Fabrication of Polymeric Microneedles using Novel Vacuum Compression Molding Technique for Transdermal Drug Delivery.

Abstract

To demonstrate the feasibility of vacuum compression molding as a novel technique for fabricating polymeric poly (D, L-lactic-co-glycolic acid) microneedles. First, polydimethylsiloxane molds were prepared using metal microneedle templates and fixed in the MeltPrep® Vacuum Compression Molding tool. Poly (D, L-lactic-co-glycolic acid) (EXPANSORB® DLG 50-5A) was added, enclosed, and heated at 130°C for 15 min under a vacuum of -15 psi, cooled with compressed air for 15 min, followed by freezing at -20°C for 30 min, and stored in a desiccator. The microneedles and microchannels were characterized by a variety of imaging techniques. In vitro permeation of model drug lidocaine as base and hydrochloride salt was demonstrated across intact and microporated dermatomed human skin. Fabricated PLGA microneedles were pyramid-shaped, sharp, uniform, and mechanically robust. Scanning electron microscopy, skin integrity, dye-binding, histology, and confocal laser microscopy studies confirmed the microchannel formation. The receptor delivery of lidocaine salt increased significantly in microporated (270.57 ± 3.73 μg/cm2) skin as compared to intact skin (142.19 ± 13.70 μg/cm2) at 24 h. The receptor delivery of lidocaine base from microporated skin was significantly higher (312.37 ± 10.57 μg/cm2) than intact skin (169.68 ± 24.09 μg/cm2) up to 8 h. Lag time decreased significantly for the base (2.24 ± 0.17 h to 0.64 ± 0.05 h) and salt (4.76 ± 0.31 h to 1.47 ± 0.21 h) after microporation. Vacuum compression molding was demonstrated as a novel technique to fabricate uniform, solvent-free, strong polymer microneedles in a short time.