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Original Article

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

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Pages 371-377 | Received 20 Jun 2012, Accepted 03 Sep 2012, Published online: 08 Oct 2012
 

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.

Acknowledgments

We would like to thank Haifa Hattab, for her valuable help in sample preparation and TEM imaging. We also thank Wadah Faris for his valuable help in SEM imaging. All thanks are also given to Ayat Bozeya for her tremendous help in HPLC optimization and valuable discussions and suggestions.

Declaration of interest

The authors report no conflict of interest.

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