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Synthesis, characterization and evaluation of pegylated-citric acid based dendrimers as drug delivery agents

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Abstract

In the present study, four different types of fourth-generation pegylated citric acid based dendrimers namely PE/TMP-MC-PEG-CA-PEG and PE/TMP-MS-PEG-CA-PEG were synthesized. The dendrimers were further conjugated with cefotaxime (CFTX) sodium drug. The structures of these dendrimers and drug-dendrimer conjugates were confirmed by using 1H-NMR, 13C-NMR, and FTIR spectroscopy. The confirmation of particle size, surface topography and structure of drug-dendrimer conjugates was done using Zeta sizer, AFM, and HR-TEM techniques. Cytotoxicity investigation revealed that the CFTX-encapsulated dendrimers are safe against normal epithelial cells and showed 20–22% anticancer activity against A549 Lung carcinoma cells; besides that, the synthesized dendrimers and drug-dendrimer conjugates also showed 15–28% and 2–3% hemolytic toxicity, respectively, against red blood cells (RBC). The antibacterial activity of all synthesized third and fourth generation drug-dendrimer conjugates were investigated on Gram-positive and Gram-negative bacteria. The results show that drug conjugate with third generation dendrimers depicted a greater effective zone of inhibition (ZOI) as compared to fourth generation drug-dendrimer conjugates against these pathogenic bacteria.

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Acknowledgements

The authors are grateful to Ministry of Human Resource Development (MHRD), India, National Institute of Technology Hamirpur, Himachal Pradesh, India, for funding the research and RK Government Medical College Hamirpur for providing fresh human blood to perform the hemolytic toxicity of drug-dendrimer conjugates.

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Authors and Affiliations

  1. Department of Chemistry, National Institute of Technology, Hamirpur, Himachal Pradesh, 177005, India

    Avtar Chand & Bharti Gaur

  2. Pharmacology and Toxicology Lab, Dietetics and Nutrition Technology Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh, 176061, India

    Smita Kapoor

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  1. Avtar Chand
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Correspondence to Bharti Gaur.

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Chand, A., Gaur, B. & Kapoor, S. Synthesis, characterization and evaluation of pegylated-citric acid based dendrimers as drug delivery agents. J Polym Res 31, 61 (2024). https://doi.org/10.1007/s10965-024-03908-6

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