Usefulness of Liposomes as an Intranasal Dosage Formulation for Topical Drug Application
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概要
- 論文の詳細を見る
The potential of liposomes as an intranasal dosage formulation for topical application was investigated in rats. When 5(6)-carboxyfluorescein (CF), a model absorbable drug, dissolved in phoshate-buffered saline (PBS)was administered intranasally, CF was rapidly absorbed into the systemic circulation and no adhesion of CF to the nasal mucosa was observed. The fraction of CF absorbed from the nasal mucosa reached about 48% 1 h after administration. On the other hand, only 3% of the dose was absorbed when CF was encapsulated in liposomes consisting of dipalmitoylphosphatidylcholine and cholesterol (DPPC-liposomes). In addition, the amount of CF adhering to the nasal mucosa after administration as DDPC-liposomes was 20- to 28-fold greater than that in PBS solution. In particular, positively charged liposomes markedly enhanced the adhesion of CF to the nasal mucosa. Differences in the lipid composition of liposomes did not affect the absorption of CF. However, the ability of liposomes to adhere to the nasal mucosa was consistent with the fluidity of the liposomal membrane. Furthermore, the action of liposomes on the anti-histaminic effect of diphenhydramine hydrochloride (DH) was studied in rats by measuring the amount of protein leaking into the nasal cavity under quasi-allergic conditions. The anti-histaminic effect of DH was strong but of short-duration when DH was administered as a PBS solution. However, liposomes prolonged the anti-histaminic effect of DH, suggesting that liposomes may adhere to the nasal mucosa and release DH slowly. In conclusion. liposomes suppress drug absorption into the systemic circulation and concurrently increase drug retention in the nasal cavity.
- 公益社団法人日本薬学会の論文
- 2000-03-01
著者
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Kakemi M
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Kakemi Masao
大阪薬科大学 薬剤学
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MORIMOTO Kazuhiro
Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical Uni
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KIMURA Toshikiro
Department of Pharmaceutics, Okayama University Graduate School of Medicine, Dentistry and Pharmaceu
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IWANAGA Kazunori
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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Kakemi M
Osaka Univ. Pharmaceutical Sci. Takatsuki Jpn
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KAKEMI Masawo
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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Yamashita Shinji
Department Of Electronic Engineering The University Of Tokyo
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Morimoto Kazuhiro
Department Of Applied Chemistry Faculty Of Engineering Doshisha University
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Morimoto K
Hokkaido Pharmaceutical University School Of Pharmacy
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Kimura Toshikiro
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Okayama University
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Yamashita Shinji
Department Of Pharmaceutics Faculty Of Pharmaceutial Sciences Setsunan Universicty
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Yamashita Shinji
Department De Mathematique Universite Metropolitaine De Tokyo
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MATSUMOTO Sumiyo
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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Iwanaga Kazunori
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Matsumoto Sumiyo
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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