Preparation and Evaluation of Folate Receptor Mediated Targeting Liposomes
Liposomes have been well used as an efficient delivery system for cancer therapy. Overexpressed folate receptor is a confirmed tumor-associated antigen that binds folate and folate-targeted liposomes with very high affinity. Folate receptor shuttles these bound molecules inside cells via an endocytic mechanism. It is described as an efficient folate-modified liposome preparation method in this chapter based on a post-insertion technique. Conjugate of 1,2-dipalmitoyl-sn-glycerophosphoethanolamine-polyethylene glycol-folate (DPPE-PEG-folate), derived from PEG with molecular masses of 2000 Da, is synthesized and characterized by 1H NMR and mass spectrometer. By micellization of folate conjugates and their controlled insertion into preformed liposomes, DOX-loaded folate-targeted liposome is prepared. The selectivity and specificity of folate target liposome is evaluated in KB, C6, and cortical cells. It was found that KB cells took up significant amounts of DOX relative to the C6 cells or relative to normal cortical tissue.
KeywordsFolate Ligand-modified targeting liposome Cancer Drug delivery Post-insertion
- Antony AC (1992) The biological chemistry of folate receptors. Blood 79:2807–2820Google Scholar
- Kamen BA, Wang MT, Streckfuss AJ, Peryea X, Anderson RGW (1988) Delivery of folates to the cytoplasm of Ma104 cells is mediated by a surface-membrane receptor that recycles. J Biol Chem 263:13602–13609Google Scholar
- Lee RJ, Low PS (1994) Delivery of liposomes into cultured kb cells via folate receptor-mediated endocytosis. J Biol Chem 269:3198–3204Google Scholar
- van der Heijden JW, Oerlemans R, Dijkmans BAC, Qi H, van der Laken CJ, Lems WF, Jackman AL, Kraan MC, Tak PP, Ratnam M, Jansen G (2009) Folate receptor beta as a potential delivery route for novel folate antagonists to macrophages in the synovial tissue of rheumatoid arthritis patients. Arthritis Rheum-Us 60:12–21CrossRefGoogle Scholar
- Yan Y, Qi XR (2008) Preparation and properties of folate receptor-targeted cationic liposomes. Yao xue xue bao = Acta pharmaceutica Sinica 43:1134–1139Google Scholar