RRC ID |
65997
|
著者 |
Račić A, Čalija B, Milić J, Jurišić Dukovski B, Lovrić J, Dobričić V, Micov A, Vuković M, Stepanović-Petrović R, Krajišnik D.
|
タイトル |
Formulation of olopatadine hydrochloride viscous eye drops - physicochemical, biopharmaceutical and efficacy assessment using in vitro and in vivo approaches.
|
ジャーナル |
Eur J Pharm Sci
|
Abstract |
The aim of this work was the formulation and the comprehensive evaluation of the viscous eye drops using vehicles containing medium chain chitosan (0.5% w/v), hydroxypropyl guar gum (0.25% w/v) and their combination as carriers for olopatadine (0.1% w/v). Physicochemical properties (appearance, clarity, pH, osmolality, viscosity and drug content) of the tested formulations were within acceptable ranges for the ophthalmic preparations, while DSC and FT-IR techniques demonstrated the compatibility between olopatadine and polymers. The drug permeability was successfully estimated in vitro using both HCE-T cell-based models (Model I and Model II) and the parallel artificial membrane permeability assay (PAMPA), considering the impact of chitosan as a permeation enhancer. The MTT cytotoxicity assay demonstrates that the tested formulations (diluted 10-fold in HBSS pH 5.5) were non-toxic and well tolerated. An ocular itch test on mice was carried out with the formulation containing the combination of polymers comparable with a commercially available olopatadine eye drops without viscosity enhancers. The tested eye drops produced a slightly higher anti-pruritic/analgesic-like effect than the commercial preparation. It could be assumed that the use of this viscous ophthalmic vehicle due to its advanced mucoadhesive properties and good safety profile is a feasible strategy to improve the efficacy of olopatadine.
|
巻・号 |
166
|
ページ |
105906
|
公開日 |
2021-11-1
|
DOI |
10.1016/j.ejps.2021.105906
|
PII |
S0928-0987(21)00207-4
|
PMID |
34118409
|
MeSH |
Animals
Biological Products*
Mice
Olopatadine Hydrochloride
Ophthalmic Solutions
Spectroscopy, Fourier Transform Infrared
Viscosity
|
IF |
3.616
|
リソース情報 |
ヒト・動物細胞 |
HCE-T(RCB2280) |