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Acyclovir (ACV) is a guanine nucleoside analog widely used against herpes simplex virus (HSV-1, HSV-2) and varicella-zoster virus (VZV). It inhibits viral DNA synthesis with high selectivity and low cytotoxicity. Various synthesis routes from purine or guanine derivatives have been developed to achieve high yield and cost-effectiveness. Structural modifications, such as valacyclovir (prodrug) and lipophilic derivatives, improve bioavailability, solubility, and transdermal delivery. Analytical methods for ACV quantification include UV/visible spectrophotometry, thin-layer chromatography, and high-performance liquid chromatography (HPLC), with HPLC being preferred for biological matrices due to its sensitivity. Mass spectrometry coupled with HPLC enables detection at low concentrations. These modifications and analytical tools help optimize ACV’s pharmacological profile, reduce side effects, and ensure quality control in pharmaceutical formulations.
Fig. 1 Synthesis, antiviral mechanism, modifications of Acyclovir. (Hassan Abed Z.; et al. 2025)
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Acrylamide-based hydrogels containing MgO nanoparticles and carboxymethyl cellulose (NaCMC) were developed as potential vaginal ring formulations for acyclovir delivery. Maximum drug loading (24.32%) and entrapment efficiency (79.97%) were achieved at pH 7.5. Hydrogels with 6.4% w/w acyclovir showed the highest hardness. Field emission scanning electron microscopy (FESEM) revealed increased permeability and uniform drug distribution after loading. The point of zero charge (pH PZC) shifted from 4.5 to 4.7 upon drug loading. The hydrogels are designed for sustained release in vaginal rings to treat herpes simplex virus (HSV) and varicella-zoster virus (VZV) infections, offering improved retention and protection of acyclovir.
Fig. 2 FESEM imaging of powderized hydrogel with Acyclovir loaded. (Sabbagh F.; et al. 2018)
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