期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 129, 期 -, 页码 257-266出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2018.06.011
关键词
Spray drying; Dry powder; Nasal cast; Nose-to-brain; Peptide, chitosan
The nose-to-brain delivery of ghrelin loaded in liposomes is a promising approach for the management of cachexia. It could limit the plasmatic degradation of ghrelin and provide direct access to the brain, where ghrelin's specific receptors are located. Anionic liposomes coated with chitosan in either a liquid or a dry-powder formulation were compared. The powder formulation showed stronger adhesion to mucins (89 +/- 4% vs 61 +/- 4%), higher ghrelin entrapment efficiency (64 +/- 2% vs 55 +/- 4%), higher enzymatic protection against trypsin (26 +/- 2% vs 20 +/- 3%) and lower ghrelin storage degradation at 25 degrees C (2.67 +/- 1.1% vs 95.64 +/- 0.85% after 4 weeks). The powder formulation was also placed in unit-dose system devices that were able to generate an appropriate aerosol characterized by a Dv50 of 38 +/- 61 mu m, a limited percentage of particles smaller than 10 mu m of 4 +/- 1% and a reproducible mass delivery (CV: 1.49%). In addition, the device was able to deposit a large amount of powder (52.04% w/w) in the olfactory zone of a 3D-printed nasal cast. The evaluated combination of the powder formulation and the device could provide a promising treatment for cachexia.
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