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Fructose and biotin co-modified liposomes for dual-targeting breast cancer
1Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, China.
Abstract:
Chemotherapy, as the main treatment for breast cancer, inevitably damages normal tissues due to the lack of targeting. Various nano targeting drug delivery systems (TDDS) have the potential to be developed as anticancer therapeutics. Although mono-ligand-directed liposomes have been used with some success, dual-ligand-directed liposomes exhibit promising advantages. In current work, we synthesized a Y-shaped ligand covalently linking fructose and biotin (Fru-Bio-Chol) to prepare a dual-targeting liposome Fru-Bio-Lip for breast cancer. The targeting ability was evaluated by comparing the Fru-Bio-Lip with the non-modified liposome (Lip), fructose or biotin mono modified liposomes (Fru-Lip and Bio-Lip), and another dual-targeting liposome (Fru + Bio-Lip) physically mixing fructose and biotin mono modified ligands (Fru-Chol and Bio-Chol). The cellular uptake of Fru-Bio-Lip is 3.27-, 1.81-, 2.19-, 1.15-times that of Lip, Fru-Lip, Bio-Lip and Fru + Bio-Lip on 4T1 cells, and 3.11-, 1.80-, 1.89-, 1.15-times on MCF-7 cells. Additionally, the uptake mechanism indicates the uptake of Fru-Bio-Lip is energy-dependently achieved through multiple endocytosis pathway with a dual recognition of fructose and biotin by GLUT5 and SMVT. The cytotoxicity and apoptosis assay show PTX-Fru-Bio-Lip among liposomes have the strongest proliferation inhibitory effect on breast cancer cells, and the apoptosis rate is 1.7-times that of PTX-Lip. In vivo images indicate Fru-Bio-Lip have the strongest tumour enrichment ability, which is 2.76-, 1.60-, 1.96-, 1.40-times that of Lip, Fru-Lip, Bio-Lip and Fru + Bio-Lip, respectively. Overall, the fructose and biotin covalently modified liposomes improved breast cancer targeting ability, demonstrating great potential as a drug delivery system for breast cancer.
Insights
Dual-ligand liposomes combining fructose and biotin show enhanced targeting and efficacy for breast cancer treatment. This novel drug delivery system significantly improves tumor enrichment and cancer cell inhibition compared to single-ligand or non-modified liposomes.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Chemotherapy for breast cancer lacks specificity, damaging normal tissues.
- Targeting drug delivery systems (TDDS) offer potential for improved anticancer therapeutics.
- Dual-ligand liposomes present advantages over mono-ligand systems for enhanced targeting.
Purpose of the Study:
- To synthesize and evaluate a dual-targeting liposome (Fru-Bio-Lip) for breast cancer treatment.
- To assess the targeting efficiency and cellular uptake of Fru-Bio-Lip compared to various control liposomes.
- To investigate the in vitro and in vivo efficacy of the dual-targeting liposome.
Main Methods:
- Synthesis of a Y-shaped ligand covalently linking fructose and biotin (Fru-Bio-Chol).
- Preparation of dual-targeting liposomes (Fru-Bio-Lip) and comparison with non-modified (Lip), mono-modified (Fru-Lip, Bio-Lip), and physically mixed dual-modified liposomes (Fru+Bio-Lip).
- Evaluation of cellular uptake, cytotoxicity, apoptosis induction, and in vivo tumor enrichment.
Main Results:
- Fru-Bio-Lip demonstrated significantly higher cellular uptake in 4T1 and MCF-7 breast cancer cells compared to control liposomes.
- Uptake mechanism involves energy-dependent endocytosis via dual recognition of fructose (GLUT5) and biotin (SMVT).
- PTX-Fru-Bio-Lip exhibited the strongest proliferation inhibition and highest apoptosis rate in breast cancer cells; in vivo studies showed superior tumor enrichment.
Conclusions:
- Covalently modified dual-ligand liposomes (Fru-Bio-Lip) enhance breast cancer targeting ability.
- This dual-targeting liposome system shows great potential as an effective drug delivery system for breast cancer.
- The synergistic targeting of fructose and biotin receptors improves therapeutic outcomes.
