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


CONCLUSIONS
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.
Pedersen
Brian Thoning
BT
Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Ostergaard
Jesper
J
Larsen
Susan Weng
SW
Cornett
Claus
C
Ankersen
Michael
M
Larsen
Claus
C
D000595:Amino Acid Sequence; D001702:Biopharmaceutics; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D007270:Injections, Intra-Articular; D008969:Molecular Sequence Data; D009821:Oils / Q000737:chemistry*; D057786:Peptidomimetics / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D014677:Pharmaceutical Vehicles / Q000737:chemistry*; D010938:Plant Oils / Q000737:chemistry; D012995:Solubility; D014867:Water / Q000737:chemistry
D003692:Delayed-Action Preparations; D009821:Oils; D057786:Peptidomimetics; D014677:Pharmaceutical Vehicles; D010938:Plant Oils; D014867:Water