Transdermal Film Loaded with Garlic Oil-Acyclovir Nanoemulsion to Overcome Barriers for Its Use in Alleviating Cold Sore Conditions

Abstract

The exponentially mounting cases of herpes simplex virus infection or cold sores have become a serious global concern. Acyclovir (ACV) and garlic oil (GO)-loaded lipid nanocarrier could be a promising therapeutic approach in alleviating cold sores, as well as limiting the biopharmaceutical constraints associated with ACV absorption and therapeutic efficacy. Therefore, the objective of the current research study was to formulate an ACV-GO self-nanoemulsifying drug delivery system (ACV-GO-SNEDDS) as transdermal films. The prepared SNEDDS was optimized using an experimental mixture design. The optimized ACV-GO SNEDDS was loaded in transdermal film and was evaluated for ex vivo skin permeation and in vivo pharmacokinetic prospects. An optimized ACV-GO SNEDDs formulation constituted of 10.4% (w/w) of GO, 64.8% (w/w) of surfactant mixture (Tween 20®-Span 20®); 24.8%(w/w) of co-surfactant (Propylene glycol®), and 200mg of ACV, respectively, were prepared and characterized for particle size (Y). The observed globule size of the optimized ACV-GO SNEDDS is 170 ± 13.45 nm. The results of stability studies indicated that the stability index of optimized ACV-GO-SNEDDS was more than 92 ± 3%. This optimized ACV-GO SNEDDS was loaded in hydroxypropyl cellulose transdermal film. The outcome of the ex vivo skin permeation study demonstrated a 2.3-fold augmented permeation of ACV from the optimized ACV-GO SNEDDS HPC transdermal film in comparison to the raw ACV transdermal film. There was a 3-fold increase in the relative bioavailability of the optimized ACV-GO SNEDDS transdermal film compared to the raw ACV-HPC film. The study findings confirmed that the ACV-GO SNEDDS transdermal film exhibited excellent potential to enhance the bioavailability of ACV.

Garlic (Allium sativum L.) Bioactives and Its Role in Alleviating Oral Pathologies

“…GE consists of specific bioactive compounds like alliin, allicin, SAC, DAS, allymethyltrisulphide and ajoene [ 53 ]. Specifically, allicin, also known as diallyl-thiosulfinate, is a class of organo-sulphur secondary metabolites immensely present in garlic with distinguished antibacterial properties [ 54 , 55 ]. The emergence of resistance against the allicin is also 1000 times slower than antibiotic resistance.…”

Black Garlic as an Antiviral for Herpes Simplex Virus-2 in Lung Cells

“…Almehmady and Ali (2021) assessed a nano-emulsion composed of garlic oil and acyclovir, amongst other types of essential oils like tea tree, peppermint and thyme. The garlic oil was found to increase the bioavailability of the acyclovir nearly three times [28]. A combination therapeutic, like the garlic oil-acyclovir emulsion, could result in a decreased dosage and delay antiviral resistance.…”

Plant-derived Ren's oligopeptide has antiviral effects on influenza virus and SARS-CoV-2

“…Organosulfurs (such as allicin and alliin) and flavonoids (such as quercetin) are the main antiviral components of garlic extract ( 29 ). The antiviral potential of garlic has been widely reported against various viruses such as HIV ( 30 ), dengue virus ( 31 ), herpes simplex virus ( 32 ), and influenza virus ( 33 ). The anti-influenza activity of garlic extract may be due to inhibition of viral replication or blocking virus budding from infected cells ( 33 ).…”