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Enhanced nose-to-brain delivery of tranilast using liquid crystal formulations
Get PDFIntranasal administration is poised as a competent method in delivering drugs to the brain, because the nasal route has a direct link with the central nervous system bypassing the formidable blood-brain barrier. C17-monoglycerol ester (MGE) and glyceryl monooleate (GMO) as liquid crystal (LC)-forming lipids possess desirable formulation characteristics as drug carriers for intranasally administered drugs. This study investigated the effect of LC formulations on the pharmacokinetics of tranilast (TL), a lipophilic model drug, and its distribution in the therapeutic target regions of the brain in rats. The anatomical biodistribution of LC formulations was monitored using micro-computed tomography tandem in vivo imaging systems. MGE and GMO effectively formed LC with suitable particle size, zeta potential, and viscosity supporting the delivery of TL to the brain. MGE and GMO LC formulations enhanced brain uptake by 10- to 12-fold and 2- to 2.4- fold, respectively, compared with TL solution. The olfactory bulb had the highest TL concentration and fluorescent signals among all the brain regions, indicating a direct nose-to-brain delivery pathway of LC formulations. LC-forming lipids, MGE and GMO, are potential biomaterials in formulations intended for intranasal administration
Transition of the Roof on Shurijo Castle Seiden
Get PDF琉球王国の王城であった首里城，その中心となる正殿の屋根について，本稿は出土遺物，文献，写真，絵図といった様々な資料を用いて，その変遷を学際的に明らかにすることを目的とする。首里城正殿の歴史は10段階に分けられ，少しずつ西側に拡大していく。屋根は当初は瓦葺きだったがやがて板葺きに変わり，17世紀からは様々な色の瓦が混ざり合う屋根となる。瓦は灰色や褐色が中心だったが，18世紀以降は赤色瓦が少しずつ葺かれるようになり，19世紀までに赤色が半数以上を占めるようになったと考えられる。Shurijo Castle Seiden was main shrine and the royal seat of the Ryukyu Kingdom. In this paper I study about the transition of the roof of Shurijo Castle Seiden using various materials such as excavated remains, literature, photographs, and drawn pictures. Shurijo Castle's history is divided to ten stages and gradually expands to the west. Seiden was initially roofed with Kyusyu style clay rooftile, but eventually changed to wooden tile and from the 17th century it became a mixture of clay rooftiles of various colors, mainly gray and brown. Red clay rooftiles gradually began to be roofed in the 18th century, and occupied more than half by the 19th century.研究ノート, 冊子版178p.に誤りがあったため2020.6.2更
Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids
Get PDFWe examined the physicochemical and biochemical properties of mono-O-(5,9,13-trimethyl-4-tetradecenyl)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 NLLC-forming 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