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Influence of heat treatment on spray-dried mixtures of Amioca (R) starch and Carbopol (R) 974P used as carriers for nasal drug delivery

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Abstract
A mucoadhesive spray-dried starch/poly(acrylic acid) powder underwent different heat treatments in order to induce cross-linking between the functional groups of starch (Amioca (R)) and poly(acrylic acid) (Carbopol (R) 974P). After heat treatment the water-absorbing capacity, viscosity and elasticity of the mucoadhesive powder increased. NMR analysis in combination with FT-IR indicated that heat treatment induced a low degree of cross-linking between the polymers. Nasal administration of Amioca (R)/Carbopol (R) 974P powders without heat treatment resulted in an absolute bioavailability in rabbits of 8.2 +/- 3.0% for insulin. Due to the difference in water-absorbing capacity (which opened the tight junctions of the nasal mucosa), elasticity and plasticity (which reduced mucociliairy clearance and prolonged residence time) heat treatment at 120 degrees C improved the bioavailability: 26.4 +/- 21.9, 36.5 +/- 11.0 and 19.3 +/- 17.3% after heat treatment during 30 min, 1 h and 4 h, respectively. Heat treatment at 60 degrees C was less efficient. This study demonstrated that the nasal insulin absorption improved via heat treatment of the Amioca (R)/Carbopol (R) 974P powder (prior to the addition of insulin). The bioavailability-enhancing effect of a 1 h heat treatment at 120 degrees C was confirmed using the same polymer matrix in combination with different drugs (salmon calcitonin, human growth hormone and metoprolol tartrate). (C) 2009 Elsevier B.V. All rights reserved.
Keywords
Amioca (R)/Carbopol (R) 974P powder formulation, NMR spectroscopy, Heat treatment, ABSORPTION, INSULIN, MICROSPHERES, Insulin, Nasal delivery, SYSTEM

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Chicago
Coucke, Delphine, Eveline Pringels, P Foreman, P Adriaensens, R Carleer, Jean Paul Remon, and Chris Vervaet. 2009. “Influence of Heat Treatment on Spray-dried Mixtures of Amioca (R) Starch and Carbopol (R) 974P Used as Carriers for Nasal Drug Delivery.” International Journal of Pharmaceutics 378 (1-2): 45–50.
APA
Coucke, D., Pringels, E., Foreman, P., Adriaensens, P., Carleer, R., Remon, J. P., & Vervaet, C. (2009). Influence of heat treatment on spray-dried mixtures of Amioca (R) starch and Carbopol (R) 974P used as carriers for nasal drug delivery. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 378(1-2), 45–50.
Vancouver
1.
Coucke D, Pringels E, Foreman P, Adriaensens P, Carleer R, Remon JP, et al. Influence of heat treatment on spray-dried mixtures of Amioca (R) starch and Carbopol (R) 974P used as carriers for nasal drug delivery. INTERNATIONAL JOURNAL OF PHARMACEUTICS. 2009;378(1-2):45–50.
MLA
Coucke, Delphine, Eveline Pringels, P Foreman, et al. “Influence of Heat Treatment on Spray-dried Mixtures of Amioca (R) Starch and Carbopol (R) 974P Used as Carriers for Nasal Drug Delivery.” INTERNATIONAL JOURNAL OF PHARMACEUTICS 378.1-2 (2009): 45–50. Print.
@article{740862,
  abstract     = {A mucoadhesive spray-dried starch/poly(acrylic acid) powder underwent different heat treatments in order to induce cross-linking between the functional groups of starch (Amioca (R)) and poly(acrylic acid) (Carbopol (R) 974P). After heat treatment the water-absorbing capacity, viscosity and elasticity of the mucoadhesive powder increased. NMR analysis in combination with FT-IR indicated that heat treatment induced a low degree of cross-linking between the polymers. Nasal administration of Amioca (R)/Carbopol (R) 974P powders without heat treatment resulted in an absolute bioavailability in rabbits of 8.2 +/- 3.0\% for insulin. Due to the difference in water-absorbing capacity (which opened the tight junctions of the nasal mucosa), elasticity and plasticity (which reduced mucociliairy clearance and prolonged residence time) heat treatment at 120 degrees C improved the bioavailability: 26.4 +/- 21.9, 36.5 +/- 11.0 and 19.3 +/- 17.3\% after heat treatment during 30 min, 1 h and 4 h, respectively. Heat treatment at 60 degrees C was less efficient. This study demonstrated that the nasal insulin absorption improved via heat treatment of the Amioca (R)/Carbopol (R) 974P powder (prior to the addition of insulin). The bioavailability-enhancing effect of a 1 h heat treatment at 120 degrees C was confirmed using the same polymer matrix in combination with different drugs (salmon calcitonin, human growth hormone and metoprolol tartrate). (C) 2009 Elsevier B.V. All rights reserved.},
  author       = {Coucke, Delphine and Pringels, Eveline and Foreman, P and Adriaensens, P and Carleer, R and Remon, Jean Paul and Vervaet, Chris},
  issn         = {0378-5173},
  journal      = {INTERNATIONAL JOURNAL OF PHARMACEUTICS},
  keyword      = {Amioca (R)/Carbopol (R) 974P powder formulation,NMR spectroscopy,Heat treatment,ABSORPTION,INSULIN,MICROSPHERES,Insulin,Nasal delivery,SYSTEM},
  language     = {eng},
  number       = {1-2},
  pages        = {45--50},
  title        = {Influence of heat treatment on spray-dried mixtures of Amioca (R) starch and Carbopol (R) 974P used as carriers for nasal drug delivery},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2009.05.041},
  volume       = {378},
  year         = {2009},
}

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