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◆ Therapeutic delivery2026-09-11

Soluble ocular insert of brinzolamide and timolol maleate: in-vitro, ex-vivo and in-vivo characterization.

Nikunj Prajapati, Priyal Vaghela, Hetal Thakkar

一句话结论 · In one sentence

The optimized soluble ocular inserts were found to be transparent, homogeneous, flexible and demonstrated acceptable surface pH (7.21 ± 0.12), bioadhesive strength (11.88 ± 0.89 g), and tensile strength (1.016 ± 0.13 MPa). In-vitro studies demonstrated sustained drug release up to 24 h following Higuchi kinetics. Ex-vivo permeation across goat cornea and in-vivo pharmacodynamic studies demonstrated enhanced and prolonged intraocular pressure reduction compared to the marketed suspension. The short-term stability testing indicated that the ocular insert retained the characteristics of %Transmittance, pH, Assay and % drug release. Overall, the results suggest that for better therapeutic efficacy and adherence in glaucoma treatment, the dual-drug loaded ocular insert provides a new, patient-friendly substitute for traditional ophthalmic dosage forms.

原始摘要(英文原文)· Original abstract
AIMS: The present study aimed to formulate and evaluate a novel transparent and soluble ocular insert containing a fixed-dose combination of Brinzolamide (210 µg) and Timolol maleate (105 µg). MATERIALS AND METHODS: The soluble ocular inserts were formulated using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as film-forming polymers. Optimization of the parameters was done using a D-optimal design. RESULTS AND CONCLUSIONS: The optimized soluble ocular inserts were found to be transparent, homogeneous, flexible and demonstrated acceptable surface pH (7.21 ± 0.12), bioadhesive strength (11.88 ± 0.89 g), and tensile strength (1.016 ± 0.13 MPa). In-vitro studies demonstrated sustained drug release up to 24 h following Higuchi kinetics. Ex-vivo permeation across goat cornea and in-vivo pharmacodynamic studies demonstrated enhanced and prolonged intraocular pressure reduction compared to the marketed suspension. The short-term stability testing indicated that the ocular insert retained the characteristics of %Transmittance, pH, Assay and % drug release. Overall, the results suggest that for better therapeutic efficacy and adherence in glaucoma treatment, the dual-drug loaded ocular insert provides a new, patient-friendly substitute for traditional ophthalmic dosage forms.
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Soluble ocular insert of brinzolamide and timolol maleate: in-vitro, ex-vivo and in-vivo characterization. — 科研速览 Science Skim