Compositions and methods for treating conditions of the nail unit

Preparation of Terbinafine Microparticles and In Vitro Release of Terbinafine

[0072] A predetermined amount of the drug terbinafine HCl (3.3 g) is added to the oil phase (polymer in solvent 5.0 g / 7.0 g). The polymer is 50 / 50 polylactic acid / glycolic acid with a molecular weight of about 40,000 g / mol, and the solvent is methylene chloride. The aqueous phase (23.5 g) contains the emulsifier polyvinyl alcohol (2.5 g) to adjust viscosity. Approximately three drops of octanol is added to the aqueous phase to prevent or minimize foaming. Furthermore, to prevent drug loss into the aqueous phase, the aqueous phase is saturated with the drug.

[0073] Next, a one inch impeller mixer is used to agitate the continuous phase at about 600 rpm. The oil phase is then slowly added to the aqueous phase. This mixture is stirred for about an hour, and air passed over it to remove the evaporating solvent. After ten minutes, the stirrer speed is reduced to 400 rpm. At about 30 minutes, most of the me

Itraconazole Microparticles and In Vitro Release of Itraconazole

[0076] Microparticles including itraconazole are prepared according to the method described in Example 1 at a size of about 400 microns. In vitro drug release is measured in the same manner as Example 1. These microparticles are expected to have a drug release profile as shown in the following table:

TimeDay 2Day 14Day 30Day 45% release20-2560-6580-8595-100

Ciprofloxacin Microparticles and In Vitro Release of Ciprofloxacin

[0077] Microparticles are prepared as described in Example 1, except that ciprofloxacin is added instead of terbinafine. The size of the microparticles should be about 250 microns. These microparticles are expected to have a drug release profile as shown in the following table:

TimeDay 1Day 2Day 14Day 30% release20-2530-3570-7590-95

[0078] These microparticles provide a high initial burst of active agent, which would, in the clinical environment, generate locally high anti-infective concentration levels. This is desirable, for example, after surgery, to prevent microorganisms that may be introduced during the surgical procedure from replicating and causing an infection of the wound area. Subsequent drug release would be lower, but sufficient to generate an in vivo maintenance level that can prevent the microbial re-colonization of the surgical area. At day 7, it is believed that the cumulative drug release will equal th