Miller, Tobias and Rachel, Reinhard and Besheer, Ahmed and Uezguen, Senta and Weigandt, Markus and Goepferich, Achim (2012) Comparative Investigations on In Vitro Serum Stability of Polymeric Micelle Formulations. PHARMACEUTICAL RESEARCH, 29 (2). pp. 448-459. ISSN 0724-8741,
Full text not available from this repository. (Request a copy)Abstract
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. 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). 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%). 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.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | AMPHIPHILIC DIBLOCK COPOLYMERS; KINETICALLY FROZEN COLLOIDS; DRUG-DELIVERY; NONIONIC SURFACTANT; BLOCK-COPOLYMERS; VIVO STABILITY; NANOPARTICLES; SYSTEMS; PEG; MACROSURFACTANTS; field flow fractionation; foerster resonance energy transfer; polymeric micelles; serum stability; transmission electron microscopy |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Technology (Prof. Göpferich) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 20 May 2020 06:30 |
| Last Modified: | 20 May 2020 06:30 |
| URI: | https://pred.uni-regensburg.de/id/eprint/19335 |
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