Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used by topical
application in management of joint pain and inflammation. Little is known,
however, about their pharmacokinetics, especially in the synovial compartme
nt versus the plasma compartment, following topical administration.
Ketoprofen, a NSAID, was delivered by a single topical application (KETUM (
R) 2.5% gel) on the rabbit knee-joint region of one hind limb. Concentratio
ns of ketoprofen were measured in plasma, synovial fluid, joint capsule and
synovial fat tissue at 2, 4, 6 and 12 hours after application. Whatever th
e time period after application, ketoprofen concentrations in synovial flui
d were much higher than in plasma. The time-course of the decrease in ketop
rofen plasma concentrations was more rapid than that in synovial fluid. Sim
ilarly, concentrations in joint capsule were higher than those found in syn
ovial fat tissue. Finally, while ketoprofen concentrations decreased rapidl
y in plasma and in synovial fat tissue, concentrations in joint capsule and
particularly in synovial fluid were more sustained. The increase in reside
nce time of ketoprofen in synovial fluid could be in favour of its efficien
cy in the management of joint pain and inflammation.