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Title: The enhancement of percutaneous absorption by chemical modification of therapeutic agents
Author: Gullick, Darren R.
ISNI:       0000 0001 3522 1311
Awarding Body: University of Portsmouth
Current Institution: University of Portsmouth
Date of Award: 2007
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Most drugs are designed primarily for oral administration, but the activity and Stability profiles desirable for this route often make them unsuitable for transdermal delivery. There is current interest in the prodrug approach to enhance percutaneous absorption, and this project investigates the application of QSPRs (quantitative structurepermeability relationships) for prodrug selection by prediction of permeability. Captopril (an ACE-inhibitor) was selected as a model drug with poor percutaneous penetration, for which the sustained steady-state blood plasma level associated with transdermal delivery (and which is unattainable orally) would be particularly beneficial. QSPRs predicted that ester prodrug derivatives of captopril would have higher permeability coefficients (kp) than the parent drug, but lower flux (Jm) values due to the effect of the (predicted) relatively low aqueous solubility. Therefore, the aim of this study was to synthesize a series of prodrugs of captopril and to determine if a QSPR model could be used to design therapeutically viable prodrugs.
Supervisor: Not available Sponsor: Not available
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available