Development and characterization of exendin-4 loaded self-nanoemulsifying system and in vitro evaluation on Caco-2 cell line. (2nd January 2020)

• Record Type: Journal Article
• Authors: Aktas, Yesim; Celik Tekeli, Merve; Celebi, Nevin
• Is Part Of: Journal of microencapsulation. Volume 37:Number 1(2020)
• Page Start: 41
• Page End: 51
• Publication Date: 2020-01-02
• Subjects: Exendin-4 -- self-nanoemulsifying drug delivery system -- oral delivery -- lipolysis -- intestinal permeability; Microencapsulation -- Periodicals; Controlled release technology -- Periodicals; 615.19
• DOI: 10.1080/02652048.2019.1692945
• Languages: English
• ISSNs: 0265-2048

Abstract

Abstract: Aim: Aim of this study was to develop exendin-4 and exendin-4/chymostatin loaded self-nanoemulsifying drug delivery system (SNEDDS). Methods: Surfactants and co-surfactants were mixed, oil phase containing exendin-4 or exendin-4/chymostatin was added dropwise for SNEDDS. Short term physical stability test was performed prior to the release, lipolysis and permeability studies. Results: SNEDDS containing ethyl oleate: Cremophor EL ® : Labrasol ® : propylene glycole (15:42.5:21.25: 21.25) were selected for in vitro release and intestinal permeability studies for suitable parameters and physical stability test results. SNEDDS were obtained which yielded Grade B nanoemulsions having droplet size below 25 nm. In vitro release studies showed that 73.79% of the peptide was released for 2 h at pH 6.8. Both exendin-4 and exendin-4/chymostatin loaded SNEDDS were non-toxic to Caco-2 cells. Permeability coefficients of both exendin-4 loaded SNEDDS and exendin-4/chymostatin loaded SNEDDS were higher than exendin-4 solution. Conclusions: Intestinal permeability of exendin-4 has been improved by SNEDDS formulations.