[논문]In vitro Transport of Fexofenadine.HCl in Deformable Liposomes Across the Human Nasal Epithelial Cell Monolayers

Lin, Hong-Xia; Lee, Chi-Ho; Shim, Chang-Koo; Chung, Suk-Jae; Kim, Dae-Duk

doi:10.4333/kps.2004.34.6.483

In vitro Transport of Fexofenadine.HCl in Deformable Liposomes Across the Human Nasal Epithelial Cell Monolayers 원문보기

藥劑學會誌 = Journal of Korean pharmaceutical sciences, v.34 no.6, 2004년, pp.483 - 489

Lin, Hong-Xia (College of Pharmacy, Pusan National university) , Lee, Chi-Ho (College of Pharmacy, Pusan National university) , Shim, Chang-Koo (College of Pharmacy, Seoul National University) , Chung, Suk-Jae (College of Pharmacy, Seoul National University) , Kim, Dae-Duk (College of Pharmacy, Seoul National University)

Abstract ▼ AI-Helper

Fexofenadine HCl is non-sedating histamine H1 receptor antagonist that can be used for the treatment of seasonal allergic rhinitis. The objective of this study was to investigate whether the carriers of deformable liposomes can enhance the transepithelial permeability of fexofenadine HCl across the in vitro ALI human nasal monolayer model. Characterization of this model was achieved by bioelectric measurements and morphological studies. The passage 2 and 3 of cell monolayers exhibited the TEER value of $2852\;{\pm}\;482\;ohm\;{\times}\;cm^2$ on 11 days of seeding and maintained high TEER value for 5 days. The deformable liposome of fexofenadine HCl was prepared with phosphatidylcholine (PC) and cholic acid using extruder method. The mean particle size was about 200 nm and the maximum entrapment efficiency of 33.0% was obtained in the formulation of 1% PC and $100\;{\mu}g/ml$ fexofenadine HCl. The toxicity of the deformable liposome to human nasal monolayers was evaluated by MTT assay and TEER value change. MTT assay showed that it has no toxic effect on the nasal epithelial cells in 2-hour incubation when the PC concentration was below 1%. However, deformable liposome could not enhance the transepithelial permeability $(P_{app})$ and cellular uptake of fexofenadine HCl. In conclusion, the in vitro model could be used in nasal drug transport studies and evaluation of transepithelial permeability of formulations.

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제안 방법

The samples of fexofenadine , HC₁ were directly analyzed using an isocratic HPLC method on a Shimadzu HPLC system (SPD-10AV, Shimadzu Co., Kyoto, Japan) equipped with a pump and an automatic injector (SPD-10AVVP). A reversed phase C-18 column (Lichrospher® 100, RP-18, 125x4 mm, 5 ㎛, Merck Darmstadt, Germany) was used as stationary phase.
The transport studies were performed by initially incubating the monolayers in transport medium (HBSS supplemented with 15 mM 응hicose and 15 mM HEPES, pH 7.4) for 20 min at 37℃. Each transport experiment was performed by adding 0.

대상 데이터

The specimens were dehydrated through an alcohol series and allowed to air-dry overnight. The specimens were mounted on stubs with adhesive tape, sputter coated, and viewed in a Hitachi S-4200 scanning electron microscope (Hitachi, Japan).

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DOI : 10.4333/KPS.2004.34.6.483
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