Preparations of Rectal Suppositories Containing Artesunate.

Suzanne Persaud,Hyunah Cho,Sandra Eid,Natalia Swiderski,Ioannis Serris

doi:10.3390/pharmaceutics12030222

Abstract

Rectal artesunate suppositories are a useful option for pre-referral treatment of severe malaria, specifically in children under 6 years of age in remote malaria-endemic areas. The main challenges are to improve the solubility of drugs in the rectal fluids and prevent the product from turning rancid or melting in a tropical climate. In this short proof-of-concept study, three types of rectal suppositories of artesunate were prepared: (i) polyethylene glycol (PEG)-based suppositories carrying free artesunate (non-modified artesunate), (ii) PEG-based suppositories carrying artesunate-loaded micelles and (iii) 3D-printed suppositories carrying a PEG/artesunate mixture. Physical parameters of suppositories, release profiles of artesunate (the fastest to the slowest: ii≥i>iii) and thermostability (the most stable to the least stable: iii>ii>i) of suppositories at increased temperature were assessed to determine the advantages and disadvantages of each formulation.

Highlights

Per Center for Disease Control and Prevention (CDC), malaria is a fatal disease caused by the protozoan parasite Plasmodium [1]
There are four types of Plasmodium, but the type that causes the most severe reaction is Plasmodium falciparum, which infects anopheles mosquitoes that feed on human blood
Up to 80% of the children who live in rural areas die before reaching the hospital, due to a lack of resources [4]

Summary

Introduction

Per Center for Disease Control and Prevention (CDC), malaria is a fatal disease caused by the protozoan parasite Plasmodium [1]. There are four types of Plasmodium, but the type that causes the most severe reaction is Plasmodium falciparum, which infects anopheles mosquitoes that feed on human blood. The occurrence of malaria is highly dependent on the climatic factors such as humidity and rainfall, with temperature being the most critical factor. This is because P. falciparum cannot complete its growth cycle in the anopheles mosquitoes at temperatures below 20 ◦C, preventing any mode of transmission. Transmission occurs most frequently where the regions are hotter and declines as the temperature decreases. The highest transmission is found south of the Sahara Desert in Africa and Papua New Guinea

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