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Trastuzumab-conjugated boron-containing liposomes for tumor-cell targeting; development and cellular studies
Qichun Wei1, Erika Bohl Kullberg, Lars Gedda
1Division of Biomedical Radiation Sciences, Department of Oncology, Radiology and Clinical Immunology, Rudbeck Laboratory, Uppsala University, SE-751 85 Uppsala, Sweden. weiqichun@hotmail.com
Abstract:
The goal of the present study was to investigate HER-2-targeted boron-containing liposomes as a potential drug delivery vehicle for boron neutron capture therapy (BNCT). Trastuzumab was conjugated to the distal end of PEG-DSPE-NHS in micelles and the Trastuzumab-PEG-DSPE were then transferred to preformed liposomes, either empty or loaded with water soluble boronated acridine (WSA), using the micelle transfer method. The final conjugates were referred to as Trastuzumab-liposome and Trastuzumab-liposome-WSA. The binding specificity, uptake, retention and internalization of Trastuzumab-liposome-WSA conjugates were studied in cultured SK-BR-3 cells, with regard to the targeting agent, carrier, and the load. The subcellular location of WSA was studied using confocal microscopy. The conjugates showed specific binding to the HER-2 receptors of SK-BR-3 cells. High cellular uptake and internalization of the conjugates was seen, reaching 132 ppm of boron in the targeted cells after 24 h. WSA was distributed mainly in the cytoplasm and was shown to have long cellular retention, with 90% and 67% of the boron remained in the cells after 24 h and 48 h, respectively. The conjugate Trastuzumab-liposome-WSA could be considered as a potent drug delivery system for BNCT.
Insights
HER-2-targeted liposomes loaded with boronated acridine show promise for boron neutron capture therapy (BNCT). These drug delivery systems demonstrate specific binding, high cellular uptake, and long retention in HER-2-positive cancer cells.
Area of Science:
- Oncology
- Nanotechnology
- Biomedical Engineering
Background:
- Boron neutron capture therapy (BNCT) is an emerging cancer treatment.
- Targeted drug delivery systems are crucial for enhancing BNCT efficacy.
- HER-2 receptors are overexpressed in certain aggressive cancers, making them a viable therapeutic target.
Purpose of the Study:
- To develop and evaluate HER-2-targeted, boron-containing liposomes for BNCT.
- To assess the binding specificity, cellular uptake, retention, and internalization of these liposomes.
- To investigate the potential of these conjugates as a drug delivery vehicle for BNCT.
Main Methods:
- Conjugation of Trastuzumab to PEG-DSPE-NHS micelles.
- Transfer of Trastuzumab-PEG-DSPE to preformed liposomes (empty or loaded with water-soluble boronated acridine - WSA).
- Assessment of Trastuzumab-liposome-WSA conjugates' binding, uptake, retention, and internalization in SK-BR-3 cells using confocal microscopy.
Main Results:
- Conjugates demonstrated specific binding to HER-2 receptors on SK-BR-3 cells.
- High cellular uptake and internalization were observed, with targeted cells accumulating 132 ppm of boron after 24 hours.
- Water-soluble boronated acridine (WSA) showed long cellular retention (90% at 24h, 67% at 48h) and primarily localized in the cytoplasm.
Conclusions:
- HER-2-targeted liposomes loaded with WSA are a potent drug delivery system for BNCT.
- The developed system exhibits specific targeting, efficient cellular uptake, and sustained drug retention.
- This approach holds significant potential for improving BNCT outcomes in HER-2-positive cancers.
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