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概要

Novel Solid Lipid Nanoparticles Formulation of Ion Paired Cefepime for Enhanced Oral Absorption

Wala’a AlBenayan, Basel Karzoun, Eman Atef, Christianne Rizkalla

We report a successful formulation of (CEF) ion paired Solid Lipid Nanoparticle (SLN) with a demonstrated improvement of the intestinal membrane permeability up to 41 folds. Cefepime is a parentally administered fourthgeneration cephalosporin zwitterion. The class 3 BCS drug has high water solubility and low permeability, which result in low oral bioavailability. Our goal is to overcome the low oral bioavailability challenge using double techniques, a molecular alteration ion pairing, and a Nano carrier formulation approaches.

The CEF ion pair was prepared by freeze-drying dispersions of an anionic lipid, Sodium Stearate (NaSA), with CEF. Then a combination of Precirol ATO ® 5 and Compritol 888 ATO ® lipids was used in preparing the SLNs using the microemulsion-ultrasonication technique. The enhanced drug permeability was confirmed using an ex vivo rat intestine in a side-by-side chamber.

The IR and Raman spectra confirmed the formation of the ion pair. The ex vivo studies showed a significant increase in the permeability and the percentage of drug transported of the encapsulated ion paired CEF compared to the unencapsulated control CEF by approximately 13 and 41 folds respectively. We thus concluded that SLN is a propitious formulation for improving the CEF oral bioavailability and that the CEF-stearate ion pair can further enhance the CEF SLN encapsulation and intestinal permeability.