Inclusion complexed iloperidone loaded dissolving microneedles: Characterization, in-vitro study, and dermatopharmacokinetics

Schizophrenia is among the most complicated and critical psychological conditions. The current research was envisioned to improve the permeability of the second-generation antipsychotic drug iloperidone by incorporating it in dissolving microneedle which is optimized by a 32 factorial design. The inclusion complex was synthesized by kneading a drug with a complexing agent and auxiliary agent to increase the solubility of the drug. Physicochemical, mechanical characterization, skin insertion studies, and stability studies of microneedles (MNs) were performed. Further dermatokinetics studies were carried out. Scanning electron microscopy (SEM) depicts pyramidal shape of MNs which were sharp with intact needles and a smooth surface. The polymeric MNs have good mechanical properties with piercing capabilities. The in-vitro and ex-vivo permeation showed an extended drug release profile. The ex-vivo study of the optimized batch exhibited 34.04 ± 3.60 mcg/cm2 release from the skin at the end of 24 h. The optimized batch exhibits the highest deposition of drugs in the skin. Stability studies showed optimized MNs were stable for 6 months at accelerated conditions. Our findings suggest that inclusion-complexed iloperidone-loaded dissolving microneedle can serve as a good platform for transepidermal delivery of the antipsychotic drug. [Display omitted] •Solubility of Iloperidone enhanced by complexing with hydroxypropyl beta-cyclodextrin and auxiliary agent.•Micromolding to fabricate dissolving microneedle arrays which have effectual strength to pierce the stratum corneum.•A significant amount of drug was retained in the skin over 24 h from microneedles.•Iloperidone microneedles can be a good alternate for the existing dosage form.