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Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying

Delphine Coucke UGent, Chris Vervaet UGent, P. Foreman, P. Adriaensens, R. Carleer and Jean Paul Remon UGent (2009) International Journal of Pharmaceutics. 379(1). p.67-71
abstract
A mucoadhesive combination of a maize starch (Amioca(R), mainly consisting of amylopectine) and a cross-linked acrylic acid-based polymer (Carbopol(R) 974P) was spray-dried with metoprolol tartrate (used as model molecule) in order to develop a powder suitable for nasal drug delivery via a one-step manufacturing process. The bioavailability of metoprolol tartrate after nasal administration of this powder to rabbits was compared with powders manufactured via other procedures: (a) freeze-drying of a dispersion prepared using the co-spray-dried powder, (b) freeze-drying of a dispersion prepared using a physical mixture of drug and mucoadhesive polymers. After co-processing via spray-drying a low bioavailability (BA 10.8 +/- 2.3%) was obtained, whereas manufacturing procedures based on freeze-drying yielded a higher BA: 37.9 +/- 12.8% using the co-processed powder and 73.6 +/- 24.9% using the physical mixture. The higher bioavailability was due to the deprotonation of poly(acrylic acid) during neutralisation of the dispersion prior to freeze-drying. This induced repulsion of the ionised carboxyl groups and a lower interaction between poly(acrylic acid) and starch, creating a less compact matrix upon hydration of the polymer and allowing an easier escape of metoprolol tartrate from the matrix. This study showed that co-processing of a mucoadhesive Amioca(R)/Carbopol(R) 974P formulation with metoprolol tartrate via co-spray-drying did not provide any added value towards the bioavailability of the drug after nasal administration of the mucoadhesive powder.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
Co-spray-drying as all-in-one process, Amioca (R)/Carbopol (R) 974P powder formulation, FORMULATION, Nasal administration, DELIVERY, INFLUENZA VACCINE, Metoprolol tartrate, METOPROLOL, INSULIN, MIXTURES
journal title
International Journal of Pharmaceutics
Int. J. Pharm.
volume
379
issue
1
pages
67 - 71
publisher
Elsevier
Web of Science type
Article
Web of Science id
000269809600009
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
2.962 (2009)
JCR rank
78/236 (2009)
JCR quartile
2 (2009)
ISSN
0378-5173
DOI
10.1016/j.ijpharm.2009.06.008
language
English
UGent publication?
yes
classification
A1
copyright statement
I don't know the status of the copyright for this publication
id
761490
handle
http://hdl.handle.net/1854/LU-761490
date created
2009-10-07 14:08:29
date last changed
2009-11-06 09:08:01
@article{761490,
  abstract     = {A mucoadhesive combination of a maize starch (Amioca(R), mainly consisting of amylopectine) and a cross-linked acrylic acid-based polymer (Carbopol(R) 974P) was spray-dried with metoprolol tartrate (used as model molecule) in order to develop a powder suitable for nasal drug delivery via a one-step manufacturing process. The bioavailability of metoprolol tartrate after nasal administration of this powder to rabbits was compared with powders manufactured via other procedures: (a) freeze-drying of a dispersion prepared using the co-spray-dried powder, (b) freeze-drying of a dispersion prepared using a physical mixture of drug and mucoadhesive polymers. After co-processing via spray-drying a low bioavailability (BA 10.8 +/- 2.3\%) was obtained, whereas manufacturing procedures based on freeze-drying yielded a higher BA: 37.9 +/- 12.8\% using the co-processed powder and 73.6 +/- 24.9\% using the physical mixture. The higher bioavailability was due to the deprotonation of poly(acrylic acid) during neutralisation of the dispersion prior to freeze-drying. This induced repulsion of the ionised carboxyl groups and a lower interaction between poly(acrylic acid) and starch, creating a less compact matrix upon hydration of the polymer and allowing an easier escape of metoprolol tartrate from the matrix. This study showed that co-processing of a mucoadhesive Amioca(R)/Carbopol(R) 974P formulation with metoprolol tartrate via co-spray-drying did not provide any added value towards the bioavailability of the drug after nasal administration of the mucoadhesive powder.},
  author       = {Coucke, Delphine and Vervaet, Chris and Foreman, P. and Adriaensens, P. and Carleer, R. and Remon, Jean Paul},
  issn         = {0378-5173},
  journal      = {International Journal of Pharmaceutics},
  keyword      = {Co-spray-drying as all-in-one process,Amioca (R)/Carbopol (R) 974P powder formulation,FORMULATION,Nasal administration,DELIVERY,INFLUENZA VACCINE,Metoprolol tartrate,METOPROLOL,INSULIN,MIXTURES},
  language     = {eng},
  number       = {1},
  pages        = {67--71},
  publisher    = {Elsevier},
  title        = {Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2009.06.008},
  volume       = {379},
  year         = {2009},
}

Chicago
Coucke, Delphine, Chris Vervaet, P. Foreman, P. Adriaensens, R. Carleer, and Jean Paul Remon. 2009. “Effect on the Nasal Bioavailability of Co-processing Drug and Bioadhesive Carrier via Spray-drying.” International Journal of Pharmaceutics 379 (1): 67–71.
APA
Coucke, D., Vervaet, C., Foreman, P., Adriaensens, P., Carleer, R., & Remon, J. P. (2009). Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying. International Journal of Pharmaceutics, 379(1), 67–71.
Vancouver
1.
Coucke D, Vervaet C, Foreman P, Adriaensens P, Carleer R, Remon JP. Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying. International Journal of Pharmaceutics. Elsevier; 2009;379(1):67–71.
MLA
Coucke, Delphine, Chris Vervaet, P. Foreman, et al. “Effect on the Nasal Bioavailability of Co-processing Drug and Bioadhesive Carrier via Spray-drying.” International Journal of Pharmaceutics 379.1 (2009): 67–71. Print.