Physicochemical properties of carrier affect morphological, dimensional and release behaviour of acetazolamide-loaded proniosomes

MARTIN-MORAL F; COZAR BERNAL M,; PALMA S. D; RABASCO ALVAREZ A,; GONZALEZ -RODRIGUEZ M.

Córdoba

Congreso; Tercera Reunión Internacional de Ciencias Farmacéuticas - RICIFA 2014; 2014

Facultad de Ciencias Quimicas - UNC

Nowadays,lipid vesicle systems such as liposomes, niosomes or transfersomes represent an interesting therapeutic alternative due to diverse advantages such as biodegradability, biocompatibility and non-immunogenicity. However, the most important disadvantages are their physical and chemical instability. For these reasons, technological alternatives are the proniosomes which incorporate the drug in a suitable carrier together with nonionic surfactantsand other lipids, which can be converted into niosomes when they are reconstituted. The aim of this study wasto analyze how the carriers (maltodextrins, sorbitol, trehalose, maltose, alginate and chitosan)can affect the characteristics of solid proniosomes.The study was completed with a stability analysis. Proniosomes were made from the slurry method, previously described in the literature.Samples were morphologically characterized by scanning electron microscopy. Then, reconstituted niosomes were characterized in terms of size, by dynamic light scattering, and zeta potential byphoton correlation spectroscopy; the PDE was determined by centrifugation (9000 rpm, 4ºC and 60 minutes)and drug content was quantified by HPLC. Stability studies were developed along one month, and PDE was monitored. Generally, results showed homogeneous reconstituted samples witha negative zeta potential andPDE from25% to 80%. Dimensional parameter ranged from 1100 to 1900 nm, as exception of alginate, which hada higher size. Stability testingdemonstrated a high stability of acetazolamide into niosomes, because a very low percentage of drugwas lost. With respect to the carrier, studies indicated a great influence of this compound on the dimensions of proniosomes. In this sense, samples made with maltodextrins and sorbitol hadsmaller sizes and relative homogeneity, making them especially useful.However,alginate wasrejectedfrom the study because proniosomes were high in size and instability of reconstituted niosomes was appreciated. Regarding the chitosan and trehalose, interesting results were found in terms of characterization parameter