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A smart micellar system with an amine-containing polycarbonate shell

Paper ID Volume ID Publish Year Pages File Format Full-Text
1459 84 2012 10 PDF Available
Title
A smart micellar system with an amine-containing polycarbonate shell
Abstract

The present paper reports the design and preparation of an amphiphilic triblock co-polymer poly(ε-caprolactone) (PCL)–poly(6,14-dimethyl-1,3,9,11-tetraoxa-6,14-diaza-cyclohexadecane-2,10-dione) (PADMC)–PCL and the use of micelles composed of them as carriers for pH-sensitive drug release. The triblock co-polymers were synthesized via two-step ring-opening polymerization with catalysis by Novozym-435 lipase. By adjusting the feed ratio, three co-polymers with different PCL lengths and the same PADMC length were produced. The block structure of the co-polymers obtained was confirmed by comparative studies on PCL–PADMC–PCLs and the corresponding random poly(ε-caprolactone-random-6,14-dimethyl-1,3,9,11-tetraoxa-6,14-diaza-cyclohexadecane-2,10-dione) (poly(CL-r-ADMC)) by means of nuclear magnetic resonance and differential scanning calorimetry. Cell cytotoxicity tests showed that the co-polymer displayed no apparent cytotoxicity to 293T and HeLa cells. Transmissions electron microscopy indicates that the self-assembled micelles exhibited a well-defined spherical shape with a diameter between ∼30 and 50 nm. The critical aggregation concentration was dependent on the block composition. Due to the presence of ionizable tertiary amine groups in the PADMC block, acid-induced variation in the micellar morphology was evident with respect to micelle size and size distribution. The size–pH curve was characterized by a smooth sigmoid form, and had a dramatic upward shift with decreasing pH from 6.5 to 4.5, which correlated well with the buffer range of hydrophilic PADMC. As a demonstration of the potential of PCL–PADMC–PCL micelles to control drug delivery, acid induced drug release for prednisone acetate-loaded micelles was explored. PCL–PADMC–PCL micelles show good promise as smart drug carriers, sensing the local specific pH decrease around lesion sites.

Keywords
Triblock co-polymers PCL–PADMC–PCL; Controlled drug release; Micelles; pH sensitivity; Prednisone acetate
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Publisher
Database: Elsevier - ScienceDirect
Journal: Acta Biomaterialia - Volume 8, Issue 2, February 2012, Pages 589–598
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us