title: Evaluation of Microemulsion and Lamellar Liquid Crystalline Systems for Transdermal Zidovudine Delivery.
abstract: This study proposed to investigate and to compare colloidal carrier systems containing Zidovudine (3'-azido-3'-deoxythymidine) (AZT) for transdermal administration and optimization of antiretroviral therapy. Microemulsion (ME) and lamellar phase (LP) liquid crystal were obtained and selected from pseudoternary diagrams previously developed. Small-angle X-ray scattering and rheology analysis confirmed the presence of typical ME and liquid crystalline structures with lamellar arrangement, respectively. Both colloidal carrier systems, ME, and LP remained stable, homogeneous, and isotropic after AZT addition. In vitro permeation study (using pig ear skin) showed that the amount of permeated drug was higher for ME compared to the control and LP, obtaining a permeation enhancing effect on the order of approximately 2-fold (p < 0.05). Microscopic examination after in vivo skin irritation studies using mice suggested few histological changes in the skin of animals treated with the ME compared to the control group (hydrogel). Thus, ME proved to be adequate and have promising effects, being able to promote the drug permeation without causing apparent skin irritation. On the order hand, LP functioned as a drug reservoir reducing AZT partitioning into the skin.
authors.affiliation: Núcleo de Desenvolvimento Farmacêutico e Cosmético, Departamento de Ciências Farmacêuticas, UFPE, Recife, Pernambuco 50739-520, Brazil.
authors.forename: André Luis Menezes
authors.initials: AL
authors.lastname: Carvalho
authors.affiliation: Departamento de Farmácia, UEPB, Campina Grande, Paraíba 58100-001, Brazil.
authors.forename: José Alexsandro da
authors.initials: JA
authors.lastname: Silva
authors.affiliation: Departamento de Farmácia, UFS, São Cristóvão, Sergipe 49100-000, Brazil. Electronic address: ana_lira2@hotmail.com.
authors.forename: Ana Amélia Moreira
authors.initials: AA
authors.lastname: Lira
authors.affiliation: Departamento de Farmácia, UFS, São Cristóvão, Sergipe 49100-000, Brazil.
authors.forename: Tamara Matos Freire
authors.initials: TM
authors.lastname: Conceição
authors.affiliation: Departamento de Farmácia, UFS, São Cristóvão, Sergipe 49100-000, Brazil.
authors.forename: Rogéria de Souza
authors.initials: Rde S
authors.lastname: Nunes
authors.affiliation: Laboratório de Morfologia e Biologia Estrutural, Instituto de Tecnologia e Pesquisa, UNIT, Aracaju, Sergipe 49032-490, Brazil.
authors.forename: Ricardo Luiz Cavalcanti
authors.initials: RL
authors.lastname: de Albuquerque Junior
authors.affiliation: Departamento de Química, UFS, Campus Alberto Carvalho, Itabaiana, Sergipe 49500-000, Brazil.
authors.forename: Victor Hugo Vitorino
authors.initials: VH
authors.lastname: Sarmento
authors.affiliation: Núcleo de Desenvolvimento Farmacêutico e Cosmético, Departamento de Ciências Farmacêuticas, UFPE, Recife, Pernambuco 50739-520, Brazil.
authors.forename: Leila Bastos
authors.initials: LB
authors.lastname: Leal
authors.affiliation: Núcleo de Desenvolvimento Farmacêutico e Cosmético, Departamento de Ciências Farmacêuticas, UFPE, Recife, Pernambuco 50739-520, Brazil.
authors.forename: Davi Pereira
authors.initials: DP
authors.lastname: de Santana
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D004655:Emulsions; D005260:Female; D020100:Hydrogels; D007509:Irritants; D050866:Liquid Crystals; D051379:Mice; D036103:Nanotechnology; D012542:Scattering, Radiation; D012869:Skin Absorption; D013552:Swine; D014965:X-Rays; D015215:Zidovudine / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics
chemical_list: D019380:Anti-HIV Agents; D004655:Emulsions; D020100:Hydrogels; D007509:Irritants; D015215:Zidovudine
keywords: antiretroviral; lamellar liquid crystal; microemulsion; transdermal; zidovudine