Publication: Encapsulation of poorly water-soluble drugs into organic nanotubes for improving drug dissolution
Issued Date
2014-07-20
Resource Type
ISSN
18733476
03785173
03785173
Other identifier(s)
2-s2.0-84900438463
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Mahidol University
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SCOPUS
Bibliographic Citation
International Journal of Pharmaceutics. Vol.469, No.1 (2014), 190-196
Suggested Citation
Kunikazu Moribe, Takashi Makishima, Kenjirou Higashi, Nan Liu, Waree Limwikrant, Wuxiao Ding, Mitsutoshi Masuda, Toshimi Shimizu, Keiji Yamamoto Encapsulation of poorly water-soluble drugs into organic nanotubes for improving drug dissolution. International Journal of Pharmaceutics. Vol.469, No.1 (2014), 190-196. doi:10.1016/j.ijpharm.2014.04.005 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/34900
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Title
Encapsulation of poorly water-soluble drugs into organic nanotubes for improving drug dissolution
Abstract
Hydrocortisone (HC), a poorly water-soluble drug, was encapsulated within organic nanotubes (ONTs), which were formed via the self-assembly of N-{12-[(2-α,β-d-glucopyranosyl) carbamoyl]dodecanyl}- glycylglycylglycine acid. The stability of the ONTs was evaluated in ten organic solvents, of differing polarities, by field emission transmission electron microscopy. The ONTs maintained their stable tubular structure in the highly polar solvents, such as ethanol and acetone. Furthermore, solution-state1H-NMR spectroscopy confirmed that they were practically insoluble in acetone at 25 °C (0.015 mg/mL). HC-loaded ONTs were prepared by solvent evaporation using acetone. A sample with a 3/7 weight ratio of HC/ONT was analyzed by powder X-ray diffraction, which confirmed the presence of a halo pattern and the absence of any crystalline HC peak. HC peak broadening, observed by solid-state13C-NMR measurements of the evaporated sample, indicated the absence of HC crystals. These results indicated that HC was successfully encapsulated in ONT as an amorphous state. Improvements of the HC dissolution rate were clearly observed in aqueous media at both pH 1.2 and 6.8, probably due to HC amorphization in the ONTs. Phenytoin, another poorly water-soluble drug, also showed significant dissolution improvement upon ONT encapsulation. Therefore, ONTs can serve as an alternative pharmaceutical excipient to enhance the bioavailability of poorly water-soluble drugs. © 2014 Elsevier B.V.