Novel Umbelliferone Phytosomes: Development and Optimization Using Experimental Design Approach and Evaluation of Photo-Protective and Antioxidant Activity

Abstract

<p><strong>Objective: </strong>The objective of this study was to develop a novel formulation (Phytosome) of umbelliferone with phospholipid for improved permeability, solubility and hence better pharmacological action.</p><p><strong>Methods: </strong>The phytosomal complex was prepared by using solvent evaporation method and optimised by applying the Box-Behnken design on the basis of complexation rate and partition coefficient. The formation of phytosomes was confirmed by FTIR, DSC, SEM, XRD, HPTLC and NMR by comparing the results of the complex with the drug. The photoprotective potential of complex against UV-exposure was evaluated in rats and compared with the drug by incorporating it in a gel and estimating the antioxidant enzymes in skin namely reduced glutathione, superoxide dismutase, lipid peroxidation and catalase.</p><p><strong>Results: </strong>The crystalline drug was completely converted to amorphous complex. The complex showed a good practical yield, drug content and particle size was in the range. The solubility of the complex was determined by partition coefficient method and was found to be better than the drug. The <em>ex vivo</em> and <em>in-vitro</em> permeation of the complex showed improved permeation for complex than the drug. The <em>in vitro</em> antioxidant activity of complex was evaluated by DPPH and ferrozine antioxidant assay and was better than the drug. The photoprotective action of the complex was found to be better than drug on the basis of the content of antioxidant enzymes estimated in the skin.</p><strong>Conclusion: </strong>The phytosomal complex was found to show better solubility in the water phase and oil phase, better permeation, better antioxidant activity and a better photo-protective activity when compared to umbelliferone.

Rutin–phospholipid complex in polymer matrix for long-term delivery of rutin via skin for the treatment of inflammatory diseases

“…These results suggest that the RNPs are more permeable than free rutin (p < .05), across both the skin specimens. Our results are in good agreement with previous studies reported with phospholipid complex of sinigrin [57], elagic acid [58], curcumin [59], puerarin [60], oxymatrine [61], lawsone [62], ferrulic acid [63], morin [64] and umbelliferon [65]. Compared to free drug, drug-phospholipid complex enhanced the rate and extent of drug permeation across the biomembrane.…”

Design and Characterization of PLA Bilayer Films Containing Lignin and Cellulose Nanostructures in Combination With Umbelliferone as Active Ingredient

“…FTIR analysis was performed on powders (Figure 2A), monolayer (Figure 2B), and bilayer films (Figure 2C) in order to identify the influence of the additives on the chemical structure of the PLA. The FT-IR spectrum of umbelliferone showed a sharp peak of OH group at 3,153 cm −1 (Ittadwar and Puranik, 2017), frequencies identified at 3,122 and 2,987 cm −1 are designated to C-H stretching vibrations, single bonded carbonyl group vibrations at 1388, 1,345, and 1,233 cm −1 , while frequencies at 1,578, 1,454, 1,446, 1,409, and 1,386 cm −1 have been designated to C-C stretching vibrations (Rexali, 2007).…”

Antibacterial Activity of Chlorogenic Acid Phytovesicles Against Resistant Bacteria: Development, Optimization and Evaluation

“…The spectra of Phospholipon 90H gave characteristic C-H stretching band of long chain fatty acid at 2916.37 cm -1 and 2848.86 cm -1 [28]. Also, a C=O band at 1467.83 cm -1 ; a − a (so3)3 band at 923.90 cm -1 and a P-O-C stretch at 968.27 cm -1 [29].…”