Efficacy Interactions of PEG–DOX–N-acetyl Glucosamine Prodrug Conjugate for Anticancer Therapy |
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| Institution: | 1. INSERM U1148, Laboratory for Vascular Translational Science (LVTS), Institut Galilée, Université Paris 13, Sorbonne Paris Cité, 99 Avenue Jean-Baptiste Clément, Villetaneuse, F-93430, France;2. Inserm U1148, Laboratory for Vascular Translational Science, UFR SMBH, Université Paris 13, Sorbonne Paris Cité, Groupe Biothérapies et Glycoconjugués, Bobigny, F-93430, France;1. Agricultural and Ecological Research Unit, Indian Statistical Institute, 203, B. T. Road, Kolkata 700108, India;2. Department of Mathematics, Visva-Bharati University, Santiniketan 731235, India;3. Dipartimento di Matematica “Giuseppe Peano”, Università di Torino, via Carlo Alberto 10, 10123 Torino, Italy;4. Department of Mathematics and Statistics, College of Science, Sultan Qaboos University, P.O. Box 36 Al-Khod, Postal Code 123, Oman;1. Department of Orthopedics and Rehabilitation, University of Wisconsin-Madison, Madison, WI, USA;2. Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI, USA;3. Department of Medicine, University of Wisconsin-Madison, School of Medicine and Public Health, Madison, WI, USA;1. Department of Chemistry, University of Connecticut, Storrs, CT 06269-3060, USA;2. Photosynthetic Antenna Research Center, Washington University in St. Louis, MO 63130, USA;3. Department of Chemistry, School of Science and Technology, Kwansei Gakuin University, Gakuen, Sanda, Hyogo 669-1337, Japan;4. Graduate School of Science, Osaka City University, 3-3-138 Sugimoto, Sumiyoshi-ku, Osaka 558-8585, Japan;5. Osaka City University Advanced Research Institute for Natural Science and Technology, 3-3-138 Sugimoto, Sumiyoshi-ku, Osaka 558-8585, Japan;1. TIFR Center for Interdisciplinary Sciences, Tata Institute of Fundamental Research Hyderabad, 21 Brundavan Colony, Narsingi, Hyderabad 500075, India;2. Department of Chemical Sciences, Tata Institute of Fundamental Research, Homi Bhabha Road, Colaba, Mumbai 400005, India |
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| Abstract: | Present investigation is exploring structure–biocompatibility interaction of tumour targeted polyethylene glycol (PEG) based drug conjugate of doxorubicin using N-acetyl glucosamine as targeting ligand. The synthesized polymer drug conjugate was evaluated for particle size, zeta potential, molecular weight, haemolysis activity, cytotoxicity, protein binding and in vitro receptor (lectin) binding study. The particle size of synthesized conjugate was observed to be around 30 nm with polydispersability index of 0.213 indicating mono-disperse particles. Fluorescence quenching assay addressed relatively lower binding interactions of polymer drug conjugate to bovine serum albumin in comparison with free doxorubicin which may be governed to the hydrophilicity of polyethylene glycol and N-acetyl glucosamine. The cell compatibility and haemolysis study showed that PEG drug conjugate was nontoxic and biocompatible, which recommends the suitability of polymer drug conjugates for delivering biological active agents systemically. In vitro ligand–lectin receptor binding assays of synthesized targeted polymer conjugate suggest the possibility of promising interaction of N-acetyl glucosamine in vivo. Thus, the study indicated the suitability of N-acetyl glucosamine anchored targeted polymer drug conjugate in delivering bio-therapeutics for specifically targeting to tumour tissues. |
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| Keywords: | Doxorubicin N-acetyl glucosamine Haemolysis Fluorescence quenching assay Lectin Concanavallin A |
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