Related Experiment Videos
Transdermal delivery of levosimendan
R Valjakka-Koskela1, J Hirvonen, J Mönkkönen
1Pharmaceutical Development Department, Orion Corporation Orion Pharma, P.O. Box 1780, 70701, Kuopio, Finland. riitta.valjakka-koskela@orion.fi
Summary
Formulation modifications significantly enhance transdermal drug delivery of levosimendan. This novel approach may enable therapeutic plasma concentrations via skin penetration, improving drug accessibility.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Dermatology
Background:
- Levosimendan is a novel positive inotropic drug.
- Transdermal drug delivery offers potential advantages for drug administration.
- Optimizing levosimendan's transdermal penetration is crucial for therapeutic efficacy.
Purpose of the Study:
- To investigate formulation modifications for enhancing transdermal levosimendan penetration.
- To assess the feasibility of achieving therapeutic plasma concentrations of levosimendan through the skin.
- To explore various enhancers and techniques for controlled drug delivery.
Main Methods:
- In vitro permeation studies using human epidermis and diffusion cells.
- Evaluation of formulation strategies including pH adjustment, co-solvents, cyclodextrins, surfactants, liposomes, and iontophoresis.
- Pharmacokinetic analysis to predict steady-state plasma concentrations.
Main Results:
- Several agents, including sodium lauryl sulfate, ethanol, oleic acid, and soya phosphatidylcholine, significantly increased levosimendan permeation.
- Iontophoresis proved effective in enhancing transdermal drug delivery.
- Hydrophilic co-solvents or penetration enhancers are necessary for improved levosimendan permeability.
Conclusions:
- Transdermal delivery of levosimendan can be substantially improved through targeted formulation modifications.
- Achieving therapeutic plasma concentrations via transdermal routes is potentially feasible.
- This research paves the way for novel transdermal levosimendan formulations.