Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery

Hari Krishnareddy Rachamalla, Santanu Bhattacharya, Ajaz Ahmad, Kathyayani Sridharan, Vijay Sagar Madamsetty, Sujan Kumar Mondal, Enfeng Wang, Shamit K. Dutta, Basit L. Jan, Sudhakar Jinka, Madan Mohan Chandra Sekhar Jaggarapu, Venu Yakati, Debabrata Mukhopadhyay, Khalid M. Alkharfy, Rajkumar Banerjee

Research output: Contribution to journalArticlepeer-review

Abstract

Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.

Original languageEnglish (US)
Pages (from-to)641-656
Number of pages16
JournalNanomedicine
Volume16
Issue number8
DOIs
StatePublished - Apr 2021

Keywords

  • cationic lipid
  • liposomes
  • pancreatic cancer
  • pharmacokinetic evaluation
  • thymoquinone

ASJC Scopus subject areas

  • Bioengineering
  • Medicine (miscellaneous)
  • Biomedical Engineering
  • Materials Science(all)

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