Fabrication of betaxolol hydrochloride-loaded highly permeable ocular bilosomes (HPOBs) to combat glaucoma: In vitro, ex vivo & in vivo characterizations

Betaxolol hydrochloride is a water-soluble antiglaucoma drug suffering from poor ocular bioavailability necessitating frequent dosing that impede patient adherence to treatment. This is the first research to encapsulate BH into highly permeable ocular bilosomes (HPOBs). The goal of this study was to design BH-loaded HPOBs for enhancing BH corneal permeability and prolonging their intraocular pressure (IOP) lowering efficacy. BH-loaded HPOBs were prepared utilizing a modified ethanol injection method using 23 full factorial design using Design-Expert® 11 that adopted to investigate the formulation variables and suggest the optimum formula. Soybean phosphatidylcholine (SPC) and cholesterol (CH) constituted the lipid content, Span60 and Cremophor EL were used as surfactant and edge activator, respectively with the selected bile salts. The optimized bilosomes (HPOB-4) were visualized under transmission electron microscopy (TEM), tested for their stability, in vitro drug-release, ex vivo, in vivo behaviors. The entrapment efficiency, vesicle size, PDI and ZP values of HPOB-4 were 76.46% ± 2.25%, 119.2 ± 1.86 nm, 0.298 ± 0.04 and −30.7 ± 0.72 mV, respectively. TEM revealed spherical-shaped vesicles of HPOB-4. HPOB-4 exhibited a biphasic profile with sustained release for BH of approximately 95.65% over 24 h. HPOB-4 had 2.2-fold enhancement in BH permeation compared to marketed eye drop (Epitaxol®), p < 0.05. HPOB-4 does not show any toxicity as confirmed by histopathology examination. HPOBs were also superior in their IOP lowering efficacy when tested using male albino rabbits over Epitaxol®. HPOBs displayed a significant and prolonged maximum reduction in IOP % over 24 h (57.81%) in comparison with Epitaxol ® (35.27%) that kept IOP at normal baseline value for only 4 h (p < 0.05). Hence, the overall results suggested the potential use of HPOBs in delivering hydrophilic molecule like BH efficiently by improving its transcorneal permeation.

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