Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy "Carol Davila", Bucharest 020956, Romania.
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, University of Medicine and Pharmacy "Carol Davila", Bucharest 020956, Romania.
Mar Drugs. 2018 Oct 9;16(10):373. doi: 10.3390/md16100373.
Ocular in situ gels are a promising alternative to overcome drawbacks of conventional eye drops because they associate the advantages of solutions such as accuracy and reproducibility of dosing, or ease of administration with prolonged contact time of ointments. Chitosan is a natural polymer suitable for use in ophthalmic formulations due to its biocompatibility, biodegradability, mucoadhesive character, antibacterial and antifungal properties, permeation enhancement and corneal wound healing effects. The combination of chitosan, pH-sensitive polymer, with other stimuli-responsive polymers leads to increased mechanical strength of formulations and an improved therapeutic effect due to prolonged ocular contact time. This review describes in situ gelling systems resulting from the association of chitosan with various stimuli-responsive polymers with emphasis on the mechanism of gel formation and application in ophthalmology. It also comprises the main techniques for evaluation of chitosan in situ gels, along with requirements of safety and ocular tolerability.
眼用原位凝胶是克服传统滴眼液缺点的一种很有前途的替代方法,因为它们结合了溶液的优点,如剂量的准确性和重现性,或易于给药与软膏的延长接触时间。壳聚糖是一种适合用于眼科制剂的天然聚合物,因为它具有生物相容性、生物降解性、粘膜粘附性、抗菌和抗真菌特性、渗透增强和角膜愈合作用。壳聚糖与 pH 敏感聚合物与其他刺激响应聚合物的结合导致制剂的机械强度增加,并由于延长的眼部接触时间而提高治疗效果。本文综述了壳聚糖与各种刺激响应聚合物结合形成的原位凝胶系统,重点介绍了凝胶形成的机制及其在眼科中的应用。它还包括壳聚糖原位凝胶评价的主要技术,以及安全性和眼部耐受性要求。
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