18F-Labeled Modified Porous Silicon Particles for Investigation of Drug Delivery Carrier Distribution In Vivo with Positron Emission Tomography

Mirkka Sarparanta, Ermei Mäkilä, Teemu Heikkilä, Jarno Juhani Salonen, Edwin Kukk, Vesa-Pekka Lehto, Hélder A. Santos, Jouni Hirvonen, Anu Airaksinen

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Sammanfattning

Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step 18F-radiolabeling of three types of PSi microparticles, thermally hydrocarbonized THCPSi, thermally oxidized TOPSi, and thermally carbonized TCPSi for the investigation of their biodistribution in vivo with positron emission tomography as part of their evaluation as carriers for particle-mediated drug delivery. FTIR and XPS characterization of the PSi materials after carrier-added 18F/19F-radiolabeling reveals that depending on the material the 18F-labeling is likely to be accomplished either by substitution for surface silyl hydrogen, silyl fluoride or by nucleophilic attack of 18F- to Si-O-Si bridges. With the selected 18F-radiolabeling method, good to excellent in vitro radiolabel in simulated gastric and intestinal fluids and in plasma is achieved for all the particle types studied. Finally, a preliminary evaluation of 18F-THCPSi microparticle biodistribution in the rat gastrointestinal tract after oral administration is reported illustrating the utility of using 18F-radiolabeled PSi as imaging probes for PSi-based drug delivery carrier distribution in vivo.
Originalspråkengelska
TidskriftMolecular Pharmaceutics
Volym8
Utgåva5
Sidor (från-till)1799-1806
ISSN1543-8384
DOI
StatusPublicerad - 2011
MoE-publikationstypA1 Tidskriftsartikel-refererad

Vetenskapsgrenar

  • 317 Farmaci

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title = "18F-Labeled Modified Porous Silicon Particles for Investigation of Drug Delivery Carrier Distribution In Vivo with Positron Emission Tomography",
abstract = "Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step 18F-radiolabeling of three types of PSi microparticles, thermally hydrocarbonized THCPSi, thermally oxidized TOPSi, and thermally carbonized TCPSi for the investigation of their biodistribution in vivo with positron emission tomography as part of their evaluation as carriers for particle-mediated drug delivery. FTIR and XPS characterization of the PSi materials after carrier-added 18F/19F-radiolabeling reveals that depending on the material the 18F-labeling is likely to be accomplished either by substitution for surface silyl hydrogen, silyl fluoride or by nucleophilic attack of 18F- to Si-O-Si bridges. With the selected 18F-radiolabeling method, good to excellent in vitro radiolabel in simulated gastric and intestinal fluids and in plasma is achieved for all the particle types studied. Finally, a preliminary evaluation of 18F-THCPSi microparticle biodistribution in the rat gastrointestinal tract after oral administration is reported illustrating the utility of using 18F-radiolabeled PSi as imaging probes for PSi-based drug delivery carrier distribution in vivo.",
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author = "Mirkka Sarparanta and Ermei M{\"a}kil{\"a} and Teemu Heikkil{\"a} and {Juhani Salonen}, Jarno and Edwin Kukk and Vesa-Pekka Lehto and Santos, {H{\'e}lder A.} and Jouni Hirvonen and Anu Airaksinen",
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18F-Labeled Modified Porous Silicon Particles for Investigation of Drug Delivery Carrier Distribution In Vivo with Positron Emission Tomography. / Sarparanta, Mirkka; Mäkilä, Ermei ; Heikkilä, Teemu ; Juhani Salonen, Jarno ; Kukk, Edwin ; Lehto, Vesa-Pekka ; Santos, Hélder A.; Hirvonen, Jouni; Airaksinen, Anu.

I: Molecular Pharmaceutics, Vol. 8, Nr. 5, 2011, s. 1799-1806.

Forskningsoutput: TidskriftsbidragArtikelVetenskapligPeer review

TY - JOUR

T1 - 18F-Labeled Modified Porous Silicon Particles for Investigation of Drug Delivery Carrier Distribution In Vivo with Positron Emission Tomography

AU - Sarparanta, Mirkka

AU - Mäkilä, Ermei

AU - Heikkilä, Teemu

AU - Juhani Salonen, Jarno

AU - Kukk, Edwin

AU - Lehto, Vesa-Pekka

AU - Santos, Hélder A.

AU - Hirvonen, Jouni

AU - Airaksinen, Anu

PY - 2011

Y1 - 2011

N2 - Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step 18F-radiolabeling of three types of PSi microparticles, thermally hydrocarbonized THCPSi, thermally oxidized TOPSi, and thermally carbonized TCPSi for the investigation of their biodistribution in vivo with positron emission tomography as part of their evaluation as carriers for particle-mediated drug delivery. FTIR and XPS characterization of the PSi materials after carrier-added 18F/19F-radiolabeling reveals that depending on the material the 18F-labeling is likely to be accomplished either by substitution for surface silyl hydrogen, silyl fluoride or by nucleophilic attack of 18F- to Si-O-Si bridges. With the selected 18F-radiolabeling method, good to excellent in vitro radiolabel in simulated gastric and intestinal fluids and in plasma is achieved for all the particle types studied. Finally, a preliminary evaluation of 18F-THCPSi microparticle biodistribution in the rat gastrointestinal tract after oral administration is reported illustrating the utility of using 18F-radiolabeled PSi as imaging probes for PSi-based drug delivery carrier distribution in vivo.

AB - Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step 18F-radiolabeling of three types of PSi microparticles, thermally hydrocarbonized THCPSi, thermally oxidized TOPSi, and thermally carbonized TCPSi for the investigation of their biodistribution in vivo with positron emission tomography as part of their evaluation as carriers for particle-mediated drug delivery. FTIR and XPS characterization of the PSi materials after carrier-added 18F/19F-radiolabeling reveals that depending on the material the 18F-labeling is likely to be accomplished either by substitution for surface silyl hydrogen, silyl fluoride or by nucleophilic attack of 18F- to Si-O-Si bridges. With the selected 18F-radiolabeling method, good to excellent in vitro radiolabel in simulated gastric and intestinal fluids and in plasma is achieved for all the particle types studied. Finally, a preliminary evaluation of 18F-THCPSi microparticle biodistribution in the rat gastrointestinal tract after oral administration is reported illustrating the utility of using 18F-radiolabeled PSi as imaging probes for PSi-based drug delivery carrier distribution in vivo.

KW - 317 Pharmacy

U2 - 10.1021/mp2001654

DO - 10.1021/mp2001654

M3 - Article

VL - 8

SP - 1799

EP - 1806

JO - Molecular Pharmaceutics

JF - Molecular Pharmaceutics

SN - 1543-8384

IS - 5

ER -