| Title |
Preparation, characterization, in vivo pharmacokinetics, and biodistribution of polymeric micellar dimethoxycurcumin for tumor targeting
|
|---|---|
| Published in |
International Journal of Nanomedicine, October 2015
|
| DOI | 10.2147/ijn.s91961 |
| Pubmed ID | |
| Authors |
Hui Liu, Hui Xu, Yunxia Jiang, Shengyuan Hao, Feirong Gong, Hongjie Mu, Ke Liu |
| Abstract |
Dimethoxycurcumin (DMC) is an analog of curcumin with superior efficacy in various disease models. Currently, drug delivery system research on DMC is very limited, and it has become a huge challenge to realize further developments and clinical applications. In the present study, a kind of amphiphilic block copolymer, N-t-butoxycarbonyl-phenylalanine terminated monomethoxyl poly (ethylene glycol)-b-poly (ε-caprolactone), or mPEG-PCL-Phe(Boc), was prepared from monomethoxyl poly (ethylene glycol)-b-poly (ε-caprolactone) (mPEG-PCL) with its hydroxyl terminal chemically converted into N-t-butoxycarbonyl-phenylalanine (Boc-Phe). This copolymer was determined to have a fairly low critical micelle concentration (2.56×10(-3) mg/mL) and passive targeting potential to tumor tissue, and thus was applied to develop a polymeric micellar formulation of DMC for the first time. The DMC-loaded micelles prepared by thin-film hydration method had typical shell-core structure, with an average particle size of 17.9±0.4 nm and a polydispersity index of 0.045±0.011. The drug loading capacity and entrapment efficiency were 9.94%±0.15% and 97.22%±0.18%, respectively, indicating a high-affinity interaction between DMC and the copolymer. At a concentration of 2 mg/mL, the reconstituted micelle solution could be maintained for at least 10 days at room temperature, and displayed a low initial burst release followed by a sustained release in vitro. Pharmacokinetic study in rats revealed that in vivo drug exposure of DMC was significantly increased and prolonged by intravenously administering DMC-loaded micelles when compared with the same dose of free DMC dissolved in dimethyl sulfoxide. Furthermore, in vivo distribution results from tumor-bearing nude mice demonstrated that this micellar formulation significantly changed the biodistribution profile of DMC and increased drug accumulation in tumors. Therefore, the polymeric micellar formulation of DMC, based on the amphiphilic block copolymer, mPEG-PCL-Phe(Boc), could provide a desirable method for delivering DMC, especially for applications in cancer therapy. |
X Demographics
The data shown below were collected from the profiles of 4 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Canada | 1 | 25% |
| Unknown | 3 | 75% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 3 | 75% |
| Members of the public | 1 | 25% |
Mendeley readers
The data shown below were compiled from readership statistics for 51 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 51 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 10 | 20% |
| Student > Master | 9 | 18% |
| Student > Bachelor | 5 | 10% |
| Student > Doctoral Student | 3 | 6% |
| Lecturer > Senior Lecturer | 2 | 4% |
| Other | 8 | 16% |
| Unknown | 14 | 27% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 10 | 20% |
| Pharmacology, Toxicology and Pharmaceutical Science | 8 | 16% |
| Chemistry | 3 | 6% |
| Materials Science | 3 | 6% |
| Engineering | 2 | 4% |
| Other | 5 | 10% |
| Unknown | 20 | 39% |
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 15 October 2015.
All research outputs
#15,738,224
of 25,371,288 outputs
Outputs from International Journal of Nanomedicine
#1,775
of 4,121 outputs
Outputs of similar age
#147,353
of 286,859 outputs
Outputs of similar age from International Journal of Nanomedicine
#56
of 133 outputs
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