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1.
Curr Drug Metab ; 21(3): 226-234, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32348213

RESUMEN

BACKGROUND: Cancer is one of the main causes of death by disease; several alternative treatments have been developed to counteract this condition. Curcumin (diferuloylmethane), extracted from the rhizome of Curcuma longa, has antioxidant, anti-inflammatory, and anti-cancer properties; however, it has low water solubility and poor intestinal absorption. Carrier systems, such as nanoemulsions, can increase the bioavailability of lipophilic bioactive compounds. OBJECTIVE: To evaluate the effect of curcumin nanoemulsions prepared with lecithin modified with medium-chain fatty acids as an emulsifier, on the expression of the Cdk4, Ccne2, Casp8 and Cldn4 genes involved in the carcinogenesis process in K14E6 transgenic mice. METHODS: The emulsifier was prepared by interesterification of medium-chain fatty acids, pure lecithin, and immobilized phospholipase-1 on Duolite A568. An Ultraturrax homogenizer and a Branson Ultrasonic processor were used for the preparation of nano-emulsions, and a Zetasizer evaluated the particle size. qRT-PCR analysis was performed to quantify the cancer-related genes expressed in the K14E6 mice. The development and evolution of skin carcinogenesis were assessed through histological analysis to compare cell morphology. RESULTS: Ca 59% of the MCFA were incorporated via esterification into the PC within 12 hours of the reaction. An emulsifier yield used to formulate the NE of 86% was achieved. Nanoemulsions with a particle size of 44 nm were obtained. The curcumin nano-emulsion group had a 91.81% decrease in the tumorigenesis index and a reduction in tumor area of 89.95% compared to the sick group. Histological analysis showed that the group administered with free curcumin developed a microinvasive squamous cell carcinoma, as opposed to the group with nanoemulsion which presented only a slight inflammation. In gene expression, only a significant difference in Cdk4 was observed in the nanoemulsion group.


Asunto(s)
Carcinogénesis/efectos de los fármacos , Curcumina/farmacología , Composición de Medicamentos/métodos , Fosfatidilcolinas/química , Neoplasias Cutáneas/tratamiento farmacológico , Animales , Disponibilidad Biológica , Caspasa 8/metabolismo , Claudina-4/metabolismo , Curcumina/administración & dosificación , Quinasa 4 Dependiente de la Ciclina/metabolismo , Ciclinas/metabolismo , Emulsiones/química , Lecitinas , Ratones , Ratones Transgénicos , Nanopartículas/química , Neoplasias Cutáneas/patología
2.
J Oleo Sci ; 69(2): 123-131, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32023579

RESUMEN

Curcumin is a bioactive compound with proven antioxidant and anti-inflammatory activities, but has low water solubility and dermal absorption. The inflammatory process is considered as the biological response to damage induced by various stimuli. If this process fails to self-regulate, it becomes a potential risk of cancer. The objective of this work was to evaluate the anti-inflammatory activity of curcumin administered to mice with induced atrial edema using two topical vehicles: organogels and O/W-type nanogels at pH 7, Organogels and O/W-type nanogels at pH 7 were prepared, characterized and the anti-inflammatory activity was assessed. A histopathological analysis of mouse ears was performed and two gel formulations were selected. Thermograms of organogels indicated that increasing the gelling agent improved the stability of the system. Deformation sweeps confirmed a viscoelastic behavior characteristic of gels in both systems. During the anti-inflammatory activity evaluations, the nanogels demonstrated greater activity (61.8 %) than organogels; Diclofenac® (2-(2,6-dichloranilino) phenylacetic acid), used as a control medication achieved the highest inhibition (85.4%); however, the drug produced the death of 2 (40%) of the study subjects caused by secondary adverse events. Histopathological analysis confirmed the data.


Asunto(s)
Antiinflamatorios , Cardiomiopatías/tratamiento farmacológico , Curcumina/administración & dosificación , Curcumina/farmacología , Portadores de Fármacos , Edema/tratamiento farmacológico , Geles , Fitoterapia , Animales , Atrios Cardíacos , Ratones
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