Large Porous Particles for Respiratory Drug Delivery. Glycine-Based Formulations | Sciact - CRIS-system of Boreskov Institute of Catalysis

Large Porous Particles for Respiratory Drug Delivery. Glycine-Based Formulations Full article

Journal

European Journal of Pharmaceutical Sciences
ISSN: 0928-0987 , E-ISSN: 1879-0720

Output data

Year: 2017, Volume: 110, Pages: 148-156 Pages count : 9 DOI: 10.1016/j.ejps.2017.05.007

Tags

Spray freeze-drying Salbutamol Budesonide Glycine Clathrate hydrates Dry powder inhaler formulation Large porous particles

Authors

Ogienko A.G. ^1,2 , Bogdanova E.G. ² , Trofimov N.A. ³ , Myz S.A. ⁴ , Ogienko A.A. ⁵ , Kolesov B.A. ^1,2 , Yunoshev A.S. ^2,6 , Zubikov N.V. ³ , Manakov A.Yu. ^1,2 , Boldyrev V.V. ^2,4 , Boldyreva E.V. ^2,4

Affiliations

1	Nikolaev Institute of Inorganic Chemistry SB RAS, Novosibirsk, Russia
2	Novosibirsk State University, Novosibirsk, Russia
3	JSC ‘Nativa’, Moscow, Russia
4	Institute of Solid State Chemistry and Mechanochemistry SB RAS, Novosibirsk, Russia
5	Institute of Cytology and Genetics SB RAS, Novosibirsk, Russia
6	Lavrentiev Institute of Hydrodynamics SB RAS, Novosibirsk, Russia

Funding (3)

1	Council for Grants of the President of the Russian Federation	СП-1144.2013.4
2	Council for Grants of the President of the Russian Federation	СП-680.2013.4
3	Federal Agency for Scientific Organizations	0301-2016-0014 (АААА-А17-117030310274-5)

Large porous particles are becoming increasingly popular as carriers for pulmonary drug delivery with both local and systemic applications. These particles have high geometric diameters (5–30 μm) but low bulk density (~0.1 g/cm3 or less) such that the aerodynamic diameter remains low (1–5 μm). In this study salbutamol and budesonide serve as model inhalable drugs with poor water solubility. A novel method is proposed for the production of dry powder inhaler formulations with enhanced aerosol performance (e.g. for salbutamol-glycine formulation the fine particle fraction (FPF ≤ 4.7 μm) value is 67.0 ± 1.3%) from substances that are poorly soluble in water. To overcome the problems related to extremely poor aqueous solubility of the APIs, not individual solvents are used for spray freeze-drying of API solutions, but organic-water mixtures, which can form clathrate hydrates at low temperatures and release APIs or their complexes as fine powders, which form large porous particles after the clathrates are removed by sublimation. Zwitterionic glycine has been used as an additive to API directly in solutions prior to spray freeze-drying, in order to prevent aggregation of powders, to enhance their dispersibility and improve air-flow properties. The clathrate-forming spray freeze-drying process in the multi-component system was optimized using low-temperature powder X-ray diffraction and thermal analysis.

Ogienko A.G. , Bogdanova E.G. , Trofimov N.A. , Myz S.A. , Ogienko A.A. , Kolesov B.A. , Yunoshev A.S. , Zubikov N.V. , Manakov A.Y. , Boldyrev V.V. , Boldyreva E.V.
Large Porous Particles for Respiratory Drug Delivery. Glycine-Based Formulations
European Journal of Pharmaceutical Sciences. 2017. V.110. P.148-156. DOI: 10.1016/j.ejps.2017.05.007 WOS Scopus РИНЦ AN OpenAlex

Submitted:	Jan 10, 2017
Accepted:	May 4, 2017
Published online:	May 4, 2017
Published print:	Dec 15, 2017

Web of science:	WOS:000414696100006
Scopus:	2-s2.0-85018931544
Elibrary:	31023768
Chemical Abstracts:	2017:779454
OpenAlex:	W2611759838

DB	Citing
Scopus	33
Web of science	29
OpenAlex	34