Amphotericin B containing microneedle ocular patch for effective treatment of fungal keratitis.

Autor: Roy G; Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Hyderabad 500078, Telangana State, India., Galigama RD; Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Hyderabad 500078, Telangana State, India., Thorat VS; Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Hyderabad 500078, Telangana State, India., Mallela LS; Tej Kohli Cornea Institute, KAR Campus, L. V. Prasad Eye Institute, Hyderabad 500034, Telangana State, India., Roy S; Tej Kohli Cornea Institute, KAR Campus, L. V. Prasad Eye Institute, Hyderabad 500034, Telangana State, India., Garg P; Tej Kohli Cornea Institute, KAR Campus, L. V. Prasad Eye Institute, Hyderabad 500034, Telangana State, India. Electronic address: prashant@lvpei.org., Venuganti VVK; Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Hyderabad 500078, Telangana State, India. Electronic address: vamsi@hyderabad.bits-pilani.ac.in.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2019 Dec 15; Vol. 572, pp. 118808. Date of Electronic Publication: 2019 Oct 31.
DOI: 10.1016/j.ijpharm.2019.118808
Abstrakt: Topical application of poorly water-soluble antibiotics cannot achieve the desired therapeutic concentration within cornea. The purpose of this study was to fabricate, characterize and evaluate in-vivo effectiveness of amphotericin B (AmB) containing microneedle ocular patch (MOP) against fungal keratitis. MOP containing free or liposomal AmB was fabricated using micromolding technique to mimic contact lens. MOPs were prepared using dissolvable polymeric matrix including polyvinyl alcohol and polyvinyl pyrrolidone. AmB loaded MOP were studied for their physical and mechanical properties, drug loading and dissolution rate, corneal insertion and drug permeability. MOP loaded with 100 µg AmB had a compression strength of 35.1 ± 6.7 N and required an insertional force of 1.07 ± 0.17 N in excised human cornea. Ex-vivo corneal permeation studies revealed significant enhancement in AmB corneal retention with the application of MOP compared with free AmB or liposomal AmB application. Furthermore, AmB loaded MOP application significantly (P < 0.05) reduced the Candida albicans load within cornea as evaluated in both ex-vivo model and in-vivo rabbit infection model. Histological examination showed that AmB MOP treatment improved the epithelial and stromal differentiation of corneal membrane. AmB containing MOPs can be developed as minimally invasive corneal delivery device for effective treatment of fungal keratitis.
(Copyright © 2019 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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