Effects of Lipid Composition on the Transcorneal Penetration of Liposomes Containing Disulfiram, a Potential Anti-cataract Agent, in the Rabbit
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概要
- 論文の詳細を見る
We previously demonstrated that topical treatment with disulfiram (DSF) prevented the development of cataracts in sodium selenite-injected rat pups. In biological systems, DSF is rapidly reduced to diethyldithiocarbamate (DDC), a potent antioxidant. In this study, we investigated the effect of altering the lipid composition of liposomes containing DSF on the transcorneal transit of DDC. Liposomes containing DSF were prepared with various molar ratios of dimyristoylphosphatidylcholine (DMPC), dipalmitoylphosphatidylcholine (DPPC) and cetylpyridinum chloride (CPC) by reverse-phase evaporation. Liposomes with a DMPC to DPPC molar ratio of 5 : 5,examined by differential scanning calorimetry, had the highest enthalpy of transition and the presence of one molar ratio of CPC further enhanced the enthalpy value. The addition of bovine serum albumin or a homogenate of rabbit cornea to the incunation buffer resulted in the release of DDC, but not DSF from the liposomes. The amount of DDC present in the aqueous humor of rabbit eyes following topical administration increased with increase in DMPC to DPPC ratios and was also enhanced by the addition of CPC to the liposomes. The results of this study suggest that liposome formulations are effective for transorneal drug delivery of anticataract agents such as DSF. DSF in liposomes consisting of DMPC, DPPC, and CPC with a molar ratio of 8 : 2 : 1 may be a potential drug formulation for the prevention and/or treatment of cataracts.
- 社団法人日本薬学会の論文
- 2000-03-01
著者
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Ito Yoshimasa
School of Pharmacy, Kinki University
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Kimura Takayoshi
Faculty of Sciences and Technologies, Kinki University
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Ito Yoshimasa
School Of Pharmacy
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Cai Hong
School of Pharmaceutical Sciences, Kinki University
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KOIZUMI Yuichi
School of Pharmaceutical Sciences, Kinki University
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TOMOHIRO Masayuki
Research and Development, Research Department, Pharmacia & Upjohn
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TERAO Motome
Pharmaceutical Research and Technology Institute
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HORI Ryohei
Pharmaceutical Research and Technology Institute
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TAKAGI Sadao
Faculty of Science and Technology, Kinki University
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Tomohiro Masayuki
Research And Development Research Department Pharmacia & Upjohn:(present Address)department Of M
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Terao M
Pharmaceutical Research And Technology Institute
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Ito Yoshimasa
School Of Pharmaceutical Sciences Kinki University
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Takagi Sadao
Faculty Of Science And Technology Kinki University
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Koizumi Yuichi
School Of Pharmacy Kinki University
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Kimura Takayoshi
Faculty Of Science And Technology Kinki University
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Takagi Sadao
Faculty Of Science And Engineering Kinki University
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Cai Hong
School of Pharmacy, Kinki University
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Ito Yoshimasa
School of Pharmaceutical science, Kinki University
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