Transdermal drug delivery avoids complications related to oral or parenteral delivery - the need for sterility, contamination, gastrointestinal side effects, patient unconsciousness or nausea and compliance. For malaria treatment, we demonstrate successful novel transdermal delivery of artemisone (ART) and artesunate. The incorporation of ART into a microemulsion (ME) overcomes the limitations of the lipophilic drug and provides high transcutaneous bioavailability. ART delivery to the blood (above 500 ng/ml) was proved by examining the sera from treated mice, using a bioassay in cultured Plasmodium falciparum. Skin spraying of ART-ME eliminated P. berghei ANKA in an infected mouse model of cerebral malaria (CM) and prevented CM, even after a late treatment with a relatively small amount of ART (13.3 mg/kg). For comparison, the artesunate (the most used commercial artemisinin) formulation was prepared as ART. However, ART-ME was about three times more efficient than artesunate-ME. The solubility and stability of ART in the ME, taken together with the successful transdermal delivery leading to animal recovery, suggest this formulation as a potential candidate for transdermal treatment of malaria.
|Original language||American English|
|Number of pages||7|
|Journal||International Journal for Parasitology: Drugs and Drug Resistance|
|State||Published - Aug 2021|
Bibliographical noteFunding Information:
The work was supported by the Deutsche Forschungsgemeinschaft [DFG grants GR 972/47-2 and MA 1648/12-2 ]. The funders had no role in study design, data collection and interpretation, or the decision to submit the work for publication.
© 2021 The Authors
- Cerebral malaria
- Drug delivery
- Transdermal delivery