Development and Optimization of Orally and Topically Applied Liquid Crystal Drug Formulations

Kadhum, Wesam R.; Hada, Tomoki; Hijikuro, Ichiro; Todo, Hiroaki; Sugibayashi, Kenji

doi:10.5650/jos.ess17032

Cited by 16 publications

(18 citation statements)

References 68 publications

(20 reference statements)

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“…Release Test of TA from Spray Preparations Regenerated cellulose membrane (Cellulose tube 24/32 with a pore size of 50 Å, Eidia Co., Ltd., Tokyo, Japan) was set in a Franz type diffusion cell (receiver volume: 6.0 mL, effective diffusion area: 1.77 cm 2 ) as described previously. 8,10,11) Then, the spray formulation or commercial formulation (Aftach ® Adhesive Tablet or Kenalog ® in Orabase) containing the same amount of TA (25 µg) was applied onto the regenerated cellulose membrane after applying 200 µL of artificial saliva (Salibeht ® ) on the membrane. The spray formulation was applied with a pipette over the area to ensure uniform distribution and Kenalog ® was spread with a spatula.…”

Section: Holding Areamentioning

confidence: 99%

“…Self-organizing lipids (SOLs) form non-lamellar lyotropic liquid crystals (NLLCs) and have been a recent focus as a new type of pharmaceutical additive [6][7][8][9][10][11] because they show high drug entrapment ability, high adhesion to biological membranes, sustained drug release ability, and enhanced biological membrane permeability and absorption. SOLs may be a next-generation material for biomimetic drug de-livery systems such as liposomes.…”

Section: Introductionmentioning

confidence: 99%

“…SOLs may be a next-generation material for biomimetic drug de-livery systems such as liposomes. SOLs that form NLLCs on contact with water, such as 2,3-dihydroxypropyl oleate (1-mono (cis-9-octadecenoyl)glycerol [GMO], Table 1) [6][7][8][9][10] and 3,7,11,15-tetramethyl-1,2,3-hexadecanetriol (Phytantriol) 6,7,9) are well known. However, both of these SOLs are difficult to handle because of their solid or highly viscous aqueous solutions at room temperature.…”

Section: Introductionmentioning

confidence: 99%

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Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

Sugibayashi

Yamamoto

Itakura

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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We examined the physicochemical and biochemical properties of mono-O-(5,9,13-trimethyl-4tetradecenyl)glycerol ester (MGE), including ease of handling, high bioadhesiveness, quick and stable in vivo self-organization (forming a non-lamellar lyotropic liquid crystal [NLLC]), and high biomembrane permeation enhancement. We prepared MGE oral mucosa-applied spray preparations containing triamcinolone acetonide (TA), which is widely used in the treatment of stomatitis, and we examined the usefulness of the MGE preparations compared with commercially available oral mucosal application preparations containing 2,3-dihydroxypropyl oleate (1-mono(cis-9-octadecenoyl)glycerol (GMO) (previously studied as an NLLCforming lipid) preparation. As a result, the MGE preparation applied to the oral mucosa can rapidly formed an NLLC with reverse hexagonal or cubic structures, or a mixture, on contact with water. In addition, by adding hydroxypropyl cellulose to the MGE preparation, similar retention properties on the oral mucous membrane were obtained to that using marketed drug preparations. Furthermore, the MGE spray formulation on the oral mucosa showed an equivalent or higher TA release as well as oral mucous membrane permeability compared with commercial formulations. Because MGE forms a stable NLLC and is easy to handle compared with GMO, MGE was considered to be a useful pharmaceutical additive for a spray preparation applied to the oral mucosa in combination.

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Section: Holding Areamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

Sugibayashi

Yamamoto

Itakura

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Одной из важнейших биофармацевтических характеристик любой лекарственной формы является высвобождение лекарственного вещества. На стадии фармацевтической разработки для микроэмульсионных и ЖК-носителей можно использовать методы, основанные на диализе через полупроницаемую мембрану [5,[20][21][22]. Для изучения кинетики высвобождения водорастворимых лекарственных веществ была использована модельная система: перенос водорастворимого красителя Родамина С из образцов микроэмульсии и ЖК, помещенных в диализный мешок, в физиологический раствор при Т = 37°С.…”

Section: экспериментальная частьunclassified

“…Скорость переноса веществ из лиотропных ЖК или микроэмульсии через диализную мембрану зависит от многих факторов: структурной организации носителя (например, типа ЖК), содержания водной фазы в составе носителя, гидрофильности или липофильности переносимого вещества [5,21]. В обратной микроэмульсии диффузия водорастворимого красителя будет происходить за счет столкновения и слияния капель.…”

Section: экспериментальная частьunclassified

Микроэмульсии И Лиотропные Жидкие Кристаллы Лецитина Как Системы Для Трансдермальной Доставки Лекарственных Веществ

Мурашова¹,

Трофимова²,

Костюченко³

et al. 2019

Rossijskie nanotehnologii

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Enhancement of Skin Permeation of a Hydrophilic Drug from Acryl-Based Pressure-Sensitive Adhesive Tape

et al. 2021

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Purpose Penetration enhancers are necessary to overcome a formidable barrier function of the stratum corneum in the development of topical formulations. Recently, non-lamella liquid crystal (NLLC)-forming lipids such as glycerol monooleate and phytantriol (PHY) are gaining increasing attention as a novel skin permeation enhancer. In the present study, fluorescein sodium (FL-Na) was used as a model hydrophilic drug, and acryl-base pressure-sensitive adhesive (PSA) tape containing NLLC forming lipids, mono-O-(5,9,13-trimethyl-4-tetradecenyl) glycerol ester (MGE) or PHY, was prepared to enhance drug permeation through the skin. Methods A PSA patch containing FL-Na was prepared by mixing FL-Na entrapped in NLLC and acrylic polymer. FL permeation through excised hairless rat skin, and also human skin, was investigated. Changes in lipid structure, folding/unfolding state of keratin in the stratum corneum, and penetration of MGE into the stratum corneum were investigated using confocal Raman microscopy. Results Enhanced FL permeation was observed by the application of a PSA patch containing MGE and PHY. Especially, dramatically enhancement effect was confirmed by 15% of MGE contained formulation. Penetration of MGE provided diminished orthorhombic crystal structure and a peak shift of the aliphatic CH3 vibration of keratin chains toward lower wavenumbers. ConclusionThe present results suggested that the formulation development by adding MGE may be useful for improving the skin permeation of mal-permeable drugs such as hydrophilic drugs.

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Development and Optimization of Orally and Topically Applied Liquid Crystal Drug Formulations

Cited by 16 publications

References 68 publications

Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

Микроэмульсии И Лиотропные Жидкие Кристаллы Лецитина Как Системы Для Трансдермальной Доставки Лекарственных Веществ

Enhancement of Skin Permeation of a Hydrophilic Drug from Acryl-Based Pressure-Sensitive Adhesive Tape

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