Alonso María José, Sánchez Alejandro
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
J Pharm Pharmacol. 2003 Nov;55(11):1451-63. doi: 10.1211/0022357022476.
This paper presents an overview of the potential of chitosan-based systems for improving the retention and biodistribution of drugs applied topically onto the eye. Besides its low toxicity and good ocular tolerance, chitosan exhibits favourable biological behaviour, such as bioadhesion- and permeability-enhancing properties, and also interesting physico-chemical characteristics, which make it a unique material for the design of ocular drug delivery vehicles. The review summarizes the techniques for the production of chitosan gels, chitosan-coated colloidal systems and chitosan nanoparticles, and describes their mechanism of action upon contact with the ocular mucosa. The results reported until now have provided evidence of the potential of chitosan gels for enhancing and prolonging the retention of drugs on the eye surface. On the other hand, chitosan-based colloidal systems were found to work as transmucosal drug carriers, either facilitating the transport of drugs to the inner eye (chitosan-coated colloidal systems containing indometacin) or their accumulation into the corneal/conjunctival epithelia (chitosan nanoparticles containing ciclosporin). Finally, the tolerance, toxicity and biodegradation of the carriers under evaluation were reviewed.
本文概述了基于壳聚糖的体系在改善眼部局部用药的药物滞留和生物分布方面的潜力。除了低毒性和良好的眼部耐受性外，壳聚糖还表现出良好的生物学行为，如生物黏附性和通透性增强特性，以及有趣的物理化学特性，这使其成为设计眼部药物递送载体的独特材料。该综述总结了壳聚糖凝胶、壳聚糖包衣胶体系统和壳聚糖纳米颗粒的制备技术，并描述了它们与眼黏膜接触时的作用机制。目前报道的结果证明了壳聚糖凝胶在增强和延长药物在眼表面滞留方面的潜力。另一方面，发现基于壳聚糖的胶体系统可作为透黏膜药物载体，要么促进药物向眼内转运（含吲哚美辛的壳聚糖包衣胶体系统），要么使其在角膜/结膜上皮中蓄积（含环孢素的壳聚糖纳米颗粒）。最后，对所评估载体的耐受性、毒性和生物降解进行了综述。
