• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

脂质化拟肽配体功能化的HER2靶向脂质体作为纳米载体用于癌症治疗中阿霉素的递送

Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.

作者信息

Naik Himgauri, Sonju Jafrin Jobayer, Singh Sitanshu, Chatzistamou Ioulia, Shrestha Leeza, Gauthier Ted, Jois Seetharama

机构信息

School of Basic Pharmaceutical and Toxicological Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71201, USA.

Department of Pathology, Microbiology & Immunology (PMI), School of Medicine, USC, SC 6439 Garners Ferry Rd, Columbia, SC 29208, USA.

出版信息

Pharmaceuticals (Basel). 2021 Mar 6;14(3):221. doi: 10.3390/ph14030221.

DOI:10.3390/ph14030221
PMID:33800723
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8002094/
Abstract

The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer cells. In this study, we prepared a peptidomimetic conjugate (SA-5)-tagged doxorubicin (Dox) incorporated liposome (LP) formulation (SA-5-Dox-LP) to evaluate the targeted delivery potential of SA-5 in human epidermal growth factor receptor-2 (HER2) overexpressed non-small-cell lung cancer (NSCLC) and breast cancer cell lines. The liposome was prepared using thin lipid film hydration and was characterized for particle size, encapsulation efficiency, cell viability, and targeted cellular uptake. In vivo evaluation of the liposomal formulation was performed in a mice model of NSCLC. The cell viability studies revealed that targeted SA-5-Dox-LP showed better antiproliferative activity than non-targeted Dox liposomes (Dox-LP). HER2-targeted liposome delivery showed selective cellular uptake compared to non-targeted liposomes on cancer cells. In vitro drug release studies indicated that Dox was released slowly from the formulations over 24 h, and there was no difference in Dox release between Dox-LP formulation and SA-5-Dox-LP formulation. In vivo studies in an NSCLC model of mice indicated that SA-5-Dox-LP could reduce the lung tumors significantly compared to vehicle control and Dox. In conclusion, this study demonstrated that the SA-5-Dox-LP liposome has the potential to increase therapeutic efficiency and targeted delivery of Dox in HER2 overexpressing cancer.

摘要

通过使用纳米载体介导的化疗药物递送，可以提高化疗药物的治疗指数。配体靶向药物递送可用于实现化疗药物向癌细胞的选择性和特异性递送。在本研究中，我们制备了一种掺入了拟肽缀合物（SA-5）标记的阿霉素（Dox）的脂质体制剂（SA-5-Dox-LP），以评估SA-5在人表皮生长因子受体2（HER2）过表达的非小细胞肺癌（NSCLC）和乳腺癌细胞系中的靶向递送潜力。脂质体采用薄膜水化法制备，并对其粒径、包封率、细胞活力和靶向细胞摄取进行了表征。在NSCLC小鼠模型中对脂质体制剂进行了体内评估。细胞活力研究表明，靶向的SA-5-Dox-LP比非靶向的阿霉素脂质体（Dox-LP）表现出更好的抗增殖活性。与非靶向脂质体相比，HER2靶向脂质体递送在癌细胞上表现出选择性细胞摄取。体外药物释放研究表明，阿霉素在24小时内从制剂中缓慢释放，Dox-LP制剂和SA-5-Dox-LP制剂之间的阿霉素释放没有差异。在NSCLC小鼠模型中的体内研究表明，与载体对照和阿霉素相比，SA-5-Dox-LP可以显著减少肺部肿瘤。总之，本研究表明，SA-5-Dox-LP脂质体有潜力提高阿霉素在HER2过表达癌症中的治疗效率和靶向递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/6264b820aaa8/pharmaceuticals-14-00221-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/b82b67f2de01/pharmaceuticals-14-00221-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/b02b92169812/pharmaceuticals-14-00221-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/c584ae5a6644/pharmaceuticals-14-00221-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/599f09f668ee/pharmaceuticals-14-00221-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/3e8dc3b1bba4/pharmaceuticals-14-00221-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/06537a2a962e/pharmaceuticals-14-00221-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/24f51a39684c/pharmaceuticals-14-00221-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/6264b820aaa8/pharmaceuticals-14-00221-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/b82b67f2de01/pharmaceuticals-14-00221-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/b02b92169812/pharmaceuticals-14-00221-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/c584ae5a6644/pharmaceuticals-14-00221-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/599f09f668ee/pharmaceuticals-14-00221-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/3e8dc3b1bba4/pharmaceuticals-14-00221-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/06537a2a962e/pharmaceuticals-14-00221-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/24f51a39684c/pharmaceuticals-14-00221-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a5c6/8002094/6264b820aaa8/pharmaceuticals-14-00221-g008.jpg

相似文献

1
Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.脂质化拟肽配体功能化的HER2靶向脂质体作为纳米载体用于癌症治疗中阿霉素的递送
Pharmaceuticals (Basel). 2021 Mar 6;14(3):221. doi: 10.3390/ph14030221.
2
Lyophilized liposomal formulation of a peptidomimetic-Dox conjugate for HER2 positive breast and lung cancer.用于 HER2 阳性乳腺癌和肺癌的肽模拟物-Dox 缀合物的冻干脂质体制剂。
Int J Pharm. 2023 May 25;639:122950. doi: 10.1016/j.ijpharm.2023.122950. Epub 2023 Apr 12.
3
Ultrasound-mediated cavitation enhances the delivery of an EGFR-targeting liposomal formulation designed for chemo-radionuclide therapy.超声介导空化增强了一种针对 EGFR 的靶向脂质体制剂的递释，该制剂旨在用于化学放射治疗。
Theranostics. 2019 Jul 28;9(19):5595-5609. doi: 10.7150/thno.34669. eCollection 2019.
4
Cell-penetrating corosolic acid liposome as a functional carrier for delivering chemotherapeutic drugs.细胞穿透性熊果酸脂质体作为一种功能性载体，用于递送达卡巴他赛等化疗药物。
Acta Biomater. 2020 Apr 1;106:301-313. doi: 10.1016/j.actbio.2020.02.013. Epub 2020 Feb 17.
5
A pH-sensitive liposome formulation of a peptidomimetic-Dox conjugate for targeting HER2 + cancer.一种针对 HER2+癌症的肽模拟物-Dox 缀合物的 pH 敏感脂质体制剂。
Int J Pharm. 2022 Jan 25;612:121364. doi: 10.1016/j.ijpharm.2021.121364. Epub 2021 Dec 9.
6
Tumor targeting using anti-her2 immunoliposomes.使用抗HER2免疫脂质体进行肿瘤靶向
J Control Release. 2001 Jul 6;74(1-3):95-113. doi: 10.1016/s0168-3659(01)00315-7.
7
GE11-modified liposomes for non-small cell lung cancer targeting: preparation, ex vitro and in vivo evaluation.用于非小细胞肺癌靶向的GE11修饰脂质体：制备、体外和体内评价
Int J Nanomedicine. 2014 Feb 12;9:921-35. doi: 10.2147/IJN.S53310. eCollection 2014.
8
Aptamer-drug conjugate: targeted delivery of doxorubicin in a HER3 aptamer-functionalized liposomal delivery system reduces cardiotoxicity.适配体-药物偶联物：在HER3适配体功能化脂质体递送系统中靶向递送阿霉素可降低心脏毒性。
Int J Nanomedicine. 2018 Feb 5;13:763-776. doi: 10.2147/IJN.S149887. eCollection 2018.
9
Dual-Ligand-Functionalized Liposomes Based on Glycyrrhetinic Acid and cRGD for Hepatocellular Carcinoma Targeting and Therapy.基于甘草次酸和 cRGD 的双配体功能化脂质体用于肝癌靶向治疗。
Mol Pharm. 2023 Apr 3;20(4):1951-1963. doi: 10.1021/acs.molpharmaceut.2c00842. Epub 2023 Mar 23.
10
A Novel Diosgenin-Based Liposome Delivery System Combined with Doxorubicin for Liver Cancer Therapy.一种基于薯蓣皂苷元的新型脂质体递送系统联合阿霉素用于肝癌治疗
Pharmaceutics. 2022 Aug 12;14(8):1685. doi: 10.3390/pharmaceutics14081685.

引用本文的文献

1
Strategic advances in liposomes technology: translational paradigm in transdermal delivery for skin dermatosis.脂质体技术的战略进展：用于皮肤疾病透皮给药的转化范例
J Nanobiotechnology. 2025 Aug 21;23(1):576. doi: 10.1186/s12951-025-03660-z.
2
Doxorubicin Toxicity and Recent Approaches to Alleviating Its Adverse Effects with Focus on Oxidative Stress.多柔比星毒性以及近期减轻其不良反应的方法，重点关注氧化应激
Molecules. 2025 Aug 7;30(15):3311. doi: 10.3390/molecules30153311.
3
Liposomal glytrexate formulation: improving antitumour efficacy and minimizing toxicity in breast cancer therapy.

本文引用的文献

1
Peptide-functionalized liposomes as therapeutic and diagnostic tools for cancer treatment.肽修饰的脂质体作为癌症治疗的治疗和诊断工具。
J Control Release. 2021 Jan 10;329:624-644. doi: 10.1016/j.jconrel.2020.09.055. Epub 2020 Oct 1.
2
HER2-targeted therapies - a role beyond breast cancer.曲妥珠单抗等 HER2 靶向治疗——超越乳腺癌的应用。
Nat Rev Clin Oncol. 2020 Jan;17(1):33-48. doi: 10.1038/s41571-019-0268-3. Epub 2019 Sep 23.
3
Dual-active targeting liposomes drug delivery system for bone metastatic breast cancer: Synthesis and biological evaluation.
脂质体吉西他滨制剂：提高乳腺癌治疗中的抗肿瘤疗效并将毒性降至最低
Int J Pharm X. 2025 Jul 10;10:100356. doi: 10.1016/j.ijpx.2025.100356. eCollection 2025 Dec.
4
Treatment of lung diseases nanoparticles and nanorobots: Are these viable alternatives to overcome current treatments?肺部疾病的治疗——纳米颗粒与纳米机器人：它们是克服现有治疗方法的可行替代方案吗？
Mater Today Bio. 2025 Feb 26;31:101616. doi: 10.1016/j.mtbio.2025.101616. eCollection 2025 Apr.
5
Engineered Hybrid Vesicles and Cellular Internalization in Mammary Cancer Cells.工程化杂交囊泡与乳腺癌细胞的细胞内化作用
Pharmaceutics. 2024 Mar 22;16(4):440. doi: 10.3390/pharmaceutics16040440.
6
Adjuvant Novel Nanocarrier-Based Targeted Therapy for Lung Cancer.基于新型纳米载体的肺癌辅助靶向治疗
Molecules. 2024 Feb 29;29(5):1076. doi: 10.3390/molecules29051076.
7
Pneumonic Injury and Repair: A Synopsis.肺损伤与修复：概述
Pharmaceuticals (Basel). 2023 Sep 5;16(9):1255. doi: 10.3390/ph16091255.
8
Antioxidant Activity of Quercetin-Containing Liposomes-in-Gel and Its Effect on Prevention and Treatment of Cutaneous Eczema.含槲皮素脂质体凝胶的抗氧化活性及其对皮肤湿疹防治的作用
Pharmaceuticals (Basel). 2023 Aug 21;16(8):1184. doi: 10.3390/ph16081184.
9
Lipid Nanocarrier-Based Drug Delivery Systems: Therapeutic Advances in the Treatment of Lung Cancer.基于脂质纳米载体的药物传递系统：肺癌治疗的治疗进展。
Int J Nanomedicine. 2023 May 18;18:2659-2676. doi: 10.2147/IJN.S406415. eCollection 2023.
10
Application of nanomaterials in diagnosis and treatment of glioblastoma.纳米材料在胶质母细胞瘤诊断与治疗中的应用。
Front Chem. 2022 Dec 9;10:1063152. doi: 10.3389/fchem.2022.1063152. eCollection 2022.
载双主动靶向配体脂质体药物传递系统用于治疗骨转移性乳腺癌：合成与生物学评价。
Chem Phys Lipids. 2019 Sep;223:104785. doi: 10.1016/j.chemphyslip.2019.104785. Epub 2019 Jun 11.
4
Preparation and Characterization of New Liposomes. Bactericidal Activity of Cefepime Encapsulated into Cationic Liposomes.新型脂质体的制备与表征。头孢吡肟包封于阳离子脂质体中的杀菌活性。
Pharmaceutics. 2019 Feb 6;11(2):69. doi: 10.3390/pharmaceutics11020069.
5
Immunotherapy for HER2-positive breast cancer: recent advances and combination therapeutic approaches.HER2阳性乳腺癌的免疫治疗：最新进展与联合治疗方法
Breast Cancer (Dove Med Press). 2019 Jan 17;11:53-69. doi: 10.2147/BCTT.S175360. eCollection 2019.
6
Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.用于靶向HER2+癌症中表皮生长因子受体异二聚化的新型脂化拟肽缀合物的设计
Bioorg Med Chem Lett. 2018 Dec 1;28(22):3506-3513. doi: 10.1016/j.bmcl.2018.10.005. Epub 2018 Oct 3.
7
Development of High-Functionality and -Quality Lipids with RGD Peptide Ligands: Application for PEGylated Liposomes and Analysis of Intratumoral Distribution in a Murine Colon Cancer Model.具有 RGD 肽配体的高功能和高质量脂质的开发：用于 PEG 化脂质体的应用以及在小鼠结肠癌模型中的肿瘤内分布分析。
Mol Pharm. 2018 Oct 1;15(10):4481-4490. doi: 10.1021/acs.molpharmaceut.8b00476. Epub 2018 Sep 4.
8
Targeting Aberrations in Non-Small Cell Lung Cancer with Osimertinib.奥希替尼靶向治疗非小细胞肺癌的研究进展
Clin Cancer Res. 2018 Jun 1;24(11):2594-2604. doi: 10.1158/1078-0432.CCR-17-1875. Epub 2018 Jan 3.
9
In vivo study of doxorubicin-loaded cell-penetrating peptide-modified pH-sensitive liposomes: biocompatibility, bio-distribution, and pharmacodynamics in BALB/c nude mice bearing human breast tumors.载有多柔比星的细胞穿透肽修饰的pH敏感脂质体的体内研究：在携带人乳腺肿瘤的BALB/c裸鼠中的生物相容性、生物分布和药效学
Drug Des Devel Ther. 2017 Oct 26;11:3105-3117. doi: 10.2147/DDDT.S149814. eCollection 2017.
10
A systematic investigation of the maximum tolerated dose of cytotoxic chemotherapy with and without supportive care in mice.在有和没有支持性护理的情况下，对小鼠进行最大耐受剂量的细胞毒性化疗的系统研究。
BMC Cancer. 2017 Oct 16;17(1):684. doi: 10.1186/s12885-017-3677-7.