Preparation and evaluation of extended release ocular inserts of rebamipide for local effect using casting technique

الملخص EN

The aim of this study is to prepare and evaluate an extended release rebamipide ocular insert using hydroxypropyl methylcellulose as the main components of this drug delivery system for dry eye syndrome management, to have the advantage of both rebamipide inducing mucin secretion and hydroxypropyl methylcellulose lubricating properties.

Solvent casting technique was used to prepare the inserts; the amino acid L-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (HPMC E5 and K15M) and poly ethylene glycol 200 were used as excipients.

The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release.

The use of L-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by approximately 274 and 2.8 folds, respectively.

The formulae showed uniform weight, thickness and drug content except for formula (F1) that composed mostly of HPMC E5: HPMC K15M at ratio of 1: 0.17 and had no plasticizer (poly ethylene glycol 200) in its composition; it showed haziness in its appearance and brittleness of the insert.

While formula (F3) which contained mainly HPMC E5: HPMC K15M at ratio of 1: 0.4 with poly ethylene glycol 200 showed good physical and mechanical properties thus was selected for in vitro release and was compared to the marketed brand Mucosta® ophthalmic suspension unit dose 2%w/v; F3 showed significant larger T50% and T80% (p-values 0.034 and 0.015) compared to those of the reference marketed brand and similarity factor value was (f2 = 37.27).

The results of this study showed that rebamipide ocular inserts have good potential for futuristic rebamipide extended release ocular delivery system