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曲妥珠单抗靶向生物大分子修饰脂质体提高卡培他滨在乳腺癌中的疗效。

HER2 targeted biological macromolecule modified liposomes for improved efficacy of capecitabine in breast cancer.

机构信息

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, The Nilgiris, Tamil Nadu, India.

Department of Pharmacology, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, The Nilgiris, Tamil Nadu, India; Department of Pharmacology, School of Pharmaceutical Sciences & Technologies, JNT University Kakinada, Kakinada, Andhra Pradesh, India.

出版信息

Int J Biol Macromol. 2020 May 1;150:631-636. doi: 10.1016/j.ijbiomac.2020.02.131. Epub 2020 Feb 13.

DOI:10.1016/j.ijbiomac.2020.02.131
PMID:32061845
Abstract

The present research reports the beneficial effects of surface modified chitosan and tumor-homing peptide conjugated liposomes of capecitabine (CAP) for treating breast cancer. Liposomal formulation of CAP was prepared by film hydration method using cholesterol-THP conjugate (CTHP-CAP-LPs) to achieve active targeting through HER2 receptors. CTHP-CAP-LPs significantly improved the specificity and efficacy of CAP by improving cell uptake, cytotoxicity and tumor regression in tumor bearing mice. CTHP-CAP-LPs, therefore, is a promising approach to improve the anticancer effects of CAP.

摘要

本研究报告了表面修饰壳聚糖和肿瘤归巢肽偶联卡培他滨(CAP)脂质体治疗乳腺癌的有益效果。通过使用胆固醇-THP 轭合物(CTHP-CAP-LPs)的薄膜水化法制备 CAP 的脂质体制剂,以通过 HER2 受体实现主动靶向。CTHP-CAP-LPs 通过提高细胞摄取、细胞毒性和荷瘤小鼠的肿瘤消退,显著提高了 CAP 的特异性和疗效。因此,CTHP-CAP-LPs 是提高 CAP 抗癌效果的一种有前途的方法。

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