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Published on: February 19, 2016
Design of Folate-Containing Liposomal Nucleic Acid Delivery Systems for Antitumor Therapy
Elena V Shmendel1, Pavel A Puchkov1, Michael A Maslov1
1Lomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, Vernadsky Ave. 86, 119571 Moscow, Russia.
Abstract:
The delivery of therapeutic nucleic acids is a prospective method for the treatment of both inherited and acquired diseases including cancer. To achieve maximal delivery efficiency and selectivity, nucleic acids should be targeted to the cells of interest. In the case of cancer, such targeting may be provided through folate receptors overexpressed in many tumor cells. For this purpose, folic acid and its lipoconjugates are used. Compared to other targeting ligands, folic acid provides low immunogenicity, rapid tumor penetration, high affinity to a wide range of tumors, chemical stability, and easy production. Different delivery systems can utilize targeting by folate ligand including liposomal forms of anticancer drugs, viruses, and lipid and polymer nanoparticles. This review focuses on the liposomal gene delivery systems that provide targeted nucleic acid transport into tumor cells due to folate lipoconjugates. Moreover, important development step, such as rational design of lipoconjugates, folic acid content, size, and ζ-potential of lipoplexes are discussed.
Insights
Folic acid lipoconjugates enable targeted delivery of therapeutic nucleic acids to cancer cells via folate receptors. This review explores liposomal gene delivery systems utilizing folate targeting for enhanced cancer treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Therapeutic nucleic acid delivery offers promise for inherited and acquired diseases, including cancer.
- Targeting nucleic acids to specific cells, like cancer cells overexpressing folate receptors, is crucial for efficacy.
- Folic acid is a preferred targeting ligand due to its low immunogenicity, tumor penetration, and stability.
Purpose of the Study:
- To review liposomal gene delivery systems that use folate lipoconjugates for targeted nucleic acid delivery to tumor cells.
- To discuss key design considerations for effective folate-targeted liposomal delivery systems.
Main Methods:
- Review of existing literature on folate-targeted liposomal gene delivery systems.
- Analysis of the role of folate receptors in cancer cell targeting.
- Discussion of lipoconjugate design, folic acid content, lipoplex size, and zeta-potential.
Main Results:
- Folate lipoconjugates facilitate targeted delivery of nucleic acids to cancer cells via folate receptors.
- Liposomal systems are effective vehicles for folate-targeted gene delivery.
- Rational design of lipoconjugates and optimization of lipoplex characteristics are critical for delivery efficiency.
Conclusions:
- Folate-targeted liposomal gene delivery systems represent a promising strategy for cancer therapy.
- Further research into rational design and optimization of these systems can improve therapeutic outcomes.
