Optimization of self-nanoemulsifying systems for the enhancement of in vivo hypoglycemic efficacy of glimepiride transdermal patches. (July 2014)

• Record Type: Journal Article
• Authors: Ahmed, Osama AA; Afouna, Mohsen I; El-Say, Khalid M; Abdel-Naim, Ashraf B; Khedr, Alaa; Banjar, Zainy M
• Is Part Of: Expert opinion on drug delivery. Volume 11:Number 7(2014:Jul.)
• Page Start: 1005
• Page End: 1013
• Publication Date: 2014-07
• Subjects: Drug delivery devices -- Periodicals; Drug delivery systems -- Periodicals; 615.605
• DOI: 10.1517/17425247.2014.906402
• Languages: English
• ISSNs: 1742-5247

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold> <italic>Objectives:</italic> </bold> To optimize and use of glimepiride (GMD)-loaded self-nanoemulsifying delivery systems (SNEDs) for the preparation of transdermal patches.</p> <p> <bold> <italic>Methods:</italic> </bold> Mixture design was utilized to optimize GMD-loaded SNEDs in acidic and aqueous pH media. Optimized GMD-loaded SNEDs were used in the preparation of chitosan (acidic) and hydroxypropyl methyl cellulose (HPMC) (aqueous) films. The prepared optimized formulations were investigated for <italic>ex vivo</italic> skin permeation, for <italic>in vivo</italic> hypoglycemic activity and for their pharmacokinetic parameters using animal model.</p> <p> <bold> <italic>Results:</italic> </bold> The optimized formulations showed flux value of (2.88 and 4.428 μg/cm<sup>2</sup>/h) through rat skin for chitosan and HPMC films, respectively. The pattern of GMD release from both formulations was in favor of Higuchi and approaching zero order models. The n values for Korsmeyer–Peppas equation were characteristic of anomalous (non-Fickian) release mechanism. Moreover, HPMC patches have shown significant reductions (p < 0.05) in blood glucose levels; (213.33 ± 15.19) mg/100 ml from the base-line measurement after 12 h of application.</p> <p> <bold> <italic>Conclusions:</italic> </bold> Optimized GMD SNEDs patches were found to improve GMD skin permeability and the essential pharmacokinetic parameters. Further extensive pre/clinical studies are necessary prior to use transdermal GMD as a valuable alternative to peroral dosage forms with improved bioavailability, longer duration of action and more patient convenience.</p> </abstract>