Chitosan coated liposomes as an innovative nanocarrier for drugs.

Chitosomes are chitosan coated liposomes that represent an alternative to conventional liposomes since they present better stability and bioadhesivity. The aim of this work was to develop and evaluate the physico-chemical stability of melatonin (MEL)-loaded chitosomes as well as to compare their properties with that of MEL loaded liposomes. Structural characteristics of nanovesicles were also studied by dynamic light scattering and small angle X-ray scattering. The liposome and chitosome suspensions presented mean diameters between 150 nm and 254 nm, polydispersity indexes around 0.4, zeta potential values between -38 mV and -28 mV, pH values close to 4.0, MEL content close to 100% and encapsulation efficiency between 34.4% and 60.8%. Small angle X-rays scattering showed the presence of unilamelar structures, which were also observed by transmission electronic microscopy. Stability studies focusing on the particle diameter indicated that, within 90 days, the liposome suspensions had a decrease in mean diameter values and in polydispersity indexes, but no alterations were detected in zeta potentials and MEL content. The chitosome suspensions remained stable in relation to these parameters during 90 days. Multiple light scattering analysis (Turbiscan LAb) corroborated the the findings in the stability studies. The result sets pointed out the physico-chemical stability of chitosomes and the chitosan influence in their supramolecular structure.

NTPDase and 5'-nucleotidase activities of synaptosomes from hippocampus of rats subjected to hyperargininemia.

ATP is an important excitatory neurotransmitter and adenosine acts as a neuromodulatory structure inhibiting neurotransmitters release in the central nervous system. Since the ecto-nucleotidase cascade that hydrolyzes ATP to adenosine is involved in the control of brain functions and previous studies realized in our laboratory have recently reported that acute administration of Arg decreases the NTPDase and 5'-nucleotidase activities of rat blood serum, in the present study we investigated the effect of arginine administration on NTPDase and 5'-nucleotidase activities by synaptosomes from hippocampus of rats. First, sixty-days-old rats were treated with a single or a triple intraperitoneal injection of arginine (0.8 g/Kg) or an equivalent volume of 0.9% saline solution (control) and were killed 1 h later. Second, rats received an intracerebroventricular injection of 1.5 mM arginine solution or saline (5 microL) and were killed 1 h later. We also tested the in vitro effect of arginine (0.1-1.5 mM) on nucleotide hydrolysis in synaptosomes from rat hippocampus. Results showed that intraperitoneal arginine administration did not alter nucleotide hydrolysis. On the other hand, arginine administered intracerebroventricularly reduced ATP (32%), ADP (30%) and AMP (21%) hydrolysis, respectively. In addition, arginine added to the incubation medium, provoked a decrease on ATP (19%), ADP (17%) and AMP (23%) hydrolysis, respectively. Furthermore, kinetic studies showed that the inhibitory effect of arginine was uncompetitive in relation to ATP, ADP and AMP. In conclusion, according to our results it seems reasonable to postulate that arginine alters the cascade involved in the extracellular degradation of ATP to adenosine.