Physicochemical characteristics and in vitro release from oil-based vehicles of peptidomimetics: parenteral depots for intra-articular administration

Brian Thoning Pedersen; Jesper Østergaard; Susan Weng Larsen; Claus Cornett; Michael Ankersen; Claus Selch Larsen

doi:10.3109/03639045.2010.491831

Physicochemical characteristics and in vitro release from oil-based vehicles of peptidomimetics: parenteral depots for intra-articular administration

Brian Thoning Pedersen, Jesper Østergaard, Susan Weng Larsen, Claus Cornett, Michael Ankersen, Claus Selch Larsen

3 Citations (Scopus)

Abstract

Results: Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model. Conclusion: The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.

Original language	English
Journal	Drug Development and Industrial Pharmacy
Volume	37
Issue number	1
Pages (from-to)	62-71
ISSN	0363-9045
DOIs	https://doi.org/10.3109/03639045.2010.491831
Publication status	Published - Jan 2011

Keywords

Former Faculty of Pharmaceutical Sciences

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10.3109/03639045.2010.491831

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Physicochemical characteristics and in vitro release from oil-based vehicles of peptidomimetics: parenteral depots for intra-articular administration. / Pedersen, Brian Thoning; Østergaard, Jesper ; Larsen, Susan Weng et al.
In: Drug Development and Industrial Pharmacy, Vol. 37, No. 1, 01.2011, p. 62-71.

Research output: Contribution to journal › Journal article › Research › peer-review

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abstract = "Results: Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model. Conclusion: The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.",

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AU - Cornett, Claus

AU - Ankersen, Michael

AU - Larsen, Claus Selch

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N2 - Results: Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model. Conclusion: The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.

AB - Results: Basic physicochemical properties including their apparent solubility in aqueous buffer and vegetable oils of a series of 11 peptidomimetics varying with respect to chain length and degree of N-methylation were estimated. It was observed that the compounds in contact with water transformed into sticky, slowly dissolving semisolid materials. Based on these observations, the in vitro release behavior of selected peptide derivatives from oil solutions and in situ formed precipitates was investigated using a validated in vitro release model. Conclusion: The results of this investigation suggest that both types of oil-based drug delivery systems might constitute alternative sustained release formulation principles of such amorphous peptide derivatives for the intra-articular route of administration.

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Physicochemical characteristics and in vitro release from oil-based vehicles of peptidomimetics: parenteral depots for intra-articular administration

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