title: 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 (Cmax), and the time to reach maximum concentration (Tmax), 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.
authors.affiliation: a College of Pharmaceutical and Medical Technology, Putian University , Fujian , China and.
authors.forename: Jianmin
authors.initials: J
authors.lastname: Chen
authors.affiliation: b Key Laboratory of Photochemical Conversion and Optoelectronic Materials , Technical Institute of Physics and Chemistry, Chinese Academy of Sciences , Beijing , China.
authors.forename: Yuqin
authors.initials: Y
authors.lastname: Qiu
authors.affiliation: b Key Laboratory of Photochemical Conversion and Optoelectronic Materials , Technical Institute of Physics and Chemistry, Chinese Academy of Sciences , Beijing , China.
authors.forename: Suohui
authors.initials: S
authors.lastname: Zhang
authors.affiliation: b Key Laboratory of Photochemical Conversion and Optoelectronic Materials , Technical Institute of Physics and Chemistry, Chinese Academy of Sciences , Beijing , China.
authors.forename: Yunhua
authors.initials: Y
authors.lastname: Gao
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000917:Antibody Formation / Q000276:immunology; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000008:administration & dosage* / Q000276:immunology; D008297:Male; D008845:Microinjections / Q000379:methods*; D009339:Needles; D051381:Rats; D017207:Rats, Sprague-Dawley; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000276:immunology; D012869:Skin Absorption; D013552:Swine
chemical_list: D000077190:Interferon alpha-2; D016898:Interferon-alpha; D011994:Recombinant Proteins
keywords: Dissolving microneedles; immunogenicity analysis; interferon; intradermal drug delivery; pharmacokinetic analysis; stability