Intra-articular depot formulation principles: role in the management of postoperative pain and arthritic disorders.
The joint cavity constitutes a discrete anatomical compartment that allows for local drug action after intra-articular injection. Drug delivery systems providing local prolonged drug action are warranted in the management of postoperative pain and not least arthritic disorders such as osteoarthritis. The present review surveys various themes related to the accomplishment of the correct timing of the events leading to optimal drug action in the joint space over a desired time period. This includes a brief account on (patho)physiological conditions and novel potential drug targets (and their location within the synovial space). Particular emphasis is paid to (i) the potential feasibility of various depot formulation principles for the intra-articular route of administration including their manufacture, drug release characteristics and in vivo fate, and (ii) how release, mass transfer and equilibrium processes may affect the intra-articular residence time and concentration of the active species at the ultimate receptor site.
Larsen
Claus
C
Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. csl@farma.ku.dk
Ostergaard
Jesper
J
Larsen
Susan W
SW
Jensen
Henrik
H
Jacobsen
Stine
S
Lindegaard
Casper
C
Andersen
Pia H
PH
D000700:Analgesics / Q000008:administration & dosage* / Q000627:therapeutic use; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005240:Feasibility Studies; D006801:Humans; D007596:Joints; D010003:Osteoarthritis / Q000188:drug therapy*; D010149:Postoperative Pain / Q000188:drug therapy*
D000700:Analgesics; D003692:Delayed-Action Preparations