Leonelli Francesca, La Bella Angela, Migneco Luisa Maria, Bettolo Rinaldo Marini
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.
Molecules. 2008 Feb 12;13(2):360-78. doi: 10.3390/molecules13020360.
Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatment of breast and ovarian cancer, suffers from significant disadvantages such as low solubility, certain toxicity and specific drug-resistance of some tumor cells. To overcome these problems 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 biocompatible polymer offers, in general, many advantages such as better drug solubilization, better stabilization, specific localization and controlled release. Hereafter the design, synthesis and applications of hyaluronic acid-paclitaxel bioconjugates are reviewed. An overview of HA-paclitaxel combinations is also given.
紫杉醇(1a)是一种主要用于治疗乳腺癌和卵巢癌的著名抗肿瘤药物,但存在显著缺点,如溶解度低、有一定毒性以及某些肿瘤细胞具有特定耐药性。为克服这些问题,人们开展了广泛研究。在各种提出的策略中,将紫杉醇(1a)与生物相容性聚合物(如透明质酸(HA,2))偶联也被考虑在内。一般来说,将生物活性化合物与生物相容性聚合物偶联具有许多优点,如更好的药物增溶、更好的稳定性、特定定位和控释。以下将对透明质酸 - 紫杉醇生物共轭物的设计、合成及应用进行综述。还将对HA - 紫杉醇组合进行概述。