Journal
JOURNAL OF CONTROLLED RELEASE
Volume 160, Issue 2, Pages 164-171Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2012.01.004
Keywords
Celecoxib; Protein micelles; Drug delivery; Amphiphilic block copolymers; Nanomedicine
Funding
- RBNI at the Technion
- Barenholz Fund at HUJI
- Center for Absorption in Science of the Ministry of Immigrant Absorption
- Committee for Planning and Budgeting of the Council for Higher Education
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beta-casein is an amphiphilic protein that self-organizes into well-defined core-shell micelles. We developed these micelles as efficient nanocarriers for oral drug delivery. Our model drug is celecoxib, an anti-inflammatory hydrophobic drug utilized for treatment of rheumatoid arthritis and osteoarthritis, now also evaluated as a potent anticancer drug. This system is unique as it enables encapsulation loads >100-fold higher than other beta-casein/drug formulations, and does not require additives as do other formulations that have high loadings. This is combined with the ability to lyophilize the formulation without a cryoprotectant, long-term physical and chemical stability of the resulting powder, and fully reversible reconstitution of the structures by rehydration. The dry dosage form, in which >95% of the drug is encapsulated, meets the daily dose. Cryo-TEM and DLS prove that drug encapsulation results in micelle swelling, and X-ray diffraction shows that the encapsulated drug is amorphous. Altogether, our novel dosage form is highly advantageous for oral administration. (C) 2012 Elsevier B. V. All rights reserved.
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