Comparison of the Characteristics of Transfersomes and Protransfersomes Containing Azelaic Acid

Abstract

Objectives: Recently developed agent carriers, transfersomes, which are sufficiently deformable to penetrate into or across the skin barrier. Protransfersome is the lyophilization of transfersome by removing the water system with freeze-drying method to improve the protransfersome characterizations, especially entrapment efficiency. The aim of this study was to comparethe characteristics ofazelaic acid transfersomes and protransfersomes.Materials and Methods: Transfersome was prepared by thin layer hidration method. Protransfersome was prepared by freeze-drying method and trehalose as lyoprotectant. The characterizations that measured were entrapment efficiency, morphological structure, particel size, and zeta potential.Results: The result of Transfersome particel size characterization, pointed out measurement with 89,06 nm. Whereas, after freeze- drying process, Protransfersome A has 735 nm, Protransfersome B has 1218 nm, and Protransfersome C has723,1 nm. There are excalations from 40,98% of entrapment efficiency after freeze-drying process, Protransfersome A with percentage 45,20%, Protransfersome B with percentage 45,65%, and Protransfersome C with percentage 52,90%. The spheric vesicle morphology of transfersome and protransfersomes is determined by transmission electron microscope.Conclusion: Protransfersomes have a better stability in entrapment efficiency by using trehalose or no trehalose with indirect cooling rate within 4 weeks of storage period.Key message: There has been no research yet that compares the stability of azelaic acid transfersome to protransfersome of azelaic acid which uses freeze-drying method with three different steps, which are fast-freezing trehalose step, slow-freezing trehalose step, and slow-freezing step without trehalose.

Keywords: Azelaic acid; Entrapment afficiency; Freeze-drying; Protransfersome; Transfersome