Comparison of PEG chain length and density on amphiphilic macromolecular nanocarriers: self-assembled and unimolecular micelles.

Abstract:

:Two classes of amphiphilic macromolecules were evaluated for drug delivery applications: those that exist as unimolecular micelles and those that self-assemble in aqueous solution to form micelles. This study compares the poly(ethylene glycol) (PEG) chain length and density that constitute the corona of both classes. In particular, the effect of PEG branching on micellar size, water-solubility, resolubilization rate, drug loading efficiency and drug release rate were analyzed. Pluronic P85 and Cremophor EL, commonly used in pharmaceutical applications, were used as controls. Indomethacin (IMC) was used as the drug for encapsulation, release and resolubilization experiments. Results indicated that smaller micellar sizes, higher water solubilities and faster resolubilization rates were achieved from higher PEG densities compared to linear PEG analog of similar mass. Further, micellar sizes of both higher density PEG and linear PEG macromolecules were constant over a wide temperature range (2-70 degrees C). In contrast, Cremophor EL formed aggregates at 15 degrees C and Pluronic P85 underwent a size transition at 45 degrees C. IMC loading efficiencies for all amphiphilic macromolecules were comparable to controls. However, faster resolubilization and slower drug release were observed for higher density PEG macromolecules compared to linear PEG analogs and controls.

journal_name

Acta Biomater

journal_title

Acta biomaterialia

authors

Wang J,del Rosario LS,Demirdirek B,Bae A,Uhrich KE

doi

10.1016/j.actbio.2008.10.019

subject

Has Abstract

pub_date

2009-03-01 00:00:00

pages

883-92

issue

3

eissn

1742-7061

issn

1878-7568

pii

S1742-7061(08)00335-8

journal_volume

5

pub_type

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