article · Drug Delivery
Ocular drug delivery for conditions such as pterygium and cataract often faces challenges with rapid clearance and poor corneal permeation. A topical formulation using hyaluronan-enriched cubosomes loaded with bromfenac sodium was developed to improve drug retention and penetration. Created via an emulsification process using glycerol monoolein, poloxamer 407, and polyvinyl alcohol, the optimised formulation formed stable, cubic nanoparticles with a mean size of approximately 149 nanometres. Histopathological evaluation confirmed that the formulation produced no ocular irritation. In ex vivo tests on goat corneas, the cubosomes showed superior drug deposition and permeability compared to standard drug solutions. In vivo assessments in aqueous humour revealed that the formulation provided more than double the overall drug exposure and a longer residence time compared to marketed eye drops, indicating its potential for safe, effective topical ocular delivery.
Delivering medications to the eye using conventional eye drops is challenging because natural fluid drainage quickly washes active ingredients away. By encasing the anti-inflammatory drug bromfenac inside nanoscale lipid particles, this method enhances corneal penetration and keeps the drug active in eye tissues for longer. This may lead to more effective topical treatments for conditions like cataracts, potentially reducing how often patients must administer drops.
This technology could provide pharmaceutical developers with a more effective delivery mechanism for ocular anti-inflammatory medications. The work is at an applied and tested stage, having demonstrated superior pharmacokinetic performance compared to a commercial comparator in animal models. Reaching clinical and commercial adoption will require further development through formal non-clinical toxicity programmes and human clinical trials to validate therapeutic efficacy and safety in patients.
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To design and evaluate hyaluronan-based cubosomes loaded with bromfenac sodium (BS) for ocular application to enhance the corneal permeation and retention in pterygium and cataract treatment. BS-loaded cubosomes were prepared by the emulsification method, employing 23 full factorial design using Design-Expert® software. Glycerol monoolein (GMO) and poloxamer 407 (P407) as lipid phase and polyvinyl alcohol (PVA) as stabilizer were the used ingredients. The optimized formulation (OBC; containing GMO (7% w/w), P407 (0.7% w/w) and PVA (2.5% w/w)) was further evaluated. OBC had an entrapment efficiency of 61.66 ± 1.01%, a zeta potential of −30.80 ± 0.61 mV, a mean particle size of 149.30 ± 15.24 nm and a polydispersity index of 0.21 ± 0.02. Transmission electron microscopy confirmed its cubic shape and excellent dispersibility. OBC exhibited high stability and no ocular irritation that was ensured by histopathology. Ex vivo permeation study showed a significant increase in drug deposition and permeability parameters through goat cornea, besides, confocal laser microscopy established the superior permeation capability of OBC, as compared to drug solution. In vivo pharmacokinetics in aqueous humor indicated higher AUC0-tlast (18.88 µg.h/mL) and mean residence time (3.16 h) of OBC when compared to the marketed eye drops (7.93 µg.h/mL and 1.97 h, respectively). Accordingly, hyaluronan-enriched cubosomes can be regarded as a promising carrier for safe and effective topical ocular delivery.
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DOI: 10.1080/10717544.2022.2162162
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