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Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper–Lin small composite design

Overview of attention for article published in Drug Design, Development and Therapy, February 2016
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Title
Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper–Lin small composite design
Published in
Drug Design, Development and Therapy, February 2016
DOI 10.2147/dddt.s101900
Pubmed ID
Authors

Khalid M. El-Say

Abstract

This study was aimed at developing a controlled-release cetirizine hydrochloride (CTZ)-loaded polymethacrylate microsphere by optimization technique using software-based response surface methodology. The emulsion solvent evaporation method was utilized in the preparation of microspheres. Four process variables were selected, namely, Eudragit RLPO loading percentage in total polymer, the emulsifier hydrophilic lipophilic balance (HLB), the antitacking percentage, and the dispersed phase volume. The desired responses were particle size, angle of repose, production yield, encapsulation efficiency, loading capacity, initial drug release, and the time for 85% of drug release from the microspheres. Optimization was carried out by fitting the experimental data to the software program (Statgraphics Centurion XV). Moreover, 18 batches were subjected to various characterization tests required for the production of dosage form. The pharmacokinetic parameters were evaluated after the oral administration of 10 mg CTZ in both optimized formulation and commercial product on healthy human volunteers using a double-blind, randomized, cross-over design. The optimized formulation showed satisfactory yield (84.43%) and drug encapsulation efficiency (87.1%). Microspheres were of spherical shape, smooth surface, and good flowability with an average size of 142.3 μm. The developed optimized batch of microspheres ensured 28.87% initial release after 2 hours, and the release of CTZ extended for >12 hours. In addition, the relative bioavailability of the optimized formulation was 165.5% with respect to the marketed CTZ tablets indicating a significant enhancement of CTZ bioavailability. Thus, there is an expectation to decrease the administered dose and the frequency of administration, and subsequently minimize the adverse effects that are faced by the patient during the treatment.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 73 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 73 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 15 21%
Student > Ph. D. Student 11 15%
Student > Bachelor 8 11%
Other 6 8%
Professor > Associate Professor 3 4%
Other 10 14%
Unknown 20 27%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 19 26%
Chemistry 7 10%
Biochemistry, Genetics and Molecular Biology 5 7%
Agricultural and Biological Sciences 4 5%
Medicine and Dentistry 4 5%
Other 11 15%
Unknown 23 32%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. 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 25 February 2016.
All research outputs
#6,288,808
of 7,282,696 outputs
Outputs from Drug Design, Development and Therapy
#635
of 945 outputs
Outputs of similar age
#237,552
of 282,564 outputs
Outputs of similar age from Drug Design, Development and Therapy
#63
of 87 outputs
Altmetric has tracked 7,282,696 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 945 research outputs from this source. They receive a mean Attention Score of 3.2. This one is in the 1st percentile – i.e., 1% 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 282,564 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 87 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.