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In vitro evaluation of chloroquine-loaded and heparin surface-functionalized solid lipid nanoparticles

Overview of attention for article published in Malaria Journal, April 2018
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In vitro evaluation of chloroquine-loaded and heparin surface-functionalized solid lipid nanoparticles
Published in
Malaria Journal, April 2018
DOI 10.1186/s12936-018-2302-9
Pubmed ID

Joseph O. Muga, Jeremiah W. Gathirwa, Matshawandile Tukulula, Walter G. Z. O. Jura


Use of chloroquine, an otherwise safe and relatively affordable anti-malarial drug, was discontinued due to widespread prevalence of resistant parasites. Many entrant anti-malarial drugs for treatment of chloroquine resistant malaria raises the concerns of cost and safety among other challenges. Innovative ways of circumventing chloroquine resistance is of paramount importance. Such may include nanoparticulate delivery strategies and targeting. This study evaluated physicochemical properties and in vitro antiplasmodial activity of chloroquine encapsulated heparin functionalized solid lipid nanoparticles (CQ-Hep-SLNs) and non-heparin functionalized SLNs (CQ-SLN) against Plasmodium falciparum. The modified double-emulsion solvent evaporation technique was used to prepare the nanoparticles. HPLC/UV was used to determine the in vitro drug release. The semi-automated micro-dilution technique was adapted in assessing the in vitro antiplasmodial activity to give drug concentration capable of inhibiting 50% of the P. falciparum (IC50), as a function of antiplasmodial efficacy. Prepared nanoparticles were below 500 nm in size with % drug loading (%DL) between 21 and 25% and encapsulation efficiency (%EE) of 78-90%. The drug-loaded SLN exhibited a biphasic drug release profile at pH 7.4, with an initial burst release during the first 24 h followed by sustained release in both formulations. Nanoformulated CQ-SLN (4.72 ± 0.14 ng/mL) and CQ-Hep-SLN (2.41 ± 0.27 ng/mL), showed enhanced in vitro antiplasmodial activities against chloroquine sensitive (D6) strain of P. falciparum, albeit with no activity against the chloroquine resistant W2 strain, compared to free CQ standard (5.81 ± 0.18 ng/mL). These findings suggest that the nanoformulated drugs displayed enhanced anti-malarial activities against chloroquine sensitive (D6) strains of P. falciparum compared to the free CQ standard. There is some form of potential dual synergistic effect of CQ-loaded heparinized solid lipid nanoparticles (Hep-SLN), meaning that combining heparin and CQ in SLNs has beneficial effects, including potential for specific targeting of parasitized red blood cells as afforded by heparin. Thus, the study has produced SLNs nanoparticles that have superior in vitro activities than CQ on CQ-sensitive parasites.

Twitter Demographics

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Mendeley readers

The data shown below were compiled from readership statistics for 79 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 79 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 16 20%
Researcher 9 11%
Student > Master 7 9%
Lecturer 6 8%
Student > Bachelor 6 8%
Other 17 22%
Unknown 18 23%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 14 18%
Chemistry 9 11%
Agricultural and Biological Sciences 7 9%
Biochemistry, Genetics and Molecular Biology 5 6%
Immunology and Microbiology 4 5%
Other 16 20%
Unknown 24 30%

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 31 December 2018.
All research outputs
of 14,079,326 outputs
Outputs from Malaria Journal
of 4,064 outputs
Outputs of similar age
of 275,972 outputs
Outputs of similar age from Malaria Journal
of 2 outputs
Altmetric has tracked 14,079,326 research outputs across all sources so far. This one is in the 37th percentile – i.e., 37% of other outputs scored the same or lower than it.
So far Altmetric has tracked 4,064 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.6. This one is in the 24th percentile – i.e., 24% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 275,972 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 40th percentile – i.e., 40% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 2 others from the same source and published within six weeks on either side of this one. This one has scored higher than all of them