Development of phospholipid based depot antimalarial tablets of azadirachta indica leaf extract and artemether/lumefantrine for oral delivery

Prof. Dr. A. A. Attama1), University of Nigeria/Africa

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Prof. Dr. Anthony A. AttamaDrug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, University of Nigeria, Nsukka/Nigeria


Malaria affects millions of people annually in malaria-endemic regions of the world and cases of treatment failure have been recorded with artemisinin combination therapies (ACTs), e.g. artemether and lumefantrine, the first line drug combination for the treatment of Plasmodium falciparum malaria.1) This calls for urgent research into design and development of more effective and affordable drug delivery systems, especially in low-income settings, as drug resistance can also be combated through engineering of novel drug delivery systems.

This research focuses on development of novel delivery system of an antimalarial extract clinically proven to be effective against P. falciparum malaria, together with long standing use in traditional settings and an alternative delivery system of artemether/lumefantrine combination (ACT).2)3) The novel oral phospholipid-based tablets will be prepared using a very simple technology with high accuracy, which would make it amenable for people in low-income settings, where conventional sophisticated preparation procedures are not possible. This will lead to greater accessibility to antimalarial drugs and reduction of malaria burden in many communities. The novel oral phospholipid-based tablets, which will contain upwards of 50% of phospholipid, will be compared with commercial ACT – artemether/lumefantrine tablets on the market. Overall, these novel formulations will increase the utilization of phospholipids as very important pharmaceutical multifunctional excipient

Benefit for the community

The research outcome will lead to the reduction of malaria burden in many communities. The phospholipid-based oral tablets differently containing conventional artemisinin combination therapies (ACT) and the antimalarial ethanol extract of Azadirachta indica can be prepared in local community hospitals/clinics since the preparation procedure requires simple equipment and is not complicated. It is expected to make reliable anti-malarials accessible and affordable. In addition, most of the excipients can be sourced locally. The only scale up technology that would be required is mass production of the mold.

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World Health Organization 2010
Guidelines for the treatment of malaria
2nd Edition, World Health Organization, Geneva
Anagu OL, Attama AA, Okore VC, Gugu HT, Ngene AA, Esimone CO, 2014
Azadirachta indica extract-artesunic acid combination produces increased cure rate of Plasmodium berghei-infected mice
Pharm. Biol. 52, 883-889
Attama AA, Kenechukwu FC, Onuigbo EB, Nnamani PO, Obitte N, Finke JH, Pretor S, Muller-Goymann CC, 2016
Solid lipid nanoparticles encapsulating a fluorescent marker (coumarin 6) and antimalarials – artemether and lumefantrine: evaluation of cellular uptake and antimalarial activity
Eur. J. Nanomed. 8, 129-138
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