Preparation and evaluation of optimized zolmitriptan niosomal emulgel

Abstract

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 topical 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- Expert 10 was used to design twelve formulations using Box-Behnken. Zt loaded niosomes were prepared by the thin film hydration method using Span 60(S 60), Span 80(S 80) along with cholesterol(Ch) at three different levels. The optimized formulation (F11) was formulated in Emulgel (1:1 emulsion/gel ratio).

Results: The vesicles revealed vesicle size (VS) ranging from 133.1 to 851.3 nm, zeta potential (ZP) −43.8 to −82.8 mV, 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 (133.1 nm), highest EE (88.7%), high ZP (−80.6 mV) and satisfactory release after 4 h (61.5%). There was a significant difference (p <.05) in drug permeation after 8 h for niosomal F11(460.98 ug/cm²) and niosomal F11 loaded Emulgel (336.92 ug/cm²) compared to plain Zt loaded emulgel (160.83 ug/cm²). Niosomal F11 loaded emulgel showed thixotropic behavior of rapid recovery, significant bioavailability and pharmacokinetic parameters as compared to the plain Zt-loaded Emulgel.

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

Keywords:

• Zolmitriptan
• Design-Expert 10
• niosomes
• skin permeation
• thixotropy
• bioavailability
• pharmacokinetic parameters

Acknowledgement

The auhtors acknowledge that the funding of this research came from the self-financing of the authors.

Disclosure statement

The authors report no conflicts of interest. The authors are responsible for this research.