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治疗性纳米乳剂在眼科药物给药中的应用:眼部药物递送的制剂概念和特性技术。

Therapeutic nanoemulsions in ophthalmic drug administration: Concept in formulations and characterization techniques for ocular drug delivery.

机构信息

Molecular Genetics Laboratory, Department of Biotechnology, Institute of Biotechnology, College of Life and Applied Sciences, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk 38541, Republic of Korea.

Molecular Genetics Laboratory, Department of Biotechnology, Institute of Biotechnology, College of Life and Applied Sciences, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk 38541, Republic of Korea; Stemforce, 313 Institute of Industrial Technology, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk 38541, Republic of Korea.

出版信息

J Control Release. 2020 Dec 10;328:895-916. doi: 10.1016/j.jconrel.2020.10.025. Epub 2020 Oct 16.

Abstract

The eye is the specialized part of the body and is comprised of numerous physiological ocular barriers that limit the drug absorption at the action site. Regardless of various efforts, efficient topical ophthalmic drug delivery remains unsolved, and thus, it is extremely necessary to advance the contemporary treatments of ocular disorders affecting the anterior and posterior cavities. Nowadays, the advent of nanotechnology-based multicomponent nanoemulsions for ophthalmic drug delivery has gained popularity due to the enhancement of ocular penetrability, improve bioavailability, increase solubility, and stability of lipophilic drugs. Nanoemulsions offer the sustained/controlled drug release and increase residence time which depend on viscosity, compositions, and stabilization process, etc.; hence, decrease the instillation frequency and improve patient compliance. Further, due to the nanosized of nanoemulsions, the sterilization process is easy as conventional solutions and cause no blur vision. The review aims to summarizes the various ocular barriers, manufacturing techniques, possible mechanisms to the retention and deep penetration into the eye, and appropriate excipients with their under-lying selection principles to prevent destabilization of nanoemulsions. This review also discusses the characterization parameters of ocular drug delivery to spike the interest of those contemplating a foray in this field. Here, in short, nanoemulsions are abridged with concepts to design clinically advantageous ocular drug delivery.

摘要

眼睛是人体的专门部位,由许多生理眼部屏障组成,这些屏障限制了作用部位的药物吸收。尽管进行了各种努力,但高效的局部眼科药物输送仍然未得到解决,因此,非常有必要推进影响前房和后房的眼部疾病的当代治疗方法。如今,基于纳米技术的多组分纳米乳剂在眼科药物输送中的应用越来越受欢迎,因为它可以增强眼部通透性、提高生物利用度、增加亲脂性药物的溶解度和稳定性。纳米乳剂提供了持续/控制药物释放和增加滞留时间,这取决于粘度、组成和稳定化过程等;因此,减少了滴眼次数,提高了患者的依从性。此外,由于纳米乳剂的纳米尺寸,其灭菌过程与常规溶液一样简单,不会造成视力模糊。本综述旨在总结各种眼部屏障、制造技术、可能的保留和深入穿透眼睛的机制,以及适当的辅料及其潜在的选择原则,以防止纳米乳剂的失稳。本综述还讨论了眼部药物输送的特征参数,以激发那些有兴趣涉足这一领域的人的兴趣。在这里,简而言之,纳米乳剂的设计概念被简化为临床优势的眼部药物输送。

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