Glimepiride Nanoemulgel: An innovative carrier with improved antidiabetic effect

Author(s): Syed Haroon Khalid

The aim was to develop a topical nanoemulgel of a BCS class II drug, Glimepiride (GLP) in both and inclusion complexed form. In our previous studies, we prepared binary and ternary inclusion complexes of GLP by physical trituration and kneading methods and found the optimized ternary inclusion of GLP with βCD and Gelucire-44/14 in the ratio of 1:4:10 %. In the present study, nanoemulsion formulations were prepared using clove oil, Tween-80 and PEG-400 following spontaneous emulsification technique and characterized for pH, conductivity, viscosity, particle size, polydispersity index and zeta potential. The gel base was developed using xanthan gum (3%) and incorporated the prepared nanoemulsion in 1:1 to devise nanoemulgels (NEGs). The prepared NEGs were further evaluated for their pH, viscosity, spreadability, drug content, ex-vivo permeation and in-vivo hypoglycemic activity. Franz diffusion cell was used for ex-vivo permeability in excised rat skin. The antidiabetic activity was performed using streptozocin induced diabetic rats against marketed glimepiride per oral medication. Nanoemulgel formulations loaded with pure and inclusion complexed presented high permeation flux in comparison to control drug solution (11.64±2.61 µg/cm2/hr) with ICI-NEG showing the highest drug flux (70.06±6.60 µg/cm2/hr). In-vivo studies also produced the similar results to control hyperglycemia for unto 24 hours in comparison to its oral delivery which lasted for 6 hours only. Nanoemulgel loaded with inclusion complex showed a more profound outcome in comparison to pure drug loaded formulation. In conclusion, the inclusion complexed nanoemulgel could be regarded as an effective delivery system in the treatment of diabetes hence overlaying the path for management of diabetes by topical application

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