Transcorneal Permeation of Ciprofloxacin Liposomes: Effect of Surface Charge and Nonionic Surfactants

Abstract

The success of an ocular delivery system is dependent on the reduction in the precorneal loss of the drug by prolonging the contact time and increasing permeability across the corneal barrier which makes the drug more bioavailable to the ocular tissue. The current investigation aimed to improve the transcorneal permeation of ciprofloxacin hydrochloride by loading into liposomes. The liposomes were prepared and investigated the role of surface charge and nonionic surfactants on the permeation of ciprofloxacin from liposomes across isolated corneal membrane. Among the formulations tested, the liposomes containing stearylamine and polysorbate 80 exhibited higher transcorneal permeation compared to other formulations. A two fold increase in the flux and enhancement ratio was observed for these formulations. The corneal hydration levels tested for the liposomal formulations were within the limits. The data reveals the potential of positive charge and nonionic surfactants in successful delivery of ciprofloxacin across the corneal barrier.

Keywords:

• Dicetyl phosphate
• liposomes
• nonionic surfactants
• stearylamine
• transcorneal permeation

Notes

CL: ciprofloxacin hydrochloride liposomes, CL-SA, CL-DCP, CL-P20, and CL-P80: ciprofloxacin liposomal formulations containing stearylamine, dicetyl phosphate, polysorbate 20 and 80, respectively.

P.I.: polydispersity index; each point represents mean ± SD.

CL: ciprofloxacin hydrochloride liposomes, CL-SA, CL-DCP, CL-P20, and CL-P80: ciprofloxacin liposomal formulations containing stearylamine, dicetyl phosphate, polysorbate 20 and 80, respectively.

CS: ciprofloxacin hydrochloride solution, CL: ciprofloxacin hydrochloride liposomes, CL-SA, CL-DCP: ciprofloxacin liposomal formulations containing stearylamine and dicetyl phosphate, respectively.

Jss: steady state flux, Kp: permeability coefficient, ER: enhancement ratio.

a, b, c indicates significant at p < 0.05, p < 0.01 and p < 0.001, respectively.

1, 2, 3, 4 represent CS, CL, CL-SA, and CL-DCP, respectively.

CS: ciprofloxacin hydrochloride solution, CL: ciprofloxacin hydrochloride liposomes, CL-P20, CL-P80: ciprofloxacin liposomal formulations containing polysorbate 20 and polysorbate 80, respectively.

Jss: steady state flux, Kp: permeability coefficient, ER: enhancement ratio.

a, b, c indicates significant at p < 0.05, p < 0.01 and p < 0.001, respectively.

1, 2, 3, 4 represent CS, CL, CL-P20, and CL-P80, respectively.