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Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†
Dipartimento di Chimica and Istituto di Chimica Biomolecolare del CNR, Sezione di Roma, Università degli Studi di Roma "La Sapienza”, P.le Aldo Moro 5, BOX n. 34 ROMA 62, I-00185 Roma, Italy
* Author to whom correspondence should be addressed.
Received: 29 January 2008; in revised form: 11 February 2008 / Accepted: 11 February 2008 / Published: 12 February 2008
(This article belongs to the Special Issue Prodrugs
Abstract: Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatmentof breast and ovarian cancer, suffers from significant disadvantages such as low solubility,certain toxicity and specific drug-resistance of some tumor cells. To overcome theseproblems extensive research has been carried out. Among the various proposed strategies,the conjugation of paclitaxel (1a) to a biocompatible polymer, such as hyaluronic acid(HA, 2), has also been considered. Coupling a bioactive compound to a biocompatiblepolymer offers, in general, many advantages such as better drug solubilization, betterstabilization, specific localization and controlled release. Hereafter the design, synthesisand applications of hyaluronic acid-paclitaxel bioconjugates are reviewed. An overview ofHA-paclitaxel combinations is also given.
Keywords: Paclitaxel; Hyaluronic Acid; Hyaluronic Acid-Paclitaxel Bioconjugate; Synthesis; Biological Activity.
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Leonelli, F.; La Bella, A.; Migneco, L.M.; Bettolo, R.M. Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†. Molecules 2008, 13, 360-378.
Leonelli F, La Bella A, Migneco LM, Bettolo RM. Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†. Molecules. 2008; 13(2):360-378.
Leonelli, Francesca; La Bella, Angela; Migneco, Luisa M.; Bettolo, Rinaldo M. 2008. "Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†." Molecules 13, no. 2: 360-378.