Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability

Abstract

Aim: The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using in situ single-pass intestinal perfusion (SPIP) technique. Methods: Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated. Results: Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine. Conclusion: The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.

Article highlights

• A mixture of turpentine oil/castor oil (3:1) and ethyl oleate was selected as the oil phase and Tween 80 and PEG 600 are selected as the surfactant and cosolvent to prepare the fexofenadine-loaded self-microemulsifying drug-delivery systems (SMEDDS).

• 36 different SMEDDS formulations with varying ratios of oil, surfactant and cosolvent were prepared and their state of homogeneity and stability were evaluated.

• F8 formulation produced droplets with smaller sizes compared with F6, F7 and F15.

• All of the SMEDDS formulations have released more than 50% of their drug content in 30 min.

• There were no signs of creaming, phase separation, layering and droplet size change in F6, F and F8 formulations after facing to freeze–thaw and centrifugation tests.

• The ratios of corrected outlet to inlet fexofenadine concentrations obtained from SPIP studies were used to determine reaching the steady state and calculating intestinal effective permeabilities.

• An approximately threefold improvement was seen in the intestinal effective permeability of fexofenadine from SMEDDS compared with free fexofenadine suspension.

• Human intestinal permeabilities of SMEDDS formulaton and free fexofenadine suspension was predicted.

Keywords: :

• dissolution
• fexofenadine
• permeability
• self-microemulsifying
• SPIP

Supplemental material

Supplemental data for this article can be accessed at https://doi.org/10.1080/20415990.2024.2363635

Acknowledgments

The authors would like to thank the Research Council of Kermanshah University of Medical Sciences. Also, faithfully thanks S Taghe for her assistance and Rahesh Daru Novin Co. for kind cooperation in providing materials and equipment.

Author contributions

A Barfar performed the experiments and carried out the analysis. Z Islambulchilar drafted the manuscript. Z Islambulchilar and S Mirzaeei designed the study. S Mirzaeei conceived the original idea and supervised the whole project.

Financial disclosure

The authors would like to thank the Research Council of Kermanshah University of Medical Sciences (Grant Number: 4000233) for financial support of this work. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Competing interests disclosure

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, stock ownership or options and expert testimony.

Writing disclosure

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The protocol was approved by the Local Ethical Committee of Kermanshah University of Medical Sciences; approval number: IR.KUMS.REC.1400.099.

Additional information

Funding

The authors would like to thank the Research Council of Kermanshah University of Medical Sciences (Grant Number: 4000233) for financial support of this work.