A Long-Lasting Triamcinolone-Loaded Microneedle Patch for Prolonged Dermal Delivery.

ABSTRACT

Background: Scar is an unpleasant skin lesion that occurs following deep wounds or burns. The application of local triamcinolone is a common treatment for scar treatment and prevention, which should be repeated several times in conventional dosage forms. An effort has been made here to provide a prolonged triamcinolone dermal delivery by microneedle technology, which can also be used for wound closure. Objectives: This study aimed to develop a long-lasting polylactic acid (PLA) microneedle patch for the prolonged release of triamcinolone acetonide (TrA) that could potentially be used for closure of wound edges and scar prevention and treatment. Methods: In this study, 3% and 10% TrA-containing polymeric microneedles were fabricated using the micro molding-solvent casting method. Optical microscopy, X-ray diffraction analysis (XRD), Fourier-transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) were used for the characterization of microneedles. Mechanical strength was evaluated using a compression test and methylene blue staining. Additionally, the insertion depth was determined by histopathological sectioning of human skin samples and also insertion into Parafilm®M as a skin model. The in vitro drug release profile of the microneedles was studied over 34 days, and the kinetic model was determined. The ex-vivo skin permeation of TrA was studied using a Franz-diffusion cell. Results: The TrA-containing PLA microneedles were fabricated with a uniform structure without any failure, deterioration, or loss of needles. Fourier-transform infrared spectroscopy and differential scanning calorimetry showed no interaction between TrA and PLA, and no effect on crystallinity and thermal behavior of TrA on polymer was detected. Microneedles showed appropriate mechanical properties, which were able to penetrate to about 900 - 1000 µm depth. Release profile from the whole body of 10% and 3% microneedle fitted to Higuchi model with cumulative amounts of 625 µg and 201.64 µg over 34 days. Release from the needles followed zero-order kinetic with cumulative amounts of 30.04 µg and 20.36 µg for 10% and 3%, respectively, for 34 days. Permeation was calculated to be 17 µg/day for 10% TrA-containing microneedle. Conclusions: The results suggested that suitable PLA microneedles containing TrA with prolonged release behavior can be successfully constructed with the solvent casting method.