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

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

Research output: Contribution to journalArticleScientificpeer-review

83 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.
Original languageEnglish
Pages (from-to)3353-3362
JournalBiomaterials
Volume33
Issue number11
DOIs
Publication statusPublished - 2012
MoE publication typeA1 Journal article-refereed

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

  • Silicon
  • hydrophobin
  • nanoparticle
  • drug delivery
  • adhesion
  • biocompatibility

Cite this

Sarparanta, M. P., Bimbo, L. M., Mäkilä, E. M., Salonen, J. J., Laaksonen, P., 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 ; 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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Sarparanta, MP, Bimbo, LM, Mäkilä, EM, Salonen, JJ, Laaksonen, P, 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. (Corresponding Author); Bimbo, Luis M.; Mäkilä, Ermei M.; Salonen, Jarno J.; Laaksonen, Päivi; Helariutta, A.M. Kerttuli; Linder, Markus B.; Hirvonen, Jouni T.; Laaksonen, Timo J.; Santos, Hélder A.; Airaksinen, Anu J. (Corresponding Author).

In: Biomaterials, Vol. 33, No. 11, 2012, p. 3353-3362.

Research output: Contribution to journalArticleScientificpeer-review

TY - JOUR

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

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.

PY - 2012

Y1 - 2012

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.

AB - 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.

KW - Silicon

KW - hydrophobin

KW - nanoparticle

KW - drug delivery

KW - adhesion

KW - biocompatibility

U2 - 10.1016/j.biomaterials.2012.01.029

DO - 10.1016/j.biomaterials.2012.01.029

M3 - Article

VL - 33

SP - 3353

EP - 3362

JO - Biomaterials

JF - Biomaterials

SN - 0142-9612

IS - 11

ER -