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Iontophoretic delivery of apomorphine. I: In vitro optimization and validation
R van der Geest1, M Danhof, H E Boddé
1Division of Pharmaceutical Technology, Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.
Pharmaceutical Research
|February 7, 1998
Summary
Transdermal iontophoretic delivery of apomorphine is feasible for Parkinson's disease. Optimized conditions show controlled transport rates, suggesting potential for effective plasma concentrations.
Area of Science:
- Pharmacology
- Biomedical Engineering
- Dermatology
Background:
- Parkinson's disease management often requires effective drug delivery.
- Transdermal drug delivery offers a non-invasive alternative for systemic medication.
- Apomorphine is a dopamine agonist used to treat Parkinson's disease symptoms.
Purpose of the Study:
- To assess the feasibility of transdermal iontophoretic delivery of apomorphine.
- To optimize and validate transdermal transport rates in vitro using human skin models.
Main Methods:
- Utilized R-apomorphine hydrochloride in an anodal compartment.
- Investigated effects of current density, pH, concentration, temperature, and skin type on flux using flow-through cells.
- Validated transport across human stratum corneum and dermatomed skin.
Main Results:
- Transdermal apomorphine transport was directly controlled by electrical current; passive delivery was minimal.
- Steady-state flux showed a linear relationship with current density and was maximized at high donor concentrations.
- Increasing temperature to 37°C significantly increased flux and decreased lag time; skin type impacted flux.
Conclusions:
- Iontophoretic delivery of apomorphine can be accurately controlled and manipulated by applied current.
- Optimized in vitro conditions suggest feasible transport rates for therapeutic plasma concentrations.
- Further in vitro/in vivo correlation studies are warranted to confirm therapeutic efficacy.