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Researchers from Fudan University Describe Findings in Antineoplastics

February 19, 2014

By a News Reporter-Staff News Editor at Biotech Week -- Current study results on Drugs and Therapies have been published. According to news reporting from Shanghai, People's Republic of China, by NewsRx journalists, research stated, "Lapatinib is a dual EGFR and HER2 inhibitor that is used to treat HER2-overexpressing cancers. However, its poor water solubility hinders its clinical use."

The news correspondents obtained a quote from the research from Fudan University, "Proteobionics is a promising way to solve this problem. Lapatinib-incorporated core-shell nanoparticles (LTNPs) were prepared and characterized by cryo-transmission electron micrograph. Then, in vitro cellular uptake and in vivo glioma targeting effect were determined by both qualitative and quantitative studies. After that, anti-glioma effect of LTNPs was determined by cytotoxicity and life-span study. Finally, the mechanism was elucidated by western blot. LTNPs elevated the water solubility of the drug from 0.007 mg/mL to over 10 mg/mL, which was better than most commercially available injection solvents. Glioma is an increasing threat to humans' health. Here, we evaluated the treatment effects of LTNPs on glioma and explored their mechanism. LTNPs were taken up by U87 cells, inhibiting their proliferation and causing a G2 phase arrest. The uptake was energy-, time- and concentration-dependent, and several pathways were involved. LTNPs inhibited the phosphorylation of the survival (phosphatidylinositol 3-kinase/Akt) pathways, which caused the antiproliferative effect. In vivo experiments determined that LTNPs were distributed to and accumulated in glioma by the enhanced permeation and retention effect. The distribution was colocalized with SPARC expression, which may mediate endocytosis. In pharmacokinetics and glioma distribution study, LTNPs displayed a higher blood AUC, glioma concentration and glioma/brain ratio than Tykerb. A pharmacodynamics study confirmed that LTNPs could significantly expand the median survival time of glioma-bearing mice at a cumulative dose of 40 mg/kg, which was only 5% of the dose of the commercially available lapatinib tablet (Tykerb)."

According to the news reporters, the research concluded: "LTNPs effectively increased the solubility of lapatinib and improved the treatment of glioma."

For more information on this research see: Incorporation of lapatinib into core-shell nanoparticles improves both the solubility and anti-glioma effects of the drug. International Journal of Pharmaceutics, 2014;461(1-2):478-488. International Journal of Pharmaceutics can be contacted at: Elsevier Science Bv, PO Box 211, 1000 Ae Amsterdam, Netherlands. (Elsevier -; International Journal of Pharmaceutics -

Our news journalists report that additional information may be obtained by contacting H.L. Gao, Fudan University, Sch Pharm, Key Lab Smart Drug Delivery, Minist Educ, Shanghai 201203, People's Republic of China. Additional authors for this research include Y.C. Wang, C. Chen, J. Chen, Y. Wei, S.L. Cao and X.G. Jiang (see also Drugs and Therapies).

Keywords for this news article include: Asia, Antineoplastics, Shanghai, Lapatinib, Treatment, Nanoparticle, Nanotechnology, EGFR Inhibitors, HER2 Inhibitors, Drugs and Therapies, Emerging Technologies, People's Republic of China, Tyrosine Kinase Inhibitors

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Source: Biotech Week

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