Development, optimization and characterization of zaltoprofen-loaded bilosomes using response surface methodology

Year 2025, Volume: 29 Issue: 6, 2253 - 2266, 02.11.2025

Aymen Al-Shaybani , Fatima J Jawad

https://doi.org/10.12991/jrespharm.1796232

Abstract

This study aims to generate and optimize Zaltoprofen-loaded bilosomes for improved transdermal delivery, utilizing a Box-Behnken design to evaluate the influence of formulation factors on bilosome characteristics. Bilosomes were produced utilizing a blend of Span 60 and various amounts of Tween 60., Cholesterol, and Sodium Deoxycholate. The impact of these formulation variables was assessed on entrapment efficiency, vesicle size, polydispersity index, and zeta potential. The morphology and surface characteristics of the bilosomes were analyzed using Transmission Electron Microscopy and Scanning Electron Microscopy. The improved formulations underwent invitro drug release and permeation experiments to evaluate their efficacy. The results of the present study showed that the optimized bilosomal formulation (F3) demonstrated an entrapment efficiency of 89.38%, a vesicle size of 227.252 nm, polydispersity index of 0.2714, and zeta potential of -29.841 mV. The values of the formulation variables for F3 were 15 mg Sodium Deoxycholate, 37.5 mg Cholesterol, and 100 mg tween 60. Transmission Electron Microscopy and Scanning Electron Microscopy analyses confirmed the spherical shape and uniform surface morphology of the bilosomes. In-vitro drug release studies showed sustained release over 480 minutes, with a maximum release of 96.63%. In-vitro permeation studies indicated a 43.924-fold increase in permeation compared to the Zaltoprofen dispersion. In conclusion, the findings of this study demonstrate that Zaltoprofen-loaded bilosomes significantly enhance drug permeation and stability compared to Zaltoprofen dispersions. The optimized formulation exhibited improved drug stability, enhanced permeation, and sustained release, offering a viable alternative to conventional oral and injectable drug administration routes.

Keywords

Zaltoprofen , bilosomes , transdermal delivery , Box-Behnken design; , optimization , drug release

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