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Iontophoresis enhances voriconazole antifungal potency and corneal penetration.
Gelfuso, Guilherme M; Ferreira-Nunes, Ricardo; Dalmolin, Luciana F; Dos S Ré, Ana C; Dos Santos, Giselly A; de Sá, Fernando A P; Cunha-Filho, Marcilio; Alonso, Antonio; Neto, Sebastião A Mendanha; Anjos, Jorge L V; Aires, Carolina P; Lopez, Renata F V; Gratieri, Taís.
Afiliação
  • Gelfuso GM; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil.
  • Ferreira-Nunes R; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil.
  • Dalmolin LF; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-903 Ribeirão Preto, SP, Brazil.
  • Dos S Ré AC; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-903 Ribeirão Preto, SP, Brazil.
  • Dos Santos GA; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil.
  • de Sá FAP; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil.
  • Cunha-Filho M; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil.
  • Alonso A; Institute of Physics - Catalão Reginal, Federal University of Goiás (UFG), 75704-020 Catalão, GO, Brazil.
  • Neto SAM; Institute of Physics, Federal University of Goiás (UFG), 74690-900 Goiânia, GO, Brazil.
  • Anjos JLV; Institute of Physics, Federal University of Goiás (UFG), 74690-900 Goiânia, GO, Brazil.
  • Aires CP; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-903 Ribeirão Preto, SP, Brazil.
  • Lopez RFV; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-903 Ribeirão Preto, SP, Brazil.
  • Gratieri T; Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia, 70910-900 Brasília, DF, Brazil. Electronic address: tgratieri@gmail.com.
Int J Pharm ; 576: 118991, 2020 Feb 25.
Article em En | MEDLINE | ID: mdl-31884059
Strategies to enhance corneal penetration of voriconazole (VOR) could improve the treatment of fungal keratitis. Here, we evaluated the use of iontophoresis for ocular VOR delivery from either: (i) a cyclodextrin inclusion complex (CD VOR), (ii) a liposome (LP VOR), and (iii) a chitosan-coated liposome (LP VOR CS). LP VOR CS presented mean diameter of 139.2 ±â€¯1.3 nm and zeta potential equal to + 3.3 ±â€¯1.5 mV compared to 134.6 ±â€¯1.7 and -8.2 ±â€¯3.0 mV of LP VOR, which, together with mucin mucoadhesion study, confirmed chitosan-coating. Both drug and liposomal formulations were stable under the influence of an applied electric current. Interestingly, in vitro studies in Candida glabrata culture indicated a decrease in VOR MIC values following iontophoresis (from 0.28 to 0.14 µg/mL). Iontophoresis enhanced drug penetration into the cornea. After 10 min of a 2 mA/cm2 applied current, corneal retained amounts were 45.4 ±â€¯11.2, 30.4 ±â€¯2.1 and 30.6 ±â€¯2.9 µg/cm2 for, respectively, CD VOR, LP VOR, and LP VOR CS. In conclusion, iontophoresis increases drug potency and enhances drug penetration into the cornea, showing potential to be used as "an emergency burst delivery approach".
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Iontoforese / Córnea / Candida glabrata / Voriconazol / Antifúngicos Limite: Animals Idioma: En Revista: Int J Pharm Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Iontoforese / Córnea / Candida glabrata / Voriconazol / Antifúngicos Limite: Animals Idioma: En Revista: Int J Pharm Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda