Jacob Shery, Nair Anroop B, Shah Jigar, Gupta Sumeet, Boddu Sai H S, Sreeharsha Nagaraja, Joseph Alex, Shinu Pottathil, Morsy Mohamed A
Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman 4184, United Arab Emirates.
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Pharmaceutics. 2022 Feb 27;14(3):533. doi: 10.3390/pharmaceutics14030533.
Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via invasive/non-invasive or minimally invasive drug administration methods. Biocompatible and biodegradable lipid nanoparticles have emerged as a potential alternative to conventional ocular drug delivery systems to overcome various ocular barriers. Lipid-based nanocarrier systems led to major technological advancements and therapeutic advantages during the last few decades of ocular therapy, such as high precorneal residence time, sustained drug release profile, minimum dosing frequency, decreased drug toxicity, targeted site delivery, and, therefore, an improvement in ocular bioavailability. In addition, such formulations can be given as fine dispersion in patient-friendly droppable preparation without causing blurred vision and ocular sensitivity reactions. The unique advantages of lipid nanoparticles, namely, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and liposomes in intraocular targeted administration of various therapeutic drugs are extensively discussed. Ongoing and completed clinical trials of various liposome-based formulations and various characterization techniques designed for nanoemulsion in ocular delivery are tabulated. This review also describes diverse solid lipid nanoparticle preparation methods, procedures, advantages, and limitations. Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems.
由于眼部组织复杂的解剖学和物理特性，将药物靶向递送至眼部组织仍然是制剂科学家面临的关键挑战。目前正在进行各种尝试，通过将治疗性分子封装在各种纳米载体系统或装置中，并通过侵入性/非侵入性或微创给药方法进行给药，以提高其体内性能。生物相容性和可生物降解的脂质纳米颗粒已成为克服各种眼部屏障的传统眼部给药系统的潜在替代品。在过去几十年的眼部治疗中，基于脂质的纳米载体系统带来了重大的技术进步和治疗优势，例如角膜前停留时间长、药物持续释放曲线、给药频率低、药物毒性降低、靶向部位递送，从而提高了眼部生物利用度。此外，此类制剂可以以细分散液的形式制成患者友好的可滴眼制剂，而不会引起视力模糊和眼部敏感反应。本文广泛讨论了脂质纳米颗粒，即固体脂质纳米颗粒、纳米结构脂质载体、纳米乳剂和脂质体在各种治疗药物眼内靶向给药中的独特优势。列出了各种基于脂质体的制剂正在进行和已完成的临床试验，以及为眼内给药设计的纳米乳剂的各种表征技术。本综述还描述了多种固体脂质纳米颗粒的制备方法、步骤、优点和局限性。克服脂质纳米颗粒缺点的功能化方法，以及探索具有提高大分子药物渗透性潜力的新型功能添加剂，将迅速推动眼部给药系统这一具有挑战性的领域的发展。
