Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

ABSTRACT Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p < 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm2, respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm2, respectively). Further studies to evaluate skin sensitization and irritation are now necessary.

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Vitamin E TPGS based nanogel for the skin targeting of high molecular weight anti-fungal drug: development and in vitro and in vivo assessment

RSC Advances ◽

10.1039/c5ra08374e ◽

2015 ◽

Vol 5 (66) ◽

pp. 53671-53686 ◽

Cited By ~ 11

Author(s):

Lakhvir Kaur ◽

Subheet Kumar Jain ◽

Kanwaldeep Singh

Keyword(s):

Molecular Weight ◽

Vitamin E ◽

Skin Permeation ◽

Deposition Potential ◽

Vitamin E Tpgs ◽

Skin Targeting ◽

Anti Fungal ◽

In Vivo Assessment

Enhanced skin permeation and deposition potential of nanogel containing Vitamin E TPGS.

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In vitro evaluation of transdermal nicotine delivery systems commercially available in Brazil

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502013000300020 ◽

2013 ◽

Vol 49 (3) ◽

pp. 579-588 ◽

Cited By ~ 11

Author(s):

André Luís Morais Ruela ◽

Eduardo Costa Figueiredo ◽

Aline Gravinez Perissinato ◽

Ana Carolina Zogbi Lima ◽

Magali Benjamim Araújo ◽

...

Keyword(s):

Release Kinetics ◽

Skin Permeation ◽

Delivery Systems ◽

Regenerated Cellulose ◽

Nicotine Patches ◽

Nicotine Delivery ◽

Transdermal Nicotine ◽

Experimental Apparatus ◽

Permeation Studies

The aim of this study was to develop and validate a method for evaluating the release and skin permeation from transdermal nicotine patches using the vertical diffusion cell (VDC). The VDC is an experimental apparatus employed in research, development, and the pharmaceutical field because it can simulate conditions closest to those established in clinical trials. Two transdermal nicotine delivery systems marketed in Brazil to release 14 mg over 24 hours were evaluated. Release studies were carried out using a regenerated cellulose dialysis membrane and permeation studies were carried out using excised porcine ear skin. The results indicated that nicotine release from both evaluated patches follows Higuchi's release kinetics, while skin permeation studies indicated zero-order release kinetics. Nicotine release rates were different between both evaluated patches, but drug permeation rates were not significantly different. According to validation studies, the method was appropriate for evaluating in vitro performance of nicotine patches. The proposed method can be applied to in vitro comparative studies between different commercial nicotine patches and may be used as an auxiliary tool in the design of new transdermal nicotine delivery systems.

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In vitro comparative studies of transdermal nicotine delivery systems

International Journal of Pharmaceutics ◽

10.1016/s0378-5173(96)04843-0 ◽

1997 ◽

Vol 148 (2) ◽

pp. 177-189 ◽

Cited By ~ 5

Author(s):

Derek Lewis ◽

Mário Paulo ◽

Eduardo Faustino ◽

Asçensão Farinha

Keyword(s):

Comparative Studies ◽

Delivery Systems ◽

Nicotine Delivery ◽

Transdermal Nicotine

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Improved oral bioavailability and target delivery of 6-shogaol via vitamin E TPGS-modified liposomes: Preparation, in-vitro and in-vivo characterizations

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2020.101842 ◽

2020 ◽

Vol 59 ◽

pp. 101842

Author(s):

Rui Bao ◽

Qi-Long Wang ◽

Ran Li ◽

Michael Adu-Frimpong ◽

Elmurat Toreniyazov ◽

...

Keyword(s):

Vitamin E ◽

Oral Bioavailability ◽

Target Delivery ◽

Vitamin E Tpgs

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Central composite design-based optimization of lopinavir vitamin E-TPGS micelle: In vitro characterization and in vivo pharmacokinetic study

Colloids and Surfaces B Biointerfaces ◽

10.1016/j.colsurfb.2020.111149 ◽

2020 ◽

Vol 194 ◽

pp. 111149 ◽

Cited By ~ 1

Author(s):

Hitendra Shaligram Mahajan ◽

Payal Hasmukhlal Patil

Keyword(s):

Vitamin E ◽

Central Composite Design ◽

Pharmacokinetic Study ◽

In Vitro Characterization ◽

Vitamin E Tpgs ◽

Central Composite

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Antifungal efficacy of Itraconazole loaded PLGA-nanoparticles stabilized by vitamin-E TPGS: In vitro and ex vivo studies

Journal of Microbiological Methods ◽

10.1016/j.mimet.2019.01.020 ◽

2019 ◽

Vol 161 ◽

pp. 87-95 ◽

Cited By ~ 10

Author(s):

Adel A. Alhowyan ◽

Mohammad A. Altamimi ◽

Mohd Abul Kalam ◽

Abdul Arif Khan ◽

Mohamed Badran ◽

...

Keyword(s):

Vitamin E ◽

Ex Vivo ◽

Plga Nanoparticles ◽

Vitamin E Tpgs ◽

Antifungal Efficacy

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Exemestane encapsulated vitamin E-TPGS–polymeric nanoparticles: preparation, optimization, characterization, and in vitro cytotoxicity assessment

Artificial Cells Nanomedicine and Biotechnology ◽

10.3109/21691401.2016.1163714 ◽

2016 ◽

Vol 45 (3) ◽

pp. 522-534 ◽

Cited By ~ 6

Author(s):

Brahmeshwar Mishra ◽

Ravi Padaliya ◽

Ravi R. Patel

Keyword(s):

Vitamin E ◽

Polymeric Nanoparticles ◽

In Vitro Cytotoxicity ◽

Vitamin E Tpgs ◽

Cytotoxicity Assessment

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Optimized Preparation of Capsaicin-Loaded Nanoparticles Gel by Box-Behnken Design

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.1061-1062.359 ◽

2014 ◽

Vol 1061-1062 ◽

pp. 359-368 ◽

Cited By ~ 1

Author(s):

Mei Ling Tang ◽

Li Hua Chen ◽

Dong Sheng Zhou ◽

Wei Feng Zhu ◽

Yong Mei Guan ◽

...

Keyword(s):

Skin Permeation ◽

Skin Irritation ◽

Morphological Characteristics ◽

Entrapment Efficiency ◽

Box Behnken Design ◽

Irritation Test ◽

Predicted Values ◽

Skin Irritation Test

A three-factor three-level Box-Behnken design(BBD) was employed to optimize capsaicin-loaded nanoparticles(Cap-NPs), and its properties in vitro and in vivo were evaluated. Particle size, morphological characteristics, entrapment efficiency of Cap-NPs were investigated respectively by Zetasizer, H7000 TEM and HPLC. Release, skin permeation and skin irritation test were investigated on mouse and rabbits. The predicted values of Cap-NPs were 94.50±6.33% for entrapment efficiency(EE) and 170.30±7.81 nm for particle mean diameter(PMD) under optimal conditions which were 346.33 bar (homogenization pressure, X1), 4.67 min(homogenization time, X2), and 15421.42 rpm (shear rate, X3). The in vitro permeation study showed that capsaicin permeability in NPs-gel was a 2.80-fold greater flux values than conventional ointment after 24 h. Cap-NPs-gel produce no observable skin irritation in rabbits within 72h. The optimized Cap-NPs-gel would be a good candidate for transdermal delivery.

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