A variety of factors were systemically evaluated in order to establish the characteristics of the niosomes obtained with a high-pressure homogenizer. The vesicular sizing parameters, electrical properties, drug entrapment data and drug release characteristics were investigated using two groups of factors. The first group presented the physical process variables such as pressure of the homogenizer and the times that the samples were processed (cycles). The second group encompassed the compositional variables such as the drug loading, surfactant chain length, cholesterol level and the level of the charge imparting agent. The obtained data showed that the drug distributed within both the aqueous and lipid phases of the formed niosomes. Saturation-like behaviors for both the effect of homogenization cycles on the produced size and the effect of the pressure on the size homogeneity were recorded. In contrast to the drug entrapment and conductivity of the niosomal suspension, the vesicular size parameters as well as the zeta potential were inversely proportional with the homogenization parameters. Drug release was significantly affected by the compositional factors rather than the physical ones. The current study demonstrated the usefulness of the microfluidization for the production and further scale-up of anti-HIV niosomes with very small mean vesicular sizes.
Published by Elsevier B.V.