Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
J Pharm Sci. 2019 Jun;108(6):1923-1933. doi: 10.1016/j.xphs.2019.01.016. Epub 2019 Jan 23.
With the significant advances made in nanotechnology, research efforts focused on developing novel drug delivery platforms that can overcome the multitude of challenges encountered in ophthalmic drug delivery. Surface active agents (SAAs) have been extensively used for the formulation of many of the dosage forms targeting ocular tissues. Novel ophthalmic carriers utilizing SAAs were broadly classified into particulate, vesicular, and controlled release drug delivery systems. Depending on their physicochemical properties, SAAs can perform a variety of roles ranging from wetting agents, emulsifiers, stabilizers, charge inducers, solubilizers, antimicrobial agents, corneal permeation enhancers, and gelling agents. Nevertheless, their use is limited by their potential toxicity and possible interactions with other formulation ingredients. This review provides a comprehensive analysis of the different functional roles of SAAs in novel ophthalmic drug delivery platforms, their mechanism of action, and limitations that need to be considered during formulation to maximize their potential benefit. Understanding the mechanisms by which they perform their different roles and the possible interactions between SAAs and other formulation ingredients can help orientate the choice of formulators toward the SAA most suitable for the intended ocular application at a concentration that is both safe and effective.
随着纳米技术的重大进展，研究工作集中在开发新的药物传递平台，以克服眼科药物传递中遇到的多种挑战。表面活性剂 (SAAs) 已广泛用于许多针对眼部组织的剂型的配方。利用 SAAs 的新型眼科载体广泛分为颗粒状、囊泡状和控制释放药物传递系统。根据它们的物理化学性质，SAAs 可以发挥多种作用，包括润湿剂、乳化剂、稳定剂、电荷诱导剂、增溶剂、抗菌剂、角膜渗透增强剂和胶凝剂。然而，它们的使用受到潜在毒性和与其他制剂成分可能相互作用的限制。本综述全面分析了 SAAs 在新型眼科药物传递平台中的不同功能作用、作用机制以及在配方中需要考虑的局限性，以最大限度地发挥它们的潜在益处。了解它们发挥不同作用的机制以及 SAAs 与其他制剂成分之间的可能相互作用，可以帮助制剂师根据预期的眼部应用选择最适合的 SAA，浓度既安全又有效。
