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Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors

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dc.contributor.author Aderibigbe, BA
dc.contributor.author Mhlwatika, Z
dc.contributor.author Nwamadi, M
dc.contributor.author Balogun, Mohammed O
dc.contributor.author Matshe, William MR
dc.date.accessioned 2019-11-28T08:15:04Z
dc.date.available 2019-11-28T08:15:04Z
dc.date.issued 2019-04
dc.identifier.citation Aderibigbe, B.A., Mhlwatika, Z., Nwamadi, M., Balogun, M.O. & Matshe, W.M.R. 2019. Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors. Journal of Drug Delivery Science and Technology, vol 50:388-401 en_US
dc.identifier.issn 1773-2247
dc.identifier.issn 1157-1489
dc.identifier.uri https://www.sciencedirect.com/science/article/pii/S1773224718306051
dc.identifier.uri https://doi.org/10.1016/j.jddst.2019.01.038
dc.identifier.uri http://hdl.handle.net/10204/11236
dc.description Copyright: 2019 Elsevier. Due to copyright restrictions, the attached PDF file contains the abstract version of the full-text item. For access to the full-text item, please consult the publisher's website. The definitive version of the work is published in the Journal of Drug Delivery Science and Technology, vol 50:388-401 en_US
dc.description.abstract Malaria is an acute disease that is caused by the protozoan Plasmodium parasites. Drug resistance is the major problem that is hindering the control of this disease. In order to overcome drug resistance to commonly used antimalarials, nanocarriers which are biocompatible, non-toxic, and are able to deliver drugs to the target site were designed. Polyaspartamide-drug conjugates containing antimalarials that inhibit dihydrofolate reductase were prepared and characterized by nuclear magnetic resonance spectroscopy (NMR), Fourier transform spectroscopy (FTIR), X-ray diffraction (XRD), Thermogravimetric analysis (TGA), Scanning electron microscope (SEM), Energy-dispersive X-ray analysis (EDX), particle size analysis, as well as in vitro antiplasmodial analysis and drug release studies at physiological pH values. NMR and FTIR results confirmed the successful incorporation of the drugs onto the conjugates. SEM images of the conjugates showed predominant spherical and cluster of globular morphologies. In vitro release mechanisms of the drugs from the conjugates were slow and sustained. Conjugates containing 4-aminosalicylic acid and pyrimethamine were found to be the most active against the asexual stage of the parasite with an IC50 value of 332.37 en_US
dc.language.iso en en_US
dc.publisher Elsevier en_US
dc.relation.ispartofseries Workflow;22904
dc.subject Antimalarials en_US
dc.subject Drug delivery en_US
dc.subject Drug resistance en_US
dc.subject Nanocarriers en_US
dc.subject Polyaspartamide-drug conjugates en_US
dc.title Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors en_US
dc.type Article en_US
dc.identifier.apacitation Aderibigbe, B., Mhlwatika, Z., Nwamadi, M., Balogun, M. O., & Matshe, W. M. (2019). Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors. http://hdl.handle.net/10204/11236 en_ZA
dc.identifier.chicagocitation Aderibigbe, BA, Z Mhlwatika, M Nwamadi, Mohammed O Balogun, and William MR Matshe "Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors." (2019) http://hdl.handle.net/10204/11236 en_ZA
dc.identifier.vancouvercitation Aderibigbe B, Mhlwatika Z, Nwamadi M, Balogun MO, Matshe WM. Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors. 2019; http://hdl.handle.net/10204/11236. en_ZA
dc.identifier.ris TY - Article AU - Aderibigbe, BA AU - Mhlwatika, Z AU - Nwamadi, M AU - Balogun, Mohammed O AU - Matshe, William MR AB - Malaria is an acute disease that is caused by the protozoan Plasmodium parasites. Drug resistance is the major problem that is hindering the control of this disease. In order to overcome drug resistance to commonly used antimalarials, nanocarriers which are biocompatible, non-toxic, and are able to deliver drugs to the target site were designed. Polyaspartamide-drug conjugates containing antimalarials that inhibit dihydrofolate reductase were prepared and characterized by nuclear magnetic resonance spectroscopy (NMR), Fourier transform spectroscopy (FTIR), X-ray diffraction (XRD), Thermogravimetric analysis (TGA), Scanning electron microscope (SEM), Energy-dispersive X-ray analysis (EDX), particle size analysis, as well as in vitro antiplasmodial analysis and drug release studies at physiological pH values. NMR and FTIR results confirmed the successful incorporation of the drugs onto the conjugates. SEM images of the conjugates showed predominant spherical and cluster of globular morphologies. In vitro release mechanisms of the drugs from the conjugates were slow and sustained. Conjugates containing 4-aminosalicylic acid and pyrimethamine were found to be the most active against the asexual stage of the parasite with an IC50 value of 332.37 DA - 2019-04 DB - ResearchSpace DP - CSIR KW - Antimalarials KW - Drug delivery KW - Drug resistance KW - Nanocarriers KW - Polyaspartamide-drug conjugates LK - https://researchspace.csir.co.za PY - 2019 SM - 1773-2247 SM - 1157-1489 T1 - Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors TI - Synthesis, characterization and in vitro analysis of polymer-based conjugates containing dihydrofolate reductase inhibitors UR - http://hdl.handle.net/10204/11236 ER - en_ZA


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