Objective: Grape seed extract (GSE) contains abundant phenolic compounds with high antioxidant activity. Phenolic compounds in GSE have an inadequate penetration due to its hydrophilicity. The objective of this research was to formulate GSE phytosome serum to overcome its penetration problem. Methods: Phytosomes were prepared in three formulas based on the mass ratio between the extract and the phosphatidylcholine, 1:0.5, 1:1, and 1:2, using the thin layer hydration method. Phytosomes were then characterized their morphology, particle size distribution, zeta potential and their entrapment efficiency. The selected phytosome was formulated into a gel-based serum. Then, physicochemical evaluations of the serum, including organoleptic test (color, odor, and syneresis), homogeneity, pH, viscosity and rheology properties, were conducted. An in vitro penetration study using the Franz diffusion cells was performed on phytosome and nonphytosome serum (as a control). Results: The results showed that F2 was the optimal phytosome among other formula with a spherical shape, Dmean volume was 398.23 nm, zeta potential at -25.2 mV and entrapment efficiency of 75.01±0.25%. The cumulative amount of total phenolic penetrated from the phytosome serum and control were 27.25±0.67% and 11.97±0.49%, respectively. The phytosome serum had a flux value of 243.11±7.94 μg/cm2.hour, while the control serum was 68.56±5.54 μg/cm2. hour. Conclusion: This research demonstrated that phytosome could increase the penetration of the drug in serum dosage form.
Key words: Franz diffusion Cell, Grape seed extract, Penetration, Phytosome, Serum, Total phenolic.