Transdermal Microneedle-Mediated Delivery of Rasagiline Nanoparticles.

Abstract

In the transdermal drug delivery system, the drug is administered through the skin and attains a systemic effect. It is a drug administration route that includes drug transport to the epidermis and potentially dermal tissue of the skin for locally therapeutic effect, while an exceptionally significant drug division is transported in systemic blood circulation. This study aimed to formulate rasagiline mesylate (RM) as a transdermal microneedle (MN) delivery. The RM is an antiparkinson drug that can be classified as class III with low permeability and subjected to extensive first-pass metabolism. At first, it was formulated as nanoparticles using the chitosan polymer and ion gelation method. Afterward, the prepared nanoparticles were incorporated into a transdermal MN formulated by a polydimethylsiloxane template. The two-step casting process uses two polymer concentrations of polyvinyl alcohol and mixes them with other polymers in a 3:1 ratio (polyvinylpyrrolidone and chitosan) and glycerin as a plasticizer. The selected MN formula was MN4 with a promising shape, no bubbles, fine and well-formed sharp needles that passed the folding endurance test with 130 folding times before broken, drug content of 97±10.02%, and ex vivo permeation. The results showed a significant (P>0.05) permeability enhancement and increase of flux (160%), compared to the transdermal patch. The RS polymeric nanoparticles were successfully prepared and loaded within dissolving MNs of sufficient mechanical strength to penetrate the stratum corneum and enhance the amount permeated through it to induce the systemic effect transdermally.