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Synthesis and antitumor activity of doxorubicin conjugated stearic acid-g-chitosan oligosaccharide polymeric micelles

Paper ID Volume ID Publish Year Pages File Format Full-Text
8779 605 2009 9 PDF Available
Title
Synthesis and antitumor activity of doxorubicin conjugated stearic acid-g-chitosan oligosaccharide polymeric micelles
Abstract

Doxorubicin conjugated stearic acid-g-chitosan oligosaccharide polymeric micelles (DOX–CSO–SA) was synthesized via cis-aconityl bond between the anticancer drug doxorubicin (DOX) and stearic acid grafted chitosan oligosaccharide (CSO–SA) in this paper. The CSO–SA micelles had been demonstrated faster internalization ability into tumor cells. Here, the CSO–SA with 6.47% amino substituted degree (SD%) was used to synthesize DOX–CSO–SA. The critical micelle concentration (CMC) was about 0.14 mg mL−1. The micelles with 1 mg mL−1 CSO–SA concentration had 32.7 nm number average diameter with a narrow size distribution and 51.5 mV surface potential. After conjugating with doxorubicin, CMC of DOX–CSO–SA descended; the micellar size increased; and the zeta potential decreased. The DOX–CSO–SA micelles indicated pH-dependent DOX release behavior. The release rate of DOX from DOX–CSO–SA micelles increased significantly with the reductions of the pH for release medium from 7.2 to 5.0. In vitro antitumor activity tests of DOX–CSO–SA micelles against human breast carcinoma (MCF-7) cells and their multi-drug resistant (MCF-7/Adr) cells presented the reversal activity against DOX resistance MCF-7 cells (MCF-7/Adr). The in vivo antitumor activity results showed that DOX–CSO–SA micelles treatments effectively suppressed the tumor growth and reduced the toxicity against animal body than commercial doxorubicin hydrochloride injection.

Keywords
Chitosan oligosaccharide; Polymeric micelles; Doxorubicin; Cis-aconityl linkage; Antitumor activity; Drug resistance
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Synthesis and antitumor activity of doxorubicin conjugated stearic acid-g-chitosan oligosaccharide polymeric micelles
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 30, Issue 36, December 2009, Pages 6955–6963
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