Planta Med 2011; 77 - PK15
DOI: 10.1055/s-0031-1282645

Development and evaluation of conventional and PEGylated curcumin liposomes, absorption and tissue distribution studies in mice

F Mazzacuva 1, B Isacchi 1, M Bergonzi 1, S Arrigucci 2, S Fallani 2, A Novelli 2, A Bilia 1
  • 1Department of Pharmaceutical Science, University of Florence, via U. Schiff 6, 50019 Sesto Fiorentino, Florence (Italy)
  • 2Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50139, Firenze, Italy

Curcumin is the main biological active polyphenolic compound present in the rhizomes of turmeric (Curcuma longa Linn.), has a wide biological and pharmacological profile. It has been reported to possess anti-oxidative, anti-inflammatory and anti-carcinogenic properties [1–3]. Many clinical study reports have revealed that curcumin has many beneficial properties in the treatment of various diseases in man such as pancreatic cancer and inflammatory bowel disease [4,5]. Despites these promising effects a poor oral absorption due to its extremely low aqueous solubility and rapid metabolism result in very low oral systemic bioavailability, thus limiting its clinical use. In order to overcome bioavailability drawbacks, this work proposes inclusion of curcumin into liposomal carriers.

Liposomes were prepared by thin layer evaporation technique using phospholipon 90G, cholesterol and PEG-GSPE. Temperature of rehydration of thin film and curcuminamounts were optimized in order to maximise efficiency of entrapment of drug inside the vesicles. Vesicles were characterized by dynamic light scattering and HPLC/DAD. The pharmacokinetic profile was tested in mice after i.p administration using stealth and conventional vesicles and an alcoholic solution of the drug. After two hours administration organs (liver, spleen, intestine, mesentery and lung) were removed and curcumin dosed by HPLC/DAD/MS analysis.

Liposomal inclusion increases bioavailability of curcumin in plasma, in particular, stealth formulation. A different accumulation was found among the different tested formulations. A further advantage of PEGylated liposomes is the high EE% of curcumin in the vesicles (70% compared to 47% of conventional liposomes).

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