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Preparation and Evaluation of Optimized Zolmitriptan Niosomal Emulgel

Magdy Ibrahim Mohamed, Aly Ahmed Abdelbary, Soha Mohamed Kandil, Tamer Mohamed Mahmoud
Drug Development and Industrial Pharmacy 2019 March 28, : 1-38

OBJECTIVE: Novel niosomal formulation may be successfully applied to treat a systemic disease such as migraine through transdermal drug delivery system (TDDS), moreover, the treatment of tropical diseases such as mycotic infections by targeting and localizing the drug to the stratum corneum. The current study aims to formulate zolmitriptan (Zt) in niosomal vesicles to potentiate its transdermal effect.

SIGNIFICANCE: The development of a promising niosomal formulation will push the scaling up of pharmaceutical industry in this field.

METHODS: Design- Expert10 was used to design twelve formulations using Box-Behnken. Zt loaded museums were prepared by the thin film hydration method using Span 60, Span 80 along with cholesterol at three different levels, the optimized formulation (F11) was formulated in Emulgel (1:1 emulsion/gel ratio).

THE RESULTS: The obtained vesicle revealed vesicle size (VS) ranging from 133.1 to 851.3 mm, zeta potential (ZP) -43.8 to -82.8 mg, entrapment efficiency (EE%) from 66.7 to 88.7%, and Zt release after 4 h up to 67%. Optimized niosomal formulation (F11) depicted the smallest VS (133.1nm), highest EE (88.7%), high ZP (-80.6mg) and satisfactory release after 4h (61.5%). F11 depicted significant (p<0.05) drug permeation 346.92, 460.98 ug/cm2 after 8 h for niosomal F11 and niosomalF11 loaded Emulgel respectively, thixotropic behavior of rapid recovery, significant bioavailability and pharmacokinetic parameters as compared to the Zt-loaded Emulgel.

CONCLUSION: Optimized F11 represents a promising formulation for transdermal drug delivery system to treat both topical and systemic diseases.


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