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Penetration of the blood-brain barrier by the antiviral drug (E)-5-(2-iodovinyl)-2'-deoxyuridine in a rat model of herpes encephalitis.
- Source :
-
Drug design and delivery [Drug Des Deliv] 1988 Jul; Vol. 3 (1), pp. 57-67. - Publication Year :
- 1988
-
Abstract
- The blood-brain barrier penetration of a radiohalogenated (125I) derivative of the antiviral drug (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU) was investigated in a rat model of herpes encephalitis. CNS delivery was assessed by external gamma camera scintigraphic imaging in vivo, a technique which may have general application in evaluating brain specific delivery of drugs, and by autoradiography of cryostat sections of rat brain. Radiohalogenated IVDU was found to be almost totally excluded from the CNS. These findings may be explained in terms of the poor lipid solubility of IVDU (in vitro oil/aqueous salt solution partition coefficient 0.012). Since IVDU appears in CSF after carotid artery administration, our results stress the necessity, in the design of compounds for the treatment of CNS infections, of distinguishing blood-brain, blood-CSF, and CSF-brain drug barriers. The significance of our data both in relation to the development of neuro-radiological diagnosis and antiviral chemotherapy of CNS infection is discussed.
- Subjects :
- Animals
Antiviral Agents pharmacology
Autoradiography
Brain diagnostic imaging
Chemical Phenomena
Chemistry, Physical
Chromatography, Thin Layer
Idoxuridine analogs & derivatives
Idoxuridine pharmacokinetics
Idoxuridine pharmacology
Iodine Radioisotopes
Radionuclide Imaging
Rats
Simplexvirus
Antiviral Agents pharmacokinetics
Blood-Brain Barrier drug effects
Encephalitis metabolism
Herpes Simplex metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0884-2884
- Volume :
- 3
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Drug design and delivery
- Publication Type :
- Academic Journal
- Accession number :
- 2855575