By a News Reporter-Staff News Editor at Biotech Week -- Investigators publish new report on Drugs and Therapies. According to news reporting out of Suzhou, People's Republic of China, by NewsRx editors, research stated, "Endosomal pH-activatable paclitaxel (PTX) prodrug micellar nanoparticles were designed and prepared by conjugating PTX onto water-soluble poly(ethylene glycol)-b-poly(acrylic acid) (PEG-PAA) block copolymers via an acid-labile acetal bond to the PAA block and investigated for potent growth inhibition of human cancer cells in vitro. PTX was readily conjugated to PEG-PAA with high drug contents of 21.6, 27.0, and 42.8 wt % (denoted as PTX prodrugs 1, 2, and 3, respectively) using ethyl glycol vinyl ether (EGVE) as a linker."
Our news journalists obtained a quote from the research from Soochow University, "The resulting PTX conjugates had defined molecular weights and self-assembled in phosphate buffer (PB, pH 7.4, 10 mM) into monodisperse micellar nanoparticles with average sizes of 158.3-180.3 nm depending on PTX contents. The in vitro release studies showed that drug release from PTX prodrug nanoparticles was highly pH-dependent, in which ca. 86.9%, 66.4% and 29.0% of PTX was released from PTX prodrug 3 at 37 degrees C in 48 h at pH 5.0, 6.0, and pH 7.4, respectively. MTT assays showed that these pH-sensitive PTX prodrug nanoparticles exhibited high antitumor effect to KB and HeLa cells (IC50 = 0.18 and 0.9 mu g PTX equiv/rnL, respectively) as well as PTX-resistant A549 cells. Notably, folate-decorated PTX prodrug micellar nanoparticles based on PTX prodrug 3 and 20 wt % folate-poly(ethylene glycol)-b-poly(D,L-lactide) (FA-PEG-PLA) displayed apparent targetability to folate receptor-overexpressing KB cells with IC50 over 12 times lower than nontargeting PTX prodrug 3 under otherwise the same conditions. Furthermore, PTX prodrug nasioparticles could also load doxorubicin (DOX) to simultaneously release PTX and DOX under mildly acidic pH."
According to the news editors, the research concluded: "These acetal-linked PTX prodrug micellar nanoparticles have appeared as a highly versatile and potent platform for cancer therapy."
For more information on this research see: Acetal-Linked Paclitaxel Prodrug Micellar Nanoparticles as a Versatile and Potent Platform for Cancer Therapy. Biomacromolecules, 2013;14(8):2772-2780. Biomacromolecules can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society - www.acs.org; Biomacromolecules - www.pubs.acs.org/journal/bomaf6)
Our news journalists report that additional information may be obtained by contacting Y.D. Gu, Soochow Univ, Jiangsu Key Lab Adv Funct Polymer Design & Applic, Dept. of Polymer Sci & Engn, Coll Chem Chem Engn & Mat Sci, Suzhou 215123, People's Republic of China. Additional authors for this research include Y.N. Zhong, F.H. Meng, R. Cheng, C. Deng and Z.Y. Zhong (see also Drugs and Therapies).
Keywords for this news article include: Asia, Antineoplastics, Pharmaceuticals, Suzhou, Cancer, Taxoids, Oncology, Terpenes, Paclitaxel, Hydrocarbons, Nanoparticle, Cycloparaffins, Nanotechnology, Organic Chemicals, Mitotic Inhibitors, Drugs and Therapies, Emerging Technologies, People's Republic of China
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