Rheumatoid arthritis (RA) is a chronic inflammatory disease with complex pathology characterized by inflammation of joints, devastation of the synovium, pannus formation, bones and cartilage destruction and often is associated with persistent arthritic pain, swelling, stiffness and work disability. In conventional RA therapy, because of short biological half-life, poor bioavailability, high and frequent dosing is required. Thereby, these anti-RA medications, which unable to selectively target affected zone, may cause severe side effects in extra-articular tissues. Today, nanotechnology has emerged as promising tool in the development of novel drug delivery systems for the treatment and diagnosis of intractable diseases such as RA. Active targeting in RA nanomedicine has also been introduced a successful way for facilitating specific uptake of therapeutic agents by the disease cells. In this review, it is attempted to describe various targeted drug delivery systems (localized and receptor-based) used for RA diagnosis and therapy. Then, we highlight recent developments related to various non-viral gene delivery systems for RA gene therapy.

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Poly(glycerol sebacate) (PGS) is a new biodegradable polymer with good biocompatibility used in many fields of biomedicine and drug delivery. Sunitinib-loaded PGS/gelatine nanoparticles were prepared by the de-solvation method for retinal delivery and treatment of diabetic retinopathy. The nanoparticles were characterised by Fourier-transform infrared and differential scanning calorimetry. The effects of different formulation variables including drug-to-carrier ratio, gelatine-to-PGS ratio, and glycerine-to-sebacate ratio were assessed on the encapsulation efficiency (EE%), particle size, release efficiency (RE), and zeta potential of the nanoparticles. The in vitro cytotoxicity of PGS/gelatine nanoparticles was studied on L929 cells. Draize test on rabbit eyes was also done to investigate the possible allergic reactions caused by the polymer. Glycerine/sebacic acid was the most effective parameter on the EE and RE. Gelatine-to-PGS ratio had the most considerable effect on the particle size while the RE was more affected by the glycerine/sebacic acid ratio. The optimised formulation (S 1 G 0.7 D 21.2) exhibited a particle size of 282 nm, 34.6% EE, zeta potential of −8.9 mV, and RE% of about 27.3% for drug over 228 h. The 3-(4,5dimethylthuazol-2-yl)-2,5-diphenyltetrazolium bromide assay indicated PGS/gelatine nanoparticles were not cytotoxic and sunitinib-loaded nanoparticles were not toxic at concentrations <36 nM.

The purpose of the present study was to compare mesoporous and fumed silica nanoparticles (NPs) to enhance the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RH). Mesoporous silica NPs (MSNs) and fumed silica NPs were used by freeze-drying or spray-drying methods. MSNs were obtained with different ratios of cetyltrimethylammonium bromide. Saturation solubility of the NPs was compared with the pure drug. The optimised formulation was characterised by scanning electron microscopy (SEM), X-ray diffraction (XRD) and differential scanning calorimetry. The pharmacokinetic studies were done by oral administration of a single dose of 15 mg/kg of pure drug or fumed silica NPs of RH in Wistar rats. MSNs enhanced the solubility of RH from 19.88 ± 0.12 to 76.5 μg/ml. Freeze-dried fumed silica increased the solubility of the drug more than MSNs (140.17 ± 0.45 μg/ml). However, the spray-dried fumed silica caused about 26-fold enhancement in its solubility (525.7 ± 93.5 μg/ml). Increasing the ratio of silica NPs enhanced the drug solubility. The results of XRD and SEM analyses displayed RH were in the amorphous state in the NPs. Oral bioavailability of NPs showed 3.5-fold increase compared to the pure drug. The RH loaded fumed silica NPs prepared by spray-drying technique could more enhance the solubility and oral bioavailability of RH.

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