Ako-Adounvo Ann-Marie, Nagarwal Ramesh C, Oliveira Lais, Boddu Sai H S, Wang Xiang S, Dey Surajit, Karla Pradeep K
Howard University, Department of Pharmaceutical Sciences, College of Pharmacy, Rm 309, 2300 4th Street NW, Washington D.C. 20059, USA.
Recent Pat Drug Deliv Formul. 2014;8(3):193-201. doi: 10.2174/1872211308666140926112000.
Nanoformulations (NF) are widely explored as potential alternatives for traditional ophthalmic formulation approaches. The effective treatment of ocular diseases using conventional eye drops is often hampered by factors such as: physiological barriers, rapid elimination, protein binding, and enzymatic drug degradation. Combined, these factors are known to contribute to reduced ocular residence time and poor bioavailability. Recent research studies demonstrated that NF can significantly enhance the therapeutic efficacy and bioavailability of ocular drugs, compared to the established ophthalmic drug delivery strategies. The research studies resulted in a number of patent inventions, reporting a significant increase in therapeutic efficacy for various chronic ocular disease states of both the anterior and posterior ocular segments. This article reviews these patent disclosures in detail and emphasizes the therapeutic advantages conferred by the following nanoformulation approaches: Calcium Phosphate (CaP) nanoparticles, Liposomes, Nanoemulsions, Nanomicelles, and Hydrogels. The nanoformulation approaches were shown to enhance the ocular bioavailability by reducing the drugprotein binding, increasing the corneal resident time, enhancing the drug permeability and providing a sustained drug release. Further, the article discusses United States Food and Drug Administration (USFDA) approved ocular drugs employing nanotechnology and future developments. It should be noted that, despite the potential therapeutic promise demonstrated by nanotechnology for ocular drug delivery, the bench to bed transition from patent inventions to marketed drug products has been insignificant. Majority of the discussed technologies are still in development and testing phase for commercial viability. Further, studies are in progress to assess ocular tolerance and nanotoxicity for prolonged use of NF.
纳米制剂(NF)作为传统眼科制剂方法的潜在替代方案受到广泛探索。使用传统眼药水有效治疗眼部疾病常常受到诸如生理屏障、快速消除、蛋白质结合和酶促药物降解等因素的阻碍。综合起来,这些因素会导致眼部停留时间缩短和生物利用度不佳。最近的研究表明,与既定的眼科药物递送策略相比,NF可以显著提高眼部药物的治疗效果和生物利用度。这些研究产生了许多专利发明,报告了对眼前段和眼后段各种慢性眼部疾病状态的治疗效果有显著提高。本文详细回顾了这些专利披露内容,并强调了以下纳米制剂方法所赋予的治疗优势:磷酸钙(CaP)纳米颗粒、脂质体、纳米乳剂、纳米胶束和水凝胶。纳米制剂方法显示出通过减少药物与蛋白质的结合、增加角膜停留时间、提高药物渗透性和提供持续药物释放来提高眼部生物利用度。此外,本文还讨论了美国食品药品监督管理局(USFDA)批准的采用纳米技术的眼部药物以及未来的发展。应该注意的是,尽管纳米技术在眼部药物递送方面显示出潜在的治疗前景,但从专利发明到上市药品的从实验室到临床的转变并不显著。所讨论的大多数技术仍处于商业可行性的开发和测试阶段。此外,正在进行研究以评估长期使用NF的眼部耐受性和纳米毒性。