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载多西紫杉醇和吲哚菁绿的 RGD 靶向氧化还原响应性纳米胶束:用于治疗肿瘤。

RGD-targeted redox responsive nano micelle: co-loading docetaxel and indocyanine green to treat the tumor.

机构信息

School of Pharmacy, Nanjing Tech University, Nanjing, China.

Department of Microbiology and Immunology, Stanford University, Stanford, CA, USA.

出版信息

Drug Deliv. 2021 Dec;28(1):2024-2032. doi: 10.1080/10717544.2021.1977425.

Abstract

Cancer, also known as a malignant tumor, has developed into a type of disease with the highest fatality rate, seriously threatening the lives and health of people. Chemotherapy is one of the most important methods for the treatment of cancer. However, chemotherapy drugs have some problems, such as low solubility and lack of targeting, which severely limit their clinical applications. To solve these problems, we designed a block copolymer that has a disulfide bond response. The polymer uses RGD peptide (arginine-glycine-aspartic acid) as the active targeting group, PEG (polyethylene glycol) as the hydrophilic end, and PCL (polycaprolactone) as the hydrophobic end. Then we utilized the amphiphilic polymer as a carrier to simultaneously deliver DOC (docetaxel) and ICG (indocyanine green), to realize the combined application of chemotherapy and photothermal therapy. The antitumor efficacy and histology analysis showed that the DOC/ICG-loaded micelle exhibited higher antitumor activity. The drug delivery system improved the solubility of DOC and the stability of ICG, realized NIR-guided photothermal therapy, and achieved an ideal therapeutic effect.

摘要

癌症,也被称为恶性肿瘤,已经发展成为一种死亡率最高的疾病,严重威胁着人们的生命和健康。化疗是治疗癌症最重要的方法之一。然而,化疗药物存在一些问题,如溶解度低和缺乏靶向性,严重限制了它们的临床应用。为了解决这些问题,我们设计了一种具有二硫键响应的嵌段共聚物。该聚合物以 RGD 肽(精氨酸-甘氨酸-天冬氨酸)为活性靶向基团,PEG(聚乙二醇)为亲水端,PCL(聚己内酯)为疏水端。然后,我们利用两亲聚合物作为载体,同时递送 DOX(多西他赛)和 ICG(吲哚菁绿),实现化疗和光热治疗的联合应用。肿瘤治疗效果和组织学分析表明,载 DOX/ICG 的胶束表现出更高的抗肿瘤活性。药物递送系统提高了 DOX 的溶解度和 ICG 的稳定性,实现了近红外光引导的光热治疗,达到了理想的治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b79d/8477929/0105db09f246/IDRD_A_1977425_F0001_C.jpg

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