Abstract
Objective: This research was carried out to optimize luteolin-loaded transfersome formula with independent variables such as lipid–surfactant (totallipid) concentration and luteolin concentration.Methods: Luteolin-loaded transfersome was optimized by response surface methodology based on four parameters, namely, particle size (Z-average),polydispersity index, zeta potential, and entrapment efficiency. The transfersome formula was prepared using central composite design, and theselected independent variables were the total lipid (mixture of phospholipid and Tween 80) and luteolin concentrations. 14 formulas of luteolinloadedtransfersome were prepared by thin film hydration, followed by the sonication method.Results: The total lipid and luteolin concentration significantly affected the entrapment efficiency only. The other parameters were not affected by achange in these variables. The optimum formula of 4.88% total lipid and 0.5% luteolin with desirability value of 0.609 conformed with the predictionparameters. Vesicle imaging using transmission electron microscopy revealed spherical particles and the occurrence of particle aggregation. Theoptimum formula of luteolin-loaded transfersome possessed the following characteristics: Particle size of 286.03±8.46 nm, polydispersity indexof 0.480±0.013, zeta potential of -18.67±0.379 mV, and entrapment efficiency of 94.97±0.28 %. However, these values did not correspond to thepredicted values and were confirmed by the low adjusted and predicted R-squared values.Conclusion: This method can be applied to optimize the entrapment efficiency, and in the future, it can be used for further optimizing formula oftransfersome by including more variables.
Highlights
Luteolin is a chemical compound found in celery, chamomile flower, broccoli, and nutshell
Total lipid and luteolin concentration showed no effect on particle size, polydispersity index, and zeta potential, but influenced the entrapment efficiency of the luteolin-loaded transfersome
The total lipid concentration did not affect the Polydispersity index (PDI), and the luteolin concentration had a weak effect on the PDI
Summary
Luteolin is a chemical compound found in celery, chamomile flower, broccoli, and nutshell. It is a flavonoid present in plants in the aglycone form and glycoside (bonds with sugar molecules), such as cynaroside (luteolin 7-O-glycoside) [1]. It has the potential for the treatment of inflammation or gout owing to its anti-inflammatory activity and xanthine oxidase inhibition. The structure–activity relationship indicates that the presence of hydroxyl group at positions 7 and 5 in flavonoids significantly lowers the xanthine oxidase IC50 value [2]. Drug administration through the skin is supported to overcome the metabolism problem and increase the bioavailability of the drug
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