicine Northwestern University Chicago, IL, 60611, USA;

    Department of Surgery Robert H. Lurie Comprehensive Cancer Center Feinberg School of Medicine Northwestern University Chicago, IL, 60611, USA;

    Department of Biopharmaceutical Sciences College of Pharmacy University of Illinois Chicago, IL, 60612, USA;

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