Synthesis,characterization, biological evaluation,and drug release study of polyamidoamine-containing neridronate |
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| Authors: | Hembe E Mukaya Robyn L Van Zyl Natasha C Jansen van Vuuren Chien-Teng Chen |
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| Affiliation: | 1. Department of Applied Chemistry;2. Faculty of Science, University of Johannesburg, Johannesburg, Republic of South Africa;3. Pharmacology Division, Department of Pharmacy and Pharmacology;4. WITS Research Institute for Malaria (WRIM), Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, Republic of South Africa |
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| Abstract: | Polyamidoamines were synthesized by Michael-type polyaddition reaction and conjugates characterized by 1H NMR, 31 Mosmann, T. Rapid Colorimetric Assay for Cellular Growth and Survival: Application to Proliferation and Cytotoxicity Assays. J. Immunol. Meth. 1983, 65, 55–63.Crossref], PubMed], Web of Science ®] , Google Scholar]P NMR, FTIR, SEM, and EDX. The biological evaluation of the new materials revealed 12–30% inhibition of the human breast cancer cells (MCF7) and 25% of the Plasmodium falciparum malaria parasites by the conjugates. The hemolysis assay revealed that these materials did not have any effect on the host red blood cell membrane. The release mechanism of neridronate followed Korsmeyer–Peppas model at pH 1.2 with a diffusion coefficient of 0.45 indicating a Fickian diffusion mechanism; Higuchi model at pH 6.0 thus indicating a diffusion mechanism. |
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| Keywords: | Anticancer activity antimalaria activity bisphosphonates drug release neridronate polyamidoamine conjugate |
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