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Identification and molecular interpretation of the effects of drug incorporation on the self-emulsification process using spectroscopic, micropolarimetric and microscopic measurements

Mercuri, A., Belton, P.S., Royall, P.G., Barker, S.A. (2012) Identification and molecular interpretation of the effects of drug incorporation on the self-emulsification process using spectroscopic, micropolarimetric and microscopic measurements. Molecular Pharmaceutics, 9 (9). pp. 2658-2668. ISSN 1543-8384. (doi:10.1021/mp300219h) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:78847)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL:
https://doi.org/10.1021/mp300219h

Abstract

Addition of a drug to a self-emulsifying drug delivery system (SEDDS) can affect the emulsification process after administration, leading to variation in the emulsion droplet size formed and potentially its clinical behavior (Mercuri et al., Pharm. Res., 2011, 28, 1540-1551). However, the mechanisms involved and, in particular, the location of the drug within the system are poorly understood. Here, we have investigated the location of a model drug, ibuprofen, in the emulsions formed from a simple anhydrous SEDDS (soybean oil, Tween 80 and Span 80), using a range of physical characterization techniques. 1H NMR studies showed an interaction between the drug and the polyoxyethylene chains of the surfactant Tween 80. Micropolarity assessment of the emulsion droplet interfacial region, using the chemical probes pyrene and Reichardts dye, confirmed this interaction, and suggested that the drug was altering the microenvironment around the surfactants, and hence the behavior of the SEDDS with water during emulsification. Both dielectric spectroscopy and polarized light microscopy highlighted the differential behavior with water of placebo and drug-loaded SEDDS, also seen in the initial visual observational studies on the emulsification performance of the SEDDS. 1H NMR studies with three other NSAIDs indicate that this effect is not confined to ibuprofen alone. The study has therefore indicated that the drug's influence on the emulsification process may be related to interactions within the microenvironment of the surfactant layer. Furthermore, such interactions may be usefully identified and characterized using a combination of micropolarity, spectroscopic and microscopic methods.

Item Type: Article
DOI/Identification number: 10.1021/mp300219h
Uncontrolled keywords: dielectric, emulsification, ibuprofen, micropolarity, NMR, SEDDS, flurbiprofen, ibuprofen, indometacin, naproxen, placebo, pyrene, article, drug delivery system, drug distribution, drug formulation, drug solubility, emulsion, microenvironment, molecular interaction, particle size, priority journal, proton nuclear magnetic resonance, Anti-Inflammatory Agents, Non-Steroidal, Chemistry, Pharmaceutical, Drug Delivery Systems, Emulsifying Agents, Emulsions, Hexoses, Ibuprofen, Magnetic Resonance Spectroscopy, Microscopy, Polarization, Particle Size, Polyethylene Glycols, Polysorbates, Pyrenes, Pyridinium Compounds, Soybean Oil, Surface-Active Agents, Water
Divisions: Divisions > Division of Natural Sciences > Medway School of Pharmacy
Depositing User: Susan Barker
Date Deposited: 27 Nov 2019 10:09 UTC
Last Modified: 16 Nov 2021 10:26 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/78847 (The current URI for this page, for reference purposes)

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