RESUMEN
The objective of this study was to develop and characterize a novel dithranol-containing phospholipid microemulsion systems for enhanced skin permeation and retention. Based on the solubility of dithranol, the selected oils were isopropyl myristate (IPM) and tocopherol acetate (TA), and the surfactants were Tween 80 (T80) and Tween 20 (T20). The ratios of cosurfactants comprising of phospholipids and ethanol (1 : 10) and surfactant to co-surfactant (1 : 1 and 2.75 : 1) were fixed for the phase diagram construction. Selected microemulsions were evaluated for globule size, zeta potential, viscosity, refractive index, per cent transmittance, stability (freeze thaw and centrifugation), ex vivo skin permeation and retention. The microemulsion systems composed of IPM and T80 with mean particle diameter of 72.8 nm showed maximum skin permeation (82.23%), skin permeation flux (0.281 mg/cm²/h) along with skin retention (8.31%) vis-à-vis systems containing TA and T20. The results suggest that the developed novel lecithinized microemulsion systems have a promising potential for the improved topical delivery of dithranol.
Asunto(s)
Antralina , Fármacos Dermatológicos , Fosfolípidos , Absorción Cutánea/efectos de los fármacos , Administración Cutánea , Animales , Antralina/química , Antralina/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Fármacos Dermatológicos/química , Fármacos Dermatológicos/farmacología , Evaluación Preclínica de Medicamentos , Emulsiones , Ratones , Miristatos/química , Miristatos/farmacología , Aceites/química , Aceites/farmacología , Permeabilidad/efectos de los fármacos , Fosfolípidos/química , Fosfolípidos/farmacología , Polisorbatos/química , Polisorbatos/farmacología , Tensoactivos/química , Tensoactivos/farmacología , Tocoferoles/química , Tocoferoles/farmacología , ViscosidadRESUMEN
Methanol, acetone and diethyl ether extracts of Alpinia galanga have been evaluated against pathogens viz. Bacillus subtilis MTCC 2391, Enterobacter aerogene, Enterobacter cloacae, Enterococcus faecalis, Escherichia coli MTCC 1563, Klebsiella pneumoniae, Pseudomonas aeruginosa MTCC 6642, Salmonella typhimurium, Staphylococcus aureus and Streptococcus epidermis using Agar well diffusion method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of all the extracts were determined using the macrodilution method. Methanol extracts have shown excellent activity towards all the pathogens with MIC and MBC values ranging from 0.04-1.28 mg/ml and 0.08-2.56 mg/ml, respectively. The GC-MS analysis of methanol extracts have yielded compounds like 5-hydroxymethyl furfural (59.9%), benzyl alcohol (57.6%), 1,8 cineole (15.65%), methylcinnamate (9.4%), 3-phenyl-2-butanone (8.5%) and 1,2 benzenedicarboxylic acid (8.9%), which could be responsible for its broad spectrum activity. So, A. galanga can be quite resourceful for the development of new generation drugs.
Asunto(s)
Alpinia/química , Antibacterianos/química , Antibacterianos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Antralina/análogos & derivados , Antralina/química , Alcohol Bencilo/química , Furaldehído/análogos & derivados , Furaldehído/química , Cromatografía de Gases y Espectrometría de Masas , Pruebas de Sensibilidad MicrobianaRESUMEN
One new prenylated 1,4-anthraquinone and three new prenylated anthranols, named kengaquinone (1) and kenganthranols A (2), B (3), and C (4), were isolated from a hexane extract of the stem bark of Harungana madagascariensis. Six known compounds including anthraquinones, anthrones, and xanthones were also isolated and identified. The structures of the new compounds were determined by analysis of spectroscopic data and comparison with data of previously known analogues. Some isolated compounds (3-5, 7-11) were evaluated for their alpha-glucosidase inhibition activity. Compounds 3, 4, 8, and 11 showed significant activity, whereas compounds 7, 9, and 10 were inactive in this test.