Abstract
Acyclovir is widely indicated for the treatment of herpes labialis (cold sores), typically caused by the herpes simplex virus type 1 (HSV-1). However, topical acyclovir has poor efficacy, due to its low skin permeability. The purpose of this study was, therefore, to evaluate the ability of dissolving polymeric microneedle (MN) arrays to improve the local delivery of acyclovir. Acyclovir-loaded dissolving MN arrays (0.49 cm2) were formulated from aqueous blends of Gantrez® S-97 with 361 needles per array (589 ± 9.29 μm height). MN penetrated excised neonatal porcine skin, showing sufficient mechanical strength to resist compression and maintained their appearance after application of a 0.089 N per needle force for 30 s. Dissolution of the needles was observed within 15 min after application to skin and the needles had completely dissolved at 2 h in vitro. In vitro skin permeation studies revealed that the percentage of total acyclovir loading which permeated the skin over a 24 h period using MNs was approximately 45 times higher than that of a commercial cream formulation (Lipsore®). The accumulation of acyclovir at the basal epidermis, the target site of the herpes simplex virus, using MNs was a total of 21.5 μg/cm3in vitro, wh...Continue Reading
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