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Drug Dev Ind Pharm. 2016 Oct;42(10):1708-21. doi: 10.3109/03639045.2016.1171331. Epub 2016 Apr 19.

Formulation design, in vitro characterizations and anti-malarial investigations of artemether and lumefantrine-entrapped solid lipid microparticles.

Author information

1
a Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences , University of Nigeria , Nsukka , Enugu State , Nigeria ;
2
b Nanomedicines and Drug Delivery Research Group, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences , Nnamdi Azikiwe University , Awka , Anambra State , Nigeria ;
3
c Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences , University of Nigeria , Nsukka , Enugu State , Nigeria.

Abstract

CONTEXT:

Poor aqueous solubility of artemether and lumefantrine makes it important to seek better ways of enhancing their oral delivery and bioavailability.

OBJECTIVE:

To formulate and carry out in vitro and anti-malarial pharmacodynamic evaluations of solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) of artemether and lumefantrine for oral delivery and improved bioavailability.

MATERIALS AND METHODS:

Rational blends of Softisan(®)154 and Phospholipon(®)90H lipid matrices, and different concentrations of artemether and lumefantrine were used to formulate several batches of SLMs. Drug-free SLMs were also formulated. Morphology, particle size, encapsulation efficiency (EE%) and pH studies were performed. In vitro release studies were performed in alcoholic buffer, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Anti-malarial pharmacodynamic studies were conducted in mice.

RESULTS:

Stable, smooth and spherical particles with sizes ranging from 4.2 ± 0.02 to 9.3 ± 0.8 µm were formed. EE% of 92.2-97.3% and 30.2-84.7% and pH of 3.0 ± 0.02 to 4.9 ± 0.12 and 3.0 ± 0.02 to 5.8 ± 0.05 were obtained for artemether and lumefantrine SLMs, respectively. Release of 100, 88.28 and 75.49%, as well as 63.26, 34.31 and 56.17% were recorded for artemether and lumefantrine in alcoholic buffer, SGF and SIF, respectively. Pharmacodynamic studies indicated very significant (p < 0.05) clearance of parasitaemia in plasmodium-infected mice by the drug-loaded SLMs.

CONCLUSION:

Oral delivery and bioavailability of artemether and lumefantrine could be improved using SRMS-based SLMs.

KEYWORDS:

Drug delivery; Phospholipon®90H; Softisan®154; emulsion congealing; hot homogenization; parasitaemia

PMID:
27095388
DOI:
10.3109/03639045.2016.1171331
[Indexed for MEDLINE]

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