Battaglia Luigi, Serpe Loredana, Foglietta Federica, Muntoni Elisabetta, Gallarate Marina, Del Pozo Rodriguez Ana, Solinis Maria Angeles
a Dipartimento di Scienza e Tecnologia del Farmaco , Università degli Studi di Torino , Torino , Italy.
b Pharmacokinetic, Nanotechnology and Gene Therapy Group (PharmaNanoGene), Faculty of Pharmacy , Centro de investigación Lascaray ikergunea, University of the Basque Country UPV/EHU , Vitoria-Gasteiz , Spain.
Expert Opin Drug Deliv. 2016 Dec;13(12):1743-1757. doi: 10.1080/17425247.2016.1201059. Epub 2016 Jun 24.
Although eye drops are widely used as drug delivery systems for the anterior segment of the eye, they are also associated with poor drug bioavailability due to transient contact time and rapid washout by tearing. Moreover, effective drug delivery to the posterior segment of the eye is challenging, and alternative routes of administration (periocular and intravitreal) are generally needed, the blood-retinal barrier being the major obstacle to systemic drug delivery. Areas covered: Nanotechnology, and especially lipid nanoparticles, can improve the therapeutic efficiency, compliance and safety of ocular drugs, administered via different routes, to both the anterior and posterior segment of the eye. This review highlights the main ocular barriers to drug delivery, as well as the most common eye diseases suitable for pharmacological treatment in which lipid nanoparticles have proved efficacious as alternative delivery systems. Expert opinion: Lipid-based nanocarriers are among the most biocompatible and versatile means for ocular delivery. Mucoadhesion with consequent increase in pre-corneal retention time, and enhanced permeation due to cellular uptake by corneal epithelial cells, are the essential goals for topical lipid nanoparticle delivery. Gene delivery to the retina has shown very promising results after intravitreal administration of lipid nanoparticles as non-viral vectors.
尽管眼药水作为眼部前段的药物递送系统被广泛使用,但由于接触时间短暂以及泪液快速冲刷,它们的药物生物利用度也较低。此外,将药物有效递送至眼后段具有挑战性,通常需要采用其他给药途径(眼周和玻璃体内),血视网膜屏障是全身给药的主要障碍。涵盖领域:纳米技术,尤其是脂质纳米颗粒,可以提高通过不同途径给药至眼前段和眼后段的眼部药物的治疗效率、顺应性和安全性。本综述强调了药物递送的主要眼部屏障,以及适合药物治疗的最常见眼部疾病,其中脂质纳米颗粒已被证明作为替代递送系统有效。专家观点:基于脂质的纳米载体是眼部给药最具生物相容性和多功能性的手段之一。与角膜前滞留时间增加相关的粘膜粘附以及角膜上皮细胞的细胞摄取导致的渗透增强,是局部脂质纳米颗粒递送的基本目标。在玻璃体内注射脂质纳米颗粒作为非病毒载体后,向视网膜的基因递送已显示出非常有前景的结果。