Tuesday, March 28, 2017

mPEG-PCL from PolySciTech utilized in development of Chrysin-nanoparticle based therapy for lung-cancer


Lung cancer is among the leading causes of cancer-related death worldwide. Chrysin, a natural active flavone, acts to enhance the chemotherapeutic effectiveness of other chemoagents (cisplatin, docetaxel, etc.) against lung cancer. Chrysin’s usability, however, is limited by its very poor water solubility and low bioavailability. Recently, researchers at Duksung Women’s University (Korea) utilized mPEG-PCL from PolySciTech (www.polyscitech.com) (PolyVivo #: AK001) to formulate chrysin-loaded nanoparticles which were found to delay tumor progression in a mouse model. This research holds promised for improved lung-cancer therapy. Read more: Kim, Kyoung Mee, Hyun Kyung Lim, Sang Hee Shim, and Joohee Jung. "Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles." International Journal of Nanomedicine 12 (2017): 1917. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5352247/


“Abstract: Chrysin is a flavone that is found in several plants and in honeycomb and possesses various biological activities. However, its low solubility means it has poor bioavailability, which must be resolved to enable its pharmaceutical applications. In the present study, chrysin was incorporated into methoxy poly(ethylene glycol)-β-polycaprolactone nanoparticles (chrysin-NPs) using the oil-in-water technique in order to overcome problems associated with chrysin. The properties of chrysin-NPs were analyzed, and their anticancer effects were investigated in vitro and in vivo. Chrysin-NPs were 77 nm sized (as determined by dynamic laser light scattering) and showed a monodisperse distribution. The zeta potential of chrysin-NPs was −2.22 mV, and they were spherically shaped by cryo-transmission electron microscopy (cryo-TEM). The loading efficiency of chrysin-NPs was 46.96%. Chrysin-NPs retained the cytotoxicity of chrysin in A549 cells. The therapeutic efficacies of chrysin-NPs were compared with those of chrysin in an A549-derived xenograft mouse model. Chrysin-NPs were intravenously injected at a 10 times lower dosage than chrysin 3 times per week (q2d×3/week). However, free chrysin was orally administrated 5 times per week (q1d×5/week). Chrysin-NP-treated group showed significant tumor growth delay, which was similar to that of chrysin-treated group, despite the considerably lower total dosage. These results suggest that the injectable chrysin-NPs enhance therapeutic efficacy in vivo and offer a beneficial formulation for chemotherapy. Keywords: chrysin, nanoparticle, chemotherapeutic efficacy, non-small-cell lung cancer, in vivo model. Nanoparticle preparation method: Chrysin (Sigma-Aldrich, St Louis, MO, USA) was incorporated into copolymer NPs using an oil-in-water technique (Figure 1). mPEG–β-polycaprolactone copolymer (mPEG-PCL, 50 mg; 2,000:5,200 Da; PolySciTech, West Lafayette, IN, USA) and 5 mg of chrysin were dissolved in a dichloromethane (Duksan reagent, Gyeonggi-do, Korea) and methanol mixture (Duksan reagent; v/v, 1.5:1). This solution (2.5 mL) was added to a 1% aqueous polyvinyl alcohol solution (6 mL) and was emulsified by sonification for 1 min. The solvent was removed by evaporation under stirring to produce NPs. To remove polyvinyl alcohol and surplus free chrysin, the supernatant was collected after centrifugation (14,000 rpm) twice at room temperature for 1 h.”
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