Abstract
The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.
Highlights
Deferasirox (DFX) is an orally tridentate iron chelator agent that was approved by the United States Food and Drug Administration (FDA) in 2005, and the European Medicines Agency (EMA) in 2006, for chronic iron overload treatment as a result of blood transfusion in patients who are 2 years and older [1].Commercially, DFX is available on the market in three different dosage forms; EXJADE®, as a tablet for oral suspension (125, 250, and 500 mg), JADENU®, as a tablet dosage form (90, 180, and 360 mg), and Jadenu® Sprinkle Granules (90, 180, and 360 mg)
Visual observations showed that both selected self-nanoemulsifying drug delivery systems (SNEDDSs) formulations of DFX (P5-40 and P7-40) formed a clear nanoemulsion in less than one minute and this is referred to be grade A, according to the grading system mentioned in method Section 3.6.4
PharmaceAutsicsalhso20w20n, 1in3, T16a2ble 3, P5-40 and P7-40-coded SNEDDS formulations of DFX were stable at85o0f a2n4 d 100 times dilution at pH 1.2, 4.5, 6.8, and 7.4 and neither precipitation were formed, nor cloudiness or phase separation observed, even for 24 h, which indicates the stability of the reconstituted emAulssisohno.wTnheinreTsaublltes 3c,oPn5fi-r4m0 eadndthPa7t-4th0e-cfoodremduSlaNtiEoDnDs PS5f-o4r0maunldatiPo7n-s40ofwDeFreXrwoberueststtaobdleilautti5o0nawndith
Summary
Deferasirox (DFX) is an orally tridentate iron chelator agent that was approved by the United States Food and Drug Administration (FDA) in 2005, and the European Medicines Agency (EMA) in 2006, for chronic iron overload treatment as a result of blood transfusion in patients who are 2 years and older [1].Commercially, DFX is available on the market in three different dosage forms; EXJADE®, as a tablet for oral suspension (125, 250, and 500 mg), JADENU®, as a tablet dosage form (90, 180, and 360 mg), and Jadenu® Sprinkle Granules (90, 180, and 360 mg). In the case of Exjade®, the commercial preparation of deferasirox, this step is overcome by the formulation of a tablet for oral suspension in which sodium lauryl sulphate is used as a solubilizing agent to improve the dissolution of DFX
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