Detalhes bibliográficos
| Ano de defesa: |
2021 |
| Autor(a) principal: |
Meira, Rafaela Zielinski Cavalheiro de
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| Orientador(a): |
Oliveira, Paulo Renato de
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| Banca de defesa: |
Não Informado pela instituição |
| Tipo de documento: |
Tese
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| Tipo de acesso: |
Acesso aberto |
| Idioma: |
por |
| Instituição de defesa: |
Universidade Estadual do Centro-Oeste
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| Programa de Pós-Graduação: |
Programa de Pós-Graduação em Ciências Farmacêuticas (Doutorado)
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| Departamento: |
Unicentro::Departamento de Farmácia
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| País: |
Brasil
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| Palavras-chave em Português: |
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| Palavras-chave em Inglês: |
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| Área do conhecimento CNPq: |
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| Link de acesso: |
http://tede.unicentro.br:8080/jspui/handle/jspui/1764
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Resumo: |
Infections caused by the herpes simplex virus (HSV) are very common, with large medical and epidemiological importance. Among the viral species, HSV-1 has higher seroprevalence, and is typically transmitted during childhood through the orofacial route. Penciclovir is among the most used drugs for the prophylaxis and topical treatment of this infection. The number of drugs for anti-herpetic treatment is still limited, in addition to the increased incidence of viral resistance to existing ones. Innovative drugs require a lot of investment and a lot of time to enter the market, so a new strategy is in the refinement of already known and used assets, either in their molecules or in the face of already commercialized formulations, the explored incremental innovation. Special attention was given to lysine, an important antiviral agent that has been indicated for the prophylaxis and treatment of herpetic lesions, especially orofacial lesions, by oral administration, together with classic drugs. Recent studies idealizing the use of lysine in formulations for this purpose, associated or not with another active, are unknown, a fact that led us to consider the development of a cream that combines penciclovir with lysine as a possible innovative formula. In vitro analyzes of the assets showed synergistic antiviral action between them, with a reduction in the IC50 of the drugs when combined. With this observation, it followed with the pharmacotechnical development of the formulation, based on the study of compatibility between drugs and excipients, as well as on important tests in the evaluation of properties of the final product. The excipients chosen to form part of the formulation were paraffin, sodium lauryl sulfate, ceto-stearyl alcohol, propylene glycol and liquid petroleum jelly. The cream showed pseudoplastic behavior, characteristic of pharmaceutical creams. There was no growth of microorganisms in microbiological analyzes, revealing their quality and safety in the presence of a good preservative system. For the evaluation of the stability and also of the permeation of the drugs using Franz Cell, analytical methodologies by HPLC were developed and validated. The stability of the product was proven with the unchanged drug contents and penciclovir has been shown to permeate equally in formulations with and without the presence of lysine. Animal model experimentation converged with the objectives of the study, since the formulation that combines these two actives showed much faster action than the creams that presented them alone. On the third day of treatment, the group treated with the cream proposed in this study has already matched the negative control group, whereas this result can only be obtained on the seventh day by the group treated with the cream that contained only penciclovir. The idealized and developed formulation: a cream, safe and effective, containing penciclovir and lysine, then becomes an incremental innovation in the treatment of herpetic lesions (patent filing process number: BR 10 2020 014414 6). |
