didodecyl methotrexate lipid core emulsion

Didodecyl methotrexate lipid core emulsion is an injectable drug delivery system comprising a lipophilic prodrug of methotrexate, known as methotrexate didodecyl ester, incorporated into a lipid nanoemulsion. The nanoemulsion is engineered to resemble the lipid core of low-density lipoprotein (LDL) particles, enabling the drug to exploit the overexpression of LDL receptors (LDLR) on the surface of neoplastic and inflammatory cells. This biomimetic strategy enhances the selective delivery of the folate antagonist to target tissues while reducing systemic toxicity, particularly the hematological and gastrointestinal side effects associated with conventional methotrexate. Upon cellular internalization via receptor-mediated endocytosis, the ester bonds of the prodrug are cleaved by intracellular esterases, releasing active methotrexate. The released drug then binds to and inhibits dihydrofolate reductase (DHFR), disrupting the synthesis of thymidylate and purine nucleotides, which leads to the inhibition of DNA synthesis and induction of apoptosis in rapidly proliferating cells.

Other names

methotrexate didodecyl ester lipid core emulsiondidodecyl methotrexate LCEmethotrexate didodecyl ester LDE