Synthesis of non-ionic surfactants nano-vesicles for clarithromycin oral delivery

Abstract

In order to improve the solubility and bioavailability of poorly water-soluble drugs, the synthesis of cost-effective nonionic surfactants has been the subject of greater scientific interest. The present study focuses on the synthesis of sulfonyl chloride derivatives as nonionic surfactants (surfactant 1 and surfactant 2) and their evaluation for the preparation of a clarithromycin-loaded niosomal drug delivery system. Surfactants 1 and 2 were characterised by EI-MS and 1H NMR spectroscopy. The shape and size of the drug-loaded niosomal vesicles from the synthesised surfactants were examined by atomic force microscopy (AFM) and revealed a round morphology with an average size of (230.8 ± 2.35) nm and (248.1 ± 2.54) nm for the vesicles of surfactant 1 and surfactant 2, respectively. The zeta potential of surfactant 1-based niosomal vesicles was (– 7.70 ± 1.00) mV and that of surfactant 2 was (−14.6 ± 1.08) mV. The lower zeta potential values for surfactant 1 and surfactant 2-based niosomal vesicles showed that these vesicles were neutral and relatively stable. The vesicles of surfactant 1 and 2 have a capacity to entrap the drug of about (62 ± 2.26) % and (69.67 ± 3.23) %, respectively. The vesicles of surfactant 1 released the largest amount of drug, i.e. (70.00 ± 2.45) % at pH 1.2. Biocompatibility in human blood and toxic effects on various cell lines were also studied for surfactants 1 and 2, and they were found to be biocompatible and non-cytotoxic.