Abstract
Objective : The aim of the present study was to formulate and characterize rutin ethosomes and to evaluate the rutin ethosomes to enhance its skin permeation rate as compared to parent drug, rutin. Materials and Methods : Rutin ethosomes were formulated by cold method and optimized using 2 3 factorial design by design expert software (version 8.0). The optimized rutin ethosomes were characterized for particle size distribution, vesicular shape using scanning electron microscopy, zeta potential, entrapment efficiency and short term stability studies. A specially designed franz diffusion cell was used for the percutaneous absorption studies of optimized rutin ethosomes using pig ear skin and the results were analysed using DD solver 8 software. Results and Discussion : The entrapment efficiency of optimized ethosomes prepared using phospholipid concentration of 2.5 g with 30 ml ethanol for 12.5 minutes, was found to be maximum i.e. 73.9 %. Lipid vesicular system of rutin exhibited a negative zeta potential of -46.0 mV indicating a high degree of stability for rutin ethosomes. In vitro drug permeation studies of pure rutin and rutin ethosomes suggested that rutin ethosomes were better able to permeate across pig ear skin at the end of 120 minutes than pure rutin. Therefore, rutin ethosomes were better able to facilitate permeation of rutin deeply into the pig ear skin when compared with pure rutin. Conclusion : Rutin ethosomal formulation has tremendous potential to serve as a topical drug delivery system due to its enhanced rate of permeation.
Highlights
Rutin known as quercetin-3-rutinoside or sophorin is a flavonol glycoside comprised of the flavonol quercetin and the disaccharide rutinose (Figure 1)
No change in colour and sedimentation was observed in optimized rutin ethosomes stored at 4oC and 25oC, slight colour change and sedimentation occurred in the optimized rutin ethosomes stored at high temperature i.e. 40oC at the end of 30th day
We investigated the in vitro skin permeation rate of a novel vesicular system of rutin in the form of rutin ethosomes
Summary
Rutin known as quercetin-3-rutinoside or sophorin is a flavonol glycoside comprised of the flavonol quercetin and the disaccharide rutinose (Figure 1). It is a polyphenolic compound widely distributed in higher plants. High concentrations of rutin are found in buckwheat seed, fruits and fruit rinds, especially in citrus fruits (e.g. orange, grapefruit, lemon etc). It has several pharmacological activities including anti-inflammatory[1], antioxidant[2], neuroprotective[3], cardioprotective[4], antiarthritis[5] and psoriasis[6]. In the present research study, rutin has been used for formulating a novel vesicular carrier in the form of rutin because rutin is reported to have good antioxidant property
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