AB0393 IMPROVING DRUG SOLUBILITY FOR INFLAMMATORY ARTHRITIS TREATMENT: SULFASALAZINE NIOSOME

Abstract

Background Newly, many studies have been assumed upon vesicular drug delivery systems like niosomes to make an effective formulation of drugs in soluble state that can lead to enhance bioavailability as well as to provide controlled drug release [1]. Niosomes due to their capability and efficient mechanism have been proposed to explain the ability of those as potential nanocarriers for poorly soluble drugs [2]. Objectives In this study, niosomes have emerged as a drug delivery system to load sulfasalazine (SSZ) that is used to treat rheumatoid arthritis. Methods Niosomes were prepared by amphiphilic self-assembly of tween 80 and squalene through thin film hydration method. The optimal hydration condition that maximizes noisome yield was hydration duration of 24 hours at 30-35 °C. The encapsulation of sulfasalazine drug into niosome was characterized by Fourier transform infrared spectroscopy (FT-IR), UV-visible, Zeta potential, particle size, field emission scanning electron microscopy (FE-SEM), and transmission electron microscopy (TEM) to evaluate size, charge, morphology and functional properties. Results By using this method, the percentage of loaded drug, resulted by the encapsulation of micellar/niosomes was found to be 99 ± 0.2% for 5% of SSZ weight in total ingredients weight of micellar/niosomal vesicles (w/w). The drug-entrapped sulfasalazine niosomes (SSZN) nanoformulations indicated controlled release of drugs in phosphate buffer saline (PBS) at pH 7.2 making these nanoformulations ideal for colon-targeted drug delivery. It was also seen that a slower rate of the SSZ releasing of the drug encapsulated noisome was, in the range of 2-24 hours at PH 4.5-7.2. TEM examinations also confirmed the formation of 15-25 nm thick walls for the prepared SSZN particles. MTT assay revealed that the blank noisomes exhibited excellent biocompatibility. The in vitro drug loading and release behavior studier indicated the as prepared nano-noisome presented ultrahigh performance as drug carrier. Cell toxicity assay was carried out by HeLa cell line and A549 cell line demonstrated the half maximal inhibitory concentration (IC50) of SSZ to 162 µM and 173 µM, respectively. Conclusion Niosomal formulation are introduced as a novel nano drug carriers to design effective drug delivery systems. They offer a great opportunity for loading hydrophilic, lipophilic drugs, or both drugs together. Niosomal formulation has been evaluated as a safe drug delivery system. In this study, we showed that SSZN has more stability and more efficiently affect the cancer cells. It seems that SSZN is a great candidate for future in vitro and in vivo researches for evaluating potential clinical applications.