Curcumin solid dispersion based on three model acrylic polymers: formulation and release properties

Abstract To investigate structure-property relationship of polymer-based curcumin solid dispersion (SD), three acrylic polymers were used to formulate curcumin SD by solvent evaporation method. Curcumin Eudragit EPO SD (cur@EPO), curcumin Eudragit RS PO SD (cur@RSPO) and curcumin Eudragit RL PO SD (cur@RLPO) showed deep red, golden orange and reddish orange color, respectively. Cur@RSPO entrapped 15.42 wt% of curcumin followed by cur@RL PO and cur@EPO. FTIR spectra indicated that in cur@EPO, curcumin may transfer hydrogen to the dimethylaminoethyl methacrylate group and thus change its color to red. In contrast, curcumin may form hydrogen bonding with Eudragit RS PO and Eudragit RL. Curcumin exists in amorphous state in three SDs as proved by differential scanning calorimetry and X-Ray diffraction measurement. In vitro digestion presented that lower pH value in simulated gastric fluid (SGF) stimulates the curcumin release from cur@EPO while permeability influences the release profile in other two SDs. When in simulated intestinal fluid (SIF), first order release model governs the release behaviors of all three SDs which showed sustained release pattern. Our results are helpful to elucidate how structure of polymer may impact on the major properties of curcumin contained SD and will be promising to broaden its therapeutic applications.

Curcuma longa extract protects against 5-fluorouracil-induced oral mucositis in hamsters

Abstract Curcumin, contained at Turmeric (Curcumalonga), can exert many beneficial pleiotropic activities in the gastrointestinal tract. This study evaluated the antioxidant and anti-inflammatory activity of C. longa on 5-fluorouracil (5-FU)-induced oral mucositis (OM) in hamsters. Phytochemical analysis of crude C. longa extract (CLE) was performed to detect the presence of curcumin by TLC and HPLC. Golden Syrian hamsters were orally pre-treated with CLE (5, 50, or 100mg/kg). Cheek pouch samples were subjected to macroscopic and histopathological evaluation. ELISA was performed to quantify the inflammatory cytokines IL-1ß and TNF-α. Superoxide dismutase (SOD), glutathione (GSH) and malondialdehyde (MDA) levels were assessed by ultraviolet-visible spectroscopy analysis. Behavior analysis was conducted by the open field test. Curcumin content in the CLE was 0.55%m/m ± 0.0161 (2.84%). The group treated with 5mg/kg CLE showed healing evidence with macroscopic absence of ulceration (p<0.05) and microscopic aspect of re-epithelialization, discrete inflammatory infiltrate and absence of edema. Treatment with 5mg/kg CLE significantly increased GSH levels, and reduced MDA levels and SOD activity (p˂0.05), and decreased IL-1ß (p˂0.05) and TNF-α (p˂0.01) levels. A significant reduction in walking distance, ambulation, speed, and rearing was observed for motor activity. Curcumin reduced oxidative stress, inflammation, and motor activity in hamsters with 5-FU-induced OM.

Propriedades e usos da cúrcuma / Properties and uses of turmeric / Propiedades y usos de la cúrcuma

A Cúrcuma (Curcuma longa) é uma planta originária do sudoeste asiático, que faz parte da família Zingiberaceae. É uma erva amarga, adstringente, com cheiro característico e forte cor amarela e que cujas raízes (rizomas) secas e maceradas têm sido utilizadas atualmente como corante e condimento para carnes e vegetais. O principal composto bioativo da cúrcuma é a curcumina, que se encontra em percentuais de dois a cinco por cento em suas raízes, sendo também é responsável pela sua coloração. Sabendo-se das suas propriedades bioativas e de várias que ainda estão sendo testadas, esse trabalho objetivou apresentar as principais propriedades e usos da cúrcuma. Historicamente a cúrcuma é empregada em diversos medicamentos utilizados pela medicina Ayurveda (sistema medicinal característico da Índia Antiga). Quimicamente é um pó insolúvel na água e no éter etílico, mas solúvel no etanol e acetona, é um diferoilmetano com a fórmula C21H20O6 e peso molecular 368,4. Muitos trabalhos estão sendo produzidos ultimamente buscando entender o funcionamento metabólico da curcumina e suas possíveis atividades biológicas. Entre as propriedades já estudadas destacam-se as capacidades anticoagulante, antifúngica, anti-inflamatória, antimalárica, antioxidante, antiviral, cicatrizante, esquistossomicida, hipolipemiante, leishmanicida, nematocida, tripanocida neuroprotetora, anti-amiloidogênica e imunomoduladora. A curcumina possui a vantagem de ser uma molécula de fácil acesso, uma vez que pode ser adquirida como condimento doméstico em todo o mundo e possui variadas aplicações, porém devido a sua baixa biodisponibilidade, baixa solubilidade em água e alta afinidade pelas proteínas plasmáticas faz-se necessário que novos estudos sejam realizados para que ela possa ser empregada efetivamente como um bioativo vegetal.(AU)

Turmeric (Curcuma longa) is a plant originated from Southeast Asia; it belongs to the Zingiberaceae family. It is a bitter, astringent herb, with a characteristic smell and strong yellow color. Its dried and macerated roots (rhizomes) have been used as coloring and condiment for meat and vegetables. Turmeric main bioactive compound is curcumin, which is found at concentrations of approximately two to five percent on its roots, being also responsible for its coloration. With the knowledge of its bioactive properties and of several other properties that are still being tested, this paper aimed at presenting the main properties and uses of turmeric. Turmeric has historically been used in various medicines by Ayurveda medicine (a medicinal system characteristic of ancient India). Chemically, it is a powder insoluble in either water or ethyl ether, despite being soluble in ethanol and acetone. It is a difoylmethane of formula C21H20O6 and molecular weight 368.4. Many works are being produced seeking to understand the metabolic functioning of curcumin and its possible biological activities. Among the properties already studied, it has proven anticoagulant, antifungal, anti-inflammatory, antimalarial, antioxidant, antiviral, scarring, schistosomicide, hypolipidemic, leishmanicidal, nematocidal, trypanocidal neuroprotective, anti-amyloidogenic and immunomodulatory capacities. Curcumin has the advantage of being an easily accessible molecule as it can be purchased as a domestic condiment worldwide and is widely applied in several cuisines. However, due to its low bioavailability, low water solubility and high affinity for plasma proteins, further studies should be carried out so that it can be effectively employed as a plant bioactive.(AU)

La cúrcuma (Curcuma longa) es una planta originaria del sudeste asiático, pertenece a la familia Zingiberaceae. Es una hierba amarga y astringente, con un olor característico y un fuerte color amarillo y cuyas raíces (rizomas) secas y maceradas se utilizan actualmente como colorante y condimento para carnes y vegetales. El principal compuesto bioactivo de la cúrcuma es la curcumina, que se encuentra cerca del dos al cinco por ciento de sus raíces y también es responsable por su coloración. Debido a sus propiedades bioactivas y de varias que aún se están probando, ese estudio tuvo como objetivo presentar las principales propiedades y usos de la cúrcuma. Históricamente, la cúrcuma es empleada en varias medicinas utilizadas por la medicina Ayurveda (sistema medicinal característico de la antigua India). Químicamente es un polvo insoluble en agua y éter etílico, pero soluble en etanol y acetona, es un diferoilmetano de fórmula C21H20O6 y peso molecular 368.4. Últimamente se están produciendo muchos trabajos que buscan comprender el funcionamiento metabólico de la curcumina y sus posibles actividades biológicas. Entre las propiedades ya estudiadas se encuentran las capacidades anticoagulante, antifúngica, antiinflamatoria, antipalúdica, antioxidante, antiviral, cicatrizante, esquistosomicida, hipolipidémica, leishmanicida, nematocida, tripanocida, neuroprotectora, antiamiloidogénica e inmunomoduladora. La curcumina tiene la ventaja de ser una molécula de fácil acceso, ya que se puede comprar como condimento doméstico en todo el mundo y tiene una variedad de aplicaciones, pero debido a su baja biodisponibilidad, baja solubilidad en agua y alta afinidad por las proteínas plasmáticas se hace necesario que nuevos estudios sean llevados a cabo para que ella pueda ser empleada efectivamente como planta bioactiva.(AU)

Molecular docking, synthesis and in vitro antimalarial evaluation of certain novel curcumin analogues

ABSTRACT The receptor protein PfATP6 has been identified as the common target of artemisinin and curcumin. The work was initiated to assess the antimalarial activity of six curcumin derivatives based on their binding affinities and correlating the in silico docking outcome with in vitro antimalarial screening results. A ligand library of thirty two Knoevenagel condensates of curcumin were designed and docked against PfATP6 protein and six compounds with the best binding scores were synthesized and screened for their antimalarial activity against the sensitive 3D7 strain of Plasmodium falciparum. ADME/Tox, pharmacokinetic and pharmacodynamic profiles of the designed compounds were analyzed and reported. 4-FB was found to have similar binding energy to the standard artemisinin (-6.75 and -6.73 respectively) while 4-MB, 3-HB, 2-HB, B, 4-NB displayed better binding energy than curcumin (-5.95, -5.89, -5.68, -5.35, -5.29 and -5.25 respectively). At a dose of 50 µg/mL all the six compounds showed 100% schizont inhibition while at 5µg/ml, five showed more than 75% inhibition and better results than curcumin. 4-FB showed the best activity with 97.8% schizonticidal activity. The in vitro results superimpose the results obtained from the in silico study thereby encouraging development of promising curcumin leads in the battle against malaria.

Evaluation of polymeric PLGA nanoparticles conjugated to curcumin for use in aPDT

ABSTRACT Antimicrobial photodynamic therapy (aPDT) involves the association of a photosensitizing agent with a light source with the goal of causing apoptosis or microbial lysing. The use of compounds with natural active principles is gaining prominence throughout the world. Several studies from groups that are linked to the development of innovations in the pharmaceutical market have used natural dyes, such as curcumin, the efficacy of which has been demonstrated in aPDT trials. Difficulties related to physicochemical stability, solubility and cell penetration are some of the challenges associated with this field. The present work aimed to prepare, investigate the characteristics and improve the photodynamic activity of PLGA-based nanoparticles loaded with curcumin for use in aPDT therapy. Using the simple technique of emulsion during the evaporation of a solvent, the particles were built, characterized and tested against microorganisms with importance for medicine and dentistry. The results revealed that the particles were able to protect the curcumin against degradation and eliminate some microorganism species at nanomolar concentrations.

La prevención química del cáncer / The chemoprevention of cancer

El objetivo de este trabajo fue evaluar el concepto, la situación actual y las perspectivas en la prevención química del cáncer. Para dicho análisis se consideraron los mecanismos involucrados en el proceso, las características que requieren los compuestos para ubicarlos en estudios preclínicos y clínicos, y el estado actual en que se encuentran agentes como los retinoides, carotenoides, calcio, ácido alérgico y fumárico, curcumino y aspirina. La información sugiere que la estrategia planteada tiene bases sólidas y que en un futuro cercano se verán efectos positivos en el hombre