• 主页
  • 查找结果
  • A nanoparticle formulation reduces the corneal toxicity of indomethacin eye drops and enhances its corneal permeability.

A nanoparticle formulation reduces the corneal toxicity of indomethacin eye drops and enhances its corneal permeability.

Toxicology (2014-03-07)
Noriaki Nagai, Yoshimasa Ito, Norio Okamoto, Yoshikazu Shimomura
摘要

Indomethacin (IMC) has been shown to reduce post-operative inflammation and to decrease intraocular irritation after cataract extraction and in cystoid macular edema; however, the clinical use of its most commonly used eye drops is limited due to topical side-effects that include burning sensation, irritation and epithelial keratitis. It is known that decreasing direct cell stimulation and reducing the amount applied via increasing bioavailability are useful for improving these issues. In this study, we designed ophthalmic formulations containing 0.5% IMC nanoparticles using zirconia beads and Bead Smash 12 (IMCnano eye drops; particle size 76 ± 59 nm, mean ± S.D.), and investigated the corneal toxicity of these IMCnano eye drops. IMCnano eye drops are tolerated better by a human cornea epithelial cell line (HCE-T) than commercially available NDSAIDs preparations (IMC, pranoprofen, diclofenac, bromfenac and nepafenac eye drops), and corneal wound healing in rat eyes with debrided corneal epithelium instilled with IMCnano eye drops is significantly better than that of eyes instilled with commercially available IMC eye drops. In addition, the accumulation of IMC in HCE-T cells treated with the IMCnano eye drops for 30 min was 19.9% that of the accumulation from commercially available IMC eye drops. On the other hand, the corneal penetration of IMC from IMCnano eye drops was significantly greater than in the case of the commercially available IMC eye drops in both in vivo and in vitro studies using rabbit corneas. Taken together, we hypothesize that a nanoparticle formulation reduces the corneal toxicity of IMC eye drops, probably because the accumulation of IMC from IMCnano eye drops in the eye is lower than that from commercially available IMC eye drops. In addition, the nanoparticle formulation may allow a decrease in the amount of IMC used due to the increase in bioavailability, resulting in reduced drug toxicity. These findings provide significant information that can be used to design further studies aimed at developing less toxic eye drops.

材料
货号
品牌
产品描述

Sigma-Aldrich
D -甘露醇, ≥98%
Sigma-Aldrich
甲基纤维素, viscosity: 4,000 cP
Sigma-Aldrich
吲哚美辛, 98.5-100.5% (in accordance with EP)
Supelco
甘露醇, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
甲基纤维素, viscosity: 15 cP, BioReagent, suitable for cell culture
Sigma-Aldrich
甲基纤维素, viscosity: 400 cP
Sigma-Aldrich
氧化锆 (IV), powder, 5 μm, 99% trace metals basis
Sigma-Aldrich
D -甘露醇, ACS reagent
Sigma-Aldrich
D -甘露醇, meets EP, FCC, USP testing specifications
Sigma-Aldrich
D -甘露醇, BioXtra, ≥98% (HPLC)
Sigma-Aldrich
Methocel® A4M, viscosity 3000-5500 mPa.s, 2 % in H2O(20 °C)
Sigma-Aldrich
D -甘露醇, suitable for plant cell culture
Sigma-Aldrich
甲基纤维素, viscosity: 15 cP
Sigma-Aldrich
甲基纤维素, viscosity: 1,500 cP
Sigma-Aldrich
Methocel® A15 LV, 27.5-31.5% methoxyl basis
Sigma-Aldrich
氧化锆 (IV), nanopowder, <100 nm particle size (TEM)
Sigma-Aldrich
锆, powder, −100 mesh
Sigma-Aldrich
甲基纤维素, viscosity: 25 cP
USP
甘露醇, United States Pharmacopeia (USP) Reference Standard
甘露醇, European Pharmacopoeia (EP) Reference Standard
Millipore
D -甘露醇, ACS reagent, suitable for microbiology, ≥99.0%
Supelco
吲哚美辛, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
D -甘露醇, BioUltra, ≥99.0% (sum of enantiomers, HPLC)
Sigma-Aldrich
甲基纤维素, meets USP testing specifications, viscosity: 400 cP
Sigma-Aldrich
吲哚美辛, meets USP testing specifications
Sigma-Aldrich
Methocel® A15C, medium viscosity, Methoxyl content 27.5-31.5 %
Sigma-Aldrich
锆, foil, thickness 0.1 mm, 99.98% trace metals basis
Sigma-Aldrich
氧化锆 (IV), 99.99% trace metals basis (purity excludes ~2% HfO2)
Sigma-Aldrich
D -甘露醇, tested according to Ph. Eur.
Supelco
D -甘露醇, ≥99.9999% (metals basis), for boron determination

社交媒体

LinkedIn icon
Twitter icon
Facebook Icon
Instagram Icon

Merck

科研、开发、生产。

作为生命科学行业的全球领先供应商,我们致力于为科研、生物技术开发和生产,以及制药药物疗法开发和生产提供各类解决方案和服务。

© 2021年版权归德国达姆施塔特默克集团(Merck KGaA)及/或其附属公司所有。版权所有。

未经许可,严禁复制本网站上的任何资料。