Controlled drug release from polymeric delivery devices V: Hydroxy group effects on drug release kinetics and thermodynamics.
The effects of progesterone hydroxylation on silicone matrix drug release kinetics and thermodynamics were investigated. Hydroxylation at positions 11, 17, and/or 21 substantially reduced progesterone release. The magnitude of this reduction depended on the number and position of the hydroxy groups and could be attributed to decreased polymer matrix diffusivity (Dm) and polymer solubility (Cp). Thermodynamically, hydroxy group addition to positions 11 and/or 21 reduced the activation energy for matrix diffusion (Ed,m) but increased the solvation energy for dissolution in silicone polymer (delta HT,m)). Adding an hydroxy group to position 17 increased the Ed,m but decreased the delta HT,m. The overall (Ed,m) + delta H(T,m)) values were relatively constant and independent of hydroxylation.
D003692:Delayed-Action Preparations; D006900:Hydroxylation; D007700:Kinetics; D011092:Polyethylene Glycols; D011108:Polymers; D011374:Progesterone / Q000031:analogs & derivatives; D012826:Silicone Elastomers; D012995:Solubility; D013329:Structure-Activity Relationship; D013816:Thermodynamics
D003692:Delayed-Action Preparations; D011108:Polymers; D012826:Silicone Elastomers; D011092:Polyethylene Glycols; D011374:Progesterone