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Published on: December 23, 2016
Self-microemulsifiyng suppository formulation of β-artemether
Dalapathi Gugulothu1, Sulabha Pathak, Shital Suryavanshi
1Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N. P. Marg, Matunga, Mumbai , 400019, India.
AAPS Pharmscitech
|July 28, 2010
Summary
New rectal suppositories containing β-artemether offer a faster and prolonged action against malaria. This self-microemulsifying formulation demonstrated significant efficacy and improved animal survival in preclinical studies.
Area of Science:
- Pharmaceutical Sciences
- Parasitology
- Drug Delivery
Background:
- Parasitic diseases affect 30% of the global population, with malaria being a major life-threatening illness.
- Effective antimalarial drug delivery remains a critical challenge in combating malaria.
- Rectal administration offers an alternative route for antimalarial drug delivery.
Purpose of the Study:
- To formulate and evaluate novel self-microemulsifying suppositories of β-artemether for rectal administration.
- To compare the characteristics and efficacy of these novel suppositories against conventional polyethylene glycol suppositories.
- To assess the antimalarial activity and in vivo performance of the developed formulation.
Main Methods:
- Formulation of self-microemulsifying suppositories and conventional polyethylene glycol suppositories.
- Physicochemical characterization including melting range, rheology, texture analysis, disintegration, self-microemulsification time, particle size, and drug content.
- In vitro drug release studies using USP apparatus II.
- In vivo evaluation against Plasmodium berghei in a murine model.
Main Results:
- The self-microemulsifying suppositories exhibited desirable characteristics for rectal delivery.
- In vitro studies showed controlled drug release profiles.
- In vivo studies demonstrated sustained antimalarial activity (94% efficacy for 20 days) and improved animal survival compared to conventional suppositories.
Conclusions:
- Self-microemulsifying suppositories of β-artemether are a promising rectal drug delivery system for malaria treatment.
- This formulation offers a faster onset and prolonged effect, enhancing therapeutic outcomes.
- The developed suppositories represent an advancement in antimalarial drug delivery strategies.