Folic Acid-Targeted Liposome-Based Nanoparticle Loaded with Sorafenib for Liver Cancer Therapy.

IF 6.6 2区 医学 Q1 NANOSCIENCE & NANOTECHNOLOGY
International Journal of Nanomedicine Pub Date : 2025-03-29 eCollection Date: 2025-01-01 DOI:10.2147/IJN.S489777
Songyang Liu, Dan Yi, Rui Ma, Wei Zhang
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引用次数: 0

Abstract

Introduction: Sorafenib (SF) is a small molecule involved in tumor proliferation and angiogenesis. SF is inhibitor of several kinases, including RAF, VEGFR, and PDGFR. However the weak targeting ability of SF for liver tumor tissues is the major problem in clinical therapy. Therefore, a SF-loaded folic acid-targeted liposome drug delivery system was devised for targeting liver tumor therapy in this study.

Methods: Folic acid (FA), HSPC, DSPE-PEG2k, CHO, and SF were composed to prepare a folic acid-targeted SF-loaded liposome (LSF) drug delivery system. LSF and drug loading content was established through thin-film-hydration technique and HPLC, respectively. The particle size and stability of LSF were examined by dynamic light scattering (DLS). The inhibition effect of LSF was elucidated in vitro on liver cancer cells through cell cytotoxicity and apoptosis experiments. The tumor-inhibiting efficacy was measured on liver xenograft model.

Results: The drug loading content (DLC) of LSF was 3.6%. The diameter of LSF was 197.1±16.6 nm, and LSF was stable during 24 h. Liver cancer cells could be effectively inhibited by LSF in vitro. LSF could substantially induce apoptosis. Also, LSF could inhibit tumor growth effectively in vivo. LSF could reduce side effects of SF demonstrated by bio-safety tests.

Conclusion: LSF is a FA-targeted drug delivery system that could effectively inhibit the progression of liver cancer.

载索拉非尼的叶酸靶向脂质体纳米颗粒用于肝癌治疗。
索拉非尼(Sorafenib, SF)是一种参与肿瘤增殖和血管生成的小分子药物。SF是几种激酶的抑制剂,包括RAF、VEGFR和PDGFR。然而,SF对肝脏肿瘤组织的靶向能力弱是临床治疗中的主要问题。因此,本研究设计了一种载sf叶酸靶向脂质体给药系统,用于肝肿瘤的靶向治疗。方法:将叶酸(FA)、HSPC、DSPE-PEG2k、CHO、SF组成叶酸靶载SF脂质体(LSF)给药体系。采用薄膜水化法和高效液相色谱法分别测定了LSF和载药量。采用动态光散射法(DLS)检测了LSF的粒径和稳定性。通过细胞毒性和细胞凋亡实验,阐明了枸杞多糖对肝癌细胞的体外抑制作用。在异种肝脏移植模型上测定其抑瘤效果。结果:LSF的载药量(DLC)为3.6%。LSF直径为197.1±16.6 nm, 24 h内保持稳定,对肝癌细胞有较好的体外抑制作用。LSF可显著诱导细胞凋亡。LSF在体内也能有效抑制肿瘤生长。生物安全试验证明,LSF可以减少SF的副作用。结论:LSF是一种能有效抑制肝癌进展的fa靶向给药系统。
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来源期刊
International Journal of Nanomedicine
International Journal of Nanomedicine NANOSCIENCE & NANOTECHNOLOGY-PHARMACOLOGY & PHARMACY
CiteScore
14.40
自引率
3.80%
发文量
511
审稿时长
1.4 months
期刊介绍: The International Journal of Nanomedicine is a globally recognized journal that focuses on the applications of nanotechnology in the biomedical field. It is a peer-reviewed and open-access publication that covers diverse aspects of this rapidly evolving research area. With its strong emphasis on the clinical potential of nanoparticles in disease diagnostics, prevention, and treatment, the journal aims to showcase cutting-edge research and development in the field. Starting from now, the International Journal of Nanomedicine will not accept meta-analyses for publication.
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