Akhter Md Habban, Ahmad Irfan, Alshahrani Mohammad Y, Al-Harbi Alhanouf I, Khalilullah Habibullah, Afzal Obaid, Altamimi Abdulmalik S A, Najib Ullah Shehla Nasar Mir, Ojha Abhijeet, Karim Shahid
School of Pharmaceutical and Population Health Informatics (SoPPHI), DIT University, Dehradun 248009, India.
Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Khalid University, Abha 62521, Saudi Arabia.
Gels. 2022 Jan 28;8(2):82. doi: 10.3390/gels8020082.
Drug instillation via a topical route is preferred since it is desirable and convenient due to the noninvasive and easy drug access to different segments of the eye for the treatment of ocular ailments. The low dose, rapid onset of action, low or no toxicity to the local tissues, and constrained systemic outreach are more prevalent in this route. The majority of ophthalmic preparations in the market are available as conventional eye drops, which rendered <5% of a drug instilled in the eye. The poor drug availability in ocular tissue may be attributed to the physiological barriers associated with the cornea, conjunctiva, lachrymal drainage, tear turnover, blood-retinal barrier, enzymatic drug degradation, and reflex action, thus impeding deeper drug penetration in the ocular cavity, including the posterior segment. The static barriers in the eye are composed of the sclera, cornea, retina, and blood-retinal barrier, whereas the dynamic barriers, referred to as the conjunctival and choroidal blood flow, tear dilution, and lymphatic clearance, critically impact the bioavailability of drugs. To circumvent such barriers, the rational design of the ocular therapeutic system indeed required enriching the drug holding time and the deeper permeation of the drug, which overall improve the bioavailability of the drug in the ocular tissue. This review provides a brief insight into the structural components of the eye as well as the therapeutic challenges and current developments in the arena of the ocular therapeutic system, based on novel drug delivery systems such as nanomicelles, nanoparticles (NPs), nanosuspensions, liposomes, in situ gel, dendrimers, contact lenses, implants, and microneedles. These nanotechnology platforms generously evolved to overwhelm the troubles associated with the physiological barriers in the ocular route. The controlled-drug-formulation-based strategic approach has considerable potential to enrich drug concentration in a specific area of the eye.
通过局部途径进行药物滴注是首选方法,因为它具有非侵入性且药物易于进入眼睛的不同部位,便于治疗眼部疾病,既理想又方便。这种途径具有低剂量、起效快、对局部组织毒性低或无毒性以及全身作用有限等特点。市场上大多数眼科制剂都是传统眼药水形式,滴入眼内的药物只有不到5%能发挥作用。眼部组织中药物利用率低可能归因于与角膜、结膜、泪液引流、泪液更新、血视网膜屏障、药物酶促降解和反射作用相关的生理屏障,从而阻碍药物在眼腔包括后段的更深层渗透。眼中的静态屏障由巩膜、角膜、视网膜和血视网膜屏障组成,而动态屏障,即结膜和脉络膜血流、泪液稀释和淋巴清除,对药物的生物利用度有至关重要的影响。为了克服这些屏障,眼部治疗系统的合理设计确实需要延长药物保留时间并使药物更深层渗透,从而总体上提高药物在眼部组织中的生物利用度。本综述基于纳米胶束、纳米颗粒、纳米混悬液、脂质体、原位凝胶、树枝状大分子、隐形眼镜、植入物和微针等新型药物递送系统,简要介绍了眼睛的结构组成以及眼部治疗系统领域的治疗挑战和当前进展。这些纳米技术平台不断发展,以克服眼部给药途径中与生理屏障相关的问题。基于控释药物制剂的策略方法在提高眼部特定区域药物浓度方面具有相当大的潜力。