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c(RGDfK) anchored surface manipulated liposome for tumor-targeted tyrosine kinase inhibitor (TKI) delivery to potentiate liver anticancer activity

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dc.contributor.authorDeepak, Payal
dc.contributor.authorKumar, Praveen
dc.contributor.authorArya, Dilip Kumar
dc.contributor.authorPandey, Prashant
dc.contributor.authorKumar, Shiv
dc.contributor.authorParida, Bishnu Prasad
dc.contributor.authorNarayan, Gopeshwar
dc.contributor.authorSingh, Sanjay
dc.contributor.authorRajinikanth, Paruvathanahalli Siddalingam
dc.date.accessioned2025-01-28T09:41:21Z
dc.date.available2025-01-28T09:41:21Z
dc.date.issued2023
dc.description.abstractCurrent anticancer drug research includes tumor-targeted administration as a critical component because it is the best strategy to boost efficacy and decrease toxicity. Low drug concentration in cancer cells, nonspecific distribution, rapid clearance, multiple drug resistance, severe side effects, and other factors contribute to the disappointing results of traditional chemotherapy. As an innovative technique of treatments for hepatocellular carcinoma (HCC) in recent years, nanocarrier-mediated targeted drug delivery systems can overcome the aforesaid limitations via enhanced permeability and retention effect (EPR) and active targeting. Epidermal growth factor receptor (EGFR) inhibitor Gefitinib (Gefi) has dramatic effects on hepatocellular carcinoma. Herein, we developed and assessed an ?v?3 integrin receptor targeted c(RGDfK) surface modified liposomes for better targeting selectivity and therapeutic efficacy of Gefi on HCC cells. The conventional and modified Gefi loaded liposomes, i.e., denoted as Gefi-L and Gefi-c(RGDfK)-L, respectively, were prepared through the ethanol injection method and optimized via Box Behnken design (BBD). The FTIR and 1H NMR spectroscopy verified that the c(RGDfK) pentapeptides had formed an amide bond with the liposome surface. In addition, the particle size, Polydispersity index, zeta potential, encapsulation efficiency, and in-vitro Gefi release of the Gefi-L and Gefi-c(RGDfK)-L were measured and analyzed. As indicated by the MTT assay on HepG2 cells, Gefi-c(RGDfK)-L displayed considerably higher cytotoxicity than Gefi-L or Gefi alone. Throughout the incubation period, HepG2 cells took up significantly more Gefi-c(RGDfK)-L than Gefi-L. According to the in vivo biodistribution analysis, Gefi-c(RGDfK)-L accumulated more strongly at the tumor site than Gefi-L and free Gefi. Furthermore, HCC-bearing rats treated with Gefi-c(RGDfK)-L showed a substantial drop in liver marker enzymes (alanine transaminase, alkaline phosphatase, aspartate transaminase, and total bilirubin levels) compared to the disease control group. Gefi-c(RGDfK)-L suppresses tumour growth more effectively than Gefi-L and free Gefi, according to an in vivo analysis of their anticancer activities. Thus, c(RGDfK)-surface modified liposomes, i.e., Gefi-c(RGDfK)-L may serve as an efficient carrier for the targeted delivery of anticancer drugs. � 2023 Elsevier B.V.
dc.identifier.doihttps://doi.org/10.1016/j.ijpharm.2023.123160
dc.identifier.issn3785173
dc.identifier.urihttps://dl.bhu.ac.in/ir/handle/123456789/22013
dc.language.isoen
dc.publisherElsevier B.V.
dc.subjectc(RGDfK)-peptide
dc.subjectHepatocellular carcinoma
dc.subjectLiposome
dc.subjectTumor targeting
dc.subject?<sub>v</sub>?<sub>3</sub> integrin receptor
dc.titlec(RGDfK) anchored surface manipulated liposome for tumor-targeted tyrosine kinase inhibitor (TKI) delivery to potentiate liver anticancer activity
dc.typeArticle
dspace.entity.typePublication
journal.titleInternational Journal of Pharmaceutics
journalvolume.identifier.volume642

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2023