Novel strategies for the formulation and processing of poorly water-soluble drugs.

Encapsulation of NSAIDs for inflammation management: Overview, progress, challenges and prospects

Two novel nanomicellar formulations were developed to improve the poor aqueous solubility and the oral absorption of silymarin. Polymeric nanomicelles made of Soluplus and mixed nanomicelles combining Soluplus with d-α-tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS) were prepared using the thin film method. Physicochemical parameters were investigated, in particular the average diameter, the homogeneity (expressed as polydispersity index), the zeta potential, the morphology, the encapsulation efficiency, the drug loading, the critical micellar concentration and the cloud point. The sizes of ~60 nm, the narrow size distribution (polydispersity index ≤0.1) and the encapsulation efficiency >92% indicated the high affinity between silymarin and the core of the nanomicelles. Solubility studies demonstrated that the solubility of silymarin increased by ~6-fold when loaded into nanomicelles. Furthermore, the physical and chemical parameters of SLM-loaded formulations stored at room temperature and in refrigerated conditions (4 °C) were monitored over three months. In vitro stability and release studies in media miming the physiological conditions were also performed. In addition, both formulations did not alter the antioxidant properties of silymarin as evidenced by the 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) assay. The potential of the nanomicelles to increase the intestinal absorption of silymarin was firstly investigated by the parallel artificial membrane permeability assay. Subsequently, transport studies employing Caco-2 cell line demonstrated that mixed nanomicelles statistically enhanced the permeability of silymarin compared to polymeric nanomicelles and unformulated extract. Finally, the uptake studies indicated that both nanomicellar formulations entered into Caco-2 cells via energy-dependent mechanisms.

https://www.mdpi.com/1420-3049/24/9/1688/pdf

Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin.

In vitro screening of nanomedicines through the blood brain barrier: A critical review.

Drug-loaded core–sheath fibers were successfully prepared from a combination of poly(methyl methacrylate) (PMMA) and polycaprolactone (PCL) using a coaxial electrospinning system and Nimesulide as an anti-inflammatory drug model. An electric field potential of 7–8 kV was found optimal for the formation of the fibers, which were characterized using scanning and transmission electron microscopy techniques combined with attenuated total reflectance infrared spectroscopy and contact angle measurements. Results confirmed the core–sheath morphology and indicated that these fibers are larger in diameter than normal ones (prepared as controls from either PCL or PMMA, under similar conditions). The prepared core–sheath fibers were also investigated by differential scanning calorimetry and thermogravimetric analysis, and results indicated that Nimesulide is completely solubilized in the polymer matrix and that its presence improved the thermal stability of the core–sheath fibers compared to that of normal PMMA fibers. Moreover, PMMA-PCL core–sheath fibers showed an improvement in terms of mechanical properties (such as elongation at break) in comparison with pure PMMA fibers. Drug release studies demonstrated that the delivery of Nimesulide can be modulated by appropriately selecting the loading area, with faster release observed when the drug was located in the sheath. Results suggest altogether the significant potential of PMMA-PCL core–sheath fibers for applications involving delivery of hydrophobic anti-inflammatory drugs such as Nimesulide.

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Papers

Nimesulide-loaded nanoparticles for the potential coadjuvant treatment of prostate cancer.