Synthesis, characterization, biological evaluation, and drug release study of polyamidoamine-containing neridronate. Issue 9 (13th June 2019)

• Record Type: Journal Article
• Authors: Mukaya, Hembe E.; Van Zyl, Robyn L.; Jansen van Vuuren, Natasha C.; Chen, Chien-Teng; Mbianda, Xavier Y.
• Is Part Of: International journal of polymeric materials. Volume 68:Issue 9(2019)
• Page Start: 489
• Page End: 498
• Publication Date: 2019-06-13
• Subjects: Anticancer activity -- antimalaria activity -- bisphosphonates -- drug release -- neridronate -- polyamidoamine conjugate; Polymers -- Periodicals; Plastics -- Periodicals; 620.19205
• DOI: 10.1080/00914037.2018.1466135
• Languages: English
• ISSNs: 0091-4037

Abstract

Abstract: Polyamidoamines were synthesized by Michael-type polyaddition reaction and conjugates characterized by 1 H NMR, 31 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. Graphical Abstract: