Herpes Labialis: A New Possibility for Topical Treatment with Well-Elucidated Drugs

• Published in: Journal of pharmaceutical sciences 2021-10, Vol.110 (10), p.3450-3456
• Main Authors: Silva-Alvarez, Amanda F., de Carvalho, Ana Clara Wada, Benassi-Zanqueta, Érica, Oliveira, Thalita Z., Fonseca, Dyenefer P., Ferreira, Maíra P., Vicentini, Fabiana T.M.C., Ueda-Nakamura, Tania, Pedrazzi, Vinicius, de Freitas, Osvaldo
• Format: Article
• Language: English
• Subjects: Epithelial (drug) delivery; HSV; Local anesthetics; Semi-solid
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2021.06.029

Mucocutaneous infections caused by Herpes simplex virus (HSV-1 and HSV-2) are characterized by the appearance of vesicles that cause pain and embarrassment to the carrier. The standard treatment is based on the use of antivirals in gels or ointments, however, relapses are common. Local anesthetics decrease the pain caused by the lesion, in addition to showing antiviral properties. Semi-solid form facilitates application and its transformation into a thin film favors the maintenance of the formulation in place, with a more discreet final aspect. The objective of this study was to develop and evaluate formulations containing anesthetics for the treatment of cold sores. For this purpose, two semi-solid film-forming formulations were developed and evaluated, containing HPMC K100, lidocaine (LIDO) and prilocaine (PRILO) combined with adjuvants, in the presence (F1T) or not (F1) of the absorption promoter Transcutol®. The mixture of PRILO and LIDO resulted in the formation of a eutectic mixture (EM), essential for penetration of drugs into the skin. The quantification of drugs was performed by HPLC (High Performance Liquid Chromatography), and Transcutol® did not influence the release of drugs from the formulation. The bioadhesiveness of the formulation was evaluate and the drugs did not impair the adhesive potential of the polymers used. The formulations were evaluated in vivo for skin irritation and did not show any negative sign on macroscopic examination. The in vivo efficacy test proved the anesthetics' ability to decrease the lesions caused by HSV-1. Thus, the proposed formulations proved to be good alternatives to the treatment of oral lesions caused by HSV-1.