Preparation and Characterization of Lyophilised EGG PC Liposomes Incorporating Curcumin and Evaluation of Its Activity Against Colorectal Cancer Cell Lines

School of Pharmacy, Department of Pharmaceutical Technology, University of Athens, 15771, Greece.
Journal of Nanoscience and Nanotechnology (Impact Factor: 1.56). 02/2011; 11(2):1259-66. DOI: 10.1166/jnn.2011.3093
Source: PubMed


Curcumin has been associated with the treatment of various diseases in traditional medicine, among them cancer. The major problems that prevent its approval as therapeutic agent are its low water solubility and its relatively low in vivo bioavailability. Liposomes are considered as effective drug carriers because of their ability to solubilize hydrophobic compounds and to alter their pharmacokinetic properties. The purpose of this study was the development of lyophilised liposomal curcumin fully characterized in terms of its physical properties [(zeta-potential, size, size distribution and Polydispercity index (PI)], and to evaluate its in vitro cytotoxic against colorectal cancer cell lines in a short-term and in a long-term (clonogenic) assay. Curcumin was incorporated in egg-phosphatidylcholine (EPC) liposomes at a drug to lipid molar ratio 1:14 achieving high incorporation efficiency close to 85%. The liposomal curcumin was lyophilized preserving thus its stability. The reconstitution of the formulation resulted in the original liposomal suspension. The release in FBS showed a plateau near 14% at 96 hours of incubation. The in vitro studies against colorectal cancer cell lines have shown that liposomes improve the activity of curcumin especially in the long-term assay and the liposomal formulation found to be more potent against HCT116 and HCT15, cell lines which express the MDR phenotype. EPC liposomal curcumin in a molar ratio of curcumin/EPC 1:14 has shown improved cytotoxic activity versus free curcumin against colorectal cancer cell lines. In vivo studies based on the recent findings are in progress in our laboratory.

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    • "Dipeptide nanoparticle of curcumin inhibits tumor growth in mice [87]. Phosphatidylcholine encapsulated curcumin exhibits antimalarial activity [88], inhibits vaginal inflammation [116] and induce cytotoxicity of cancer cells [81]. There are several other cucrumin formulation are synthesized having more biological activities than curcumin. "
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    • "We have developed a nano-sized liposomal formulation with a narrow polydispersity, and achieved a high D/L mole ratio of 0.181 using EggPC liposomes. While a similar, high D/L, mole ratio for other lipophilic drugs such as paclitaxel (0.15),17 aryl-imidazole compound (ML220) (0.29),18 and curcumin (0.07)19 have been reported, the D/L mole ratio for other hydrophobic drugs such as ibuprofen (0.02)20 and cisplatin (0.05) were low.21 We previously achieved a maximum D/L mole ratio of 0.104 using DPPC liposomes, synthesized from a saturated lipid that maintained an IOP lowering effect for 50 days in the rabbit eyes.16 "
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