Physicochemical Performances of Indomethacin in Cholesteryl Cetyl Carbonate Liquid Crystal as a Transdermal Dosage

Aeinleng, Nunchanit; Songkro, Sarunyoo; Noipha, Kusumarn; Srichana, Teerapol

doi:10.1208/s12249-012-9768-5

Cited by 8 publications

(2 citation statements)

References 33 publications

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“…31 However, it is crucial to inhibit the interactions between the assembling molecules and the substrate in order to facilitate the molecule grouping from individual crystals to the spherulitic arrangement, especially at lower growing rates under mild nonequilibrium conditions. Two-dimensional spherulitc assemblies of small organic molecules could potentially be applied as a transdermal technology, 35,36 where SS can permeate across the skin through passive diffusion. 37 One of the advantages of using spherulites is that they possess an enhanced mechanical strength compared to their nonspherulitic deposits, 38 which indicates that the growth of SS spherulites on the surface of different substrates employed in the fabrication of mucoadhesive transdermal or buccal patches could be used to develop drug delivery systems for the control of pulmonary diseases.…”

Section: Methodsmentioning

confidence: 99%

Impact of Substrate Properties on the Formation of Spherulitic Films: A Case Study of Salbutamol Sulfate

Serrano

Mugheirbi

O’Connell

et al. 2016

Crystal Growth & Design

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Spherulitic assemblies have applications as carriers for drug delivery and as targeting vectors. Presently, the driving force behind the formation of spherulites comprising small drug molecules is not fully understood. Herein, the impact of different substrate types on spherulitic crystallization of salbutamol sulfate (SS) was investigated. Freshly cleaved mica, silicon (111) wafer (SiW), uncoated borosilicate glass (UG), silane coated glass (CG) and stainless steel (MS) were used as substrates. It was demonstrated that the spherulite growth can be controlled via the substrate selection. Spherulite formation was inhibited on hydrophilic substrates, such as mica, possibly due to stronger intermolecular interactions between SS and the substrate than SS-SS interactions. Contact angle measurements established that mica possessed the lowest contact angle (15.1±0.5°) and the values of this parameter increased in the order of UC˂SiW˂CG˂MS. Substrate roughness also played a key role in controlling spherulite formation. SiW, UC and CG had isotropic surfaces with low average roughness, facilitating spherulite formation. Overall, this work demonstrates that it is possible to successfully produce SS spherulites using a single step process at room temperature. Furthermore, the formation of SS spherulites can be tuned by the hydrophobicity of the substrate, an approach that could be applied to assembling spherulites of other small organic molecules. Presently, the driving force behind the formation of spherulites comprising small drug molecules is not fully understood. Herein, the impact of different substrate types on spherulitic crystallization of salbutamol sulfate (SS) was investigated. Freshly cleaved mica, silicon (111) wafer (SiW), uncoated borosilicate glass (UG), silane coated glass (CG) and stainless steel (MS) were used as substrates. It was demonstrated that the spherulite growth can be controlled via the substrate selection. Spherulite formation was inhibited on hydrophilic substrates, such as mica, possibly due to stronger intermolecular interactions between SS and the substrate than SS-SS interactions. Contact angle measurements established that mica possessed the lowest contact angle (15.1±0.5°) and the values of this parameter increased in the order of UC˂SiW˂CG˂MS. Substrate roughness also played a key role in controlling spherulite formation. SiW, UC and CG had isotropic surfaces with low average roughness, facilitating spherulite formation. Overall, this work demonstrates that it is possible to successfully produce SS spherulites using a single step process at room temperature. Furthermore, the formation of SS spherulites can be tuned by the hydrophobicity of the substrate, an approach that could be applied to assembling spherulites of other small organic molecules.

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Section: Methodsmentioning

confidence: 99%

Impact of Substrate Properties on the Formation of Spherulitic Films: A Case Study of Salbutamol Sulfate

Serrano

Mugheirbi

O’Connell

et al. 2016

Crystal Growth & Design

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show abstract

“…Moreover, their highly ordered internal structures offer the potential for slow drug release (Chen, Ma, Gui, 2014). Indeed, liquid crystalline systems have shown to improve the topical/ transdermal delivery of many drugs (Bender et al, 2005(Bender et al, , 2008Peng et al, 2010;Kravchenko, Boyko, Novikova, 2011;Aeinleng et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

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

Borgheti-Cardoso

Vicentini

Gratieri

et al. 2016

Braz. J. Pharm. Sci.

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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/cm 2 , 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/cm 2 , respectively). Further studies to evaluate skin sensitization and irritation are now necessary.Uniterms: Nicotine/transdermal patches. Nicotine/controlled transdermal delivery. Liquid crystalline systems/development. Vitamin E TPGS. Skin irritation/control/in vitro study. Skin irritation/use of transdermal patches.Adesivos transdérmicos de nicotina são utilizados para cessação de fumar, tratamento de problemas de pele com infiltração de eosinófilos e para melhorar a atenção em pacientes com doença de Alzheimer e enfraquecimento da memória associada à idade. No entanto, a irritação da pele com o uso prolongado dos adesivos ainda é um problema. O objetivo deste trabalho foi desenvolver sistema líquido cristalino (SLC) de preparo simples contendo vitamina E TPGS capaz de controlar a liberação de nicotina e reduzir os problemas de irritação cutânea. Os SLCs foram caracterizados por análise visual e microscopia de luz polarizada. As administrações tópica e transdérmica de nicotina foram investigadas in vitro utilizando pele de orelha de porco em célula de difusão de Franz. A permeação da nicotina veiculada pela fase cúbica desenvolvida seguiu cinética de ordem zero (r = 0,993) e foi significativamente maior do que o controle (solução de nicotina) após 12 h (p < 0,05) (138,86 ± 20,44 e 64,91 ± 4,06 µg/cm 2 , respectivamente). A fase cúbica também promoveu aumento da penetração de nicotina nas camadas viáveis da pele quando comparado ao controle (8,18 ± 1,89 e 2,63 ± 2,51 µg/cm 2 , respectivamente). Estudos futuros para avaliar a sensibilização e irritação da pele são necessários.

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Lyotropic liquid crystal systems in drug delivery: a review

Kim

Jahn

Cho

et al. 2014

Journal of Pharmaceutical Investigation

100

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Physicochemical Performances of Indomethacin in Cholesteryl Cetyl Carbonate Liquid Crystal as a Transdermal Dosage

Cited by 8 publications

References 33 publications

Impact of Substrate Properties on the Formation of Spherulitic Films: A Case Study of Salbutamol Sulfate

Impact of Substrate Properties on the Formation of Spherulitic Films: A Case Study of Salbutamol Sulfate

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

Lyotropic liquid crystal systems in drug delivery: a review

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