| Title |
Sustained-release liquisolid compact tablets containing artemether-lumefantrine as alternate-day regimen for malaria treatment to improve patient compliance
|
|---|---|
| Published in |
International Journal of Nanomedicine, November 2016
|
| DOI | 10.2147/ijn.s92755 |
| Pubmed ID | |
| Authors |
Petra Obioma Nnamani, Agatha Adaora Ugwu, Emmanuel Chinedu Ibezim, Franklin Chimaobi Kenechukwu, Paul Achile Akpa, John-Dike Nwabueze Ogbonna, Nicholas Chinedu Obitte, Amelia Ngozi Odo, Maike Windbergs, Claus-Michael Lehr, Anthony Amaechi Attama |
| Abstract |
The present study aimed to develop low-dose liquisolid tablets of two antimalarial drugs artemether-lumefantrine (AL) from a nanostructured lipid carrier (NLC) of lumefantrine (LUM) and estimate the potential of AL as an oral delivery system in malariogenic Wistar mice. LUM-NLCs were prepared by hot homogenization using Precirol(®) ATO 5/Transcutol(®) HP and tallow fat/Transcutol(®) HP optimized systems containing 3:1 ratios of the lipids, respectively, as the matrices. LUM-NLC characteristics, including morphology, particle size, zeta potential, encapsulation efficiency, yield, pH-dependent stability, and interaction studies, were investigated. Optimized LUM-NLCs were mixed with artemether powder and other dry ingredients and the resultant powder evaluated for micromeritics. Subsequent AL liquisolid tablets were tested for in vitro drug release and in vivo antiplasmodial activity in mice infected with Plasmodium berghei berghei (NK 65). Results showed that optimized LUM-NLC were stable, spherical, polydispersed but nanometric. Percentage yield and encapsulation efficiency were ~92% and 93% for Precirol(®) ATO 5/Transcutol(®) HP batch, then 81% and 95% for tallow fat/Transcutol(®) HP batch while LUM was amorphous in NLC matrix. In vitro AL release from liquisolid compacts revealed initial burst release and subsequent sustained release. Liquisolid tablet compacts formulated with Precirol(®) ATO 5/Transcutol(®) HP-AL4 achieved higher LUM release in simulated intestinal fluid (84.32%) than tallow fat/Transcutol(®) HP-BL3 (77.9%). Non-Fickian (anomalous) diffusion and super case II transport were the predominant mechanisms of drug release. Equal parasitemia reduction was observed for both batches of tablet compacts (~92%), superior to the reduction obtained with commercial antimalarial formulations: Coartem(®) tablets (86%) and chloroquine phosphate tablets (66%). No significant difference (P<0.05) in parasite reduction between double (4/24 mg/kg) and single (2/12 mg/kg) strength doses of AL compacts was observed. Our result highlights that AL could be formulated in much lower doses (4/24 mg/kg), for once-in-two days oral administration to improve patient compliance, which is currently not obtainable with conventional AL dosage forms. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 50% |
| Unknown | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 69 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 69 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 11 | 16% |
| Lecturer | 7 | 10% |
| Student > Doctoral Student | 5 | 7% |
| Researcher | 5 | 7% |
| Professor > Associate Professor | 4 | 6% |
| Other | 14 | 20% |
| Unknown | 23 | 33% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 26 | 38% |
| Chemistry | 4 | 6% |
| Biochemistry, Genetics and Molecular Biology | 2 | 3% |
| Materials Science | 2 | 3% |
| Nursing and Health Professions | 2 | 3% |
| Other | 7 | 10% |
| Unknown | 26 | 38% |
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 16 December 2016.
All research outputs
#16,048,009
of 25,374,917 outputs
Outputs from International Journal of Nanomedicine
#1,887
of 4,123 outputs
Outputs of similar age
#186,512
of 317,812 outputs
Outputs of similar age from International Journal of Nanomedicine
#46
of 94 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one is in the 34th percentile – i.e., 34% of other outputs scored the same or lower than it.
So far Altmetric has tracked 4,123 research outputs from this source. They receive a mean Attention Score of 4.7. This one is in the 49th percentile – i.e., 49% 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 317,812 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 38th percentile – i.e., 38% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 94 others from the same source and published within six weeks on either side of this one. This one is in the 48th percentile – i.e., 48% of its contemporaries scored the same or lower than it.