期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 526, 期 1-2, 页码 291-299出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.04.041
关键词
Cellulose nanofibers; Cellular solid material; Nanofoam; Indomethacin; Poorly-soluble drugs
资金
- Swedish strategic research council [ICA14-0045]
- Swedish Foundation for Strategic Research (SSF) [ICA14-0045] Funding Source: Swedish Foundation for Strategic Research (SSF)
The unique colloidal properties of cellulose nanofibers (CNF), makes CNF a very interesting new excipient in pharmaceutical formulations, as CNF in combination with some poorly-soluble drugs can create nanofoams with closed cells. Previous nanofoams, created with the model drug indomethacin, demonstrated a prolonged release compared to films, owing to the tortuous diffusion path that the drug needs to take around the intact air-bubbles. However, the nanofoam was only obtained at a relatively low drug content of 21 wt% using fixed processing parameters. Herein, the effect of indomethacin content and processing parameters on the foaming properties was analysed. Results demonstrate that a certain amount of dissolved drug is needed to stabilize air-bubbles. At the same time, larger fractions of dissolved drug promote coarsening/collapse of the wet foam. The pendant drop/bubble profile tensiometry was used to verify the wet-foam stability at different pHs. The pH influenced the amount of solubilized drug and the processing-window was very narrow at high drug loadings. The results were compared to real foaming-experiments and solid state analysis of the final cellular solids. The parameters were assembled into a processing chart, highlighting the importance of the right combination of processing parameters (pH and time-point of pH adjustment) in order to successfully prepare cellular solid materials with up to 46 wt% drug loading. (C) 2017 Elsevier B.V. All rights reserved.
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