FRI0139 IMPROVEMENT SOLUBILITY OF AMPHIPHILIC NAPROXEN-NIOSOME FOR INFLAMMATORY ARTHRITIS TREATMENT
Authors: hanzaleh balakheyli, Nafiseh Abdolahi, Alireza Soltani, Vahid Erfani-Moghadam, Sahar Moazen Rad
Journal: Annals of the Rheumatic Diseases (2019)

<h3>Background:</h3> Naproxen (S-6-methoxy-a-methyl-2-naphthaleneacetic acid) is a nonsteroidal anti-inflammatory drug (NSAID), which is used to treat rheumatoid arthritis, osteoarthritis, chronic juvenile arthritis, ankylosing spondylitis. Niosomes or nonionic surfactant vesicles (NSV's) are known as biocompatible, non-immunogenic systems and present potential applications in the delivery of hydrophilic and hydrophobic drugs in order to higher chemical stability and less production cost characteristics. Niosomes are now broadly investigated as other drug vehicles to the encapsulation and controlled release of the different drug molecules. Many studies showed micronized NSAIDs, at low dosages using nanotechnology, can increase the drug level and increase absorption and can have the best effect at the lowest dose and reduce the risk of side effects. Because insufficiently soluble and insoluble drugs exhibit low absorption and poor bioavailability, improvements in solubility and solubility are important for developing various drug preparation methods. <h3>Objectives:</h3> The purpose of the present study was to investigate the formulations of micellar/niosomal vesicles prepared from the biocompatible surfactant tween 80 (polysorbate 80) and the squalene as an excipient, through film hydration method and their potential as a drug delivery system for NPX. <h3>Methods:</h3> We prepared niosomal Naproxen from the biocompatible surfactant tween 80 (polysorbate 80) and the squalene as an excipient, through thin-film hydration method and their potential as a drug delivery system for NPX. The prepared system was characterized for by Fourier transform infrared spectroscopy (FT-IR), UV-visible, photoluminescence (PL), field emission scanning electron microscopy (FE-SEM), and transmission electron microscopy (TEM). <h3>Results:</h3> By using this method, the percent drug loading that resulted by the encapsulation of niosomes was found to be 99.5 ± 0.2% for 5% of NPX weight in total ingredients weight of niosomal vesicles (w/w). It was also seen that a slower rate of release of the NPX from the drug encapsulated noisome over 7 days, suggesting stable complexation of NPX. Cell toxicity assay was carried out by A549 and HeLa cancer cell lines and showed the half maximal inhibitory concentration (IC<sub>50</sub>) of NPX increased about 8.25 folds for A549 (from 3300 μM to 400 μM) and it decreases about 5.5 folds for HeLa (from 1920 μM to 350 μM by nanoformulation. <h3>Conclusion:</h3> Niosomal formulation has been evaluated as a safe drug delivery system. In this study, we showed that niosomal naproxen has more stability and more efficiently affect the cells. It can be explained by increasing the bioavailability of naproxen by niosomal nanocarriers which probably is based on more water solubility and more efficient cell entrance of drug. It seems that niosomal naproxen is a great candidate for future in vitro and in vivo researches for evaluating potential clinical applications. <h3>References:</h3> [1] M.R. Rodrigues, C.M. Lanzarini, E. Ricci-Junior, Preparation, in vitro characterization and in vivo release of naproxen loaded in poly-caprolactone nanoparticles, Pharm. Dev. Technol. 16 (2009) 12-21. [2] K.D. Tripathi, Essentials of Medical Pharmacology. Jaypee Brothers Medical Publishers Pvt. Ltd., New Delhi, 5, (2004) 176. [3] M. Seleci, D. Ag Seleci, R. Joncyzk, F. Stahl, C. Blume, T. Scheper, Smart multifunctional nanoparticles in nanomedicine, Bio NanoMaterials, 17 (2016) 33-41. [4] J. Du, D. Li, J. Lu, Chemiluminescence determination of naproxen based on europium(III)-sensitized KIO4–H2O2 reaction, Luminescence 25 (2010) 76-80. [5] A.H. Alomrani, M.H. Al-Agamy, M.M. Badran, In vitro skin penetration and antimycotic activity of itraconazole loaded niosomes: Various non-ionic surfactants, Journal of Drug Delivery Science and Technology 28 (2015) 8-15. <h3>Disclosure of Interests:</h3> None declared