Poloxamer 407 (P407) is a hydrophilic non-ionic surfactant. It is a triblock copolymer, which is composed of a central hydrophobic block of polypropylene glycol and two hydrophilic blocks of polyethylene glycol (PEG).
This method aimed to develop a water micelle formulation using a water-soluble derivative of vitamin E (TPGS: D-α-germinol polyethylene glycol 1000 succinate) and P407 as excipients for efficient delivery of cyclosporine to eye tissue. Firstly, cyclosporine solubility was studied, and the appropriate proportion and concentration of P407: TPGS were selected to determine the preparation method of cyclosporine-loaded formulations. Then the particle size, zeta potential, morphology, rheology, and stability after dilution and freeze-drying of formulations were characterized. Cyclosporine-loaded micelles exhibited proper characteristics for ocular administration, sufficient stability against dilution, and adequate rheological properties at 35oC, and they can be sterilized by filtration and then freeze-dried without the need for a cryoprotectant. After dilution in simulated tears, cyclosporine-loaded mixed micelles effectively retained the drug and were stable during freeze-drying in the presence of 20 mm surfactant concentration. Drug-loaded mixed micelles were applied to porcine cornea in vitro and compared with ikervis. The drug accumulation in the cornea is directly proportional to the drug concentration. Finally, it is worth mentioning that the mixed micelles described can represent a useful platform for the ocular delivery of other lipophilic drugs. This could be very interesting, considering the good results obtained in scleral accumulation and trans-scleral delivery and the growing interest in the noninvasive targeting of the retina.
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