CONICET - Universidad de Buenos Aires, Instituto de Investigaciones Farmacológicas (ININFA), Buenos Aires, Argentina.
Laboratory of Pharmaceutical Nanomaterials Science, Department of Materials Science and Engineering, Technion-Israel Institute of Technology, Technion City, Haifa, Israel.
J Control Release. 2018 Sep 10;285:106-141. doi: 10.1016/j.jconrel.2018.06.031. Epub 2018 Jun 30.
Despite the wide range of diseases affecting the eye, ocular bioavailability remains a challenge in ophthalmic drug delivery. Nowadays an extensive variety of polymers are being explored to develop colloidal drug carriers which show better performance than the more popular drug solutions. For instance, regardless of the type of polymer used, these systems prolong the residence time of the drug in the absorption site with respect to conventional aqueous eye drops which are rapidly cleared from eye surface. Furthermore, colloidal drug carriers can be internalized by cells. In addition, positively charged particles penetrate the cornea more effectively than neutral or negatively charged ones. These phenomena lead to higher ocular bioavailability. This review overviews the different polymers available to produce drug-loaded gels, microparticles and nanoparticles, highlighting the advantageous features and biocompatibility of each polymer and the major achievements in the field of ocular delivery. In addition, the design of more complex delivery systems that combine several delivery platforms is presented. Finally, regulatory aspects relevant to the clinical translation of advanced ophthalmic drug delivery systems are also discussed. All together, this manuscript is aimed at guiding pharmaceutical research and development towards the rationale polymer selection to produce drug delivery systems that improve the performance of drugs for the therapy of ophthalmic diseases.
尽管影响眼睛的疾病种类繁多,但眼部生物利用度仍然是眼科药物输送的一个挑战。如今,人们正在探索广泛的聚合物来开发胶体药物载体,这些载体的性能优于更受欢迎的药物溶液。例如,无论使用哪种类型的聚合物,这些系统都能延长药物在吸收部位的停留时间,而常规的水性眼药水会很快从眼睛表面清除。此外,胶体药物载体可以被细胞内化。此外,带正电荷的颗粒比中性或带负电荷的颗粒更有效地穿透角膜。这些现象导致更高的眼部生物利用度。本文综述了可用于制备载药凝胶、微球和纳米粒的不同聚合物,突出了每种聚合物的优势特征和生物相容性,以及在眼部给药领域的主要成就。此外,还介绍了将几种给药平台结合起来的更复杂给药系统的设计。最后,还讨论了与先进眼科药物输送系统临床转化相关的监管方面。总的来说,本文旨在指导药物研发,合理选择聚合物,以生产改善治疗眼部疾病药物性能的药物输送系统。