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Updated: May 28, 2026
Porous Silicon Microparticles for Delivery of siRNA Therapeutics
Published on: January 15, 2015
Mesoporous silicon (PSi) for sustained peptide delivery: effect of psi microparticle surface chemistry on peptide
Miia Kovalainen1, Juha Mönkäre, Ermei Mäkilä
1School of Pharmacy, Pharmaceutical Technology, Faculty of Health Sciences, University of Eastern Finland, Po Box 1627, 70211, Kuopio, Finland. Miia.Kovalainen@uef.fi
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.
