Hashikawa Yoshiko, Kato Yuki, Kaji Hirokazu, Abe Toshiaki, Nagai Nobuhiro
Division of Clinical Cell Therapy, United Centers for Advanced Research and Translational Medicine (ART), Tohoku University Graduate School of Medicine, 2-1 Seiryo-machi, Aoba-ku, Sendai 980-8575, Japan.
Department of Biomechanics, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kanda-Surugadai, Chiyoda, Tokyo 101-0062, Japan.
Heliyon. 2023 Mar 9;9(3):e14392. doi: 10.1016/j.heliyon.2023.e14392. eCollection 2023 Mar.
The objectives of this study were to develop a sustained-release device for carteolol hydrochloride (CH) and investigate any potential difference in the intraocular distribution of this agent between the transscleral administration of the device and treatment with eyedrops. The device was formulated with photocurable resin, poly (ethyleneglycol) dimethacrylate, to fit within the curve of the rabbit eyeball. study showed that CH was released in a sustained-release manner for 2 weeks. The concentration of CH in the retina, choroid/retinal pigment epithelium, sclera, iris, and aqueous humor was determined by high-performance liquid chromatography. Transscleral administration was able to deliver CH to the posterior segment (i.e., retina and choroid/retinal pigment epithelium) rather than the anterior segment (i.e., aqueous humor), while eyedrops delivered CH only to the anterior segment. Transscleral administration could deliver CH to aqueous humor at half the concentration versus treatment with eyedrops and reduced intraocular pressure (IOP) at 1 day after implantation; however, the IOP-lowering effect was not sustained thereafter. In conclusion, transscleral drug delivery may be a useful method for the reduction of IOP. Notably, the aqueous concentration must be equal to that delivered by the eyedrops, and this approach might be preferable for drug delivery to the posterior segment of the eye.
本研究的目的是开发一种盐酸卡替洛尔(CH)缓释装置,并研究该装置经巩膜给药与滴眼液治疗在眼内药物分布上的潜在差异。该装置由光固化树脂聚(乙二醇)二甲基丙烯酸酯制成,以适配兔眼球的曲线。研究表明,CH以缓释方式释放达2周。通过高效液相色谱法测定视网膜、脉络膜/视网膜色素上皮、巩膜、虹膜和房水中CH的浓度。经巩膜给药能够将CH递送至眼后段(即视网膜和脉络膜/视网膜色素上皮)而非眼前段(即房水),而滴眼液仅将CH递送至眼前段。经巩膜给药在植入后1天可将CH以滴眼液一半的浓度递送至房水并降低眼压(IOP);然而,此后眼压降低效果未持续。总之,经巩膜给药可能是降低眼压的一种有用方法。值得注意的是,房水浓度必须与滴眼液给药时相同,并且这种方法可能更适合于向眼后段给药。