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: 1.34). 02/2011; 11(2):1259-66. DOI: 10.1166/jnn.2011.3093
Source: PubMed

ABSTRACT 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.

  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: In this work we developed a nanoformulation for anticancer saponin with chitosan for an enhanced and sustained release. The saponin loaded chitosan nanoparticles showed a particle size of 65±7nm. The synthesized nanoparticles were analyzed by FTIR, TG/DTA, SEM and AFM. The cytotoxicity of the nanoparticles was analyzed on L929, NIH-3T3, KB and PC3 which showed particles are non-toxic in a concentration range of 0.1–1.0mg/ml whereas the nanosaponin showed specific toxicity on PC3 and KB cell lines. The internalization of the nanosaponin on L929 and PC3 was confirmed by Rhodamine conjugation with the nanoparticles. Our preliminary studies support that nanosaponin could be an efficient therapeutic agent for cancer.
    Carbohydrate Polymers 12/2010; 84(1). DOI:10.1016/j.carbpol.2010.11.056 · 4.07 Impact Factor
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: The polyphenol natural product curcumin has been the subject of numerous studies over the past decades, which have identified and characterized the compound's pharmacokinetic, pharmacodynamic, and clinical pharmacological properties. In in vitro and in vivo model systems, curcumin displays potent pharmacological effects, by targeting many critical cellular factors, through a diverse array of mechanisms of action. Despite this tremendous molecular versatility, however, the clinical application of curcumin remains limited due to poor pharma-cokinetic characteristics in human beings. The current trend is to develop and utilize unique delivery systems, chemical derivatives, and chemical analogs to circumvent these pharmaco-logical obstacles, in order to optimize the conditions for curcumin as a chemopreventive and chemotherapeutic agent in diseases such as cancer, diabetes, obesity, Alzheimer's disease, and inflammatory disorders. The present work seeks to review recent studies in the basic pharma-cological principles and potential clinical applications of curcumin.
    01/2011; 2011(1):1-5. DOI:10.2147/BTAT.S17244
  • [Show abstract] [Hide abstract]
    ABSTRACT: The prevalence of obesity, an established risk factor for many cancers, has risen steadily for the past several decades in the United States and in many parts of the world. This review synthesizes the evidence on key biological mechanisms underlying the obesity-cancer link, with particular emphasis on the impact of energy balance modulation, such as diet-induced obesity and calorie restriction, on growth factor signaling pathways and inflammatory processes. Particular attention is placed on the proinflammatory environment associated with the obese state, specifically highlighting the involvement of obesity-associated hormones/growth factors in crosstalk between macrophages, adipocytes, and epithelial cells in many cancers. Understanding the contribution of obesity to growth factor signaling and chronic inflammation provides mechanistic targets for disrupting the obesity-cancer link.
    Annals of the New York Academy of Sciences 07/2011; 1229(1):45-52. DOI:10.1111/j.1749-6632.2011.06096.x · 4.31 Impact Factor
Show more