ABSTRACT
The present study was aimed at the preparation and performance evaluation of Intacglobin-loaded liposomes for selective drug presentation to the lungs. Egg phosphatidylcholine- and cholesterol-based liposomes (1:1 and 1:0.25 mol/mol) were prepared by a dehydration-rehydration procedure. A tissue distribution study after single intranasal administration of 0.5 microCi 125I-Intacglobin-loaded liposomes was conducted in Balb/c mice. The efficiencies of drug entrapment (30%) and the average diameters did not differ significantly between the two liposome formulations. However, liposomes composed of an increased cholesterol amount showed a lower in vitro drug release rate. The airway penetration efficiency of the liposomal formulation was determined by the cumulative percentage of the dose reaching the lungs (AUC) and its sojourn time therein, and were 1.7- and 2.2-times higher compared with the plain 125I- Intacglobin solution-based formulation, respectively. A significantly greater (p<0.001) drug localization index after 24 h was found at the lungs in comparison with the other tissues (p<0.01), although similar values were detected between groups following administration of either liposomes or control solutions, despite the formulations attributes. In conclusion, it is suggested that longer Intacglobin exposure at the pulmonary region is observed after administration of the liposomal formulation. The results open future perspectives in assessing local passive immunization for the treatment of respiratory infectious diseases.
Subject(s)
gamma-Globulins/administration & dosage , gamma-Globulins/pharmacokinetics , Administration, Intranasal , Animals , Bronchi/drug effects , Bronchi/metabolism , Drug Carriers , Humans , Iodine Radioisotopes , Liposomes , Male , Mice , Mice, Inbred BALB C , Tissue Distribution , Trachea/drug effects , Trachea/metabolismABSTRACT
Se evaluó el efecto del ejercio físico agudo sobre la distribución y el metabolismo de la vitamina A en un modelo experimental animal. Se estudiaron las concentraciones plasmáticas, hepaticas, renales, testiculares y de glándulas suprarrenales de la vitamina A y de sus principales formas moleculares: retinol y ésteres de retinol, en animales sometidos a ejercicio físico durante 2 h sin previo entrenamiento. Se observó una disminución en la concentración hepática y testicular de la vitamina A y un incremento de ésta en los riñones de los animales ejercitados. Se demostró, además, el incremento del catabolismo hepático del retinol bajo las condiones experimentales
Subject(s)
Rats , Animals , Male , Rats, Inbred Strains/metabolism , Vitamin A/metabolism , Physical Exertion , Plasma , Liver/analysis , Kidney , Testis , Adrenal Glands , Chromatography, High Pressure LiquidABSTRACT
Se evaluó el efecto del ejercio físico agudo sobre la distribución y el metabolismo de la vitamina A en un modelo experimental animal. Se estudiaron las concentraciones plasmáticas, hepaticas, renales, testiculares y de glándulas suprarrenales de la vitamina A y de sus principales formas moleculares: retinol y ésteres de retinol, en animales sometidos a ejercicio físico durante 2 h sin previo entrenamiento. Se observó una disminución en la concentración hepática y testicular de la vitamina A y un incremento de ésta en los riñones de los animales ejercitados. Se demostró, además, el incremento del catabolismo hepático del retinol bajo las condiones experimentales
