| Title |
Self-Assembling Raloxifene Loaded Mixed Micelles: Formulation Optimization, In Vitro Cytotoxicity and In Vivo Pharmacokinetics
|
|---|---|
| Published in |
AAPS PharmSciTech, November 2017
|
| DOI | 10.1208/s12249-017-0919-6 |
| Pubmed ID | |
| Authors |
Radhika Kanade, Mithila Boche, Varsha Pokharkar |
| Abstract |
Raloxifene (RLX) has been strongly recommended for postmenopausal women at high risk of invasive breast cancer and for prevention of osteoporosis. However, low aqueous solubility and reduced bioavailability hinder its clinical application. The objective of this study was to explore the potential of RLX loaded mixed micelles (RLX-MM) using Pluronic F68 and Gelucire 44/14 for enhanced bioavailability and improved anticancer activity on human breast cancer cell line (MCF-7). RLX-MM were prepared by solvent evaporation method and optimized using 32 factorial design. The average size, entrapment efficiency and zeta potential of the optimized formulation were found to be 190 ± 3.3 nm, 79 ± 1.3%, 13 ± 0.8 mV, respectively. In vitro study demonstrated 74.68% drug release from RLX-MM in comparison to 42.49% drug release from RLX dispersion. According to the in vitro cytotoxicity assay, GI50 values on MCF-7 breast cancer cell line for RLX-MM and free RLX were found to be 22.5 and 94.71 μg/mL, respectively. Significant improvement (P < 0.05) in the anticancer activity on MCF-7 cell line was observed in RLX-MM over RLX pure drug. Additionally, oral bioavailability of RLX-MM was improved by 1.5-fold over free RLX when administered in female Wistar rats. Incorporation of RLX in the hydrophobic core and improved solubility of the drug due to hydrophilic shell attributed to the enhanced cytotoxicity and bioavailability of RLX-MM. This research establishes the potential of RLX loaded mixed micelles of Pluronic F68 and Gelucire 44/14 for improved bioavailability and anticancer activity on MCF-7 cell line. |
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 % |
|---|---|---|
| United States | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 25 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 25 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Doctoral Student | 3 | 12% |
| Professor | 3 | 12% |
| Student > Master | 3 | 12% |
| Researcher | 2 | 8% |
| Student > Ph. D. Student | 2 | 8% |
| Other | 3 | 12% |
| Unknown | 9 | 36% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 8 | 32% |
| Biochemistry, Genetics and Molecular Biology | 1 | 4% |
| Linguistics | 1 | 4% |
| Computer Science | 1 | 4% |
| Sports and Recreations | 1 | 4% |
| Other | 2 | 8% |
| Unknown | 11 | 44% |
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 29 June 2018.
All research outputs
#18,640,437
of 23,092,602 outputs
Outputs from AAPS PharmSciTech
#1,229
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Outputs of similar age
#326,354
of 438,794 outputs
Outputs of similar age from AAPS PharmSciTech
#21
of 23 outputs
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