Novel, safe, efficient, and cost effective surfactants from renewable resources has attracted attention for enhancing solubility and bioavailability of hydrophobic dugs. We report the synthesis, characterization, and biocompatibility of a novel non-ionic acyl glycoside double-tailed surfactant for niosomal drug delivery system. Structure of the surfactant was confirmed by H NMR and mass spectroscopy. Applications of surfactant in niosomal drug delivery were explored using Cefixime as model. The shape, size, and polydispersity index (PDI) of drug loaded vesicles were investigated with atomic force microscope (AFM) and dynamic light scattering (DLS). Drug entrapping efficiency (EE%) was determined using HPLC. Biocompatibility of the surfactant was evaluated by in vitro cytotoxicity, blood hemolysis, and in vivo acute toxicity. Bioavailability of the surfactant based formulation was investigated in rabbits using HPLC. Vesicles were found to be 159.76 ± 6.54 nm with narrow size distribution and spherical shape. EE% was found to be 71.39 ± 3.52%. Novel surfactant was non-cytotoxicity and hemo-compatible even at 1000 μg/mL concentration and was safe up to 2000 mg/kg body weight. The in vivo bioavailability of niosomal formulation showed elevated plasma concentration and decreased clearance of Cefixime. Current findings reveal that this novel surfactant is biocompatible and could be employed for niosomal drug delivery.

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Synthesis of biocompatible and cost-effective novel nonionic surfactants from renewable resources has been the subject of greater scientific interest for enhancing the bioavailability of less water-soluble drugs. The present study focuses on the synthesis of α-tocopherol-based novel biocompatible nonionic surfactant and its evaluation for forming clarithromycin-loaded niosomal drug delivery system. α-tocopherol was hydrophilically modified through multistep reactions and characterized using mass and H NMR spectroscopic techniques. Drug-loaded niosomal vesicles were investigated for entrapment efficiency (%EE), size, polydispersity index (PDI), zeta potential (ζ) and morphology using LC-MS, dynamic light scattering (DLS) and atomic force microscopy (AFM). Blood haemolysis, cell culture and acute toxicity tests were performed to investigate its biocompatibility. In vivo oral bioavailability of clarithromycin loaded in niosomal formulation was studied in rabbits. The vesicles were spherical in shape and entrapped up to 75 ± 2.57% of the drug. They exhibited a homogeneous size distribution with a mean diameter of 245 ± 4.66 nm. The surfactant was quite haemocompatible, low cytotoxic and safe in mice. Improved oral bioavailability of clarithromycin was achieved when carried in α-tocopherol-based niosomes. Results obtained showed that the synthesized amphiphile is biocompatible and has excellent capability for formation of niosomal vesicles and enhancing oral bioavailability of less water-soluble drugs like clarithromycin.