Effect of piroxicam on lipid membranes : Drug encapsulation and gastric toxicity aspects

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http://hdl.handle.net/10138/311787

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Wilkosz , N , Rissanen , S , Cyza , M , Szybka , R , Nowakowska , M , Bunker , A , Rog , T & Kepczynski , M 2017 , ' Effect of piroxicam on lipid membranes : Drug encapsulation and gastric toxicity aspects ' , European Journal of Pharmaceutical Sciences , vol. 100 , pp. 116-125 . https://doi.org/10.1016/j.ejps.2017.01.007

Title: Effect of piroxicam on lipid membranes : Drug encapsulation and gastric toxicity aspects
Author: Wilkosz, Natalia; Rissanen, Sami; Cyza, Malgorzata; Szybka, Renata; Nowakowska, Maria; Bunker, Alex; Rog, Tomasz; Kepczynski, Mariusz
Contributor organization: Faculty of Pharmacy
Division of Pharmaceutical Biosciences
Pharmaceutical biophysics group
Department of Physics
Drug Research Program
Date: 2017-03-30
Language: eng
Number of pages: 10
Belongs to series: European Journal of Pharmaceutical Sciences
ISSN: 0928-0987
DOI: https://doi.org/10.1016/j.ejps.2017.01.007
URI: http://hdl.handle.net/10138/311787
Abstract: Uptake of piroxicam, a non-steroidal anti-inflammatory drug, from the intestines after oral intake is limited due to its low solubility and its wide use is associated with several side effects related to the gastrointestinal tract. In this study, all-atom molecular dynamics (MD) simulations and fluorescent spectroscopy were employed to investigate the interaction of piroxicam in neutral, zwitterionic, and cationic forms with lipid bilayers composed of phosphatidylcholine, cholesterol, and PEGylated lipids. Our study was aimed to assess the potential for encapsulation of piroxicam in liposomal carriers and to shed more light on the process of gastrointestinal tract injury by the drug. Through both the MD simulations and laser scanning confocal microscopy, we have demonstrated that all forms of piroxicam can associate with the lipid bilayers and locate close to the water-membrane interface. Conventional liposomes used in drug delivery are usually stabilized by the addition of cholesterol and have their bloodstream lifetime extended through the inclusion of PEGylated lipids in the formulation to create a protective polymer corona. For this reason, we tested the effect of these two modifications on the behavior of piroxicam in the membrane. When the bilayer was PEGylated, piroxicam localize to the PEG layer and within the lipid headgroup region. This suggests that PEGylated liposomes are capable of carrying a larger quantity of piroxicam than the conventional ones. (C) 2017 Elsevier B.V. All rights reserved.
Subject: Piroxicam
NSAIDs
Lipid bilayer
PEGylated liposomes
Gastric toxicity
MD simulations
NONSTEROIDAL ANTIINFLAMMATORY DRUGS
ATOM FORCE-FIELD
LIPOSOMES
DYNAMICS
CONSTANTS
NSAIDS
FORMULATION
PORPHYRINS
SIMULATION
DELIVERY
317 Pharmacy
Peer reviewed: Yes
Rights: cc_by_nc_nd
Usage restriction: openAccess
Self-archived version: acceptedVersion


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