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ORAL DELIVERY OF A SUSTAINED ESTRADIOL DELIVERY SYSTEM

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 7203
Amount: $462,000.00
Phase: Phase II
Program: SBIR
Solicitation Topic Code: N/A
Solicitation Number: N/A
Timeline
Solicitation Year: N/A
Award Year: 1988
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
Po Box 730
Alachua, FL 32615
United States
DUNS: N/A
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 Kerry S Estes Phd
 (904) 462-1210
Business Contact
Phone: () -
Research Institution
N/A
Abstract

STUDIES ARE PROPOSED TO EVALUATE THE FEASIBILITY OF ORAL 17BETA-ESTRADIOL (E2) ADMINISTRATION USING A NOVEL REDOX SYSTEM. THIS CHEMICAL DELIVERY SYSTEM (CDS) IS BASED ON AN INTERCONVERSION OF A LIPOPHILIC DIHYDROPYRIDINE TO A HYDROPHILIC PYRIDINIUM SALT, ANALOGOUS TO THE NADH NAD+ COENZYME SYSTEM. IT PERMITS ENHANCED ANDSUSTAINED DELIVERY OF E2 TO THE CENTRAL NERVOUS SYSTEM BY HYDROLYSIS OF A "LOCKED-IN," CHARGED PRECURSOR. SUSTAINED LEUTINIZING HORMONE (LH) INHIBITION AND INCREASED BRAIN DRUGCONCENTRATIONS WERE SHOWN IN RATS AFTER INTRAVENOUS (I.V.) E2-CDS TREATMENT. NO SERUM E2 CHANGE WAS DETECTED, INDICATING THAT E2 WAS RELEASED CENTRALLY FROM CHARGED E2-CDS AND DECREASED LH VIA CENTRAL ACTION AND/OR VIA PORTALVESSEL TRANSIT OF E2 TO THE PITUITARY. DEVELOPMENT OF AN ORAL FORMULATION FOR E2-CDS OFFERS SEVERALADVANTAGES OVER CURRENTLY AVAILABLE ESTROGEN THERAPIES INCLUDING: (1) DELIVERY OF A NATURALLY OCCURRING GONADAL STEROID, (2) DECREASED PERIPHERAL ESTROGEN ACTIVITY, AND (3) INCREASED DOSING INTERVALS. THE FIRST STUDY WILL ESTABLISH BIOAVAILABILITY OF THE DRUG. THE SECOND STUDY WILL COMPARE LH-INHIBITING ACTIVITY OF ORAL AND I.V. E2-CDS ADMINISTRATION. THE THIRD STUDY WILL EXAMINE THE TISSUE DISTRIBUTION OF DRUG AND SELECTED METABOLITES OVER TIME AFTER ORAL E2-CDS TREATMENT.

* Information listed above is at the time of submission. *

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