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Prolonged Release of Anti-Retroviral Efavirenz From System Using ZIF-8 as Carrier

Author(s):

Alinne Élida Gonçalves Alves Tabosa, Aline Silva Ferreira*, Natália Millena da Silva, Débora Dolores Souza da Silva Nascimento, Leslie Raphael de Moura Ferraz, José Yago Rodrigues Silva, Severino Alves Junior, Rosali Maria Ferreira da Silva, Larissa Araújo Rolim and Pedro Jose Rolim-Neto   Pages 1 - 9 ( 9 )

Abstract:


Background: Acquired Immunodeficiency Syndrome (AIDS) is a major public health problem in the world. One of the highly effective drugs in anti-HIV therapy is efavirenz (EFZ), which is classified as Class II according to the Classification System of Biopharmaceuticals, presenting low solubility and high permeability, this being an obstacle related to the drug.

Objective: This study aimed to obtain an innovative system based on EFZ and the Zeolitic Imidazolate Framework (ZIF-8) to use in the development of prolonged-release pharmaceutical forms that can circumvent this problem.

Methods: The EFZ: ZIF-8 system was obtained by a selected ex situ method due to its higher incorporation efficiency. Different characterization techniques corroborated the obtainment of the system, and drug release was analyzed by dissolution testing under sink conditions, the profiles being adjusted to some kinetic models.

Results: At pH 1.2, the structure of ZIF-8 breaks down rapidly, releasing a large amount of drug within a either 3h or short time. In the pH 4.5 and 6.8 medium, the EFZ release from the EFZ: ZIF-8 system obtained in ethanol was prolonged, releasing 95% of the drug in 24h at the pH 4.5 and 75% medium at pH 6.8.

Conclusion: It is evident that a promising pH-sensitive system was obtained using ZIF-8 as a novel carrier of EFZ intended for the alternative treatment of AIDS.

Keywords:

HIV, AIDS, Anti-HIV Agents, Dissolution, Metal-Organic Frameworks, Drug Release.

Affiliation:

Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Laboratory Rare Earths BSTR, Fundamental Departament of Chemistry, Federal University of Pernambuco, Av. Jornalista Aníbal Fernandes, s/n - Cidade Universitária, 50740-560, Recife-PE, Laboratory Rare Earths BSTR, Fundamental Departament of Chemistry, Federal University of Pernambuco, Av. Jornalista Aníbal Fernandes, s/n - Cidade Universitária, 50740-560, Recife-PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE, Central Analytical of Drugs, Medicines and Food, Federal University of Vale do São Francisco, Av. José de Sá Maniçoba, s/n, Centro, 56304-917, Petrolina - PE, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Arthur de Sá, s/n, Cidade Universitária, 50740-521 Recife - PE



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