Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

Abayomi T Ogunjimi; Jennifer Fiegel; Nicole K Brogden

doi:10.3390/pharmaceutics12060496

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Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

Journal article

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Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

Abayomi T Ogunjimi, Jennifer Fiegel and Nicole K Brogden

Pharmaceutics, Vol.12(6), p.496

05/29/2020

DOI: 10.3390/pharmaceutics12060496

PMCID: PMC7355536

PMID: 32485999

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Abstract

Naltrexone (NTX) hydrochloride is a potent opioid antagonist with significant first-pass metabolism and notable untoward effects when administered orally or intramuscularly. Microneedle (MN)-assisted transdermal delivery is an attractive alternative that can improve therapeutic delivery to deeper skin layers. In this study, chitosan-NTX microspheres were developed via spray-drying, and their potential for transdermal NTX delivery in association with MN skin treatment was assessed. A quality-by-design approach was used to evaluate the impact of key input variables (chitosan molecular weight, concentration, chitosan-NTX ratio, and feed flow rate) on microsphere physical characteristics, encapsulation efficiency, and drug-loading capacity. Formulated microspheres had high encapsulation efficiencies (70%-87%), with drug-loading capacities ranging from 10%-43%. NTX flux through MN-treated skin was 11.6 ± 2.2 µg/cm ·h from chitosan-NTX microspheres, which was significantly higher than flux across intact skin. Combining MN-assisted delivery with the chitosan microsphere formulation enabled NTX delivery across the skin barrier, while controlling the dose released to the skin.

microneedles, naltrexone, spray-drying, quality-by-design, transdermal delivery

Details

Title: Subtitle: Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery
Creators: Abayomi T Ogunjimi - University of Iowa
Jennifer Fiegel - University of Iowa
Nicole K Brogden - University of Iowa
Resource Type: Journal article
Publication Details: Pharmaceutics, Vol.12(6), p.496
DOI: 10.3390/pharmaceutics12060496
PMID: 32485999
PMCID: PMC7355536
NLM abbreviation: Pharmaceutics
ISSN: 1999-4923
eISSN: 1999-4923
Grant note: P30 ES005605 / NIEHS NIH HHS R35 GM124551 / NIGMS NIH HHS 1R35GM124551 / NIH HHS
Language: English
Date published: 05/29/2020
Academic Unit: Dermatology; Pharmaceutical Sciences and Experimental Therapeutics; Chemical and Biochemical Engineering
Record Identifier: 9984197276602771

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