Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 576, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2019.118991
Keywords
Candida glabrata; Fungal keratitis; Liposome; Ocular iontophoresis
Categories
Funding
- CNPq
- FAPDF
- CAPES
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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 +/- 1.3 nm and zeta potential equal to + 3.3 +/- 1.5 mV compared to 134.6 +/- 1.7 and - 8.2 +/- 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 mu g/mL). Iontophoresis enhanced drug penetration into the cornea. After 10 min of a 2 mA/cm(2) applied current, corneal retained amounts were 45.4 +/- 11.2, 30.4 +/- 2.1 and 30.6 +/- 2.9 mu g/cm(2) 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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