Synthesis and characterization of novel amphiphilic peptide and its application in development of niosomal formulation as a drug delivery carrier for curcumin Humira Karim 1,2 , Khadija Rehman 1 , Sadiq Noor Khan 1,2 , Ali Asgher Shuja 1 , Tasmina Kanwal 1 , Shabana Usman Simjee 1,3 , Muhammad Raza Shah 1 , and Farzana Shaheen 1.2 1 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, Karachi University, Pakistan, 2 Third World Center for Science and Technology, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan, 3 Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan The efficacy of curcumin (CR) against different types of cancers is significantly impeded by its non-specificity, low aqueous solubility, and high metabolism. In the current study, the ability of a new amphiphilic peptide (AMP) to deliver CR into cancer cells via niosomal vesicles was investigated. Several methods, including FAB-MS, HRFAB-MS, 1 H- and 13 C-NMR spectroscopy, were employed to analyze the synthesized AMP before it was used to formulate niosomal vesicles. Zeta potential, size, PDI, and morphological studies were used to characterize CR-loaded AMP niosomal vesicles (CR-AMP-Vesicles). CR-AMP-Vesicles exhibited a smaller size of about 387.7 ±1.76 nm with 77 ±2.10% CR encapsulation and a regulated drug release profile. Moreover, the cytotoxicity of produced vesicles on human normal fibroblast 3T3 cells was performed and found to be non-cytotoxic. When tested on a chronic myeloid leukemia cell line, CR-AMP-Vesicles and CR showed 51% and 54% inhibition, respectively with the IC 50 of 25 µM. Hence, it is concluded that the newly developed novel CR-AMP-Vesicles have the potential to substantially reduce the cytotoxicity of bioactive compounds against normal cells. References 1. Aggarwal, B.B., Kumar, A., Bharti, A.C., 2003. Anticancer potential of curcumin: preclinical and clinical studies. Anticancer research 23, 363-398.Dutta, A.K., Ikiki, E., 2013. Novel drug delivery systems to improve bioavailability of curcumin. J Bioequiv Availab 6, 001-009. 2. Zhao, C., Chen, H., Wang, F., Zhang, X., 2021. Amphiphilic self-assembly peptides: Rational strategies to design and delivery for drugs in biomedical applications. Colloids and Surfaces B: Biointerfaces 208, 112040. 3. Imran, M., Shah, M.R., Ullah, F., Ullah, S., Elhissi, A.M., Nawaz, W., Ahmad, F., Sadiq, A., Ali, I., 2016b. Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin. Drug Delivery 23, 3653-3664.
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