Open AccessEnriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery
Author(s) -
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
Publication year - 2021
Publication title -
nanomedicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.947
H-Index - 109
eISSN - 1748-6963
pISSN - 1743-5889
DOI - 10.2217/nnm-2020-0470
Subject(s) - thymoquinone , bioavailability , pharmacokinetics , pharmacology , in vivo , liposome , chemistry , pancreatic cancer , medicine , cancer , biochemistry , microbiology and biotechnology , biology , antioxidant
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.