Design and Formulation of Optimized Microemulsions for Dermal Delivery of Resveratrol

The objective of this study was to formulate optimal formulations of microemulsions (MEs) and evaluate their feasibility for delivery of resveratrol into human skinex vivo.Oil-in-water MEs were formulated using surfactant (S) PEG-8 caprylic/capric glycerides and cosurfactant (CoS) polyglyceryl-6-isostearate. Ethyl oleate was used as an oily phase. MEs were formulated using 5 : 1, 6 : 1, and 7 : 1 surfactant and cosurfactant (S : CoS) weight ratios. Pseudoternary phase diagrams were constructed and optimal compositions of MEs were obtained using Design Expert software. Mean droplet size for optimized ME formulations was determined to be 68.54 ± 1.18 nm, 66.08 ± 0.16 nm, and 66.66 ± 0.56 nm for systems with S : CoS weight ratios 5 : 1, 6 : 1, and 7 : 1, respectively. Resveratrol loading resulted in mean droplet size increase. The distribution of droplet size between fractions changed during storage of formulated MEs. Results demonstrated the increase of number of droplets and relative surface area when S : CoS weight ratios were 6 : 1 and 7 : 1 and the decrease when S : CoS weight ratio was 5 : 1. The highest penetration of resveratrol into the skinex vivowas determined from ME with S : CoS weight ratio 5 : 1. It was demonstrated that all MEs were similar in their ability to deliver resveratrol into the skinex vivo.

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Dermal Delivery of Selected Polyphenols from Silybum marianum. Theoretical and Experimental Study

Molecules ◽

10.3390/molecules24010061 ◽

2018 ◽

Vol 24 (1) ◽

pp. 61 ◽

Cited By ~ 8

Author(s):

Pavel Kosina ◽

Markéta Paloncýová ◽

Alena Rajnochová Svobodová ◽

Bohumil Zálešák ◽

David Biedermann ◽

...

Keyword(s):

Human Skin ◽

Lipid Membranes ◽

In Silico ◽

High Performance ◽

Ex Vivo ◽

Chemical Properties ◽

Theoretical Models ◽

Silybum Marianum ◽

Model Lipid Membranes ◽

Dermal Delivery

Silymarin is a well-known standardized extract from the seeds of milk thistle (Silybum marianum L., Asteraceae) with a pleiotropic effect on human health, including skin anticancer potential. Detailed characterization of flavonolignans properties affecting interactions with human skin was of interest. The partition coefficients log Pow of main constitutive flavonolignans, taxifolin and their respective dehydro derivatives were determined by a High Performance Liquid Chromatography (HPLC) method and by mathematical (in silico) approaches in n-octanol/water and model lipid membranes. These parameters were compared with human skin intake ex vivo. The experimental log Pow values for individual diastereomers were estimated for the first time. The replacement of n-octanol with model lipid membranes in the theoretical lipophilicity estimation improved the prediction strength. During transdermal transport, all the studied compounds permeated the human skin ex vivo; none of them reached the acceptor liquid. Both experimental/theoretical tools allowed the studied polyphenols to be divided into two groups: low (taxifolin, silychristin, silydianin) vs. high (silybin, dehydrosilybin, isosilybin) lipophilicity and skin intake. In silico predictions can be usefully applied for estimating general lipophilicity trends, such as skin penetration or accumulation predictions. However, the theoretical models cannot yet provide the dermal delivery differences of compounds with very similar physico-chemical properties; e.g., between diastereomers.

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Water Soluble Chitosan Mediated Voriconazole Microemulsion as Sustained Carrier for Ophthalmic Application: In vitro/Ex vivo/In vivo Evaluations

Open Pharmaceutical Sciences Journal ◽

10.2174/1874844901603010215 ◽

2016 ◽

Vol 3 (1) ◽

pp. 215-234 ◽

Cited By ~ 8

Author(s):

Rohit Bhosale ◽

Omkar Bhandwalkar ◽

Anita Duduskar ◽

Rahul Jadhav ◽

Pravin Pawar

Keyword(s):

Zeta Potential ◽

Phase Diagrams ◽

Droplet Size ◽

Ex Vivo ◽

Water Soluble ◽

Polydispersity Index ◽

Modified Chitosan ◽

Mucoadhesive Polymer

Background: Voriconazole (VCZ) is a lipophilic candidate, effective against fungal infections like ocular keratitis and endopthalmitis. Objective: The purpose to develop, optimize and characterize voriconazole microemulsion as sustained medication for ophthalmic application. Methods: The pseudo-ternary phase diagrams were developed using oleic acid, isopropyl myristate and isopropyl palmitate (oil phases), tween 80 (surfactant), propylene glycol (co-surfactant), distilled water (aqueous phase) and modified chitosan (Mod.CH) as mucoadhesive polymer. The optimum composition of oil, Smix and water was selected on the basis of phase diagrams and as mucoadhesive polymer Mod.CH was used in the formulations. All the formulations were evaluated for thermodynamic stability/dispersibility, physicochemical parameters (droplet size, polydispersity index, zeta potential, drug content, viscosity, pH and conductivity), in vitro, ex vivo and in vivo studies. Results: All formulations showed droplet size below 250 nm, positive zeta potential and polydispersity index below 0.5. The in vitro drug release study performed on selected formulations showed maximum sustained release than marketed formulation. The in vitro transcorneal permeation experiment of formulations suggests that optimized formulations showed better permeation. The selected formulation of voriconazole microemulsion was able to produce maximum antifungal activity against Candida albicans when compared to marketed formulation. In vivo study performed on rabbit eyes, found more drug concentration in aqueous humor of optimized formulation; the AUC0→t of IPMVM-11 was approximately 6.84-fold higher than VOZOLE and efficiently enhanced the corneal bioavailability. Conclusion: The modified chitosan based on voriconazole loaded microemulsion was promising novel carrier for sustained action in ophthalmic medication.

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Water reorientation dynamics in colloidal water–oil emulsions

Physical Chemistry Chemical Physics ◽

10.1039/d1cp03182a ◽

2021 ◽

Author(s):

Eliane P. van Dam ◽

Roland Gouzy ◽

Eddie Pelan ◽

Krassimir P. Velikov ◽

Huib J. Bakker

Keyword(s):

Infrared Spectroscopy ◽

Surface Area ◽

Droplet Size ◽

Total Surface Area ◽

Oil Droplets ◽

Pump Probe ◽

Oil In Water ◽

Reorientation Dynamics ◽

Oil Emulsions

Polarization resolved pump–probe infrared spectroscopy of colloidal oil-in-water emulsions demonstrates that the total surface area of oil droplets is independent of the average droplet size, indicating that the oil droplets are strongly corrugated.

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Faculty Opinions recommendation of Harnessing the Secretome of Hair Follicle Fibroblasts to Accelerate Ex Vivo Healing of Human Skin Wounds.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.736855350.793573090 ◽

2020 ◽

Author(s):

Giulio Gabbiani

Keyword(s):

Hair Follicle ◽

Human Skin ◽

Ex Vivo ◽

Skin Wounds

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Stabilization and Release of Palm Tocotrienol Emulsion Fabricated Using pH-Sensitive Calcium Carbonate

Foods ◽

10.3390/foods10020358 ◽

2021 ◽

Vol 10 (2) ◽

pp. 358

Author(s):

Phui Yee Tan ◽

Beng Ti Tey ◽

Eng Seng Chan ◽

Oi Ming Lai ◽

Hon Weng Chang ◽

...

Keyword(s):

Calcium Carbonate ◽

Droplet Size ◽

Entrapment Efficiency ◽

Ph Sensitive ◽

Emulsion System ◽

Ph Responsive ◽

Small Droplet ◽

Homogenization Time ◽

Oil In Water ◽

Ph Range

Calcium carbonate (CaCO3) has been utilized as a pH-responsive component in various products. In this present work, palm tocotrienols-rich fraction (TRF) was successfully entrapped in a self-assembled oil-in-water (O/W) emulsion system by using CaCO3 as the stabilizer. The emulsion droplet size, viscosity and tocotrienols entrapment efficiency (EE) were strongly affected by varying the processing (homogenization speed and time) and formulation (CaCO3 and TRF concentrations) parameters. Our findings indicated that the combination of 5000 rpm homogenization speed, 15 min homogenization time, 0.75% CaCO3 concentration and 2% TRF concentration resulted in a high EE of tocotrienols (92.59–99.16%) and small droplet size (18.83 ± 1.36 µm). The resulting emulsion system readily released the entrapped tocotrienols across the pH range tested (pH 1–9); with relatively the highest release observed at pH 3. The current study presents a potential pH-sensitive emulsion system for the entrapment and delivery of palm tocotrienols.

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