期刊
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
卷 24, 期 9, 页码 1133-1143出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10837450.2019.1641727
关键词
Aerosol microparticles; sustained release; pulmonary drug delivery; water-soluble compounds; acetalated dextran
资金
- National Science Foundation [1508868]
- Div Of Chem, Bioeng, Env, & Transp Sys
- Directorate For Engineering [1508868] Funding Source: National Science Foundation
Objective: To design and characterize aerosol microparticles (MP) to provide sustained release of the water-soluble compound sulforhodamine B (SRB) and achieve effective aerosol dispersion. Methods: SRB and water made up an aqueous solution, while acetalated dextran (Ac-Dex) and isopropyl alcohol made up an organic solution. The two solutions were mixed together, and the solution was spray dried to produce MP. MP were characterized for morphology, size, release kinetics, aerosol dispersion, and cellular interactions. Results: Ac-Dex MP exhibited corrugated morphology and aerodynamic diameters from 2.06 to 2.86 mu m. MP deposited in all stages of a Next Generation Impactor, with >90% fine particle fraction. MP exhibited encapsulation efficiencies >129% with SRB loading values up to 16.7 mu g SRB/mg MP. MP exhibited sustained release of SRB at pH 7 and fast release at pH 5. In vitro experiments showed minimal cytotoxicity, successful uptake of MP in epithelial cells, and no disruption to the integrity of epithelial monolayers. Conclusions: Ac-Dex MP systems demonstrated the ability to provide sustained the release of a water-soluble therapeutic in addition to effective aerosol dispersion for pulmonary applications.
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