Wróblewska Katarzyna Barbara, Milanowski Bartłomiej, Kucińska Małgorzata, Plewa Szymon, Długaszewska Jolanta, Muszalska-Kolos Izabela
Department of Pharmaceutical Technology, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland.
GENERICA Pharmaceutical Lab, Regionalne Centrum Zdrowia Sp. z o.o., Na Kępie 3, 64-360 Zbąszyń, Poland.
Pharmaceuticals (Basel). 2021 Aug 26;14(9):849. doi: 10.3390/ph14090849.
This work investigated the potential of a novel formulation of eye drops containing a non-steroidal anti-inflammatory drug-choline salicylate (CS)-and hyaluronic acid (HA). Thus, these drops may exert both anti-inflammatory and regenerative activity. The experiment was conducted through the careful characterization of physicochemical properties, stability, and quality of eye drops. Moreover, microbiological analysis, as well as penetration and cytotoxic studies, were performed. The UV, HPLC-UV, and HPLC-MS/MS methods were used to determine the purity and stability of CS. The penetration rate of CS was assessed using a hydrophilic membrane and ex vivo porcine cornea model. Additionally, the cytotoxic effects were evaluated using the SIRC cell line. The interaction between HA and CS was tested using size-exclusion chromatography and IR spectrophotometry. As a result, HA increased the viscosity of the drops, which prolonged their contact with the ocular surface, thus ensuring more effective penetration of CS into the corneal structure. After long-term storage, an interaction in the pharmaceutical phase between CS and HA was observed. However, this interaction did not affect the viability of rabbit corneal cells. Our findings showed that eye drops with CS and HA, stored at 2-8 °C in light-protected conditions, met the criteria of stability and safety.
本研究探讨了一种含有非甾体抗炎药水杨酸胆碱(CS)和透明质酸(HA)的新型眼药水配方的潜力。因此,这些眼药水可能具有抗炎和再生活性。通过对眼药水的物理化学性质、稳定性和质量进行仔细表征来开展实验。此外,还进行了微生物分析以及渗透和细胞毒性研究。采用紫外、高效液相色谱-紫外和高效液相色谱-串联质谱法测定CS的纯度和稳定性。使用亲水膜和离体猪角膜模型评估CS的渗透率。此外,使用SIRC细胞系评估细胞毒性作用。使用尺寸排阻色谱法和红外分光光度法测试HA与CS之间的相互作用。结果,HA增加了眼药水的粘度,延长了它们与眼表的接触时间,从而确保CS更有效地渗透到角膜结构中。长期储存后,观察到CS与HA在药物相中发生相互作用。然而,这种相互作用并不影响兔角膜细胞的活力。我们的研究结果表明,含有CS和HA的眼药水在2-8°C避光条件下储存符合稳定性和安全性标准。