Abstract
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.
Keywords: Efavirenz, dissolution, solubility, nanoparticles, polymer, HIV.
Graphical Abstract
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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