Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model

Abstract

Background Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin. Methods Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive index (PDI), microscopy using Atomic force microscopy (AFM), Scanning electron microscope (SEM) and Transmission electron microscopy (TEM) and Interaction of drug and excipients were studied using Fourier transform infra-red (FTIR) spectroscopy, Differential scanning colorimetry (DSC), Thermo gravimetric analysis (TGA). Further, ethosomal formulations of flurbiprofen were evaluated for stability study of three months and in vitro drug permeation study was carried out using albino rat skin. In addition, skin irritation test was evaluated by Draize test and in vivo study of prepared formulation was examined through paw edema assay by inducing carrageenan and cold plate method. Results Amongst all formulations, EF5 formulation exhibited ideal surface morphology, with maximum entrapment efficiency (95%) with optimal excipient concentration i.e. 200 mg phospholipid and 35% ethanol. The ideal vesicle size was achieved as 162.2 ± 2 nm, with zeta potential − 48.14 ± 1.4 mV with the PDI of 0.341. In-vitro permeation study shows a release of 82.56 ± 2.11 g/cm 2 in 24 h and transdermal flux was found as 226.1 μg/cm 2 /h. Cold plate test indicates that the formulation EF5 showed a marked analgesic activity and Carrageenan induced paw edema test indicates that the formulation EF5 inhibits the increase in paw edema. Ethosomal suspension at 4 °C showed maximum stability. Conclusions The overall study concluded that this ethosomal approach offers a new delivery system for sustained and targeted delivery for flurbiprofen. Electronic supplementary material The online version of this article (10.1186/s12944-019-1064-x) contains supplementary material, which is available to authorized users.

Gelatin-Based Hydrogels for the Controlled Release of 5,6-Dihydroxyindole-2-Carboxylic Acid, a Melanin-Related Metabolite with Potent Antioxidant Activity

“…Severe limitations in this perspective stem from the ease of this compound to undergo oxidation with subsequent loss of its properties. In addition, proper formulation allowing for vehiculation through the skin and a controlled release would greatly add to the beneficial effects prolonging the action and taking the bioavailable concentrations relatively low.In recent years, several natural compounds have been tested for the topical treatment of skin disorders by use of a variety of transcutaneous delivery systems including lipophilic nanoparticles like liposomes [12], solid lipid nanoparticles [13,14], nanostructured lipid carriers, monoolein aqueous dispersions [15,16], ethosomes [17,18], and lecithin organogels [19,20]. Speed up of wound healing process by a nanohydrogel embedding an antioxidant compound like baicalin has been described that exhibited optimal performance for a complete skin restoration and inhibition of specific inflammatory markers [21].A variety of hydrophilic delivery systems have also been explored such as gelatin, the product of collagen hydrolysis, as it offers several advantages including the historical safe use in a wide range of medical applications, low costs, inherent electrostatic binding properties, and proteolytic degradability.…”

“…In recent years, several natural compounds have been tested for the topical treatment of skin disorders by use of a variety of transcutaneous delivery systems including lipophilic nanoparticles like liposomes [12], solid lipid nanoparticles [13,14], nanostructured lipid carriers, monoolein aqueous dispersions [15,16], ethosomes [17,18], and lecithin organogels [19,20]. Speed up of wound healing process by a nanohydrogel embedding an antioxidant compound like baicalin has been described that exhibited optimal performance for a complete skin restoration and inhibition of specific inflammatory markers [21].…”

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

“…The biphasic release pattern was observed in an in-vitro drug release assay. The burst release at initial time points is possibly due to the drug particles associated with the vesicle surface, followed by the slow release of the drug entrapped in the ethosomal core [ 12 ]. It is plausible that the high % of ethanol (~ 40% (v/v)) can increase the drug release at early time points due to increased fluidity of the ethosomal vesicle and increased drug solubility in the hydro-ethanolic core of ethosomes [ 46 ].…”

“…Ethosomes are lipid based vesicular drug carriers which consists of high ethanol concentration. The high concentration of ethanol in ethosomes imparts them the ability to modify the highly dense alignment of the lipid bilayers in the SC, thereby ensuring deeper drug penetration [ 12 ]. The presence of ethanol also impart a net negative on the surface of ethosomes that provide better stability due to electrostatic repulsion [ 13 ].…”

The New Frontiers in Neurodegenerative Diseases Treatment: Liposomal-Based Strategies

“…Flurbiprofen is largely used in ND treatments for its antiinflammatory effect. The permeation of ethosomal-flurbiprofen (EF) formulations was assessed in the albino rat model (Paliwal et al, 2019). The reported results showed a high encapsulation drug efficiency (95 %); in addition, the permeation efficacy was equal to (82.56 ± 2.11) g/cm 2 in 24 h, and transdermal flux was found as 226.1 µg/cm 2 /h.…”