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Mitotane liposomes for potential treatment of adrenal cortical carcinoma: ex vivo intestinal permeation and in vivo bioavailability.
Zancanella, Patricia; Oliveira, Daniele M L; de Oliveira, Bonald H; Woiski, Thiago D; Pinto, Cesar C; Santana, Maria H A; Souto, Eliana B; Severino, Patrícia.
Afiliação
  • Zancanella P; Department of Chemical, Federal University of Paraná, Curitiba, Paraná, Brazil.
  • Oliveira DML; Biotechnology Industrial Program, Laboratory of Nanotechnology and Nanomedicine (LNMed), University of Tiradentes, Aracaju, Sergipe, Brazil.
  • de Oliveira BH; Department of Chemical, Federal University of Paraná, Curitiba, Paraná, Brazil.
  • Woiski TD; Research Institute "Pelé Pequeno Príncipe", Curitiba, Paraná, Brazil.
  • Pinto CC; Institute of Technology and Research (ITP), Aracaju, Sergipe, Brazil.
  • Santana MHA; School of Chemical Engineering, University of Campinas, Campinas, São Paulo, Brazil.
  • Souto EB; Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, Coimbra, Portugal.
  • Severino P; CEB - Centre of Biological Engineering, University of Minho, Braga, Portugal.
Pharm Dev Technol ; 25(8): 949-961, 2020 Oct.
Article em En | MEDLINE | ID: mdl-32343624
The adrenal cortical carcinoma (ACC) treatment, for which mitotane (o,p'-DDD) is the drug of choice, still remains a challenge both because of the well-known solubility problems of the drug, and its serious side effects. Mitotane is currently administered as oral tablets. The loading of mitotane into nanocarriers has been suggested as a way to circumvent the low solubility of the drug and its limited oral bioavailability. In this work, we have developed liposomes containing mitotane to enhance its intestinal absorption and oral bioavailability. Liposomes were produced by spray-drying of a mixture of phospholipids and the developed formulation was optimized by studying the degree of crystallinity, spray-drying conditions, phospholipid/mitotane ratio, and influence of mannitol in the hydrating ethanolic solution. An optimal liposomal formulation was produced with a phospholipid:mitotane combination (3.34:1), exhibiting a mean hydrodynamic diameter around 1 µm and spherical shape. The produced mitotane liposomes were re-suspended by hydrating the spray-dried powders in a stirred tank, and tested their intestinal permeability (ex vivo) and relative bioavailability (in vivo), against a free drug solution (with or without Trigliceril®CM). Our results support the conclusion that the loading of mitotane in liposomes enhanced its intestinal absorption and relative bioavailability.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias do Córtex Suprarrenal / Carcinoma Adrenocortical / Lipossomos / Mitotano Limite: Animals Idioma: En Revista: Pharm Dev Technol Assunto da revista: FARMACIA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias do Córtex Suprarrenal / Carcinoma Adrenocortical / Lipossomos / Mitotano Limite: Animals Idioma: En Revista: Pharm Dev Technol Assunto da revista: FARMACIA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido