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Physicochemical and Stability Evaluation of Topical Niosomal Encapsulating Fosinopril/γ-Cyclodextrin Complex for Ocular Delivery

Physicochemical and Stability Evaluation of Topical Niosomal Encapsulating Fosinopril/γ-Cyclodextrin Complex for Ocular Delivery


Title: Physicochemical and Stability Evaluation of Topical Niosomal Encapsulating Fosinopril/γ-Cyclodextrin Complex for Ocular Delivery
Author: Hnin, Hay Marn
Stefánsson, Einar
Loftsson, Thorsteinn   orcid.org/0000-0002-9439-1553
Asasutjarit, Rathapon
Charnvanich, Dusadee
Jansook, Phatsawee
Date: 2022-06
Language: English
Scope:
University/Institute: Landspitali - The National University Hospital of Iceland
Department: Other departments
Faculty of Medicine
Series: Pharmaceutics; 14(6)
ISSN: 1999-4923
DOI: https://doi.org/10.3390/pharmaceutics14061147
Subject: Augnlæknisfræði; cyclodextrin; encapsulation; fosinopril sodium; niosomes; ophthalmic; stabilization; Pharmaceutical Science
URI: https://hdl.handle.net/20.500.11815/3475

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Citation:

Hnin , H M , Stefánsson , E , Loftsson , T , Asasutjarit , R , Charnvanich , D & Jansook , P 2022 , ' Physicochemical and Stability Evaluation of Topical Niosomal Encapsulating Fosinopril/γ-Cyclodextrin Complex for Ocular Delivery ' , Pharmaceutics , vol. 14 , no. 6 , 1147 . https://doi.org/10.3390/pharmaceutics14061147

Abstract:

This study aimed to develop a chemically stable niosomal eye drop containing fosinopril (FOS) for lowering intraocular pressure. The effects of cyclodextrin (CD), surfactant types and membrane stabilizer/charged inducers on physiochemical and chemical properties of niosome were evaluated. The pH value, average particle size, size distribution and zeta potentials were within the acceptable range. All niosomal formulations were shown to be slightly hypertonic with low viscosity. Span® 60/dicetyl phosphate niosomes in the presence and absence of γCD were selected as the optimum formulations according to their high %entrapment efficiency and negative zeta potential values as well as controlled release profile. According to ex vivo permeation study, the obtained lowest flux and apparent permeability coefficient values confirmed that FOS/γCD complex was encapsulated within the inner aqueous core of niosome and could be able to protect FOS from its hydrolytic degradation. The in vitro cytotoxicity revealed that niosome entrapped FOS or FOS/γCD formulations were moderate irritation to the eyes. Furthermore, FOS-loaded niosomal preparations exhibited good physical and chemical stabilities especially of those in the presence of γCD, for at least three months under the storage condition of 2–8 °C.

Description:

Funding Information: Funding: This work was financially supported by the European Union’s Eurostar Program under project No. PREVIN E11008 and by The Second Century Fund (C2F), Chulalongkorn University. Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.

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