Nagai Noriaki, Ono Hikaru, Hashino Miho, Ito Yoshimasa, Okamoto Norio, Shimomura Yoshikazu
Faculty of Pharmacy, Kinki University.
J Oleo Sci. 2014;63(2):177-86. doi: 10.5650/jos.ess13082. Epub 2014 Jan 14.
We prepared ophthalmic formulations containing 0.5% tranilast (TL) nanoparticles using 0.005% benzalkonium chloride (BAC), 0.5% D-mannitol, and 2-hydroxypropyl-β-cyclodextrin (HPβCD), and investigated their usefulness in the ophthalmologic field by evaluating corneal toxicity and permeability. TL nanoparticles were prepared using zirconia beads and Bead Smash 12, which allowed the preparation of high quality dispersions containing 0.5% TL nanoparticles (particle size, 34 ± 20 nm, means ± S.D.). Dispersions containing TL nanoparticles are tolerated better by human corneal epithelium cells than a commercially available 0.5% TL preparation (RIZABEN(®) eye drops). In addition, the addition of TL nanoparticles to the dispersions does not affect the antimicrobial activity of BAC against Escherichia coli (ATCC 8739), and the corneal penetration of TL from dispersions containing TL nanoparticles was significantly higher than in the case of the commercially available 0.5% TL eye drops. It is possible that dispersions containing TL nanoparticles will show increased effectiveness against ocular inflammation, and that ocular drug delivery systems using drug nanoparticles may lead to an expansion of their usefulness for therapy in the ophthalmologic field.
我们使用0.005%苯扎氯铵（BAC）、0.5% D-甘露醇和2-羟丙基-β-环糊精（HPβCD）制备了含0.5%曲尼司特（TL）纳米颗粒的眼科制剂，并通过评估角膜毒性和渗透性来研究它们在眼科领域的效用。使用氧化锆珠和Bead Smash 12制备TL纳米颗粒，从而能够制备出含0.5% TL纳米颗粒（粒径34±20 nm，平均值±标准差）的高质量分散体。含TL纳米颗粒的分散体比市售0.5% TL制剂（丽泽本（®）滴眼液）更易被人角膜上皮细胞耐受。此外，向分散体中添加TL纳米颗粒不会影响BAC对大肠杆菌（ATCC 8739）的抗菌活性，并且含TL纳米颗粒的分散体中TL的角膜渗透率显著高于市售0.5% TL滴眼液。含TL纳米颗粒的分散体可能对眼部炎症显示出更高的疗效，并且使用药物纳米颗粒的眼部给药系统可能会扩大其在眼科治疗领域的效用。
