14 research outputs found
Folate receptor-targeted drug delivery systems of doxorubicin for the treatment of cancer.
Supramolecular drug carriers are designed to accumulate in tumors by passive targeting via the enhanced permeability and retention (EPR) effect. The conjugation of targeting moieties results in receptor-mediated selective drug delivery. Folic acid (FA) is a low molecular weight ligand of the folate receptor (FR), widely used as targeting agent, due to overexpression of FR on many types of cancer cells1.In the present work, we compare the in vitro and in vivo pharmacological activity of two drug delivery systems bearing doxorubicin as the active drug and folic acid as the targeting moiety. In the first approach, two pullulan (Pull)-based prodrugs of doxorubicin (Dox) were synthesized, distinguished by the presence or absence of folic acid (FA) as targeting moiety, namely Pull-PEG-FA-Dox and Pull-PEG-Dox2. The second drug delivery system is the PEGylated liposomal doxorubicin (PLD, Doxil\u2122) and its folate derivate obtained by ligand post-insertion from the commercial formulation (PLD-FA)3
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Synthesis and biological evaluation of a polyglutamic acid-dopamine conjugate: a new antiangiogenic agent
Dopamine has previously been shown to inhibit angiogenesis in vitro and in vivo, but its clinical applications in this context are severely limited by its short half-life. Here we report the synthesis of a polyglutamic acid-dopamine conjugate and show that conjugation significantly extends (from 1 to 24 h) dopamine’s antiangiogenic activity in vitro and in vivo. These findings form the basis for the development of a new class of agents for the treatment of angiogenesis-dependent diseases