Niwano Yoshimi, Iwasawa Atsuo, Ayaki Masahiko
Tohoku University Graduate School of Dentistry, Sendai, Japan.
Department of Bioengineering, Tokyo Institute of Technology, Yokohama, Japan.
Ophthalmol Eye Dis. 2014 Feb 13;6:5-12. doi: 10.4137/OED.S12445. eCollection 2014.
In vitro cytotoxicity of tafluprost, which is the most recently developed anti-glaucoma prostaglandin (PG) analog, in ocular surface cells is addressed in comparison with other PG analogs. Irrespective of cell lines and models, the cytotoxicity of anti-glaucoma PG eyedrops was primarily related to the concentration of benzalkonium chloride (BAK) contained in the eyedrops as a preservative. Accordingly, preservative-free tafluprost was apparently less cytotoxic than BAK-preserved PG analogs. Furthermore, our study for cytotoxicity assays on ocular cells, conducted by comprehensive investigations covering a variety of concentrations and treatment times, which is termed the cell viability score (CVS) system, demonstrated that 0.001% BAK-preserved tafluprost was not cytotoxic, and suggested that tafluprost may even reduce the cytotoxic effect of BAK. It has been reported that adverse reactions associated with tafluprost in healthy human volunteers and patients with glaucoma include conjunctival hyperemia, eyelid pigmentation, eyelash bristles, and deepening of upper eyelid sulcus. Nonetheless, most clinical studies have demonstrated that not only preservative-free tafluprost but also BAK-preserved tafluprost is well tolerated and safe in patients with glaucoma and ocular hypertension.
与其他前列腺素（PG）类似物相比，本文探讨了最新研发的抗青光眼PG类似物他氟前列素在眼表细胞中的体外细胞毒性。无论细胞系和模型如何，抗青光眼PG眼药水的细胞毒性主要与作为防腐剂包含在眼药水中的苯扎氯铵（BAK）浓度有关。因此，不含防腐剂的他氟前列素的细胞毒性明显低于含有BAK的PG类似物。此外，我们通过涵盖各种浓度和处理时间的全面研究（即细胞活力评分（CVS）系统）对眼细胞进行的细胞毒性测定研究表明，0.001%含BAK的他氟前列素没有细胞毒性，并表明他氟前列素甚至可能降低BAK的细胞毒性作用。据报道，健康人类志愿者和青光眼患者中与他氟前列素相关的不良反应包括结膜充血、眼睑色素沉着、睫毛变粗和上睑沟加深。尽管如此，大多数临床研究表明，不仅不含防腐剂的他氟前列素，而且含BAK的他氟前列素在青光眼和高眼压患者中都具有良好的耐受性且安全。
