title: Multicomponent systems with cyclodextrins and hydrophilic polymers for the delivery of Efavirenz.
abstract: Efavirenz (EFZ) is one of the most used drugs in the treatment of AIDS and is the first antiretroviral choice. However, since it has low solubility, it does not exhibit suitable bioavailability, which interferes with its therapeutic action and is classified as a class II drug according Biopharmaceutical Classification System (low solubility and high permeability). Among several drug delivery systems, the multicomponent systems with cyclodextrins and hydrophilic polymers are a promising alternative for increasing the aqueous solubility of the drug. The present study aimed to develop and characterize in a ternary system of EFZ, MβCD and PVP K30. The results showed that the solid ternary system provided a large increase in the dissolution rate which was greater than 80% and was characterized by DSC, TG, XRD, FT-IR and SEM. The use of the ternary system (EFZ, MβCD and PVP K30 1%) proved to be a viable, effective and safe delivery of the drug. The addition of the hydrophilic polymer appeared to be suitable for the development of a solid oral pharmaceutical product, with possible industrial scale-up and with low concentration of CDs (cyclodextrins).
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Alexandre Couto Carneiro
authors.initials: AC
authors.lastname: Vieira
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Danilo Augusto
authors.initials: DA
authors.lastname: Ferreira Fontes
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Luise Lopes
authors.initials: LL
authors.lastname: Chaves
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Lariza Darlene Santos
authors.initials: LD
authors.lastname: Alves
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: José Lourenço
authors.initials: JL
authors.lastname: de Freitas Neto
authors.affiliation: Núcleo de Controle de Qualidade de Medicamentos e Correlatos - NCQMC da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Monica Felts
authors.initials: MF
authors.lastname: de La Roca Soares
authors.affiliation: Núcleo de Controle de Qualidade de Medicamentos e Correlatos - NCQMC da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil. Electronic address: joselamartine@hotmail.com.
authors.forename: Jose L
authors.initials: JL
authors.lastname: Soares-Sobrinho
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil; Colegiado de Ciências Farmacêuticas da Universidade Federal do Vale do São Francisco (UNIVASF) Campus Petrolina I, Petrolina, PE, Brazil.
authors.forename: Larissa Araújo
authors.initials: LA
authors.lastname: Rolim
authors.affiliation: Laboratório de Tecnologia Farmacêutica da Universidade Federal de Pernambuco, Rua Arthur de Sá, s/n, Cidade Universitária, 50, 740-521 Recife, PE, Brazil.
authors.forename: Pedro José
authors.initials: PJ
authors.lastname: Rolim-Neto
mesh_terms: D000480:Alkynes; D048588:Benzoxazines / Q000008:administration & dosage* / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D003505:Cyclodextrins / Q000737:chemistry*; D003521:Cyclopropanes; D016503:Drug Delivery Systems / Q000379:methods*; D008855:Microscopy, Electron, Scanning; D011145:Polyvinyls / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013818:Thermogravimetry; D014961:X-Ray Diffraction
chemical_list: D000480:Alkynes; D048588:Benzoxazines; D003505:Cyclodextrins; D003521:Cyclopropanes; D011145:Polyvinyls; D011759:Pyrrolidines; C505150:poly(N-vinylpyrrolidine); C098320:efavirenz
keywords: Delivery systems; Inclusion complex; Low solubility; Polymers; Ternary systems