Skin permeation of econazole nitrate formulated in an enhanced hydrophilic multiple emulsion

Mycoses ◽  
2016 ◽  
Vol 60 (3) ◽  
pp. 166-177 ◽  
Author(s):  
Joaquim Suñer-Carbó ◽  
Antonio Boix-Montañés ◽  
Lyda Halbaut-Bellowa ◽  
Nelvis Velázquez-Carralero ◽  
Joanna Zamarbide-Ledesma ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Multiple Emulsion ◽  
Econazole Nitrate

Oleic Acid Vesicles as a new Approach for Transdermal Delivery of Econazole Nitrate: Development, Characterization, and In-vivo Evaluation in Wistar rats

2020 ◽  
Vol 15 ◽  
Author(s):  
Shivani Verma ◽  
Puneet Utreja
Keyword(s):  
Oleic Acid ◽  
Antifungal Activity ◽  
Side Effects ◽  
Fungal Infection ◽  
Wistar Rats ◽  
Skin Permeation ◽  
Cutaneous Candidiasis ◽  
Econazole Nitrate

Background:: Cutaneous candidiasis is a deep-seated skin fungal infection that is most commonly observed in immunocompromised patients. This fungal infection is conventionally treated with various formulations like gels and creams which are having different side effects and least therapeutic efficacy. Hence, it becomes necessary to develop a novel carrier system for the treatment of this deep-seated skin fungal infection. Econazole nitrate is the most widely used antifungal for the treatment of cutaneous candidiasis, therefore, in present research work we developed and evaluated econazole nitrate loaded oleic acid vesicles for treatment of cutaneous candidiasis through transdermal route. Methods:: Econazole nitrate loaded oleic acid vesicles were prepared by thin-film hydration and characterized for drug entrapment, vesicle size, zeta potential, polydispersity index (PDI), Fourier Transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis. Furthermore, the oleic acid vesicular gel was evaluated for ex-vivo skin permeation/retention and in-vitro and in-vivo antifungal activity in Wistar rats. Results:: Econazole nitrate loaded oleic acid vesicles showed high encapsulation of drug (74.76 ± 3.0%), acceptable size (373.4 ± 2.9 nm), and colloidal characteristics (PDI = 0.231 ± 0.078, zeta potential = -13.27 ± 0.80 mV). The oleic acid vesicular gel showed high skin permeation (Transdermal flux = 61.98 ± 2.45 μg/cm2/h), skin retention (35.90 ± 2.06%), in-vitro, and in-vivo antifungal activity compared to marketed cream (EcodermR) of econazole nitrate for a prolonged period of time (4 days). Conclusion:: Developed econazole nitrate loaded oleic acid vesicles could be used effectively in the treatment of cutaneous candidiasis with minimization of side effects of econazole nitrate with increased therapeutic efficacy.

scholarly journals Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 66 ◽  
Author(s):  
Joaquim Suñer-Carbó ◽  
Ana Calpena-Campmany ◽  
Lyda Halbaut-Bellowa ◽  
Beatriz Clares-Naveros ◽  
María Rodriguez-Lagunas ◽  
...  
Keyword(s):  
Water Solubility ◽  
Histological Analysis ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Release Kinetic ◽  
Multiple Emulsion ◽  
Vertical Diffusion ◽  
Skin Integrity

Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.

Chemical Permeation Enhancers for Transdermal Delivery of Thiocolchicoside: Assessment of Ex-vivo Skin Flux and In-vivo Pharmacokinetics

2017 ◽  
Vol 10 (5) ◽  
pp. 3827-3835
Author(s):  
Y Madhusudan Rao ◽  
Gayatri P ◽  
Ajitha M ◽  
P. Pavan Kumar ◽  
Kiran kumar
Keyword(s):  
Passive Control ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vivo Studies ◽  
Permeation Enhancers ◽  
Casting Technique ◽  
Chemical Permeation Enhancers ◽  
Chemical Permeation ◽  
In Vivo Pharmacokinetics

Present investigation comprises the study of ex-vivo skin flux and in-vivo pharmacokinetics of Thiocolchicoside (THC) from transdermal films. The films were fabricated by solvent casting technique employing combination of hydrophilic and hydrophobic polymers. A flux of 18.08 µg/cm2h and 13.37µg/cm2h was achieved for optimized formulations containing 1, 8-cineole and oleic acid respectively as permeation enhancers. The observed flux values were higher when compared to passive control (8.66 µg/cm2h). Highest skin permeation was observed when 1,8-cineole was used as chemical permeation enhancer and it considerably (2-2.5 fold) improved the THC transport across the rat skin. In vivo studies were performed in rabbits and samples were analysed by LC-MS-MS. The mean area under the curve (AUC) values of transdermal film showed about 2.35 times statistically significant (p<0.05) improvement in bioavailability when compared with the oral administration of THC solution. The developed transdermal therapeutic systems using chemical permeation enhancers were suitable for drugs like THC in effective management of muscular pain.    

Overcoming the Skin Permeation Barrier: Challenges and Opportunities

2015 ◽  
Vol 21 (20) ◽  
pp. 2698-2712 ◽  
Author(s):  
Carla Vitorino ◽  
Joao Sousa ◽  
Alberto Pais
Keyword(s):  
Skin Permeation ◽  
Challenges And Opportunities

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

Formulation, Optimization,and Ex-Vivo Evaluation of Novel Lipid Carriers for Enhanced Transdermal Delivery of Hydroquinone

2020 ◽  
Vol 12 ◽  
Author(s):  
Shivani Verma ◽  
Sukhjinder Kaur ◽  
Lalit Kumar
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Minimum Size ◽  
Prolonged Release ◽  
Freeze Dried ◽  
Ft Ir ◽  
Ir Analysis ◽  
Skin Retention

Background: HQ is used for hyper-pigmentation treatment using conventional creams and gels. These formulations show various disadvantages like poor skin permeation, allergic reactions, and repeated use decreasing patient compliance. Objectives: The present work involved formulation, statistical optimization, and characterization of nanostructured lipid carriers (NLCs) for efficient topical delivery of hydroquinone (HQ) for hyperpigmentation treatment. Methods: The NLCs were optimized exploring Box–Behnken design (BBD) using three independent variables and two dependent variables. Formulation having the minimum size and maximum drug entrapment was considered as optimized formulation. Optimized formulation was evaluated for drug release followed by its freeze-drying. The freeze-dried formulation was subjected to differential scanning calorimetry (DSC) analysis, X-raydiffraction (XRD) analysis, and Fourier transform-infrared spectroscopy (FT-IR) analysis. Furthermore, NLCs based gel was prepared by using Carbopol 934 as a gelling agent. NLCs based gel was evaluated for skin permeation, skin retention, and skin distribution (through confocal microscopic analysis) using pig ear skin. Results: Optimized NLCs showed smaller particle size [(271.9 ± 9) nm], high drug entrapment [(66.4 ± 1.2) %], tolerable polydispersity index (PDI) (0.221 ± 0.012), and zeta potential [(-25.9± 1.2) mV]. The FT-IR analysis revealed excellent compatibility between HQ and other excipients. The Carbopol 934 gel containing NLCs showed high transdermal flux [(163 ± 16.2) μg/cm2/h], permeability coefficient (0.0326 ± 0.0016), and skin permeation enhancement ratio (3.7 ± 0.4) compared to marketed cream of HQ. The results of confocal microscopic (CLSM) analysis revealed the accumulation of optimized NLCs in the lower epidermal layers of skin. Conclusion: NLCs based gel was considered effective in the topical delivery of HQ to treat hyper-pigmentation due high skin permeation, skin retention, and prolonged release of HQ.

Preparation and Development of Oral Controlled Release w/o/w Multiple Emulsion of Carbamazepine

2012 ◽  
Vol 2 (3) ◽  
pp. 213-222
Author(s):  
Kalpana L. Ramchandani ◽  
Jigna D. Joshi ◽  
Anita N. Lalwani ◽  
Pragna K. Shelat
Keyword(s):  
Controlled Release ◽  
Multiple Emulsion

Enhanced Skin Permeation of Punicalagin after Topical Application of Pluronic Micelles or Vesicles Loaded with Lafoensia pacari Extract

Planta Medica ◽  
2021 ◽  
Author(s):  
Sandra Alves de Sousa Garcia ◽  
Priscila Bianca Rodrigues da Rocha ◽  
Bruno dos Santos Souza ◽  
Andressa Tuane Santana Paz ◽  
Ana Luiza Caetano Negris ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Skin Permeation ◽  
Sol Gel ◽  
Extraction Procedure ◽  
Average Diameter ◽  
Skin Aging ◽  
Chemical Degradation ◽  
Vertical Diffusion ◽  
Flowing Liquid ◽  
Span 80

AbstractPunicalagin, the principal ellagitannin of Lafoensia pacari leaves, has proven antioxidant activity, and standardized extracts of L. pacari can be topically used for skin aging management. We hypothesized that Pluronic nanomicelles or vesicles could solubilize sufficiently large amounts of the standardized extracts of L. pacari and provide chemical stability to punicalagin. The standardized extracts of L. pacari were obtained with an optimized extraction procedure, and the antioxidant activity was characterized. Formulations containing Pluronic at 25% and 35% were obtained with or without Span 80. They were characterized by average diameter, polydispersity index, punicalagin content, physicochemical stability, and rheology. A release and skin permeation study was carried out in vertical diffusion cells. The extraction procedure allowed quantifying high punicalagin content (i.e., 141.61 ± 3.87 mg/g). The standardized extracts of L. pacari showed antioxidant activity for all evaluated methods. Pluronic at 25 and Pluronic at 35 with standardized extracts of L. pacari showed an average diameter of about 25 nm. The addition of Span 80 significantly increased the mean diameter by 15-fold (p < 0.05), indicating the spontaneous formation of vesicles. Pluronic formulations significantly protected punicalagin from chemical degradation (p < 0.05). Pluronic at 25 formulations presented as free-flowing liquid-like systems, while Pluronic at 35 resulted in an increase of about 44-fold in |ƞ*|. The addition of Span 80 significantly reduced the Pluronic sol-gel transition temperature (p < 0.05), indicating the formation of vesicles. Formulations with Span 80 significantly enhanced punicalagin skin permeation compared to formulations without Span 80 (p < 0.05). Formulations with Span 80 were demonstrated to be the most promising formulations, as they allowed significant permeation of punicalagin (about 80 to 315 µg/cm2), which has been shown to have antioxidant activity.

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