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Published on: February 9, 2019
Folic Acid-Targeted Liposome-Based Nanoparticle Loaded with Sorafenib for Liver Cancer Therapy
Songyang Liu1, Dan Yi1,2, Rui Ma1
1Department of Hepatobiliary and Pancreatic Surgery, General Surgery Center, The First Hospital of Jilin University, Changchun, 130061, People's Republic of China.
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.
Insights
This study developed a sorafenib-loaded folic acid-targeted liposome (LSF) drug delivery system. LSF effectively inhibits liver cancer progression in vitro and in vivo, offering a promising targeted therapy for liver tumors.
Area of Science:
- Nanotechnology in Medicine
- Drug Delivery Systems
- Oncology
Background:
- Sorafenib (SF) is a kinase inhibitor used in cancer therapy.
- A major challenge with SF is its poor targeting of liver tumor tissues.
- Targeted drug delivery systems can improve therapeutic efficacy and reduce side effects.
Purpose of the Study:
- To develop and evaluate a folic acid-targeted liposome drug delivery system for sorafenib (LSF).
- To assess the efficacy of LSF in targeting and inhibiting liver cancer progression.
- To investigate the in vitro and in vivo performance of the LSF system.
Main Methods:
- Folic acid-targeted liposomes loaded with sorafenib (LSF) were prepared using the thin-film-hydration technique.
- Drug loading content (DLC) was determined by High-Performance Liquid Chromatography (HPLC).
- Particle size, stability, in vitro cytotoxicity, apoptosis induction, and in vivo tumor inhibition were evaluated.
Main Results:
- The LSF system exhibited a DLC of 3.6% and a particle size of 197.1±16.6 nm, remaining stable for 24 hours.
- LSF demonstrated effective inhibition of liver cancer cells in vitro and induced significant apoptosis.
- In vivo studies showed that LSF effectively inhibited tumor growth and reduced the side effects of sorafenib.
Conclusions:
- The developed folic acid-targeted liposome (LSF) system is an effective drug delivery platform for sorafenib.
- LSF demonstrates significant potential for targeting and inhibiting liver cancer progression.
- This targeted approach offers a promising strategy for improving liver cancer therapy.
