Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example

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 optimi...

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Autores principales:	Zequan Zhou, Suohui Zhang, Guozhong Yang, Yunhua Gao
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Coated microneedle Drug delivery system Sustained release Interferon alpha 1b Sodium alginate Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/7fa5ea5ec90c4690b1156ae495746a0d
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spelling	oai:doaj.org-article:7fa5ea5ec90c4690b1156ae495746a0d2021-11-20T04:57:42ZEnhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example1818-087610.1016/j.ajps.2021.05.002https://doaj.org/article/7fa5ea5ec90c4690b1156ae495746a0d2021-09-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S1818087621000507https://doaj.org/toc/1818-0876Coated 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.Zequan ZhouSuohui ZhangGuozhong YangYunhua GaoElsevierarticleCoated microneedleDrug delivery systemSustained releaseInterferon alpha 1bSodium alginateTherapeutics. PharmacologyRM1-950ENAsian Journal of Pharmaceutical Sciences, Vol 16, Iss 5, Pp 612-622 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Coated microneedle Drug delivery system Sustained release Interferon alpha 1b Sodium alginate Therapeutics. Pharmacology RM1-950
spellingShingle	Coated microneedle Drug delivery system Sustained release Interferon alpha 1b Sodium alginate Therapeutics. Pharmacology RM1-950 Zequan Zhou Suohui Zhang Guozhong Yang Yunhua Gao Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
description	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.
format	article
author	Zequan Zhou Suohui Zhang Guozhong Yang Yunhua Gao
author_facet	Zequan Zhou Suohui Zhang Guozhong Yang Yunhua Gao
author_sort	Zequan Zhou
title	Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
title_short	Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
title_full	Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
title_fullStr	Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
title_full_unstemmed	Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
title_sort	enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhifnα-1b example
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/7fa5ea5ec90c4690b1156ae495746a0d
work_keys_str_mv	AT zequanzhou enhanceddeliveryefficiencyandsustainedreleaseofbiopharmaceuticalsbycomplexationbasedgelencapsulatedcoatedmicroneedlesrhifna1bexample AT suohuizhang enhanceddeliveryefficiencyandsustainedreleaseofbiopharmaceuticalsbycomplexationbasedgelencapsulatedcoatedmicroneedlesrhifna1bexample AT guozhongyang enhanceddeliveryefficiencyandsustainedreleaseofbiopharmaceuticalsbycomplexationbasedgelencapsulatedcoatedmicroneedlesrhifna1bexample AT yunhuagao enhanceddeliveryefficiencyandsustainedreleaseofbiopharmaceuticalsbycomplexationbasedgelencapsulatedcoatedmicroneedlesrhifna1bexample
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Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example

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