SCIENCE@home

Development and evaluation of polymeric nanocapsules for cirsiliol isolated from Jordanian Teucrium polium L. as a potential anticancer nanomedicine

E. Al‐Shalabi,Muzn Alkhaldi,Suhair Sunoqrot

Published 2020 in Journal of Drug Delivery Science and Technology

ABSTRACT

Abstract Cirsiliol (CIR; 5,3′,4′-trihydroxy-6,7-dimethoxyflavone) is an abundant bioactive plant flavonoid which has been shown to exhibit inhibitory activity against phosphatidylinositol-3-kinase (PI3K), an enzyme implicated in many cancer types. Despite its promising therapeutic benefits, CIR has not yet been formulated into any type of dosage form. The purpose of this study was to develop a novel polymeric nanoscale formulation for CIR isolated from Jordanian Teucrium polium L. to enhance its biopharmaceutical properties. CIR was entrapped into core-shell nanoparticles (nanocapsules; NC) composed of a castor oil-filled core and poly(ethylene glycol)-b-poly(e-caprolactone) (PEG-PCL) polymeric shell by the nanoprecipitation technique. Highly monodisperse CIR-encapsulated NC (CIR-NC) were produced with a mean diameter of 158.1 nm and an almost neutral surface charge. CIR-NC contained on average 53.7 μg CIR/mg polymer at an encapsulation efficiency of 53.5%. The NC formulation exhibited remarkable stability with no significant increase in particle size up to 6 months at 4 °C or in the presence of serum. Lyophilization of the formulation in the presence of mannitol as lyoprotectant maintained its colloidal stability. The formulation also demonstrated sustained drug release at pH 7.4, with 41% of CIR released after 4 days. An antioxidant assay showed that the free radical scavenging activity of CIR was maintained after encapsulation. Cytotoxicity assays in MCF-7 breast cancer cells showed dose-dependent cytotoxicity of CIR-NC, with an IC50 of 53 μM, which was comparable to free CIR. Our findings present a promising nanoformulation for a naturally occurring potent anticancer compound with the potential to improve its delivery challenges.

PUBLICATION RECORD

  • Publication year

    2020

  • Venue

    Journal of Drug Delivery Science and Technology

  • Publication date

    2020-04-01

  • Fields of study

    Medicine, Materials Science, Chemistry

  • Identifiers
    DOI 10.1016/j.jddst.2020.101544
  • External record

    Open on Semantic Scholar

  • Source metadata

    Semantic Scholar

CITATION MAP

EXTRACTION MAP

CLAIMS

  • No claims are published for this paper.

CONCEPTS

  • No concepts are published for this paper.

REFERENCES

Showing 1-41 of 41 references · Page 1 of 1

CITED BY

Showing 1-25 of 25 citing papers · Page 1 of 1