title: 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.
authors.affiliation: Department of Chemistry, University of Jordan, Amman, Jordan. F.Odeh@ju.edu.jo
authors.forename: Fadwa
authors.initials: F
authors.lastname: Odeh
authors.forename: Said I
authors.initials: SI
authors.lastname: Ismail
authors.forename: Rana
authors.initials: R
authors.lastname: Abu-Dahab
authors.forename: Ismail S
authors.initials: IS
authors.lastname: Mahmoud
authors.forename: Abeer
authors.initials: A
authors.lastname: Al Bawab
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D016227:Benzoquinones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001943:Breast Neoplasms / Q000473:pathology; D002152:Calorimetry, Differential Scanning; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004355:Drug Stability; D005260:Female; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes; D008297:Male; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D017830:Octoxynol / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013499:Surface Properties
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D016227:Benzoquinones; D004337:Drug Carriers; D008081:Liposomes; D017830:Octoxynol; C003466:thymoquinone