A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

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.

Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

“…The ternary phase diagram was built between the chosen components (oil, surfactant, and co-surfactant) of SNEDDS using the aqueous phase titration method for estimation of self-emulsification efficiency [19]. The surfactant and co-surfactant (Poloxamer188, Transcutol HP, Smix) were mixed properly with oil (GML) in different compositions (3:7, 4:6, 5:5, 6:4, 7:3, 8:2, 9:1) in a glass beaker and titrated with mili Q-water with continuous magnetic stirring.…”

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

“…The produced mixtures had a range of hydrophilic-lipophilic balance (HLB) values within the range of 6.55 to 14.22. Although the characterization of SEDDs is mainly conducted using either distilled or deionized water as the dispersing medium [34,[55][56][57]], yet, in this work, the self-emulsification efficiency of various mixtures was evaluated on the bases of the produced droplet size (DS), dispersity (Ð) and transmittance percentage (T%), in three different diluents namely: distilled water (DW), 0.1 mM HCl (pH = 4), and simulated intestinal fluids (SIF) (pH = 6.8) for mimicking the oral route of administration and select the most physically stable formulation(s) [58,59]. All the used diluents were freshly prepared and filtered through a 0.45 µm nylon membrane filter before use.…”

In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility

“…In some cases, increasing the surfactant ratio in the Smix leads to an area increase. This could be due to increased surfactant amount will lower the surface tension, which leads to the formation of a more stable nanoemulsion [30]. However, in some other cases, it is also possible to observe the reverse of this situation.…”