| Title |
Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal
|
|---|---|
| Published in |
International Journal of Nanomedicine, July 2012
|
| DOI | 10.2147/ijn.s33186 |
| Pubmed ID | |
| Authors |
Manal A Elsheikh, Yosra SR Elnaggar, Eman Y Gohar, Ossama Y Abdallah |
| Abstract |
Raloxifene hydrochloride (RLX) is a selective estrogen-receptor modulator for treatment of osteoporosis and prevention of breast and endometrial cancer. By virtue of extensive presystemic clearance, RLX bioavailability is only 2%. The current study aimed to tailor and characterize RLX-loaded self-nanoemulsifying drug-delivery systems (SNEDDS) using bioactive excipients affecting drug metabolism. The potential of oral nanocarriers to enhance RLX delivery to endocrine target organs was assessed in fasted and fed female Wistar rats using high-performance liquid chromatography. RLX was loaded in the dissolved and dispersed status in the alkalinized (A-SNEDDS) and nonalkalinized (NA-SNEDDS) systems, respectively. Optimization and assessment relied on solubility studies, emulsification efficiency, phase diagrams, dilution robustness, cloud point, particle size, zeta potential (ZP), polydispersity index (PDI), and transmission electron microscopy. In vitro release was assessed using dialysis bag versus dissolution cup methods. NA-SNEDDS were developed with suitable globule size (38.49 ± 4.30 nm), ZP (31.70 ± 3.58 mV), PDI (0.31 ± 0.02), and cloud point (85°C). A-SNEDDS exhibited good globule size (35 ± 2.80 nm), adequate PDI (0.28 ± 0.06), and lower ZP magnitude (-21.20 ± 3.46 mV). Transmission electron microscopy revealed spherical globules and contended data of size analysis. Release studies demonstrated a nonsignificant enhancement of RLX release from NA-SNEDDS compared to drug suspension with the lowest release shown by A-SNEDDS. A conflicting result was elucidated from in vivo trial. A significant enhancement in RLX uptake by endocrine organs was observed after nanocarrier administration compared to RLX suspension. In vivo studies reflected a poor in vitro/in vivo correlation, recommended nanocarrier administration before meals, and did not reveal any advantage for drug loading in the solubilized form (A-SNEDDS). To conclude, NA-SNEDDS possessed superior in vitro characteristics to A-SNEDDS, with equal in vivo potential. NA-SNEDDS elaborated in this work could successfully double RLX delivery to endocrine target organs, with promising consequences of lower dose and side effects of the drug. |
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.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 120 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Malaysia | 1 | <1% |
| India | 1 | <1% |
| Denmark | 1 | <1% |
| Unknown | 117 | 98% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 25 | 21% |
| Student > Ph. D. Student | 21 | 18% |
| Researcher | 12 | 10% |
| Professor > Associate Professor | 5 | 4% |
| Lecturer | 5 | 4% |
| Other | 14 | 12% |
| Unknown | 38 | 32% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 35 | 29% |
| Medicine and Dentistry | 19 | 16% |
| Agricultural and Biological Sciences | 7 | 6% |
| Chemistry | 7 | 6% |
| Psychology | 2 | 2% |
| Other | 8 | 7% |
| Unknown | 42 | 35% |
Attention Score in Context
This research output has an Altmetric Attention Score of 10. 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 08 December 2020.
All research outputs
#3,661,761
of 25,584,565 outputs
Outputs from International Journal of Nanomedicine
#233
of 4,077 outputs
Outputs of similar age
#23,493
of 177,038 outputs
Outputs of similar age from International Journal of Nanomedicine
#4
of 85 outputs
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So far Altmetric has tracked 4,077 research outputs from this source. They receive a mean Attention Score of 4.8. This one has done particularly well, scoring higher than 93% of its peers.
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We're also able to compare this research output to 85 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 96% of its contemporaries.