Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

Abstract

Context: Vesicular systems have attracted great attention in drug delivery because of their amphiphilicity, biodegradability, non-toxicity and potential for increasing drug bioavailability. Objective: A novel sugar-based double-tailed surfactant containing renewable block was synthesized for preparing niosomal vesicles that could be exploited for Levofloxacin encapsulation, aiming to increase its oral bioavailability. Materials and methods: The surfactant was characterized by 1 H NMR, mass spectroscopy and Fourier transform infrared spectroscopy (FT-IR). Its biocompatibility was studied against cell cultures and human blood hemolysis. In vivo acute toxicity was evaluated in mice. The vesicle morphology, size, drug-excipients interaction and entrapment efficiency (EE) were examined using atomic force microscope (AFM), dynamic light scattering (DLS), FT-IR and HPLC. Oral bioavailability studies of Levofloxacin in surfactant-based niosomal formulation were carried out using rabbits and plasma samples were analyzed using HPLC. Results and discussion: Vesicles were spherical in shape and the size was 190.31 ± 4.51 nm with a polydispersity index (PDI) of 0.29 ± 0.03. The drug EE in niosomes was 68.28 ± 3.45%. When applied on cell lines, high cell viability was observed even after prolonged exposure at high concentrations. It caused 5.77 ± 1.34% hemolysis at 1000 mg/mL and was found to be safe up to 2000 mg/kg. Elevated Levofloxacin plasma concentration was achieved when delivered with novel vesicles. Conclusion:The surfactant was demonstrated to be safe and effective as carrier of Levofloxacin. The study suggests that this sugar-based double-tailed nonionic surfactant could be promising nano-vesicular system for delivery and enhancing oral bioavailability of the hydrophobic Levofloxacin.

Synthesis of Sulfur‐Based Biocompatible Nonionic Surfactants and Their Nano‐Vesicle Drug Delivery

“…Nonionic surfactant-based niosomal vesicles are preferred for encapsulation and delivery of drugs because of their higher biocompatibility, economic synthesis, and physical and chemical stabilities [13,14]. Drugs delivered through nonionic surfactant-based niosomal vesicles have been reported to have increased bioavailability due to P-glycoprotein (P-gp) efflux inhibition by these vesicles [15].…”

Synthesis of Biocompatible Double‐Tailed Nonionic Surfactants and Their Investigation for Niosomal Drug‐Loading Applications

“…Nonionic surfactants used as candidates for niosomal drug delivery should not cause any detrimental effects to biological systems including RBC (Imran et al, ). Thus, the newly synthesized double‐tailed nonionic surfactants DABP‐L and DDSB‐OA were screened out for blood hemolysis to check their suitability for drug delivery.…”

“…Composition, percent drug entrapment efficiency (EE%), mean size, zeta potential, and polydispersity index (PDI) of DDSB-OA-based and DABP-L-based drug-loaded niosomal vesicles Nonionic surfactants used as candidates for niosomal drug delivery should not cause any detrimental effects to biological systems including RBC(Imran et al, 2016b). Thus, the newly synthesized double-tailed nonionic surfactants DABP-L and DDSB-OA were screened out for blood hemolysis to check their suitability for drug delivery.…”

Benazepril Hydrochloride Loaded Niosomal Formulation for Oral Delivery: Formulation and Characterization

“…Release studies were carried out for both pure benazepril hydrochloride and the loaded niosomal formulations. Each Formulation was instilled in a dialysis membrane bag with a molecular weight cut off (8000-12 000 KDa) and sealed from both sides [9]. It was then tied to the shaft of dissolution apparatus (Vanguard/USA) and immersed in 500 ml of de-ionized water at constant temperature 37±0.5 °C and rotation speed of 50 rpm.…”