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  • Title: [Study on brain targeting 3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine pharmacosomes].
    Author: Zhang ZR, Wang JX.
    Journal: Yao Xue Xue Bao; 2001 Oct; 36(10):771-6. PubMed ID: 12579979.
    Abstract:
    AIM: To investigate the specific brain drug targeting of 5-fluoro-2'-deoxyuridine (FUdR) by synthesis of 3', 5'-dioctanoyl-5-fluoro-2'-deoxyuridine (DO-FUdR) and incorporation into DO-FUdR pharmacosomes (DO-FUdR-PS). METHODS: DO-FUdR-PS was prepared by thin-layer ultrasonication technique. In vitro drug release was studied in pH 7.4 phosphate-buffered saline containing 0.3% pancreatic enzyme at 37 degrees C using bulk-equilirium reverse dialysis bag technique. The concentration of FUdR in various organs were determined by reversed phase HPLC after i.v. administration of DO-FUdR-PS and FUdR. RESULTS: The mean particle size of DO-FUdR-PS was 76 nm with drug loading of 29.02% and entrapment efficiency of 96.62%. The in vitro drug release kinetics could be characterized by bioexponential equation. Compared with FUdR injection, DO-FUdR-PS showed high concentration in tested organs. The brain AUC ratio of DO-FUdR-PS to FUdR was 10.97. CONCLUSION: DO-FUdR-PS showed a good targeting efficiency in vivo. PS can improve the ability of drug to cross blood-brain barrier and is a promising drug targeting system for the treatment of central nervous system disorders.
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