2995277-02-4

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Imiquimod (R 837) dihydrochloride, an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].

in vivo

Imiquimod (IMQ) can be used to induce psoriasis models^[5].

Induction of psoriasis Model^[5]

Background

Lmiquimod (IMQ) induces inflamed scaly skin lesions resembling plaque-type psoriasis. IMQ induces epidermal expression of IL-23, IL-17A, and IL-17F, as well as an increase in splenic Th17 cells.

Specific Mmodeling Methods

Mice: BALB/c ? male ? 8-week-old
Administration: 3.125 mg/day ? skin ? 6 days

Note

IMQ cream preparation ^[7]:
(1) Prepare BM of lipids
STA and OA were melted at 75 °C followed by the addition of IMQ (3.5% of the BM, w/w) under continuous stirring.
Polysorbate 80 and stearoyl polyoxyl-32 glycerides at a 50:50 ratio were dispersed in water heated separately to 75 °C and added to the BM phase under continuous stirring.
(2) Prepare nanostructured lipid carriers (NLCs)
The mixture was then subjected to high-shear homogenization followed by ultrasonication.
The mixture was then rapidly cooled in an ice bath to allow the formation of NLCs.

Modeling Indicators

Behavior Observation: Induced the back skin of the mice started to display signs of erythema, scaling, and thickening.
Resulted in hyperproliferative keratinocytes and a disturbed epidermal differentiation (parakeratosis).

Correlated Product(s): /

Opposite Product(s): /

^[1].

References

[1] Athina Angelopoulou, et al. Imiquimod - A toll like receptor 7 agonist - Is an ideal option for management of COVID 19. Environ Res. 2020 Sep; 188: 109858. DOI:10.1016/j.envres.2020.109858
[2] Aditya K Gupta, et al. Imiquimod: a review. J Cutan Med Surg. Nov-Dec 2002;6(6):554-60. DOI:10.1007/s10227-001-0134-6
[3] Yuji Kan, et al. Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol. 2012 Oct;86(19):10338-46. DOI:10.1128/JVI.01196-12
[4] Michael P Sch?n, et al. The small antitumoral immune response modifier imiquimod interacts with adenosine receptor signaling in a TLR7- and TLR8-independent fashion. J Invest Dermatol. 2006 Jun;126(6):1338-47. DOI:10.1038/sj.jid.5700286
[5] Leslie van der Fits, et al. Imiquimod-induced psoriasis-like skin inflammation in mice is mediated via the IL-23/IL-17 axis. J Immunol. 2009, 182, 9. DOI:10.4049/jimmunol.0802999
[6] Ajla Smajlovi?, et al. Molecular and histopathological profiling of imiquimod induced dermatosis in Swiss Wistar rats: contribution to the rat model for novel anti-psoriasis treatments. Mol Biol Rep. 2021, 48, 5. DOI:10.1007/s11033-021-06445-3
[7] Sangseo Kim, et al. Development and Optimization of Imiquimod-Loaded Nanostructured Lipid Carriers Using a Hybrid Design of Experiments Approach. Int J Nanomedicine. 2023. DOI:10.2147/IJN.S400610

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in vivo

References

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