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Effects of Labrasol on the corneal drug delivery of baicalin

Purpose: To investigate the use of Labrasol in ocular drug delivery system. Methods: The in vivo ocular irritation of Labrasol was tested by pathological section observation using rabbits. The effects of Labrasol on corneal permeability of baicalin was investigated in vitro, using isolated rabbit corneas. The pharmacokinetics was evaluated by microdialysis in the rabbit aqueous humors. Results: The results of the ocular irritation studies showed that Labrasol was non-irritant at the concentrations studied (0.5–3.0%(v/v)), while Labrasol produced slight irritation at a concentration of 5.0%(v/v). For the in vitro study, with Labrasol at concentrations of 1.5%, 2.0%, and 3.0%(v/v), the apparent permeability coefficient (Papp) was 1.69-, 3.14-, and 2.23- fold of baicalin solution, respectively. In the pharmacokinetics studies, the AUC value of baicalin solution with 2.0% and 3.0%(v/v) Labrasol were 4.7- and 5.6-fold of that of the control group (p < 0.01), and the Cmax value of baicalin solution with 2.0% and 3.0%(v/v) Labrasol vs the control group were 3.2- and 5.7-fold (p < 0.01). Conclusion: Labrasol may have potential clinical benefits in improving the ocular drug delivery of baicalin.