The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems

Mirkka P. Sarparanta, Luis M. Bimbo, Ermei M. Mäkilä, Jarno J. Salonen, Päivi H. Laaksonen, A. M. Kerttuli Helariutta, Markus B. Linder, Jouni T. Hirvonen, Timo J. Laaksonen, Hélder A. Santos, Anu J. Airaksinen

Research output: Contribution to journalArticle

84 Citations (Scopus)

Abstract

Impediments to intestinal absorption, such as poor solubility and instability in the variable conditions of the gastrointestinal (GI) tract plague many of the current drugs restricting their oral bioavailability. Particulate drug delivery systems hold great promise in solving these problems, but their effectiveness might be limited by their often rapid transit through the GI tract. Here we describe a bioadhesive oral drug delivery system based on thermally-hydrocarbonized porous silicon (THCPSi) functionalized with a self-assembled amphiphilic protein coating consisting of a class II hydrophobin (HFBII) from Trichoderma reesei. The HFBII-THCPSi nanoparticles were found to be non-cytotoxic and mucoadhesive in AGS cells, prompting their use in a biodistribution study in rats after oral administration. The passage of HFBII-THCPSi nanoparticles in the rat GI tract was significantly slower than that of uncoated THCPSi, and the nanoparticles were retained in stomach by gastric mucoadhesion up to 3 h after administration. Upon entry to the small intestine, the mucoadhesive properties were lost, resulting in the rapid transit of the nanoparticles through the remainder of the GI tract. The gastroretentive drug delivery system with a dual function presented here is a viable alternative for improving drug bioavailability in the oral route.

LanguageEnglish
Pages3353-3362
Number of pages10
JournalBiomaterials
Volume33
Issue number11
Early online date28 Jan 2012
DOIs
Publication statusPublished - 30 Apr 2012
Externally publishedYes

Fingerprint

Porous silicon
Silicon
Drug Delivery Systems
Nanoparticles
Gastrointestinal Tract
Rapid transit
Biological Availability
Rats
Stomach
Trichoderma
Plague
Intestinal Absorption
Pharmaceutical Preparations
Solubility
Small Intestine
Oral Administration
Proteins
Coatings

Keywords

  • adhesiveness
  • administration, oral
  • animals
  • coated materials, biocompatible
  • fungal proteins
  • gastric mucosa
  • gastrointestinal tract
  • intestinal absorption
  • male
  • metabolic clearance rate
  • nanocapsules
  • organ specificity
  • porosity
  • rats, wistar
  • silicon
  • tissue distribution

Cite this

Sarparanta, M. P., Bimbo, L. M., Mäkilä, E. M., Salonen, J. J., Laaksonen, P. H., Helariutta, A. M. K., ... Airaksinen, A. J. (2012). The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems. Biomaterials, 33(11), 3353-3362. https://doi.org/10.1016/j.biomaterials.2012.01.029
Sarparanta, Mirkka P. ; Bimbo, Luis M. ; Mäkilä, Ermei M. ; Salonen, Jarno J. ; Laaksonen, Päivi H. ; Helariutta, A. M. Kerttuli ; Linder, Markus B. ; Hirvonen, Jouni T. ; Laaksonen, Timo J. ; Santos, Hélder A. ; Airaksinen, Anu J. / The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems. In: Biomaterials. 2012 ; Vol. 33, No. 11. pp. 3353-3362.
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abstract = "Impediments to intestinal absorption, such as poor solubility and instability in the variable conditions of the gastrointestinal (GI) tract plague many of the current drugs restricting their oral bioavailability. Particulate drug delivery systems hold great promise in solving these problems, but their effectiveness might be limited by their often rapid transit through the GI tract. Here we describe a bioadhesive oral drug delivery system based on thermally-hydrocarbonized porous silicon (THCPSi) functionalized with a self-assembled amphiphilic protein coating consisting of a class II hydrophobin (HFBII) from Trichoderma reesei. The HFBII-THCPSi nanoparticles were found to be non-cytotoxic and mucoadhesive in AGS cells, prompting their use in a biodistribution study in rats after oral administration. The passage of HFBII-THCPSi nanoparticles in the rat GI tract was significantly slower than that of uncoated THCPSi, and the nanoparticles were retained in stomach by gastric mucoadhesion up to 3 h after administration. Upon entry to the small intestine, the mucoadhesive properties were lost, resulting in the rapid transit of the nanoparticles through the remainder of the GI tract. The gastroretentive drug delivery system with a dual function presented here is a viable alternative for improving drug bioavailability in the oral route.",
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Sarparanta, MP, Bimbo, LM, Mäkilä, EM, Salonen, JJ, Laaksonen, PH, Helariutta, AMK, Linder, MB, Hirvonen, JT, Laaksonen, TJ, Santos, HA & Airaksinen, AJ 2012, 'The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems' Biomaterials, vol. 33, no. 11, pp. 3353-3362. https://doi.org/10.1016/j.biomaterials.2012.01.029

The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems. / Sarparanta, Mirkka P.; Bimbo, Luis M.; Mäkilä, Ermei M.; Salonen, Jarno J.; Laaksonen, Päivi H.; Helariutta, A. M. Kerttuli; Linder, Markus B.; Hirvonen, Jouni T.; Laaksonen, Timo J.; Santos, Hélder A.; Airaksinen, Anu J.

In: Biomaterials, Vol. 33, No. 11, 30.04.2012, p. 3353-3362.

Research output: Contribution to journalArticle

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T1 - The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems

AU - Sarparanta, Mirkka P.

AU - Bimbo, Luis M.

AU - Mäkilä, Ermei M.

AU - Salonen, Jarno J.

AU - Laaksonen, Päivi H.

AU - Helariutta, A. M. Kerttuli

AU - Linder, Markus B.

AU - Hirvonen, Jouni T.

AU - Laaksonen, Timo J.

AU - Santos, Hélder A.

AU - Airaksinen, Anu J.

N1 - Copyright © 2012 Elsevier Ltd. All rights reserved.

PY - 2012/4/30

Y1 - 2012/4/30

N2 - Impediments to intestinal absorption, such as poor solubility and instability in the variable conditions of the gastrointestinal (GI) tract plague many of the current drugs restricting their oral bioavailability. Particulate drug delivery systems hold great promise in solving these problems, but their effectiveness might be limited by their often rapid transit through the GI tract. Here we describe a bioadhesive oral drug delivery system based on thermally-hydrocarbonized porous silicon (THCPSi) functionalized with a self-assembled amphiphilic protein coating consisting of a class II hydrophobin (HFBII) from Trichoderma reesei. The HFBII-THCPSi nanoparticles were found to be non-cytotoxic and mucoadhesive in AGS cells, prompting their use in a biodistribution study in rats after oral administration. The passage of HFBII-THCPSi nanoparticles in the rat GI tract was significantly slower than that of uncoated THCPSi, and the nanoparticles were retained in stomach by gastric mucoadhesion up to 3 h after administration. Upon entry to the small intestine, the mucoadhesive properties were lost, resulting in the rapid transit of the nanoparticles through the remainder of the GI tract. The gastroretentive drug delivery system with a dual function presented here is a viable alternative for improving drug bioavailability in the oral route.

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KW - adhesiveness

KW - administration, oral

KW - animals

KW - coated materials, biocompatible

KW - fungal proteins

KW - gastric mucosa

KW - gastrointestinal tract

KW - intestinal absorption

KW - male

KW - metabolic clearance rate

KW - nanocapsules

KW - organ specificity

KW - porosity

KW - rats, wistar

KW - silicon

KW - tissue distribution

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DO - 10.1016/j.biomaterials.2012.01.029

M3 - Article

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T2 - Biomaterials

JF - Biomaterials

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