Development of nanoemulsions containing penciclovir for herpes simplex treatment and a liquid chromatographic method to drug assessment in porcine skin layers

Authors

  • Alianise da Silva Meira Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul image/svg+xml
    • Ana Paula Battistel Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul image/svg+xml
      • Helder Ferreira Teixeira Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul image/svg+xml
        • Nadia Maria Volpato Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul image/svg+xml

          DOI:

          https://doi.org/10.22456/2527-2616.103121

          Keywords:

          penciclovir, nanoemulsion, cutaneous delivery studies, LC method validation, porcine skin

          Abstract

          A successful formulation (penciclovir hydrogel nanoemulsion - HN) to be used in transdermal drug delivery route to treat herpes simplex virus was developed and an analytical method to quantify penciclovir (PCV) in porcine ear skin was stablished and validated. PCV nanoemulsions were prepared by high pressure homogenization and presented spherical mean droplet size 180 nm. The association efficiency and zeta potential were 87% and– 27 mV, respectively. The bioanalytical method developed showed specificity for the interferences from the skin matrixes (epidermis and dermis) and the linearity was in the range 0.1 – 25 μg/mL of drug, The mean recovery data for the three levels tested were 95.2% for the epidermis and 97.3% for the dermis and adequate results were obtained for repeatability and inter-day precision.  In vitro percutaneous absorption studies with the PCV nanoemulsion and a market cream were conducted employing the porcine skin.The cumulative amounts of PCV permeated from cream and HN, 8 h after dosing, were 2.60 and 4.15 μg/cm², respectively, representing a quite higher flux and a much higher permeability coefficient for the developed formulation. It can be concluded that HN provide a good skin targeting effect and may be a promising carrier for topical delivery of penciclovir.

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          References

          Lin L, Chen XS, Cui PG, Wang JB, Guo ZP, Lu NZ. Topical application of penciclovir cream for the treatment of herpes simplex facialis / labialis : a controlled trial BACKGROUND : 2002;67–72.

          Yu A, Guo C, Zhou Y, Cao F, Zhu W, Sun M, et al. International Immunopharmacology Skin irritation and the inhibition effect on HSV-1 in vivo of penciclovirloaded microemulsion. Int Immunopharmacol [Internet]. 2010;10(10):1305–9. Available from: http://dx.doi.org/10.1016/j.intimp.2010.07.015

          Hasler-nguyen N, Shelton D, Ponard G, Bader M, Schaffrik M, Mallefet P. penciclovir 1 % cream and acyclovir 5 % cream used to treat herpes simplex virus infection. 2009;10:1–10.

          Lv Q, Yu A, Xi Y, Li H, Song Z, Cui J, et al. Development and evaluation of penciclovir-loaded solid lipid nanoparticles for topical delivery. 2009;372:191–8.

          Lopes CM, Silva J, Real Oliveira MECD, Lúcio M. Lipidbased colloidal carriers for topical application of antiviral drugs. In: Design of Nanostructures for Versatile Therapeutic Applications. 2018. p. 565–622.

          Sadurní N, Solans C, Azemar N, García-Celma MJ. Studies on the formation of O/W nano-emulsions, by lowenergy emulsification methods, suitable for pharmaceutical applications. Eur J Pharm Sci. 2005;26(5):438–45.

          Solans C, Izquierdo P, Nolla J, Azemar N. Nanoemulsions. 2005;10:102–10.

          Almeida ME, Teixeira HF, Koester LS. Preparação de Emulsões Submicrométricas : Aspectos Teóricos sobre os Métodos Empregados na Atualidade. 2008;27(5):780–8.

          Pu X, Sun J, Li M, He Z. Formulation of Nanosuspensions as a New Approach for the Delivery of Poorly Soluble Drugs. 2009;(59):417–27.

          Mehnert W, Mäder K. Solid lipid nanoparticles ☆ Production , characterization and applications. Adv Drug Deliv Rev [Internet]. 2012;64:83–101. Available from: http://dx.doi.org/10.1016/j.addr.2012.09.021

          Jensen LB, Petersson K, Nielsen HM. European Journal of Pharmaceutics and Biopharmaceutics In vitro penetration properties of solid lipid nanoparticles in intact and barrier-impaired skin. Eur J Pharm Biopharm [Internet]. 2011;79(1):68–75. Available from: http://dx.doi.org/10.1016/j.ejpb.2011.05.012

          Trimaille T, Chaix C, Delair T, Pichot C, Teixeira H, Dubernet C, et al. Interfacial deposition of functionalized copolymers onto nanoemulsions produced by the solvent displacement method. Colloid Polym Sci. 2001;279(8):784–92.

          Schäfer-korting M, Mehnert W, Korting H. Lipid nanoparticles for improved topical application of drugs for skin diseases ☆. 2007;59:427–43.

          Jardim MRCBGBCHCICSF. Revisão - Validação de métodos cromatográficos e eletroforéticos. Quim Nova. 2004;27(5):771–80.

          Barth AB, Pereira RL, Vargas BA De, Volpato NM. A simple and rapid method to assess butena fi ne hydrochloride in skin samples and a comparative cutaneous retention study of two marketed formulations. 2010;(October).

          Fda CC. Guidance for Industry Q2B Validation of Analytical Procedures : Methodology. 1800;(November 1996).

          Mehnert W, Mader K. Solid lipid nanoparticles Production , characterization and applications. 2001;47:165–96.

          Henning A, Schaefer UF, Neumann D. Potential pitfalls in skin permeation experiments: Influence of experimental factors and subsequent data evaluation. Eur J Pharm Biopharm [Internet]. 2009;72(2):324–31. Available from: http://dx.doi.org/10.1016/j.ejpb.2008.07.016

          Patravale VB, Date AA, Kulkarni RM. Nanosuspensions : a promising drug delivery strategy. 2004;(1992):827–40.

          20. Müller RH, Schmidt S, Buttle I, Akkar A, Schmitt J, Brömer S. SolEmuls® - Novel technology for the formulation of i.v. emulsions with poorly soluble drugs. Int J Pharm. 2004;269(2):293–302.

          Lee CH, Moturi V, Lee Y. Thixotropic property in pharmaceutical formulations. J Control Release [Internet]. 2009;136(2):88–98. Available from: http://dx.doi.org/10.1016/j.jconrel.2009.02.013

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          Published

          16-07-2020 — Updated on 12-03-2026

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          How to Cite

          Meira, A. da S., Battistel, A. P., Teixeira, H. F., & Volpato, N. M. (2026). Development of nanoemulsions containing penciclovir for herpes simplex treatment and a liquid chromatographic method to drug assessment in porcine skin layers. Drug Analytical Research, 4(1), 22–27. https://doi.org/10.22456/2527-2616.103121 (Original work published July 16, 2020)

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          ORIGINAL ARTICLES