Improved brain delivery of AZT using a glycosyl phosphotriester prodrug.

摘要: The concentration of AZT in mice plasma and brain was measured using HPLC after an ingestion 20 mg/kg or the molar equivalent hexadecyl 2-(alpha-D-mannopyranosidyl)ethyl 3'-azido-3'-deoxy-5'-thymidinyl phosphate 3. results demonstrated promising qualities prodrug 3 which gave AZT-5'-phosphate as main metabolite: total derivatives detected presented a peak 156 nmol/g (5 for AZT) at 1 h; half-life about 24 h (1 with AUC 4366 nmol h/g compared to 4 AZT. lipophilic properties were confirmed by its vitro transport inside synaptosomes. derivative (2) provided also good delivery central nervous system, values intermediate between those