Development and characterization of a novel drug nanocarrier for oral delivery, based on self-assembled β-casein micelles

Michal Bachar, Amitai Mandelbaum, Irina Portnaya, Hadas Perlstein, Simcha Even-Chen, Yechezkel Barenholz, Dganit Danino*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

104 Scopus citations

Abstract

β-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 β-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.

Original languageEnglish
Pages (from-to)164-171
Number of pages8
JournalJournal of Controlled Release
Volume160
Issue number2
DOIs
StatePublished - 10 Jun 2012
Externally publishedYes

Keywords

  • Amphiphilic block copolymers
  • Celecoxib
  • Drug delivery
  • Nanomedicine
  • Protein micelles

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