yes / Ibuprofen (IBF) is an outstanding non-steroidal drug for analgesic and anti-inflammatory therapies but
it exhibits poor solubility in water [1, 2]. Increased dosage administration has been linked to gastrointestinal and
cardiovascular complications [3]. Many techniques have been employed to improve the solubility of NSAIDs [4]. In this
study, the anti-solvent precipitation method was used to make Ibuprofen nanoparticles (IBF NPs). Optimised
preparation parameters such as solvent (ethanol), raw drug concentration (400 mg), solvent/anti-solvent ratio (1:50)
and surfactant concentration (0.25 mg/ml) have been studied to yield nanoparticles with a mean size of 58.8 nm,
which is confirmed by dynamic light scattering and transmission electron microscopy. These IBF NPs posess
increased aqueous solubility compared to the micro counterpart and maintain with chemical integrity indicated by high
performance liquid chromatography and Fourier transform infrared spectroscopy.
In addition, in vitro cytotoxicity of IBF NPs has been studied on A549 and HaCat cell lines using MTT and LDH
assays. Both cells were obtained from ATCC. The A549 cells were grown in a modification of Ham’s F-12, containing
L-glutamine, called F-12K. The HaCaT cells were grown in DMEM containing sodium pyruvate (110 mg/l). Normal cell
culture and sub-culture were applied and the cells were used after around 45 passages [5]. The cell culture media
containing 105cells/ml were placed in a 96-well plate with addition of IBF NPs and Micro form at concentrations in the
range of between 6 and 500 ug/ml by diluting them with DMEM and F-12K for use with the HaCaT and A549 cells
respectively. After 24, 48 and 72h exposure, the MTT and LDH cytotoxicity assay were performed in triplicates and on
three separate experiment cultures and the absorbance was recorded at 570 nm and 492nm respectively with Elisa
micro plate reader. The cell viability (%) related to control (cells in culture medium without NPs) was calculated. A very good cytotoxicity profile was observed, indicating an in vitro cytocompatibility of the IBF NPs in these cell culture
systems and no significant changes in cytotoxicity compared with Micro IBF.
We conclude that our IBF NPs have increased solubility, same chemical integrity and unchanged cytotoxicity
compared to IBF Micro drug. Further work will concentrate on optimising more rigorous parameter to produce
excellent quality NPs. More detailed characterisation of IBF NPs is to be tested, such as using PXRD and SEM to
further corroborate particle shape and size. The range of no toxic in vitro concentrations is also to be further
confirmed. Eventually scaled up preparation of IBF NPs will be developed without relinquishing NPs quality. This
would improve the potential for in vitro/ in vivo applications and clinical use of IBF NPs and NSAIDs in general.
| Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/10910 |
| Date | January 2016 |
| Creators | Graham, Stan, Phillip, Roy, Zahid, Myra, Bano, Nadia, Iqbal, Qasim, Mahboob, Fidaa, Chen, Xianfeng, Shang, Lijun |
| Source Sets | Bradford Scholars |
| Language | English |
| Detected Language | English |
| Type | Conference paper, Accepted Manuscript |
| Rights | © 2016 The Authors. Published by the Physiological Society. Reproduced in accordance with the publisher's self-archiving policy. |
| Relation | http://www.physoc.org/proceedings/abstract/Proc%20Physiol%20Soc%2037PCA138 |
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