New Findings on Heparin Therapy from University of Ulsan Summarized (Oral delivery of a potent anti-angiogenic heparin conjugate by chemical conjugation and physical complexation using deoxycholic acid)
By a News Reporter-Staff News Editor at Biotech Week -- New research on Drugs and Therapies is the subject of a report. According to news reporting originating from Seoul, South Korea, by NewsRx correspondents, research stated, "Angiogenesis, the formation of new blood vessels, plays a pivotal role in tumor progression and for this reason angiogenesis inhibitors are an important class of therapeutics for cancer treatment. Heparin-based angiogenesis inhibitors have been newly developed as one of such classes of therapeutics and possess a great promise in the clinical context."
Our news editors obtained a quote from the research from the University of Ulsan, "Taurocholate conjugated low molecular weight heparin derivative (LHT7) has been proven to be a potent, multi-targeting angiogenesis inhibitor against broad-spectrum angiogenic tumors. However, major limitations of LHT7 are its poor oral bioavailability, short half-life, and frequent parenteral dosing schedule. Addressing these issues, we have developed an oral formulation of LHT7 by chemically conjugating LHT7 with a tetrameric deoxycholic acid named LHTD4, and then physically complexing it with deoxycholylethylamine (DCK). The resulting LHTD4/DCK complex showed significantly enhanced oral bioavailability (34.3 +/- 2.89%) and prolonged the mean residence time (7.5 +/- 0.5 h). The LHTD4/DCK complex was mostly absorbed in the intestine by transcellular pathway via its interaction with apical sodium bile acid transporter. In vitro, the VEGF-induced sprouting of endothelial spheroids was significantly blocked by LHTD4. LHTD4/DCK complex significantly regressed the total vessel fractions of tumor (77.2 +/- 3.9%), as analyzed by X-ray microCT angiography, thereby inhibiting tumor growth in vivo."
According to the news editors, the research concluded: "Using the oral route of administration, we showed that LHTD4/DCK complex could be effective and chronically administered as angiogenesis inhibitor."
For more information on this research see: Oral delivery of a potent anti-angiogenic heparin conjugate by chemical conjugation and physical complexation using deoxycholic acid. Biomaterials, 2014;35(24):6543-6552. Biomaterials can be contacted at: Elsevier Sci Ltd, The Boulevard, Langford Lane, Kidlington, Oxford OX5 1GB, Oxon, England. (Elsevier - www.elsevier.com; Biomaterials - www.elsevier.com/wps/product/cws_home/30392)
The news editors report that additional information may be obtained by contacting F. Alam, University of Ulsan, Coll Med, Asan Med Center, Dept. of Otolaryngol, Seoul 138736, South Korea. Additional authors for this research include T.A. Al-Hilal, S.W. Chung, D. Seo, F. Mahmud, H.S. Kim, S.Y. Kim and Y. Byun (see also Drugs and Therapies).
Keywords for this news article include: Asia, Seoul, Heparin, South Korea, Angiogenesis, Drugs and Therapies
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