4.7 Article

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

Journal

DRUG DELIVERY
Volume 23, Issue 9, Pages 3653-3664

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2016.1214991

Keywords

Nonionic; double-tailed surfactant; bioavailability; niosomes; levofloxacin

Funding

  1. Higher Education Commission (HEC), Pakistan [PIN: 112-23671-2BM1-136]

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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 H-1 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 190.314.51nm 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 1000g/mL and was found to be safe up to 2000mg/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.

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