Miller, Tobias and van Colen, Gwenaelle and Sander, Bjoern and Golas, Mariola Monika and Uezguen, Senta and Weigandt, Markus and Goepferich, Achim (2013) Drug Loading of Polymeric Micelles. PHARMACEUTICAL RESEARCH, 30 (2). pp. 584-595. ISSN 0724-8741,
Full text not available from this repository. (Request a copy)Abstract
To gain mechanistic insights into drug loading and lyophilization of polymeric micelles. PEGylated poly-4-(vinylpyridine) micelles were loaded with dexamethasone. Three different methods were applied and compared: O/W emulsion, direct dialysis, cosolvent evaporation. Micellar dispersions with the highest drug load were lyophilized with varying lyoprotectors: sucrose, trehalose, maltose, a polyvinylpyrrolidine derivative, and beta-cyclodextrin derivatives. For comparison, other PEGylated block copolymer micelles (PEGylated polylactic acid, polylactic acid-co-glycolic acid, polycaprolactone) were freeze-dried. Drug loading via direct dialysis from acetone was a less effective loading method which led to dexamethasone loads < 2% w/w. O/W emulsion technique from dichlormethane increased drug load up to similar to 13% w/w; optimized cosolvent evaporation increased load up to similar to 19% w/w. An important step for cosolvent evaporation was solubility screen of the drug prior to preparation. Loading was maintained upon lyophilization with beta-cyclodextrins which proved to be versatile stabilizers for other block copolymer micelles. Careful solvent selection prior to cosolvent evaporation was a beneficial approach to load hydrophobic drugs into polymeric micelles. Moreover, beta-cyclodextrins could be used as versatile lyoprotectors for these micelles.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ALPHA-CYCLODEXTRIN; WATER-STRUCTURE; NANOPARTICLES; DELIVERY; POLYPSEUDOROTAXANES; LYOPHILIZATION; STABILIZATION; PERMEABILITY; SACCHARIDES; FORMULATION; cosolvent evaporation; dexamethasone; direct dialysis; drug load; freeze-drying; HP beta CD; lyophilization; O/W emulsion; polymeric micelles; polypseudorotaxane; SBE beta CD; beta-cyclodextrins |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Technology (Prof. Göpferich) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 27 Apr 2020 07:41 |
| Last Modified: | 27 Apr 2020 07:41 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17248 |
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