933 ISSN 0326-2383 KEY WORDS: Curcumin, Drug delivery systems, Nanocapsules. * Author to whom correspondence should be addressed. E-mail: lemos@ccs.ufsc.br Latin American Journal of Pharmacy (formerly Acta Farmacéutica Bonaerense) Lat. Am. J. Pharm. 29 (6): 933-40 (2010) Original Article Received: June 14, 2009 Accepted: January 26, 2010 Curcumin-Loaded Polymeric and Lipid Nanocapsules: Preparation, Characterization and Chemical Stability Evaluation Letícia MAZZARINO 1 , Cristiana L. DORA 1 , Ismael C. BELLETTINI 2 , Edson MINATTI 2 , Simone G. CARDOSO 1 & Elenara LEMOS-SENNA 1 * 1 Departamento de Ciências Farmacêuticas, 2 Departamento de Química,Universidade Federal de Santa Catarina, Campus Universitário Trindade, 88040-900,Florianópolis, Brazil. SUMMARY. Polymeric and lipid nanocapsules suspensions of the natural compound curcumin were pre- pared in order to overcome limitations associated with its clinical applications, such as poor aqueous solu- bility and susceptibility to hydrolytic and photochemical degradation. Nanocapsule suspensions were pre- pared by nanoprecipitation and phase inversion methods, respectively. The curcumin formulations were investigated for physicochemical characteristics and in vitro drug release. The hydrolytic and photochemi- cal degradation of the drug associated with the nanocarriers was also determined. For all formulations, the entrapment efficiency values were higher than 99 %. The aqueous colloidal suspensions of curcumin resulted in an increase in drug concentration by a factor of up to 46.10 3 times. Moreover, stability studies indicated that nanoencapsulation slows down the hydrolytic and photochemical degradations of curcumin. The strategy of nanoencapsulation into polymeric and lipid nanocapsules produced a formulation of cur- cumin with high drug loading and improved stability, representing a good strategy for the delivery of this drug. INTRODUCTION Curcumin or diferuloylmethane is a low- molecular weight polyphenol extracted from the rhizome of the Curcuma longa herb, which ex- hibits a variety of biological activities and phar- macological properties such as anti-tumor, anti- inflammatory, antimicrobial, anti-oxidant, hep- atoprotective, thrombosupressive, hypo- glycemic, and antiarthritic activities 1 . In fact, mounting evidence indicate that curcumin has a wide range of molecular targets, which supports the notion that this drug influences numerous biochemical and molecular cascades. Among its molecular targets are transcription factors, growth factors and their receptors, cytokines, enzymes, and genes that regulate cell prolifera- tion and apoptosis. Pre-clinical studies have demonstrated curcumin is able to suppress the tumorigenic activity of a variety of carcinogens in several kinds of cancers, is able to inhibit the proliferation of an extremely wide array of can- cer cell types in vitro, and also displays anti-tu- mor activity in various animal models in vivo. Furthermore, clinical trials have suggested cur- cumin as a potential therapeutic agent in several diseases such as inflammatory bowel disease, ulcerative colitis, colon cancer, pancreatic can- cer, atherosclerosis, and others 2 . Despite of the potential use of curcumin in the prevention and treatment of cancer and oth- er diseases, its clinical application has been lim- ited due to several drawbacks. Curcumin ex- hibits extremely poor water solubility, which re- sults in low absorption of this drug by the gas- trointestinal tract and precludes the preparation of aqueous solutions for intravenous administra- tion 3,4 . When administered orally, most of the ingested curcumin is excreted in the feces and though no detectable amount of curcumin was found in urine some of its derivates like cur- cumin glucuronide and sulfates were observed, indicating that this drug undergoes fast metabo-