New solid state forms of antineoplastic 5-fluorouracil with anthelmintic piperazine

Moisescu-Goia, Cristina; Mureşan-Pop, Marieta; Simon, V.

doi:10.1016/j.molstruc.2017.08.076

Cited by 37 publications

(28 citation statements)

References 23 publications

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“…FTIR spectra of the 5-fluorouracil-loaded composite NGs (5FU NZ-PEGDA 700/2000 ) exhibited some of the characteristic bands of PEGDA and of the anticancer drug. The presence of 5-FU in the structure of the obtained nanocomposite was highlighted by the presence of particular bands at 3073 cm −1 (assigned to the stretching vibrations of the =C-H group) [40] and at 1246 cm −1 (assigned to the C-F bond vibrations) [24].…”

Section: Ftir Measurementsmentioning

confidence: 98%

Composite Nanogels Based on Zeolite-Poly(ethylene glycol) Diacrylate for Controlled Drug Delivery

et al. 2020

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This study presents the design of novel composites nanogels, based on poly(ethylene glycol) diacrylate and natural zeolite particles, that are able to act as materials with controlled drug delivery properties. Natural zeolite–nanogels composite, with varying zeolite contents, were obtained by an inverse mini-emulsion technique and loaded with 5-fluorouracil, a widely used chemotherapeutic drug. Herein, the possibility of adjusting final properties by means of modifying the preparation conditions was investigated. The prepared composite nanogels are characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and thermogravimetric analysis (TGA). In light of this tunable drug-loading capability, swelling behaviour, and cytotoxicity, these composite nanogels could be highly attractive as drug reservoirs.

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Section: Ftir Measurementsmentioning

confidence: 98%

Composite Nanogels Based on Zeolite-Poly(ethylene glycol) Diacrylate for Controlled Drug Delivery

et al. 2020

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“…6a. The X-ray powder diffraction (XRD) spectrum of 5-FU shows the characteristic diffraction peak of the crystalline drug at 28.26° (40). The halo pattern in the diffractogram of chitosan (13°, 19.8°) (41) is indicative of its semi-crystalline nature (42), while the absence of diffraction peaks in the pattern of sodium alginate is indicative of its amorphous nature.…”

Section: X-ray Powder Diffractionmentioning

confidence: 99%

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

et al. 2018

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Three-dimensional printing is being steadily deployed as manufacturing technology for the development of personalized pharmaceutical dosage forms. In the present study, we developed a hollow pH-responsive 3D printed tablet encapsulating drug loaded non-coated and chitosan-coated alginate beads for the targeted colonic delivery of 5-fluorouracil (5-FU). A mixture of Eudragit® L100-55 and Eudragit® S100 was fabricated by means of hot-melt extrusion (HME) and the produced filaments were printed utilizing a fused deposition modeling (FDM) 3D printer to form the pH-responsive layer of the tablet with the rest comprising of a water-insoluble poly-lactic acid (PLA) layer. The filaments and alginate particles were characterized for their physicochemical properties (thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction), their surface topography was visualized by scanning electron microscopy and the filaments' mechanical properties were assessed by instrumented indentation testing and tensile testing. The optimized filament formulation was 3D printed and the structural integrity of the hollow tablet in increasing pH media (pH 1.2 to pH 7.4) was assessed by means of time-lapsed microfocus computed tomography (μCT). In vitro release studies demonstrated controlled release of 5-FU from the alginate beads encapsulated within the hollow pH-sensitive tablet matrix at pH values corresponding to the colonic environment (pH 7.4). The present study highlights the potential of additive manufacturing in fabricating controlled-release dosage forms rendering them pertinent formulations for further in vivo evaluation.

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“…Co-crystals of structurally-related carboxylic acids with 5FU prepared using LAG in a MBM in the presence of water exhibited enhanced membrane permeability compared with the pure API [ 85 ]. The preparation of co-crystals of 5FU with other API’s (imatinib [ 86 ] and piperazine [ 87 ]) using LAG has also been reported.…”

Section: Reviewmentioning

confidence: 99%

Mechanochemistry of nucleosides, nucleotides and related materials

Eguaogie¹,

Vyle²,

Conlon³

et al. 2018

Beilstein J. Org. Chem.

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The application of mechanical force to induce the formation and cleavage of covalent bonds is a rapidly developing field within organic chemistry which has particular value in reducing or eliminating solvent usage, enhancing reaction rates and also in enabling the preparation of products which are otherwise inaccessible under solution-phase conditions. Mechanochemistry has also found recent attention in materials chemistry and API formulation during which rearrangement of non-covalent interactions give rise to functional products. However, this has been known to nucleic acids science almost since its inception in the late nineteenth century when Miescher exploited grinding to facilitate disaggregation of DNA from tightly bound proteins through selective denaturation of the latter. Despite the wide application of ball milling to amino acid chemistry, there have been limited reports of mechanochemical transformations involving nucleoside or nucleotide substrates on preparative scales. A survey of these reactions is provided, the majority of which have used a mixer ball mill and display an almost universal requirement for liquid to be present within the grinding vessel. Mechanochemistry of charged nucleotide substrates, in particular, provides considerable benefits both in terms of efficiency (reducing total processing times from weeks to hours) and by minimising exposure to aqueous conditions, access to previously elusive materials. In the absence of large quantities of solvent and heating, side-reactions can be reduced or eliminated. The central contribution of mechanochemistry (and specifically, ball milling) to the isolation of biologically active materials derived from nuclei by grinding will also be outlined. Finally non-covalent associative processes involving nucleic acids and related materials using mechanochemistry will be described: specifically, solid solutions, cocrystals, polymorph transitions, carbon nanotube dissolution and inclusion complex formation.

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New solid state forms of antineoplastic 5-fluorouracil with anthelmintic piperazine

Cited by 37 publications

References 23 publications

Composite Nanogels Based on Zeolite-Poly(ethylene glycol) Diacrylate for Controlled Drug Delivery

Composite Nanogels Based on Zeolite-Poly(ethylene glycol) Diacrylate for Controlled Drug Delivery

Controlled Release of 5-Fluorouracil from Alginate Beads Encapsulated in 3D Printed pH-Responsive Solid Dosage Forms

Mechanochemistry of nucleosides, nucleotides and related materials

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