| Title |
A novel drug–phospholipid complex enriched with micelles: preparation and evaluation in vitro and in vivo
|
|---|---|
| Published in |
International Journal of Nanomedicine, February 2013
|
| DOI | 10.2147/ijn.s39526 |
| Pubmed ID | |
| Authors |
Hai-jian Xia, Zhen-hai Zhang, Xin Jin, Qin Hu, Xiao-yun Chen, Xiao-bin Jia |
| Abstract |
Mixed micelles are widely used to increase solubility and bioavailability of poorly soluble drugs. One promising antitumor drug candidate is 20(S)-protopanaxadiol (PPD), although its clinical application is limited by low water solubility and poor bioavailability after oral administration. In this study, we developed mixed micelles consisting of PPD-phospholipid complexes and Labrasol(®) and evaluated their potential for oral PPD absorption. Micelles were prepared using a solvent-evaporation method, and their physicochemical properties, including particle size, zeta potential, morphology, crystal type, drug loading, drug entrapment efficiency, and solubility, were characterized. Furthermore, in vitro release was investigated using the dialysis method, and transport and bioavailability of the mixed micelles were investigated through a Caco-2 cell monolayer and in vivo absorption studies performed in rats. Compared with the solubility of free PPD (3 μg/mL), the solubility of PPD in the prepared mixed micelles was 192.41 ± 1.13 μg/mL in water at room temperature. The in vitro release profiles showed a significant difference between the more rapid release of free PPD and the slower and more sustained release of the mixed micelles. At the end of a 4-hour transport study using Caco-2 cells, the apical-to-basolateral apparent permeability coefficients (P(app)) increased from (1.12 ± 0.21) × 10(6) cm/s to (1.78 ± 0.16) × 10(6) cm/s, while the basolateral-to-apical P(app) decreased from (2.42 ± 0.16) × 10(6) cm/s to (2.12 ± 0.32) × 10(6). In this pharmacokinetic study, compared with the bioavailability of free PPD (area under the curve [AUC](0-∞)), the bioavailability of PPD from the micelles (AUC(0-∞)) increased by approximately 216.36%. These results suggest that novel mixed micelles can significantly increase solubility, enhance absorption, and improve bioavailability. Thus, these prepared micelles might be potential carriers for oral PPD delivery in antitumor therapies. |
Mendeley readers
The data shown below were compiled from readership statistics for 48 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| India | 1 | 2% |
| Unknown | 47 | 98% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 10 | 21% |
| Student > Master | 6 | 13% |
| Researcher | 3 | 6% |
| Student > Postgraduate | 3 | 6% |
| Professor > Associate Professor | 3 | 6% |
| Other | 4 | 8% |
| Unknown | 19 | 40% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 9 | 19% |
| Biochemistry, Genetics and Molecular Biology | 5 | 10% |
| Agricultural and Biological Sciences | 3 | 6% |
| Medicine and Dentistry | 3 | 6% |
| Chemistry | 2 | 4% |
| Other | 4 | 8% |
| Unknown | 22 | 46% |
Attention Score in Context
This research output has an Altmetric Attention Score of 4. 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 24 January 2019.
All research outputs
#8,262,445
of 25,374,917 outputs
Outputs from International Journal of Nanomedicine
#1,007
of 4,122 outputs
Outputs of similar age
#85,319
of 291,228 outputs
Outputs of similar age from International Journal of Nanomedicine
#23
of 78 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one has received more attention than most of these and is in the 66th percentile.
So far Altmetric has tracked 4,122 research outputs from this source. They receive a mean Attention Score of 4.7. This one has gotten more attention than average, scoring higher than 74% of its peers.
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 291,228 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 69% of its contemporaries.
We're also able to compare this research output to 78 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 65% of its contemporaries.