Biocompatibility Of Surfactants Research Articles

Creatinine-based non-phospholipid vesicular carrier for improved oral bioavailability of Azithromycin

Context: Novel, safe, efficient and cost effective nano-carriers from renewable resources have got greater interest for enhancing solubility and bioavailability of hydrophobic dugs.Objectives: This study reports the synthesis of a novel biocompatible non-phospholipid human metabolite "Creatinine" based niosomal delivery system for Azithromycin improved oral bioavailability.Methods: Synthesized surfactant was characterized through spectroscopic and spectrometric techniques and then the potential for niosomal vesicle formation was evaluated using Azithromycin as model drug. Drug loaded vesicles were characterized for size, polydispersity index (PDI), shape, drug encapsulation efficiency (EE), in vitro release and drug–excipient interaction using zetasizer, atomic force microscope (AFM), LC–MS/MS and FTIR. The biocompatibility of surfactant was investigated through cells cytotoxicity, blood hemolysis and acute toxicity. Azithromycin encapsulated in niosomes was investigated for in vivo bioavailability in rabbits.Results: The vesicles were spherical with 247 ± 4.67 nm diameter hosting 73.29 ± 3.51% of the drug. Surfactant was nontoxic against cell cultures and caused 5.80 ± 0.51% hemolysis at 1000 µg/mL. It was also found safe in mice up to 2.5 g/kg body weight. Synthesized surfactant based niosomal vesicles revealed enhanced oral bioavailability of Azithromycin in rabbits.Conclusions: The results of the present study confirm that the novel surfactant is highly biocompatible and the niosomal vesicles can be efficiently used for improving the oral bioavailability of poor water soluble drugs.

Double-tailed acyl glycoside niosomal nanocarrier for enhanced oral bioavailability of Cefixime

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 1H 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.

Novel fluorinated surfactants for perfluorochemical emulsification: biocompatibility assessments of glycosidic and polyol derivatives.

A novel series of fluoro-surfactants, derived from glycosides (monosaccharides) or polyols (ureas or carbamates), have been produced for use in respiratory gas-carrying perfluorochemical emulsions. Compounds were synthesised via simple, but highly selective, routes using highly fluorinated isocyanates with amino alcohols, polyethoxylated alcohols and partially protected sugars at anomeric carbon; yields were 88-95%. Resultant compounds were perfluoroalkylated with hydroxylic "head" groups. The biocompatibility of surfactants with human blood in vitro was assessed using a conventional haemolysis test. Compounds showing insignificant haemolysis at up to 10 g l-1 were further evaluated (i) for their effects on neutrophil chemiluminescence, and (ii) in a human platelet aggregation assay. Some fluoro-surfactants inhibited spontaneous platelet aggregation, in blood anti-coagulated with hirudin, at concentrations of 0.01% (w/v), suggesting possible applications as antithrombotic agents.