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- Title
Comparative Investigations on In Vitro Serum Stability of Polymeric Micelle Formulations.
- Authors
Miller, Tobias; Rachel, Reinhard; Besheer, Ahmed; Uezguen, Senta; Weigandt, Markus; Goepferich, Achim
- Abstract
Purpose: Stability of polymeric micelles upon injection is essential for a drug delivery system but is not fully understood. We optimized an analytical test allowing quantification of micellar stability in biofluids and applied it to a variety of block copolymer micelles with different hydrophobic block architechtures. Methods: Polymeric micelles were prepared from four different polymers and investigated via encapsulation of two fluorescent dyes. Samples were incubated in human serum; changes in Foerster Resonance Energy Transfer (FRET) were recorded as a function of time. This fluorescence-based approach was supported semi-quantitatively by results from Asymmetrical Flow Field-Flow-Fractionation (AF4). Results: After incubation experiments, micellar stability was determined by calculation of two stability-indicating parameters: residual micellar fractions (RMFs) and in vitro serum half-lives. Both parameters showed that PEG-PVPy micelles rapidly destabilized after 3 h (RMF < 45%), whereas PEG-PLA, PEG-PLGA and PEG-PCL micelles were far more stable (RMFs 65 to 98%). Conclusion: This FRET-based assay is a valuable tool in evaluating and screening serum stability of polymeric micelles and revealed low serum stability of PEG-PVPy micelles compared to polyester-based micelles.
- Subjects
COMPARATIVE studies; POLYMERIC drugs; INJECTIONS; DRUG delivery systems; CLINICAL drug trials; DRUG stability; TRANSMISSION electron microscopy
- Publication
Pharmaceutical Research, 2012, Vol 29, Issue 2, p448
- ISSN
0724-8741
- Publication type
Article
- DOI
10.1007/s11095-011-0555-x