Background: Efavirenz, an anti-HIV agent, has a noticeable place in the HAART regimen
for the treatment and maintenance therapy of AIDS. However, its poor water solubility accounts for
hindered absorption and bio-distribution upon administration. This results in its low and variable bioavailability.
To circumvent these limitations, various novel formulations of Efavirenz have been investigated
in order to mitigate its drawbacks and draw out its maximum therapeutic effect.
Methods: Numerous formulations explored to overcome the drawbacks of Efavirenz include modified/
controlled-release tablets, solid dispersions, polymeric nanoparticles, dendrimers, surface-engineered
nanoparticles and various other nanoformulations. Moreover, combinatorial formulations of Efavirenz
with other Anti-HIV drugs have also been reported to overcome the problem of Drug-Resistance.
Results: The nanoformulation based strategies, owing to their ability to provide controlled release profile
and targeted drug delivery were found to augment bioavailability, therapeutic efficacy and reduce
the side effects of the Efavirenz.
Conclusion: This review pivots around the challenges and recent advances in the delivery of Efavirenz
with particular emphasis on novel formulations including its patents.