Abstract：
Atropine sulfate (ATS) eye drops at low concentrations constitute a limited selection for myopia treatment, with challenges such as low ophthalmic bioavailability and inadequate stability. This study proposes a novel strategy by synthesizing ophthalmic sodium polystyrene sulfonate resin (SPSR) characterized by a spherical shape and uniform size for cationic exchange with ATS. The formulation of ATS@SPSR suspension eye drops incorporates xanthan gum and hydroxypropyl methylcellulose (HPMC) as suspending agents. In vitro studies demonstrated that ATS@SPSR suspension eye drops exhibited sustained release characteristics, and tropic acid, its degradation product, remained undetected for 30 days at 40 °C. The ATS levels in the tear fluids and aqueous humor of New Zealand rabbits indicated a significant increase in mean residence time (MRT) and area under the drug concentration-time curve (AUC0-12h) for ATS@SPSR suspension eye drops compared to conventional ATS eye drops. Moreover, safety assessment confirmed the non-irritating nature of ATS@SPSR suspension eye drops in rabbit eyes. In conclusion, the cation-responsive sustained-release ATS@SPSR suspension eye drops enhanced the bioavailability and stability of ATS, offering a promising avenue for myopia treatment.
摘要：
低浓度的硫酸阿托品（ATS）滴眼液对近视治疗的选择有限，具有诸如低的眼科生物利用度和不足的稳定性等挑战。这项研究提出了一种新颖的策略，通过合成眼用聚苯乙烯磺酸钠树脂（SPSR），其特征在于球形和均匀的尺寸与ATS进行阳离子交换。ATS@SPSR混悬滴眼剂的配方中含有黄原胶和羟丙基甲基纤维素(HPMC)作为悬浮剂。体外研究表明，ATS@SPSR混悬滴眼液具有缓释特性，和托品酸，它的降解产物，在40℃下30天内未发现。新西兰兔泪液和房水中的ATS水平表明，与常规ATS滴眼液相比，ATS@SPSR混悬液滴眼液的平均停留时间（MRT）和药物浓度-时间曲线下面积（AUC0-12h）显着增加滴眼液。此外，安全性评估证实了ATS@SPSR混悬液滴眼液对兔眼的无刺激性。总之,阳离子响应型缓释ATS@SPSR混悬滴眼液提高了ATS的生物利用度和稳定性,为近视治疗提供了一条有希望的途径。
