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- Title
Mesoporous Silicon (PSi) for Sustained Peptide Delivery: Effect of PSi Microparticle Surface Chemistry on Peptide YY3-36 Release.
- Authors
Kovalainen, Miia; Mönkäre, Juha; Mäkilä, Ermei; Salonen, Jarno; Lehto, Vesa-Pekka; Herzig, Karl-Heinz; Järvinen, Kristiina
- 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.
- Subjects
MESOPOROUS materials; SURFACE chemistry; PEPTIDES; DRUG delivery systems; SILICON; DRUG bioavailability; THERAPEUTICS
- Publication
Pharmaceutical Research, 2012, Vol 29, Issue 3, p837
- ISSN
0724-8741
- Publication type
Article
- DOI
10.1007/s11095-011-0611-6