Abstract
This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.
Highlights
Carvedilol is a beta-adrenergic blocking agent, indicated for the treatment of hypertension, angina pectoris, and heart failure [1]
In our study dimethyldidodecylammonium bromide (DDAB) leciplex formulations revealed smaller particle size than cetyltrimethylammonium bromide (CTAB) leciplex formulations (p < 0.05), these results might be attributed to stabilizing property of DDAB which was demonstrated by the high surface charge obtained by DDAB leciplex compared to CTAB leciplex
These results are in agreement with Varghese et al who found that particle size of lecithmer formulations was dependent upon stabilizing properties of cationic agent (DDAB/DOTAP)
Summary
Carvedilol is a beta-adrenergic blocking agent, indicated for the treatment of hypertension, angina pectoris, and heart failure [1]. Recent study suggests carvedilol as possible therapy for the increased intraocular pressure [2]. The intraocular pressure is controlled by the flow of aqueous humor in the eye where the excess fluid is drains through the trabecular meshwork. If the outflow is blocked, aqueous humor accumulates inside the eye leading to increased intraocular pressure (IOP). The increased IOP can damage the optic nerve, resulting in an optic neuropathy and irreversibly impaired vision [3]. Topical eye drop is usually selected for the treatment of eye diseases as it is the most desirable dosage form. Traditional eye drop usually suffers from low bioavailability due to the limited eye capacity, blinking reflex, lachrymal fluid erosion and nasolacrimal drainage. Corneal and conjunctival epithelia of human eye, along with the tear film, construct a compact barrier preventing the drug absorption into the intraocular area which shorten the retention time in the eyes and produce less absorption in the intraocular area [4], frequent instillation of eye drops is often required to achieve expected therapeutic efficacy but patients’ long term adherence to installation schedules is a major issue [5]
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