Preparation and characterization of folic acid linked poly(L-glutamate) nanoparticles for cancer targeting

Abstract

Nanoparticles of Poly(L-glutamic acid) (PG) conjugated to the anticancer drug paclitaxel and targeted moiety folic acid (FA) were synthesized and characterized in vitro. The nanoparticles were designed to take advantage of FA targeting to folate receptor (FR) positive cancer cells. The chemical composition of the conjugate was characterized by 1 H-NMR, FTIR and UV/vis spectroscopy. The selective cytotoxicity of the FA-PG-paclitaxel conjugates was evaluated in FR positive cancer cells. The interaction of the conjugate was visualized by fluorescence microscopy with results confirming the successful preparation of the conjugate and the production of nanoparticles of about 200-300 nm in diameter. The amount of paclitaxel conjugated to FA-PG was 25% by weight. Cellular uptake of the conjugate was FA dependent, and the conjugate uptake was mediated specifically by the folate receptor. These results demonstrate the improved selective toxicity and effective delivery of an anticancer drug into FR bearing cells in vitro.

Versatile strategies for fabricating polymer nanomaterials with controlled size and morphology

“…Spherical polymer nanoparticles have attracted considerable attention because of their unique properties different from those of the bulk materials (e.g, electrical, optical, thermal, mechanical and chemical characteristics). [9][10][11][12] To date, diverse synthetic ways to prepare polymer nanoparticles have been continuously developed. In particular, microemulsion polymerization has become one of the most extensively used methods.…”

Folate-decorated poly(lactide-co-glycolide)-vitamin E TPGS nanoparticles for targeted drug delivery

“…Folic acid (FOL), an oxidized form of folate, has thus widely been used as a targeting ligand due to its high binding affinity for the folate receptors (K d $10 À10 M) [6]. In the literature, folate decorated liposomes, micelles and NPs of biodegradable polymers such as DSPE-PEG, PCL-MEPG, poly(lactide-co-glycolide) (PLGA)-PEG (PLGA-PEG), PLGA have been found to increase the cellular uptake and cell cytotoxicity of the formulated anticancer drugs [2,[7][8][9][10][11].…”

Targeting and imaging cancer cells by Folate-decorated, quantum dots (QDs)- loaded nanoparticles of biodegradable polymers

“…Folic acid and its conjugate were widely used for selective delivery of anticancer agents to cells with folate receptor, which are over-expressed in many kinds of human cancer cells such as ovarian, breast and prostate cancers while only minimally distributed in normal tissues [18][19][20][21][22]. In the literature, liposomes, micelles and NPs of biodegradable polymers with folate decoration have been found to increase the cellular uptake of formulated anticancer drugs [23][24][25][26][27][28][29][30]. Recently, QDs linked with folate for caner targeting and imaging were reported.…”