Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers

Abstract

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm2·h up to 20.00 μg/cm2·h and 4.90 up to 53.52 μg/cm2, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.

Improvement in Skin Penetration Capacity of Linalool by Using Microemulsion as a Delivery Carrier: Formulation Optimization and In Vitro Evaluation

“…To determine the influenced degree of component, the powerful statistical method response surface methodology was used [ 26 , 27 , 28 ]. The obtained data (independent variables and desired responses) were fitted to linear, interactive, quadratic and cubic equations.…”

“…Male Sprague Dawley rats weighing 250–300 g were anesthetized by an intraperitoneal injection of 0.75 g/kg polyurethane aqueous solution. Then, 500 μL of distilled water (negative control), 0.8% paraformaldehyde (standard stimulation group), linalool solution and a tested linalool-loaded microemulsion formulation were evenly applied to 2.54 cm 2 of shaved abdominal skin, and a paraffin film was sealed [ 25 , 26 ]. After 24 h, the animals were sacrificed and the treated skin was excised for histological examination.…”

“…The p -values for model and lack of fit should be less than 0.05 and greater than 0.05, respectively. The coefficient of the X term represents the influence strength of the independent variable [ 25 , 26 , 28 , 29 ].…”

Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein

“…The formulation scientists have adopted many strategies to overcome GEN-described limitations. Including surface modified phytosomes (Komeil et al., 2022 ), metal-organic framework (Botet-Carreras et al., 2021 ), transmucosal solid lipid nanoparticles (Obinu et al., 2021 ), microemulsion (Vu et al., 2021 ), lactalbumin nanoparticles (Dev et al., 2021 ), phytosomes (Komeil et al., 2021 ), zein/carboxymethyl chitosan nanoparticles (Xiao et al., 2020 ), folic acid-conjugated chitosan nanoparticles (Cai et al., 2017 ) and chitosan/Eudragit nanoparticles ((Patel et al., 2015 ). After carefully reviewing these reports, we noticed that the authors only addressed the anti-cancer potential of these nanoformulations without analysis of GEN solubility, permeability, oral bioavailability, and anti-inflammatory activity.…”

Biocompatible Microemulsions Based on Oleic Acid Modified with Piperidinium Surfactants

“…These demands are to a large extent met in the case of microemulsions, which usually consist of aqueous and oil (hydrocarbon) phases separated by a layer of micelle-forming surfactant, sometimes in the presence of a co-surfactant [5][6][7]. Nonionic surfactants, which are low-toxic and compatible with many biologically active species, have been often used in the preparation of microemulsions intended for biomedical applications [8][9][10]. However, they have exhibited poorer performance in comparison with more toxic ionic surfactants.…”