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Antimicrobial Agents and Chemotherapy, April 1999, p. 972-974, Vol. 43, No. 4
0066-4804/99

Pharmacokinetics of Oral Zidovudine Entrapped in Biodegradable Nanospheres in Rabbits

Diana P. Callender,1 Nalini Jayaprakash,1 Aaron Bell,1 Vidmantas Petraitis,1 Ruta Petratienes,1 Myrna Candelario,1 Robert Schaufele,1 James M. Dunn,2 Shizuko Sei,3,dagger Thomas J. Walsh,1 and Frank M. Balis1,*

Pediatric Oncology Branch1 and HIV and AIDS Malignancy Branch,3 Division of Clinical Science, National Cancer Institute, Bethesda, Maryland 20892, and Verex Laboratories, Inc., Englewood, Colorado 801122

Received 8 July 1998/Returned for modification 2 December 1998/Accepted 17 January 1999

The pharmacokinetic profile of oral zidovudine entrapped in a 50:50 polyactide-coglycolide matrix (nanospheres) was compared to those of standard oral and parenteral zidovudine formulations in rabbits. The bioavailability of zidovudine nanospheres at 50 mg/kg of body weight was 76%, and this dose achieved prolonged exposure to zidovudine compared to standard formulations without an increase in the drug's peak concentration.


* Corresponding author. Mailing address: Pediatric Oncology Branch, NCI, Bldg. 10, Rm. 13N240, 10 Center Dr., Bethesda, MD 20892. Phone: (301) 496-0085. Fax: (301) 402-0575. E-mail: balisf{at}nih.gov.

dagger Present address: HIV Clinical Interface Laboratory, Developmental Therapeutics Program, SAIC-Frederick, NCI-FCRDC, Frederick, Md.


Antimicrobial Agents and Chemotherapy, April 1999, p. 972-974, Vol. 43, No. 4
0066-4804/99