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

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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.
Keywords
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

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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.
@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},
}

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