Self-Assembled Thermoresponsive Nanogels Prepared by Reverse Micelle → Positive Micelle Method for Ophthalmic Delivery of Muscone, a Poorly Water-Soluble Drug.

This study aimed to design a nanocarrier ophthalmic delivery system of muscone, a poorly water-soluble drug. The muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is <5 s. Compared with muscone eye drops, muscone nanogels showed longer retention time on the corneal surface using fluorescent labeling technology and produced a 3.4-fold increase in apparent permeability coefficients (Papp). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.