Long-acting injectable atovaquone nanomedicines for malaria prophylaxis.

Bakshi, Rahul P; Tatham, Lee M; Savage, Alison C; Tripathi, Abhai K; Mlambo, Godfree; Ippolito, Matthew M; Nenortas, Elizabeth; Rannard, Steve P et al. · Nat Commun · 2018

basic_science · Level V

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Abstract

Chemoprophylaxis is currently the best available prevention from malaria, but its efficacy is compromised by non-adherence to medication. Here we develop a long-acting injectable formulation of atovaquone solid drug nanoparticles that confers long-lived prophylaxis against Plasmodium berghei ANKA malaria in C57BL/6 mice. Protection is obtained at plasma concentrations above 200 ng ml<sup>-1</sup> and is causal, attributable to drug activity against liver stage parasites. Parasites that appear after subtherapeutic doses remain atovaquone-sensitive. Pharmacokinetic-pharmacodynamic analysis indicates protection can translate to humans at clinically achievable and safe drug concentrations, potentially offering protection for at least 1 month after a single administration. These findings support the use of long-acting injectable formulations as a new approach for malaria prophylaxis in travellers and for malaria control in the field.

Medical subject headings