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Preparation and optimization of fisetin loaded glycerol based soft nanovesicles by Box-Behnken design.

Abstract：

:The present study focused on the development and optimization of glycerosomes for dermal delivery of fisetin. The fisetin loaded glycerosomes formulation was optimized by Box-Behnken design. The independent variables were the lipoid S 100, glycerol, and sonication time, whereas the dependent variables were the vesicles size, entrapment efficiency, and flux. The mechanism of skin penetration of fisetin loaded glycerosomes formulation was determined by the DSC and FTIR studies. Confocal scanning microscopy was used to detect the penetration ability of glycerosomes. The optimized fisetin loaded glycerosomes formulation was converted into a Carbopol® gel matrix, and the latter was analyzed for various parameters. The optimized formulation of glycerosomes presented vesicles size, entrapment efficiency and flux of 138.8 ± 4.09 nm, 86.41 ± 2.95% and 5.04 ± 0.17 µg/cm2/h, respectively. The transmission electron microscopy of optimized fisetin loaded formulation revealed the spherical and sealed structure of glycerosomes vesicles. The confocal study confirmed that the Rhodamine B incorporated glycerosomes penetrated up to deeper layers of skin. The DSC and FTIR studies revealed that the hydration of skin layers and skin lipid fluidization could be the penetration mechanism of fisetin glycerosomes formulation. The optimized fisetin loaded glycerosomes gel formulation presented a flux of 4.24 ± 0.14 μg/cm2/h, and exhibited zero-order release kinetics. The texture analysis of fisetin glycerosomes gel displayed a sufficient hardness, consistency, cohesiveness, and index of viscosity. It was concluded that the prepared fisetin loaded glycerosomes gel was suitable for the dermal application.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Moolakkadath T,Aqil M,Ahad A,Imam SS,Praveen A,Sultana Y,Mujeeb M

doi

10.1016/j.ijpharm.2020.119125

subject

Has Abstract

pub_date

2020-03-30 00:00:00

pages

119125

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(20)30109-5

journal_volume

578

pub_type

杂志文章

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