Enhanced acyclovir delivery using w/o type microemulsion: preclinical assessment of antiviral activity using murine model of zosteriform cutaneous HSV-1 infection

Abstract

The present study was aimed to develop and evaluate a microemulsion-based dermal drug delivery of an antiviral agent, acyclovir. A water-in-oil microemulsion was prepared using isopropyl myristate, Tween 20, Span 20, water and dimethylsulphoxide. It was characterized for drug content, stability, globule size, pH, viscosity and ex vivo permeation through mice skin. In vivo antiviral efficacy of optimized formulation was assessed in female Balb/c mice against herpes simplex virus-I (HSV-I)-induced infection. It was observed that optimized formulation when applied 24-h post-infection could completely inhibit the development of cutaneous herpetic lesions vis-à-vis marketed cream.

Nanoemulsions: The rising star of antiviral therapeutics and nanodelivery system—current status and prospects

“…IC 50 values against HSV-1 at post-infection (48 h) were 0.012 and 0.156 μM for acyclovir-loaded CNS and free acyclovir, while IC 50 values against HSV-2 post-infection (24 h) were 0.100 μM and 1.608 μM for acyclovir-loaded CNS and free acyclovir, respectively [ 82 ]. Similarly, the acyclovir containing water-in-oil MEs was formulated with isopropyl myristate, span 20, Tween 20, water, and DMSO, which showed complete inhibition of cutaneous herpetic lesions development in female Balb/c mice with HSV-1-induced infection compared to the commercially marketed cream [ 83 ]. Ionic liquid (triethylammonium acetate and diethylammonium acetate) containing microemulsion formed using isopropyl myristate, Tween 80, and span 20 demonstrated very long-term stability (42 days) of acyclovir and methotrexate compared to the commercially available formulations containing 1-ethyl-3-methylimidazolium acetate [ 84 ].…”

Foray into Concepts of Design and Evaluation of Microemulsions as a Modern Approach for Topical Applications in Acne Pathology

“…microemulsion in biological fluids for oral delivery [32]. In topical therapy of dermatologic conditions, an increased solubility and bioavailability was obtained for molecules like: cyclosporine in psoriasis [33]; ceramides for skin restructuration [34]; imiquimod in actinic keratosis or basal cell carcinoma [35]; penciclovir [36], acyclovir for herpes virus simplex cutaneous infection [37]; and tenoxicam for arthritis alleviation [38].…”

“…Several discoveries with positive results can be mentioned: in ophthalmology [23], for ocular delivery of retinol [24] or sacha inchi oil for dry eye treatment [25]; intranasal delivery for zidovudine [26]; sublingual delivery of insulin [27]; application of fusidic acid in wound healing [28]; vaginal delivery for fluconazole [29]; transdermal drug delivery [30]; cosmetics [31]; self-microemulsifyied systems with in situ generation of microemulsion in biological fluids for oral delivery [32]. In topical therapy of dermatologic conditions, an increased solubility and bioavailability was obtained for molecules like: cyclosporine in psoriasis [33]; ceramides for skin restructuration [34]; imiquimod in actinic keratosis or basal cell carcinoma [35]; penciclovir [36], acyclovir for herpes virus simplex cutaneous infection [37]; and tenoxicam for arthritis alleviation [38].…”

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“…Mathematical models are described in two types empirical and theoretical. Former ones are mostly in the form of linear models, and the latter ones in nonlinear form 27 . The empirical type model depicts the relationship between a response and a factor with the help of the polynomial equation of the given order.…”

“…The 1 & 2 equations are linear in nature with flat surface and braided area in 3-D space, and equation 3 depicts a second-order linear model that shows braided curves. A theoretical model can also exist, which is usually nonlinear [27][28][29][30] .…”