Pharmaceutical Research

, Volume 29, Issue 3, pp 837–846

Mesoporous Silicon (PSi) for Sustained Peptide Delivery: Effect of PSi Microparticle Surface Chemistry on Peptide YY3-36 Release

Authors

    • School of Pharmacy, Pharmaceutical Technology, Faculty of Health SciencesUniversity of Eastern Finland
  • Juha Mönkäre
    • School of Pharmacy, Pharmaceutical Technology, Faculty of Health SciencesUniversity of Eastern Finland
  • Ermei Mäkilä
    • Department of Physics and AstronomyUniversity of Turku
  • Jarno Salonen
    • Department of Physics and AstronomyUniversity of Turku
  • Vesa-Pekka Lehto
    • Faculty of Science and Forestry, Department of Applied PhysicsUniversity of Eastern Finland
  • Karl-Heinz Herzig
    • Institute of Biomedicine, Biocenter of Oulu University of Oulu
    • Department of PsychiatryKuopio University Hospital
  • Kristiina Järvinen
    • School of Pharmacy, Pharmaceutical Technology, Faculty of Health SciencesUniversity of Eastern Finland
Research Paper

DOI: 10.1007/s11095-011-0611-6

Cite this article as:
Kovalainen, M., Mönkäre, J., Mäkilä, E. et al. Pharm Res (2012) 29: 837. doi:10.1007/s11095-011-0611-6

ABSTRACT

Purpose

To achieve sustained peptide delivery via mesoporous silicon (PSi) microparticles and to evaluate the effects of different surface chemistries on peptide YY3-36 (PYY3-36) delivery.

Methods

PYY3-36 was loaded into thermally oxidized (TOPSi), thermally hydrocarbonized (THCPSi) and undecylenic acid treated THCPSi (UnTHCPSi) microparticles with comparable porous properties. In vitro, PYY3-36 release was investigated by centrifuge. In vivo, PYY3-36 plasma concentrations were analyzed after delivery in microparticles or solution.

Results

Achieved loading degrees were high (12.2 – 16.0% w/w). PYY3-36 release was sustained from all microparticles; order of PYY3-36 release was TOPSi > THCPSi > UnTHCPSi both in vitro and in vivo. In mice, PSi microparticles achieved sustained PYY3-36 release over 4 days, whereas PYY3-36 solution was eliminated in 12 h. In vitro, only 27.7, 14.5 and 6.2% of loaded PYY3-36 was released from TOPSi, THCPSi and UnTHCPSi, respectively. Absolute PYY3-36 bioavailabilities were 98, 13, 9 and 38% when delivered subcutaneously in TOPSi, THCPSi, UnTHCPSi and solution, respectively. The results clearly demonstrate improved bioavailability of PYY3-36 via TOPSi and the importance of surface chemistry of PSi on peptide release.

Conclusions

PSi represents a promising sustained and tailorable release system for PYY3-36.

KEY WORDS

in vivomesoporous siliconpeptide deliverypharmacokineticsPYY3-36

ABBREVIATIONS

PSi

porous silicon

THCPSi

thermally hydrocarbonized porous silicon

TOPSi

thermally oxidized porous silicon

UnTHCPSi

undecylenic acid treated thermally hydrocarbonized porous silicon

Supplementary material

11095_2011_611_MOESM1_ESM.tif (8.1 mb)
High Resolution Image (TIFF 8260 kb)
11095_2011_611_MOESM2_ESM.tif (8.7 mb)
High Resolution Image (TIFF 8939 kb)

Copyright information

© Springer Science+Business Media, LLC 2011