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Covalent immobilization of doxorubicin in glycine functionalized hydroxyapatite nanoparticles for pH-responsive release


In this study, an amino acid (glycine) functionalized hydroxyapatite nanoparticles (Gly-HANPs) were synthesized in-situ by a simple co-precipitation method. The structural and morphological properties of synthesized nanoparticles were evaluated using various characterization techniques including powder X-ray diffraction, and electron microscopy. The presence of glycine functionalities at the surface of nanoparticles was ascertained from infrared spectroscopy, thermal analysis, CHN analysis and zeta potential measurements. Doxorubicin (DOX), an anthracycline antibiotic commonly used in cancer chemotherapy was covalently bound to Gly-HANPs via a pH sensitive imine linkage using glutaraldehyde as a cross-linker. The DOX loaded nanoparticles (DOX-Glut-Gly-HANPs) showed pH-responsive controlled and sustained release of drug. Especially, the drug release rate from nanoparticles was higher in the acidic pH conditions, characteristic of tumour tissues as compared to physiological pH, typical for normal tissues. The higher release of DOX at acidic pH is indicative of cleavage of the imine (-C=N-) linkage at acidic pH. The cell uptake and therapeutic efficacy of DOX conjugated nanoparticles were investigated in WEHI-164 mouse fibrosarcoma cancer cells. The in-vitro cyto-toxicity studies suggested that glutaraldehyde treated nanoparticles (Glut-Gly-HANPs) have insignificant cyto-toxicity towards WEHI-164 cancer cells, however DOX loaded nanoparticles exhibited significant dose and time dependent cyto-toxicity towards WEHI -164 cells. Further, the confocal laser scanning microscopy studies demonstrated good cellular uptake of DOX loaded nanoparticles into WEHI-164 cells. The obtained results suggested that these nanoparticles can serve as potential carrier for pH-triggered delivery of anticancer drug.

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Publication details

The article was received on 30 Nov 2017, accepted on 07 Mar 2018 and first published on 09 Mar 2018

Article type: Paper
DOI: 10.1039/C7NJ04706A
Citation: New J. Chem., 2018, Accepted Manuscript
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    Covalent immobilization of doxorubicin in glycine functionalized hydroxyapatite nanoparticles for pH-responsive release

    G. Verma, N. G. Shetake, K. C. Barick, B. Pandey, P. Hassan and I. P. Kavirayani, New J. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C7NJ04706A

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