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Pioneer Use of Antimalarial Transdermal Combination Therapy in Rodent Malaria Model

We have previously reported 1,2,6,7-tetraoxaspiro [7.11]nonadecane (N-89) as a promising antimalarial compound. In this study, we evaluated the effect of transdermal therapy (tdt) of N-89 in combination (tdct) with other antimalarials as an application for children. We prepared ointment formulas containing N-89 plus another antimalarial drug, specifically, mefloquine, pyrimethamine, or chloroquine. In a 4-day suppressive test, the ED50 values for N-89 alone or combined with either mefloquine, pyrimethamine, or chloroquine were 18, 3, 0.1, and 3 mg/kg, respectively. Interaction assays revealed that N-89 combination therapy showed a synergistic effect with mefloquine and pyrimethamine, but chloroquine provoked an antagonistic effect. Antimalarial activity and cure effect were compared for single-drug application and combination therapy. Low doses of tdct N-89 (35 mg/kg) combined with mefloquine (4 mg/kg) or pyrimethamine (1 mg/kg) gave an antimalarial effect but not a cure effect. In contrast, with high doses of N-89 (60 mg/kg) combined with mefloquine (8 mg/kg) or pyrimethamine (1 mg/kg), parasites disappeared on day 4 of treatment, and mice were completely cured without any parasite recurrence. Our results indicated that transdermal N-89 with mefloquine and pyrimethamine provides a promising antimalarial form for application to children.

 

Comments：

The study found that N-89 in combination with mefloquine or pyrimethamine showed a synergistic effect and had a better antimalarial activity and cure effect compared to N-89 alone or combined with chloroquine.

Low doses of tdct N-89 combined with mefloquine or pyrimethamine showed antimalarial effects, but not a cure effect, while high doses of N-89 combined with mefloquine or pyrimethamine cured the mice without any parasite recurrence.

Overall, the study suggests that transdermal N-89 combined with mefloquine or pyrimethamine could be a promising antimalarial form for children.

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S4420 Mefloquine HCl Mefloquine HCl(Mefloquin hydrochloride) is a blood schizonticide by inhibiting hemozoin formation, used as an antimalarial drug.

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