Stable Positively Charged Liposome during Long-Term Storage
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概要
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The effect of taurine, as an isotonic solute, and of benzalkonium chloride (BZC), as a positive membrane component, on the long-term stability of liposomal suspensions was investigated by measuring surface potential. The surface potential, which introduced electrostatic repulsion to liposomes against aggregation, increased dose-dependently with the addition of BZC, which gave a positive charge. However, a further addition of BZC caused unexpected aggregation during storage, so the optimum addition of BZC was defined. On the other hand, taurine, which forms a zwitter ion in an aqueous solution, did not reduce the surface potential, suggesting that taurine is of possible utility as an isotonic solute. As the result of stability testing, the liposomal system using taurine and BZC was stable against aggregation during 6 months at 40℃. We were successful in developing a stable, positively charged liposomal system during long-term storage, and our liposomal system is believed to be of wide utility as a drug carrier for therapeutic drugs applied topically to negatively charged mucosal tissues.We applied the Derjaguin-Landau-Verwey-Overbeek (DLVO) theory to estimate the colloidal stability of liposomes. As a result of stability testing, positively charged liposomes had a good correlation betwee maximum total repulsive energy (V_T(max)/kT) between two liposome particles and colloidal stability, suggesting that the V_T(max)/kT value is useful for estimating stability and for designing liposomal preparations containing some ionic substances.
- 公益社団法人日本薬学会の論文
- 1993-07-15
著者
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井上 圭三
Department Of Health Chemistry Faculty Of Pharmaceutical Science The University Of Tokyo
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根本 正美
Research Center, Taisho Pharmaceutical Co., Ltd.,
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根本 正美
大正製薬・開発研究所
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根本 正美
Research Center Taisho Pharmaceutical Co. Ltd.
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小山 郁夫
Research Center, Taisho Pharmaceutical Co., Ltd.
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吉田 継親
Research Center, Taisho Pharmaceutical Co., Ltd.,
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中森 克
Research Center, Taisho Pharmaceutical Co., Ltd.,
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中島 俊明
Research Center, Taisho Pharmaceutical Co., Ltd.,
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小田原 美樹子
Research Center, Taisho Pharmaceutical Co., Ltd.,
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大島 広行
Faculty of Pharmaceutical Sciences and Institute of Colloid and Interface Science, Science Universit
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中島 俊明
Research Center Taisho Pharmaceutical Co. Ltd.
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大島 広行
Faculty Of Pharmaceutical Sciences And Institute Of Colloid And Interface Science Science University
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小田原 美樹子
Research Center Taisho Pharmaceutical Co. Ltd.
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小山 郁夫
Research Center Taisho Pharmaceutical Co. Ltd.
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中森 克
Research Center Taisho Pharmaceutical Co. Ltd.
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吉田 継親
Research Center Taisho Pharmaceutical Co. Ltd.
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