RESUMEN
Current anticancer drugs exhibit limited efficacy and initiate severe side effects. As such, identifying bioactive anticancer agents that can surpass these limitations is a necessity. One such agent, curcumin, is a polyphenolic compound derived from turmeric, and has been widely investigated for its potential anti-inflammatory and anticancer effects over the last 40 years. However, the poor bioavailability of curcumin, caused by its low absorption, limits its clinical use. In order to solve this issue, in this study, curcumin was encapsulated in chitosan-coated nanoliposomes derived from three natural lecithin sources. Liposomal formulations were all in the nanometric scale (around 120 nm) and negatively charged (around -40 mV). Among the three lecithins, salmon lecithin presented the highest growth-inhibitory effect on MCF-7 cells (two times lower growth than the control group for 12 µM of curcumin and four times lower for 20 µM of curcumin). The soya and rapeseed lecithins showed a similar growth-inhibitory effect on the tumor cells. Moreover, coating nanoliposomes with chitosan enabled a higher loading efficiency of curcumin (88% for coated liposomes compared to 65% for the non-coated liposomes) and a stronger growth-inhibitory effect on MCF-7 breast cancer cells.
Asunto(s)
Antineoplásicos/farmacología , Curcumina/farmacología , Composición de Medicamentos/métodos , Sistemas de Liberación de Medicamentos/métodos , Liposomas/farmacología , Animales , Disponibilidad Biológica , Brassica rapa , Neoplasias de la Mama/tratamiento farmacológico , Quitosano , Portadores de Fármacos , Femenino , Humanos , Lecitinas , Células MCF-7 , Nanopartículas , Salmón , Células Tumorales Cultivadas/efectos de los fármacosRESUMEN
The aim of our study was to elaborate a resistant liposome that can be used in cosmetic formulations containing high amounts of surfactants and electrolytes. The stability of liposomes was increased via hydrophobized polysaccharide (Stearoyl Inulin) by anchoring its stearic acid tail into liposome bilayer. Coated and noncoated liposomes were prepared under the same conditions and their morphology, size, and resistance to surfactants and electrolytes were evaluated. We established that coated lipbsomes were more resistant to surfactants and electrolytes. It seems that a coating of polysaccharides prevents liposome destabilization in the presence of high amounts of surfactants and electrolytes. Moreover, the ability of coated liposomes to improve the skin delivery of active molecules was evaluated. Coated liposomes increased the efficacy of magnesium chloride by improving its skin availability.
Asunto(s)
Cosméticos , Liposomas , Polisacáridos/química , Técnica de Fractura por Congelación , Interacciones Hidrofóbicas e HidrofílicasRESUMEN
A phospholipopeptidic complex obtained by the enzymatic hydrolysis of salmon heads in green conditions; exert anxiolytic-like effects in a time and dose-dependent manner, with no affection of locomotor activity. This study focused on the physico-chemical properties of the lipidic and peptidic fractions from this natural product. The characterization of mineral composition, amino acid and fatty acids was carried out. Stability of nanoemulsions allowed us to realize a behavioral study conducted with four different tests on 80 mice. This work highlighted the dose dependent effects of the natural complex and its various fractions over a period of 14 days compared to a conventional anxiolytic. The intracellular redox status of neural cells was evaluated in order to determine the free radicals scavenging potential of these products in the central nervous system (CNS), after mice sacrifice. The complex peptidic fraction showed a strong scavenging property and similar results were found for the complex as well as its lipidic fraction. For the first time, the results of this study showed the anxiolytic-like and neuroprotective properties of a phospholipopeptidic complex extracted from salmon head. The applications on anxiety disorders might be relevant, depending on the doses, the fraction used and the chronicity of the supplementation.
Asunto(s)
Ansiolíticos/farmacología , Ácidos Grasos Insaturados/farmacología , Ácidos Grasos/farmacología , Péptidos/farmacología , Salmón/metabolismo , Aminoácidos/química , Aminoácidos/metabolismo , Animales , Ansiolíticos/química , Sistema Nervioso Central/efectos de los fármacos , Ácidos Grasos/química , Ácidos Grasos Insaturados/química , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Lípidos/química , Ratones , Fármacos Neuroprotectores/química , Fármacos Neuroprotectores/farmacología , Oxidación-Reducción/efectos de los fármacos , Péptidos/químicaRESUMEN
Coenzyme Q(10) (CoQ(10)) is an insoluble antioxidant molecule with great biological value but exhibit poor bioavailability. To improve the bioavailability of CoQ(10), we have proposed to formulate a nanoemulsion consisting of salmon oil, salmon lecithin, CoQ(10) and water. A commercial oily mixture, based on soybean oil and CoQ(10), was used for comparison, as well as a second oily mixture, composed of salmon lecithin, salmon oil and CoQ(10). Salmon oil and salmon lecithin were used as sources of polyunsaturated fatty acids (PUFA). The maximum solubility of CoQ(10) in salmon oil was 81.30 ± 0.08 mg/mL at 37 °C. Mean droplets size of the control and CoQ(10) nanoemulsions was 164 and 167 nm, respectively. The nanoemulsion was stable during 30 days at 25 °C. Bioavailability was evaluated as the area under the curve of CoQ(10) plasma concentration in male Wistar rats following oral administration of the three formulations of CoQ(10). The nanoemulsion increases at twice the bioavailability of CoQ(10) than conventional oily formulations regardless the nature of used fatty acids (soybean and salmon oils). Prepared nanoemulsion represents a vectorization of both LC-PUFAs and CoQ(10). That could be an interesting way to increase the absorption of these two bioactive molecules with natural low availability.
Asunto(s)
Antioxidantes/administración & dosificación , Portadores de Fármacos/administración & dosificación , Aceites de Pescado/administración & dosificación , Lecitinas/administración & dosificación , Ubiquinona/análogos & derivados , Animales , Antioxidantes/química , Antioxidantes/farmacocinética , Área Bajo la Curva , Química Farmacéutica , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Emulsiones , Ácidos Grasos/análisis , Aceites de Pescado/química , Aceites de Pescado/farmacocinética , Lecitinas/química , Lecitinas/farmacocinética , Masculino , Nanoestructuras/administración & dosificación , Nanoestructuras/química , Ratas , Ratas Wistar , Solubilidad , Ubiquinona/administración & dosificación , Ubiquinona/química , Ubiquinona/farmacocinéticaRESUMEN
Health benefits of unsaturated fatty acids have been demonstrated over the last decades. Nanotechnology provided new process to produce particles such as liposomes and nanoliposomes made of pure phospholipids. These techniques are already used in pharmaceutics to augment the bioavailability and the bioefficiency of drugs. The aim of this paper is to characterize and evaluate the potential of nanoliposomes made of three lecithins (soya, rapeseed and salmon) on cell culture in order to use them in the future as drug delivery systems for tissue engineering. We began to measure, with zetasizer, the radius size of liposomes particles which are 125.5, 136.7 and 130.3 nm respectively for rapeseed, soya and salmon lecithin. Simultaneously, solutions observed by TEM demonstrated the particles were made much of liposomes than droplet (emulsion). Finally, we found that the solutions of lecithins were enough stable over 5 days at 37 °C to be used in culture medium. We investigated the effect of soya, rapeseed and salmon lecithin liposome from 2mg/mL to 5.2 µg/mL on metabolic activity and cell proliferation on rat bone marrow stem cells (rBMSC) during 14 days. The results showed that the three lecithins (soya, rapeseed and salmon) improve cell proliferation at different concentration.
Asunto(s)
Células de la Médula Ósea/efectos de los fármacos , Brassica rapa/química , Lecitinas/farmacología , Liposomas/farmacología , Nanopartículas/química , Salmón , Aceite de Soja/farmacología , Animales , Células de la Médula Ósea/citología , Técnicas de Cultivo de Célula , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Relación Dosis-Respuesta a Droga , Sistemas de Liberación de Medicamentos , Lecitinas/química , Liposomas/química , Masculino , Tamaño de la Partícula , Ratas , Ratas Wistar , Aceite de Soja/química , Relación Estructura-Actividad , Propiedades de SuperficieRESUMEN
BACKGROUND: Nano-emulsions, as non-equilibrium systems, present characteristics and properties which depend not only on composition but also on their method of preparation. To obtain better penetration, nanocosmeceuticals use nano-sized systems for the delivery of active ingredients to targeted cells. In this work, nano-emulsions composed of miglyol, rapeseed oil and salmon oil were developed as a cosmetic matrix. Measurements of different physico-chemical properties of nano-emulsions were taken according to size, electrophoretic mobility, conductivity, viscosity, turbidity, cristallization and melting point. The RHLB was calculated for each formulation in order to achieve maximum stability. RESULTS: Both tween 80 and soya lecithin were found to stabilize formulations. The results showed that rapeseed oil and miglyol are the predominant parameters for determining the expression of results concerning the characterization of emulsion. Based on the mixture design, we achieved the optimal point using the following formulation: 56.5% rapessed oil, 35.5% miglyol, and 8% salmon oil. We considered this formulation to be the best as a nanocosmeceutical product due to the small size, good turbidity, and average HLB. CONCLUSIONS: This study demonstrates the influence of formulation on the physico-chemical properties of each nano-emulsion obtained by the mixture design.