Abstract:
:Efficacy of anticancer drug is limited by the severe adverse effects induced by drug; therefore the crux is in designing delivery systems targeted only to cancer cells. Toward this objectives, we propose, synthesis of poly(ethylene glycol) (PEG)-doxorubicin (DOX) prodrug conjugates consisting N-acetyl glucosamine (NAG) as a targeting moiety. Multicomponent system proposed here is characterized by (1)H NMR, UV spectroscopy, and HPLC. The multicomponent system is evaluated for in vitro cellular kinetics and anticancer activity using MCF-7 and MDA-MB-231 cells. Molecular modeling study demonstrated sterically stabilized conformations of polymeric conjugates. Interestingly, PEG-DOX conjugate with NAG ligand showed significantly higher cytotoxicity compared to drug conjugate with DOX. In addition, the polymer drug conjugate with NAG and DOX showed enhanced internalization and retention effect in cancer cells, compared to free DOX. Thus, with enhanced internalization and targeting ability of PEG conjugate of NAG-DOX has implication in targeted anticancer therapy.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Pawar SK,Badhwar AJ,Kharas F,Khandare JJ,Vavia PRdoi
10.1016/j.ijpharm.2012.05.078subject
Has Abstractpub_date
2012-10-15 00:00:00pages
183-93issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(12)00621-7journal_volume
436pub_type
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