Efavirenz is an anti-HIV drug categorized under Non-Nucleoside Reverse
Transcriptase Inhibitor (NNRTI). It is recognized as the first line drug of choice for treating
HIV infections. Poor aqueous solubility of the drug (< 10 µg/mL) offers specific challenges
in formulation design, leading to limited bioavailability of 40 to 50%. To address
this issue, several drug delivery options have been adopted for Efavirenz with special emphasis
on alternative routes of administration like buccal, rectal, vaginal and transdermal.
The carrier-based delivery using vesicular systems, micro/nanoparticles, hydrogels, degradable
systems, etc. was also designed through solvent evaporation, spray drying, double
emulsification and ionic gelation techniques. The nanotechnology-based drug delivery
approaches have been demonstrated with significant improvement in the solubility and
bioavailability of Efavirenz. The objective of the review is to compile and present the comprehensive report of
various researches highlighted for synthesizing nanoparticles of Efavirenz using different polymeric and nonpolymeric
materials. We have discussed the range of materials utilized for the preparation of stable nanoparticles
through the validated experimental protocol and their substantial selection of optimized formulation
through significant results.