Thermosensitive poly(organophosphazene)–paclitaxel conjugate gels for antitumor applications
✍ Scribed by ChangJu Chun; Sun Mi Lee; Sang Yoon Kim; Han Kwang Yang; Soo-Chang Song
- Book ID
- 104003796
- Publisher
- Elsevier Science
- Year
- 2009
- Tongue
- English
- Weight
- 822 KB
- Volume
- 30
- Category
- Article
- ISSN
- 0142-9612
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✦ Synopsis
A poly(organophosphazene)-PTX conjugate was synthesized by a covalent ester linkage between PTX and carboxylic acid-terminated poly(organophosphazene), which can be readily modified by various hydrophobic, hydrophilic, and other functional substitutes. The physicochemical properties, hydrolytic degradation and PTX release behaviors of the polymer-PTX conjugate were characterized, in addition to the in vitro and in vivo antitumor activities. The aqueous solutions of these conjugates showed a sol-gel transition behavior that depended on temperature changes. The in vitro antitumor activity of the polymer-PTX conjugate was investigated by an MTT assay against human tumor cell lines. From the in vivo antitumor activity studies with tumor-induced (xenografted) nude mice, the polymer-paclitaxel conjugate hydrogels after local injection at the tumor site were shown to inhibit tumor growth more effectively and longer than paclitaxel and saline alone, indicating that the tumor-active paclitaxel from the polymer-PTX conjugate hydrogel is released slowly over a longer period of time and effectively accumulated locally in the tumor sites. These combined observations suggest that this poly (organophosphazene)-PTX conjugate holds promise for use in clinical studies as single and/or combination therapies.