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1.
Braz. J. Pharm. Sci. (Online) ; 58: e20130, 2022. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1403716

RESUMEN

Abstract The purpose of this research was to develop a hydrogel containing the extract of Gac fruit (Momordica cochinchinensis Spreng) with appropriate physicochemical properties and good dermatological efficacy. The Gac aril fruit was extracted by maceration in dichloromethane, and its antioxidant activity was determined through a DPPH assay. The very low water-solubility of the Gac extract is responsible for its incompatibility with the hydrogel. To overcome this drawback, LabrafacTM PG and Tween 60 were used to develop the hydrogel due to their potent potential for solubilizing the Gac extract. The prepared hydrogels displayed good physical properties, a homogenous orange gel, appropriate pH, and viscosity. After storage in an accelerated condition for six months, the hydrogels of the Gac extract had physical stability and high remaining amounts of beta-carotene and lycopene within the range of 90.25 - 94.61%. The skin efficacy of hydrogel containing the Gac fruit extract was found using 14 healthy female volunteers over a 30-day period of daily application. Topical application of the hydrogel containing the Gac fruit extract, which contains antioxidants, significantly moisturizes the skin and enhanced its elasticity (p ≤ 0.05; ANOVA). This makes it suitable for use as a skin care product


Asunto(s)
Humanos , Femenino , Adulto , Extractos Vegetales/efectos adversos , Eficacia , Hidrogeles/análisis , Frutas/efectos adversos , Piel , Análisis de Varianza , Cuidados de la Piel , Momordica , Antioxidantes/farmacología
2.
Acta Pharm ; 70(1): 77-88, 2020 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-31677372

RESUMEN

The aim of the present study was to develop self-microemulsifying drug delivery systems (SMEDDS) of the extract of Moringa oleifera, a herbal medicinal plant. Kaempferol and quercetin, the flavonoids present in the leaf extract of M. oleifera, were chosen as markers for quantification. The optimized formulation of SMEDDS consisted of propylene glycol dicaprylocaprate, polysorbate 80, and polyethylene glycol 400 (PEG 400) in a percentage ratio of 20:60:20 (m/m). SMEDDS emulsified immediately (within 20 s) after dilution in water, resulting in transparent microemulsions with a droplet size of 49 nm. SMEDDS could increase the solubility of kaempferol and quercetin to nearly 100 % within 15 min, whereas only a 30 % improvement in solubility was achieved in the case of crude extract. These results demonstrated SMEDDS to be a promising strategy to improve the solubility of M. oleifera extract-derived drugs, which, in turn, could prove beneficial to the herbal medicine field.


Asunto(s)
Sistemas de Liberación de Medicamentos , Quempferoles/aislamiento & purificación , Moringa oleifera/química , Extractos Vegetales/administración & dosificación , Quercetina/aislamiento & purificación , Química Farmacéutica/métodos , Liberación de Fármacos , Emulsiones , Excipientes/química , Quempferoles/química , Tamaño de la Partícula , Extractos Vegetales/química , Quercetina/química , Solubilidad , Tensoactivos/química
3.
Macromol Rapid Commun ; 39(19): e1800265, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-30062740

RESUMEN

The high incidence of prostate carcinogenesis has prompted the search for novel effective treatment approaches. We have employed curcumin (Curc) and diethylstilbestrol (DES) to synthesize a series of polyacetal (PA)-based combination conjugates for prostate cancer (PCa) treatment. Given their bihydroxyl functionalities, Curc and DES molecules were incorporated into a PA mainchain using a one-pot reaction between diols and divinyl ethers. The PA-conjugates released both drugs under acidic conditions, such as those found in the tumor microenvironment, endosomes, or lysosomes, while remaining stable at neutral pH 7.4. The drug ratio was optimized to achieve anticancer drug synergism with elevated cytotoxicity against LNCaP-hormone-dependent human PCa cells conferred via the induction of S phase cell cycle arrest by the upregulation of p53 and CDK inhibitors p21Waf/CIP1 and downregulation of cyclin D1. The application of rationally designed PA-Curc-DES combination conjugates represents a potentially exciting new treatment for prostate cancer.


Asunto(s)
Acetales/química , Antineoplásicos , Curcumina/química , Dietilestilbestrol/química , Polímeros/química , Neoplasias de la Próstata/tratamiento farmacológico , Puntos de Control de la Fase S del Ciclo Celular/efectos de los fármacos , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacocinética , Antineoplásicos/farmacología , Línea Celular Tumoral , Preparaciones de Acción Retardada/síntesis química , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Preparaciones de Acción Retardada/farmacología , Humanos , Masculino , Proteínas de Neoplasias/metabolismo , Neoplasias de la Próstata/metabolismo , Neoplasias de la Próstata/patología
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