There are several significant setbacks including limited bioavailability, high clearance, and
further current therapies require higher and frequent dosing to gain desired therapeutic effects.
Nanomedicines have been widely investigated for rheumatoid arthritis (RA). Though, higher doses also
increase the incidence of dreadful adverse effects. Further, nanocarrier properties are tuned by the use
of different approaches like varied methods of loading, hydrophilic polymers and targeting ligands, to
change the physicochemical properties including higher encapsulation, better penetrating ability to biological
barriers, thus preventing the uptake of various nanocarriers by liver and spleen. Along with
these they provide longer circulation which enhances drug localization at the inflamed site and selective
targeting to enhance the therapeutic index of anti-rheumatic drugs. However, the optimal properties
also depend on the route of administration and nanocarrier size, thus larger size show more retention
upon local injection and smaller sized ones are more optimal for passive targeting. The present review
discusses the emergence of nano-carriers for anti-rheumatic drugs, which delivers drug molecule to the
inflamed site by topical, intra-articular (i.a) and intra-venous (i.v) administration to achieve therapeutic
efficacy by passive and active drug targeting. Advancements have been made extensively but still better
investigations are needed to optimize the risk-benefit ratio for the development of safe and stable targeting
nanocarriers for the effective treatment of rheumatoid arthritis (RA).