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Naringenin-loaded solid lipid nanoparticles: preparation, controlled delivery, cellular uptake, and pulmonary pharmacokinetics

Overview of attention for article published in Drug Design, Development and Therapy, March 2016
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Title
Naringenin-loaded solid lipid nanoparticles: preparation, controlled delivery, cellular uptake, and pulmonary pharmacokinetics
Published in
Drug Design, Development and Therapy, March 2016
DOI 10.2147/dddt.s97738
Pubmed ID
Authors

Peng Ji, Tong Yu, Ying Liu, Jie Jiang, Jie Xu, Ying Zhao, Yanna Hao, Yang Qiu, Wenming Zhao, Chao Wu

Abstract

Naringenin (NRG), a flavonoid compound, had been reported to exhibit extensive pharmacological effects, but its water solubility and oral bioavailability are only~46±6 µg/mL and 5.8%, respectively. The purpose of this study is to design and develop NRG-loaded solid lipid nanoparticles (NRG-SLNs) to provide prolonged and sustained drug release, with improved stability, involving nontoxic nanocarriers, and increase the bioavailability by means of pulmonary administration. Initially, a group contribution method was used to screen the best solid lipid matrix for the preparation of SLNs. NRG-SLNs were prepared by an emulsification and low-temperature solidification method and optimized using an orthogonal experiment approach. The morphology was examined by transmission electron microscopy, and the particle size and zeta potential were determined by photon correlation spectroscopy. The total drug content of NRG-SLNs was measured by high-performance liquid chromatography, and the encapsulation efficiency (EE) was determined by Sephadex gel-50 chromatography and high-performance liquid chromatography. The in vitro NRG release studies were carried out using a dialysis bag. The best cryoprotectant to prepare NRG-SLN lyophilized powder for future structural characterization was selected using differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy. The short-term stability, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay, cellular uptake, and pharmacokinetics in rats were studied after pulmonary administration of NRG-SLN lyophilized powder. Glycerol monostearate was selected to prepare SLNs, and the optimal formulation of NRG-SLNs was spherical in shape, with a particle size of 98 nm, a polydispersity index of 0.258, a zeta potential of -31.4 mV, a total drug content of 9.76 mg, an EE of 79.11%, and a cumulative drug release of 80% in 48 hours with a sustained profile. In addition, 5% mannitol (w/v) was screened as a cryoprotectant. Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies confirmed that the drug was encapsulated into SLNs in an amorphous form. The lyophilized powder was stable at both refrigeration (4°C) and ambient temperature (25°C) for 3 months, and the MTT assay demonstrated that the SLNs were nontoxic. The cellular uptake of fluorescein isothiocyanate-labeled SLNs in A549 cells was highly time dependent over a period of 3 hours, while the pharmacokinetic study in Sprague Dawley rats showed that the relative bioavailability of NRG-SLNs was 2.53-fold greater than that of NRG suspension after pulmonary administration. This study shows that SLNs offer a promising pulmonary delivery system to increase the bioavailability of the poorly water-soluble drug NRG.

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X Demographics

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

Mendeley readers

The data shown below were compiled from readership statistics for 175 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Malaysia 1 <1%
Unknown 174 99%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 27 15%
Student > Master 20 11%
Student > Bachelor 16 9%
Researcher 15 9%
Student > Doctoral Student 11 6%
Other 24 14%
Unknown 62 35%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 47 27%
Biochemistry, Genetics and Molecular Biology 17 10%
Agricultural and Biological Sciences 11 6%
Chemistry 11 6%
Medicine and Dentistry 4 2%
Other 15 9%
Unknown 70 40%
Attention Score in Context

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 02 March 2016.
All research outputs
#22,778,604
of 25,394,764 outputs
Outputs from Drug Design, Development and Therapy
#1,757
of 2,270 outputs
Outputs of similar age
#269,245
of 312,692 outputs
Outputs of similar age from Drug Design, Development and Therapy
#66
of 83 outputs
Altmetric has tracked 25,394,764 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 2,270 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.1. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 83 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.