School of Pharmacy, Nanjing Medical University, 140 Hanzhong Road, Nanjing 210029, People's Republic of China.
J Microencapsul. 2011;28(2):134-41. doi: 10.3109/02652048.2010.539304. Epub 2010 Dec 10.
Methazolamide (MTA) is an antiglaucoma drug; however, there are many side effects of its systemic administration with insufficient ocular therapeutic concentrations. The aim of this study was to formulate MTA-loaded solid lipid nanoparticles (SLNs) and evaluate the potential of SLNs as a new therapeutic system for glaucoma. SLNs were prepared by a modified emulsion-solvent evaporation method and their physicochemical characteristics were evaluated. The pharmacodynamics was investigated by determining the percentage decrease in intraocular pressure. The ocular irritation was studied by Draize test. Despite a burst release of SLNs, the pharmacodynamic experiment indicated that MTA-SLNs had higher therapeutic efficacy, later occurrence of maximum action, and more prolonged effect than drug solution and commercial product. Formulation of MTA-SLNs would be a potential delivery carrier for ocular delivery, with the advantages of a more intensive treatment for glaucoma, lower in doses and better patient compliance compared to the conventional eye drops.
甲醋唑胺（MTA）是一种抗青光眼药物；但是，全身给药会产生许多副作用，同时眼内治疗浓度不足。本研究旨在制备甲醋唑胺负载的固体脂质纳米粒（SLNs），并评估 SLNs 作为治疗青光眼的新治疗系统的潜力。SLNs 通过改良的乳化-溶剂蒸发法制备，并对其理化性质进行评价。通过测定眼压降低的百分比来研究药效动力学。通过 Draize 试验研究眼刺激性。尽管 SLNs 有突释现象，但药效学实验表明，MTA-SLNs 比药物溶液和商业产品具有更高的治疗效果，起效时间更晚，作用时间更长。MTA-SLNs 的制剂将成为眼部给药的一种有潜力的递送载体，与传统滴眼液相比，其治疗青光眼的强度更高，剂量更低，患者顺应性更好。
