首页|Formulation of olopatadine hydrochloride viscous eye drops - physicochemical, biopharmaceutical and efficacy assessment using in vitro and in vivo approaches

Formulation of olopatadine hydrochloride viscous eye drops - physicochemical, biopharmaceutical and efficacy assessment using in vitro and in vivo approaches

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  • NSTL
  • Elsevier
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.

Olopatadine hydrochlorideViscous eye dropsHCE-T cell-based modelsPAMPAMTT cytotoxicity assayOcular itch test

Micov, Ana、Racic, Andjelka、Calija, Bojan、Milic, Jela、Dukovski, Bisera Jurisic、Lovric, Jasmina、Dobricic, Vladimir、Vukovic, Milja、Stepanovic-Petrovic, Radica、Krajisnik, Danina

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Univ Belgrade, Dept Pharmacol, Fac Pharm, Vojvode Stepe 450, Belgrade 11221, Serbia

Univ Banja Luka, Fac Med, Dept Pharm, Save Mrkalja 14, Banja Luka 78000, Bosnia & Herceg

Univ Belgrade, Dept Pharmaceut Technol & Cosmetol, Fac Pharm, Vojvode Stepe 450, Belgrade 11221

Univ Zagreb, Fac Pharm & Biochem, Dept Pharmaceut Technol, Ante Kovacica 1, Zagreb 10000, Croatia

Univ Belgrade, Dept Pharmaceut Chem, Fac Pharm, Vojvode Stepe 450, Belgrade 11221, Serbia

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2021

10.1016/j.ejps.2021.105906

European journal of pharmaceutical sciences

European journal of pharmaceutical sciences

ISTP
ISSN：0928-0987
年,卷(期)：2021.166
  • 4
  • 64