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Formulation and evaluation of Pheroid vesicles containing mefloquine for the treatment of malaria.
MedLine Citation:
PMID:  24117456     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
OBJECTIVES: Mefloquine (MQ) is an antimalarial drug with high efficacy, often used in the treatment and chemoprophylaxis of malaria. However, it has low solubility in water, a long elimination half-life (4 days), and is neurotoxic, which leads to unwanted side effects.
METHODS: We investigated a lipid-based drug delivery system, Pheroid vesicles, in combination with MQ (Pheroid MQ), to promote future clinical use. MQ was incorporated into Pheroid vesicles and the formulations characterized. The formulations were evaluated in terms of in-vitro efficacy and toxicity. In-vivo bioavailability studies were conducted in C57 BL6 mice.
KEY FINDINGS: The vesicles incorporated MQ with ∼63% entrapment efficiency. The IC50 values of MQ after 48-h incubation in chloroquine-resistant (RSA11) and chloroquine sensitive (3D7) strains, were reduced by ∼50% and ∼30% respectively. In-vivo bioavailability study revealed no change in the pharmacokinetic parameters of MQ, and the incorporation of the drug in Pheroid vesicles reduced the in-vitro haemolytic activity by ∼75%. Furthermore, the cytotoxicity against human neuroblastoma cells (SH-SY5Y) of the free drug was reduced by ∼64% with Pheroid MQ.
CONCLUSIONS: Pheroid vesicles may therefore decrease the toxicity of MQ and thereby improve its therapeutic index, a strategy that may provide an effective alternative for malaria chemoprophylaxis and treatment.
Authors:
Lissinda H du Plessis; Chrizaan Helena; Este van Huysteen; Lubbe Wiesner; Awie F Kotzé
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-10-13
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  -     ISSN:  2042-7158     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2013 Oct 
Date Detail:
Created Date:  2013-10-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
© 2013 Royal Pharmaceutical Society.
Affiliation:
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
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