| RRC ID |
51778
|
| 著者 |
Hakkarainen JJ, Reinisalo M, Ragauskas S, Seppänen A, Kaja S, Kalesnykas G.
|
| タイトル |
Acute cytotoxic effects of marketed ophthalmic formulations on human corneal epithelial cells.
|
| ジャーナル |
Int J Pharm
|
| Abstract |
The purpose of the study was to devise a fast, reliable and sensitive cell viability assay for assessment of acute cytotoxicity on human corneal epithelial cells by using a clinically relevant exposure time. Acute cytotoxic effects of the pharmaceutical excipients benzalkonium chloride (BAC), macrogolglycerol hydroxystearate (MGHS40), polysorbate 80 (PS80) and marketed ophthalmic formulations (Lumigan(®), Monoprost(®), Taflotan(®), Travatan(®), Xalatan(®)) containing these excipients were tested. Human corneal epithelial cell (HCE-T) viability was assessed by measuring the reduction of resazurin to highly fluorescent resorufin. Expression of the tight junction proteins in HCE-T cells were characterized by immunofluorescence staining. Presence of tight junction proteins in HCE-T cells was demonstrated. BAC preserved ophthalmic formulations showed concentration-dependent and time-dependent cytotoxicity to human corneal epithelium. In contrast, no acute cytotoxicity of non-ionic stabilizing/solubilizing excipients (MGSH40 and PS80) or ophthalmic formulation containing these excipients was observed. Marketed ophthalmic formulations used for glaucoma medication show differential toxicity on human corneal epithelial cells. The present study revealed that BAC-preserved ophthalmic formulations were able to induce acute cytotoxic effects even during a clinically relevant exposure time, which was not observed with MGSH40 and PS80 excipients or ophthalmic formulations containing these excipients.
|
| 巻・号 |
511(1)
|
| ページ |
73-78
|
| 公開日 |
2016-9-10
|
| DOI |
10.1016/j.ijpharm.2016.06.135
|
| PII |
S0378-5173(16)30625-1
|
| PMID |
27374205
|
| MeSH |
Animals
Cell Line
Cell Survival / drug effects
Cell Survival / physiology
Cornea / drug effects
Cornea / metabolism
Cytotoxins / administration & dosage
Cytotoxins / toxicity*
Dose-Response Relationship, Drug
Drug Compounding* / methods
Epithelium, Corneal / drug effects*
Epithelium, Corneal / metabolism
Excipients / toxicity
Humans
Male
Ophthalmic Solutions / administration & dosage
Ophthalmic Solutions / toxicity*
Preservatives, Pharmaceutical / administration & dosage
Preservatives, Pharmaceutical / toxicity
Rats
Rats, Wistar
|
| IF |
4.845
|
| 引用数 |
9
|
| リソース情報 |
| ヒト・動物細胞 |
HCE-T(RCB2280) |
