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Published on: March 1, 2024
VEGF- and VEGFR2-Targeted Liposomes for Cisplatin Delivery to Glioma Cells
Sergey A Shein1,2, Ilya I Kuznetsov3, Tatiana O Abakumova1
1Department of Fundamental and Applied Neurobiology, Serbsky Medical Research Center of Psychiatry and Narcology , Moscow, Russia.
Abstract:
Targeted delivery of anticancer drugs to brain tumors, especially glioblastoma multiforme, which is the most frequent and aggressive type, is one of the important objectives in nanomedicine. Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are promising targets because they are overexpressed by not only core tumor cells but also by migrated glioma cells, which are responsible for resistance and rapid progression of brain tumors. The purpose of the present study was to develop the liposomal drug delivery system combining enhanced loading capacity of cisplatin and high binding affinity to glioma cells. This was achieved by using of highly soluble cisplatin analogue, cis-diamminedinitratoplatinum(II), and antibodies against the native form of VEGF or VEGFR2 conjugated to liposome surface. The developed drug delivery system revealed sustained drug release profile, high affinity to antigens, and increased uptake by glioma C6 and U-87 MG cells. Pharmacokinetic study on glioma C6-bearing rats revealed prolonged blood circulation time of the liposomal formulation. The above features enabled the present drug delivery system to overcome both poor pharmacokinetics typical for platinum formulations and low loading capacity typical for conventional liposomal cisplatin formulations.
Insights
This study developed a novel liposomal drug delivery system for brain tumors, enhancing cisplatin loading and targeting glioma cells via VEGF/VEGFR2 antibodies. This nanomedicine approach improves drug circulation and uptake, overcoming limitations of traditional platinum formulations.
Area of Science:
- Nanomedicine
- Oncology
- Drug Delivery
Background:
- Glioblastoma multiforme is an aggressive brain tumor with poor prognosis.
- Targeted drug delivery to brain tumors remains a significant challenge.
- Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are overexpressed in glioma cells, making them promising therapeutic targets.
Purpose of the Study:
- To develop a liposomal drug delivery system for enhanced cisplatin loading and targeted delivery to glioma cells.
- To improve the binding affinity and cellular uptake of the drug delivery system.
- To overcome the limitations of conventional platinum-based chemotherapy and liposomal formulations.
Main Methods:
- Development of liposomes encapsulating a soluble cisplatin analogue (cis-diamminedinitratoplatinum(II)).
- Conjugation of antibodies against VEGF or VEGFR2 to the liposome surface for targeted binding.
- In vitro evaluation of drug release, antigen binding affinity, and cellular uptake in glioma cell lines (C6 and U-87 MG).
- In vivo pharmacokinetic studies in glioma C6-bearing rats.
Main Results:
- The developed liposomal system demonstrated a sustained drug release profile.
- High binding affinity to VEGF and VEGFR2 antigens was observed.
- Significantly increased uptake by C6 and U-87 MG glioma cells.
- Prolonged blood circulation time of the liposomal formulation in vivo.
Conclusions:
- The novel liposomal drug delivery system effectively targets glioma cells by leveraging VEGF/VEGFR2.
- This approach enhances cisplatin delivery, improves pharmacokinetics, and overcomes low loading capacity issues.
- This nanomedicine strategy holds promise for improved glioblastoma treatment.
