Thymoquinone-loaded soy-phospholipid-based phytosomes exhibit anticancer potential against human lung cancer cells

Nabil A. Alhakamy, Shaimaa M. Badr-Eldin, Usama A. Fahmy, Nabil K. Alruwaili, Zuhier A. Awan, Giuseppe Caruso, Mohamed A. Alfaleh, Ahmed L. Alaofi, Faris O. Arif, Osama A.A. Ahmed, Adel F. Alghaith

Research output: Contribution to journalArticlepeer-review

Abstract

Thymoquinone (TQ), a natural polyphenol, has been associated with various pharmacological responses; however, low bioavailability of TQ limits its clinical application. Thus, a novel phytosomal delivery system of TQ-Phospholipon® 90H complex (TQ-phytosome) was developed by refluxing combined with anti-solvent precipitation. This TQ delivery system was optimized by a three-factor, three-level Box-Behnken design. The optimized TQ-phytosome size was (45.59 ± 1.82 nm) and the vesicle size was confirmed by transmission electron microscopy. The in vitro release pattern of the formulation indicated a biphasic release pattern, where an initial burst release was observed within 2 h, followed by a prolonged release. A remarkable increase in dose-dependent cytotoxicity was evident from the significant decrease in IC50 value of TQ-phytosomes (4.31 ± 2.21 µM) against the A549 cell line. The differential effect of TQ-phytosomes in cell cycle analysis was observed, where cancer cells were accumulated on G2-M and pre-G1 phases. Furthermore, increased apoptotic induction and cell necrosis of TQ-phytosomes were revealed with the annexin V staining technique via activation of caspase-3. In reactive oxygen species (ROS) analysis, TQ-phytosomes acted to significantly increase ROS generation in A549 cells. In conclusion, the sustained release profile with significantly-improved anticancer potential could be obtained with TQ by this phytosomal nanocarrier platform.

Original languageEnglish
Article number761
Pages (from-to)1-17
Number of pages17
JournalPharmaceutics
Volume12
Issue number8
DOIs
Publication statusPublished - Aug 2020

Keywords

  • Apoptotic potential
  • Biphasic release
  • Box-Behnken design
  • Cell cycle arrest
  • Cytotoxicity
  • ROS generation
  • Thymoquinone

ASJC Scopus subject areas

  • Pharmaceutical Science

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