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Thymoquinone in liposomes: a study of loading efficiency and biological activity towards breast cancer.

Abstract
Thymoquinone (2-isopropyl-5-methyl-1,4-benzoquinone) is a herbal-derived drug with potential chemopreventive and chemotherapeutic activity. However, thymoquinone suffers from high hydrophobicity causing poor solubility which limits its bioavailability and high lipophilicity causing poor formulation characteristics. Liposomes are versatile drug carriers that can be used to solve problems of drug solubility, instability, and bio-distribution. In this study, we were able to prepare thymoquinone-loaded liposomes (TQ-LP) and thymoquinone loaded in liposomes modified with Triton X-100 (XLP) with diameters of about 100 nm, and entrapment efficiency of more than 90% for TQ-LP and of 49.6% for XLP. The TQ-LP liposomes were effective in suppressing the proliferation of breast cancer cell lines MCF-7 and T47D, and at the same time exerting very low toxicity on normal periodontal ligament fibroblast. Altogether, this report describes the first successful encapsulation of thymoquinone into liposome; which maintains stability, improves bioavailability and maintains its anticancer activity.
AuthorsFadwa Odeh, Said I Ismail, Rana Abu-Dahab, Ismail S Mahmoud, Abeer Al Bawab
JournalDrug delivery (Drug Deliv) Vol. 19 Issue 8 Pg. 371-7 (Nov 2012) ISSN: 1521-0464 [Electronic] England
PMID23043626 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Benzoquinones
  • Drug Carriers
  • Liposomes
  • Octoxynol
  • thymoquinone
Topics
  • Antineoplastic Agents, Phytogenic (administration & dosage, chemistry, pharmacology, toxicity)
  • Benzoquinones (administration & dosage, chemistry, pharmacology, toxicity)
  • Breast Neoplasms (pathology)
  • Calorimetry, Differential Scanning
  • Cell Culture Techniques
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Drug Carriers (chemistry)
  • Drug Compounding
  • Drug Stability
  • Female
  • Fibroblasts (drug effects)
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Liposomes
  • Male
  • Microscopy, Electron, Scanning
  • Microscopy, Electron, Transmission
  • Molecular Structure
  • Octoxynol (chemistry)
  • Particle Size
  • Solubility
  • Surface Properties

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