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Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
- Source :
- Asian Journal of Pharmaceutical Sciences, Vol 16, Iss 5, Pp 612-622 (2021), Asian Journal of Pharmaceutical Sciences
- Publication Year :
- 2021
- Publisher :
- Elsevier, 2021.
-
Abstract
- Coated microneedles (MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs (GEC-MNs) was developed. The water-soluble drug coating was encapsulated with sodium alginate (SA) in situ complexation gel. The manufacturing process of GEC-MNs was optimized for mass production. Compared to the water-soluble coated MNs (72.02% ± 11.49%), the drug delivery efficiency of the optimized GEC-MNs (88.42% ± 6.72%) was steadily increased, and this improvement was investigated through in vitro drug release. The sustained-release of BSA was observed in vitro permeation through the skin. The rhIFNα-1b GEC-MNs was confirmed to achieve biosafety and 6-month storage stability. Pharmacokinetics of rhIFNα-1b in GEC-MNs showed a linearly dose-dependent relationship. The AUC of rhIFNα-1b in GEC-MNs (4.51 ng/ml·h) was bioequivalent to the intradermal (ID) injection (5.36 ng/ml·h) and significantly higher than water-soluble coated MNs (3.12 ng/ml·h). The rhIFNα-1b elimination half-life of GEC-MNs, soluble coated MNs, and ID injection was 18.16, 1.44, and 2.53 h, respectively. The complexation-based GEC-MNs have proved to be more efficient, stable, and achieve the sustained-release of water-soluble drug in coating MNs, constituting a high value to biopharmaceutical.<br />Graphical abstract In the coated microneedle produced by the layer-by-layer coating method, the water-soluble drug-containing coating is encapsulated by the complexation-based gel (GEC-MNs). After GEC-MNs are applied to the skin, the release rate of the drug is reduced by the outer layer of the gel. The pharmacokinetic results of rh-IFNα-1b showed that compared with intradermal injection and water-soluble coated microneedles, the sustained release was achieved in GEC-MNs.Image, graphical abstract
- Subjects :
- Drug
media_common.quotation_subject
Drug delivery system
Pharmaceutical Science
02 engineering and technology
RM1-950
Bioequivalence
engineering.material
010402 general chemistry
01 natural sciences
Pharmacokinetics
Coating
Drug coating
Interferon alpha 1b
Sodium alginate
media_common
Pharmacology
Chromatography
Chemistry
021001 nanoscience & nanotechnology
0104 chemical sciences
Original Research Paper
Coated microneedle
Delivery efficiency
Drug delivery
engineering
Therapeutics. Pharmacology
0210 nano-technology
Sustained release
Subjects
Details
- Language :
- English
- ISSN :
- 18180876
- Volume :
- 16
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Asian Journal of Pharmaceutical Sciences
- Accession number :
- edsair.doi.dedup.....fe15d67c795e73e3031293f2ea44023f