Dissolving microneedle-based intradermal delivery of interferon-α-2b

Abstract

The dermal and transdermal delivery of protein pharmaceuticals faces enormous challenges, and at the same time, has very significant potential for the non-invasive treatment of both localized and systemic diseases. To demonstrate the pharmaceutical usefulness of dissolving microneedles (MNs) containing interferon-α-2b (IFN), IFN MNs were prepared using a new method. IFN were encapsulated in MNs with dose from 4.94 ± 0.64 to 23.79 ± 2.48 μg, and in vitro release test showed the efficiency reached 49.2%. After percutaneous administration of IFN MNs to rats, serum IFN levels were measured for 12 h. The peak serum IFN level, maximum drug concentration (C_max), and the time to reach maximum concentration (T_max), were 11.58 ± ng/ml and 40 min, respectively, for high-dose MNs group. The area under the curve (AUC) of MNs group was 28.85 ng·h/ml, while intramuscular injection (IM) group with equal dose was 31.17 ng·h/ml. Immunogenicity analysis showed the anti-IFN antibody got back to normal level at ninth week, and there was no difference between male and female rats. IFN MNs showed good stability for 2 months and no damage to the administered rats’ skin. The results demonstrated the IFN MNs have a great potential to provide an alternative to IM.

• Dissolving microneedles
• immunogenicity analysis
• interferon
• intradermal drug delivery
• pharmacokinetic analysis
• stability

Declaration of interest

The authors report no declaration of interest. This work was partially supported by the Science Foundation of the Chinese Academy of Sciences and the National Natural Science Foundation of China (Grant No.31300763). Dr. Jian-min Chen was supported by the Natural Science Foundation of Fujian Province (Grant No. 2015J05167) and a grant from the Education Department of Fujian Province (JA14276).