Flexosomes as a promising nanoplatform for enhancing tolnaftate ocular delivery: Formulation, in vitro characterization, statistical optimization, ex vivo and microbial in vivo studies.

Autor: Aziz D; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Mohamed S; Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Tayel S; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Makhlouf A; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; Department of Pharmaceutics and Industrial Pharmacy, Faculty of pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, Egypt. Electronic address: Amal.Makhlouf@pharma.cu.edu.eg.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2023 Nov 05; Vol. 646, pp. 123471. Date of Electronic Publication: 2023 Oct 02.
DOI: 10.1016/j.ijpharm.2023.123471
Abstrakt: The eye is a complex organ with a unique physiology and anatomy. Using novel nanosystems is expected to enhance ocular drug permeation and retention. Hence, this work aimed to study the potential of flexosomes as an ocular delivery system to enhance the corneal permeation and antifungal activity of Tolnaftate (TOL). Different flexosomes formulae were formulated using ethanol injection method, employing a 3 1 .2 2 full factorial design. The studied formulation variables were: X 1 : amount of stearyl amine, X 2 : hydration volume and X 3 : type of edge activator. Encapsulation efficiency, particle size and zeta potential were selected as dependent variables. FX5 was selected as the optimal TOL flexosomes and showed encapsulation efficiency of 66.08 ± 11.38%, particle size of 154.99 ± 29.11 nm and zeta potential of 42.95 ± 0.64 mV. FX5 was subjected to further ex vivo and in vivo studies which showed that TOL flux was significantly increased through FX5 compared to TOL suspension. Draize test and histopatholoigal tests assured that FX5 is safe to be used for eye.. The in vivo fungal susceptibility testing using Aspergillus niger demonstrated the superior and more durable antifungal activity of FX5 than TOL suspension. Hence, FX5 can be considered as promising nanocarrier for safe and efficient ocular TOL delivery.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE