RESUMO
Amylin is a pancreatic hormone involved in the regulation of glucose metabolism and homeostasis. Restoration of the post-prandial and basal levels of human amylin in diabetic individuals is a key in controlling glycemia, controlling glucagon, reducing the insulin dose and increasing satiety, among other physiologic functions. Human amylin has a high propensity to aggregate. We have addressed this issue by designing a liposomal human amylin formulation. Nanoparticles of multilamellar liposomes comprising human amylin were obtained with 53% encapsulation efficiency. The in vitro kinetic release assay shows a biphasic profile. The stabilization of the lipidic nanoparticle against freeze-drying was achieved by using mannitol as a cryoprotectant, as evidenced by morphological characterization. The effectiveness of the human amylin entrapped in lipidic nanoparticles was tested by the measurement of its pharmacological effect in vivo after subcutaneous administration in mice. Collectively these results demonstrate the compatibility of human amylin with the lipidic interface as an effective pharmaceutical delivery system.
Assuntos
Polipeptídeo Amiloide das Ilhotas Pancreáticas/química , Lipídeos/química , Nanopartículas/química , Humanos , Cinética , Conformação ProteicaRESUMO
The aim of this work was to develop and validate an ultraviolet derivative spectrophotometric (UVDS) method for the quantitative determination of allantoin (ALL) in liposomes, gels and creams. Liposomes were prepared by methods of thin film hydration and mechanical agitation. Solutions of ALL in 0.1 mol/L NaOH with ethanol:water (70:30, v/v) were prepared in order to destroy liposome vesicles. Spectral interference from components of liposomes, cream, gel and ALL degradation products was eliminated using the second-order derivative of the zero-order spectrum. Characterization of ALL in 0.1 mol/L NaOH was carried out by direct infusion mass spectrometry. Absorbances of ALL solutions were measured at 266.6 nm of the second-derivative spectrum and linearity was observed in the ALL concentration range of 50-300 µgmL(-1) (correlation coefficient (r)=0.9961). The mean recovery percentage was 100.68 ± 1.61, repeatability expressed as relative standard deviation (RSD) was 1.07 and 2.12%, and intermediate precision (RSD) was 2.16%. The proposed UVDS method was found to be linear, precise, accurate, robust and selective, providing rapid and specific determination of ALL in raw materials and in topical formulations.