A series of biocompatible and stimuli-sensitive poly(N-isopropylacrylamide-co-propyl acrylic acid) (P(NIPAAm-co-PAAc)) nanogels were synthesized by emulsion polymerization. In addition, polyethyleneimine (PEI) was further grafted to modify the PNIPAAm-based nanogels. The P(NIPAAm-co-PAAc)-g-PEI nanogels exhibited good thermosensitivity as well as pH sensitivity. Transmission electron microscopy (TEM) showed that the P(NIPAAm-co-PAAc)-g-PEI and P(NIPAAm-co-PAAc) nanogels displayed well dispersed spherical morphology. The mean sizes of the nanogels measured by dynamic light scattering (DLS) were from 100 nm to 500 nm at different temperatures. The cytotoxicity study indicated P(NIPAAm-co-PAAc) nanogels exhibited a better biocompatibility than both PNIPAAm nanogel and P(NIPAAm-co-PAAc)-g-PEI nanogel although all the three kinds of nanogels did not exhibit apparent cytotoxicity. The drug-loaded nanogels, especially the PEI-grafted nanogels, showed temperature-trigged controlled release behaviors, indicating the potential applications as an intelligent drug delivery system.
Apremilast (AP) {systematic name: (S)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4-acetamidoisoindoline-1,3-dione} is an inhibitor of phosphodieasterase-4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The ability of AP to form solvates has been investigated and three solvatomorphs of AP, namely, the AP ethyl acetate hemisolvate, CHNOS·0.5CHO, the AP toluene hemisolvate, CHNOS·0.5CH, and the AP dichloromethane monosolvate, CHNOS·CHCl, were obtained. The three AP solvatomorphs were characterized by X-ray powder diffraction, thermogravimetric analysis and differential scanning calorimetry. Single-crystal X-ray diffraction was used to analyze the structures, crystal symmetry, packing modes, stoichiometry and hydrogen-bonding interactions of the solvatomorphs. In addition, dissolution analyses were performed to study the dissolution rates of different AP solvatomorph tablets in vitro and to make comparisons with commercial apremilast tablets (produced by Celgene); all three solvatomorphs showed similar dissolution rates and similar values of the similarity factor f in a comparison of their dissolution profiles.
Diatoms, known as photosynthetic unicellular algae, can produce natural biosilica frustules that exhibit great biocompatibility, superhydrophilicity, and superhemophilicity. In our study, the diatom Navicula australoshetlandica sp. was isolated from aquaculture wastewater and pretreated to obtain frustules so as to explore their hemostasis characteristics. A special “porous web” (6–8 nm) substructure in the ordered nanopores (165–350 nm) of boat-shaped diatom frustule was observed in Navicula australoshetlandica sp. using SEM and TEM analysis. Moreover, X-ray, N2 adsorption–desorption isotherms, and BET analysis showed that the diatom frustule is a mesoporous material with a surface area of 401.45 m2 g−1 amorphous silica. FTIR analysis showed that Navicula australoshetlandica sp. frustules possessed abundant OH functional groups. A low hemolysis ratio was observed for 1–5 mg mL−1 diatom frustules that did not exceed 1.55 ± 0.06%, which indicates favorable hemocompatibility. The diatom frustules exhibited the shortest clotting time (134.99 ± 7.00 s) with a hemostasis material/blood (mg/μL) ratio of 1:100, which is 1.83 times (112.32 s) shorter than that of chitosan. The activated partial thromboplastin time (aPTT) of diatom frustule was also 44.53 s shorter than the control. Our results demonstrate the potential of Navicula australoshetlandica sp. diatom frustules to be used as medical hemostasis material.
The title compound represents another solvatomorph of apremilast, containing half of an ethanol and half of a water solvent molecule per formula unit
Monodisperse and mesoporous europium (Eu)-doped titania nanoparticles (denoted as Eu-MTNs) were prepared by a co-synthesis method with the presence of a cationic surfactant (i.e., CTAB). A maximum loading amount of 8 mol% of Eu could be successfully incorporated into the framework of MTNs. The synthesized Eu-MTNs samples were characterized with X-ray diffraction (XRD) and scanning electron microscopy (SEM), with their luminescent property examined by photoluminescence (PL). Under ultraviolet irradiation, the Eu-MTNs samples exhibit several characteristic luminescence corresponding to 5D0-7F(j) for Eu+3 ions, which can be attributed to the energy transfer from titania nanocrystallite to Eu3+ ions dispersed in amorphous mesoporous titania region. The potential intracellular bio-imaging application of the synthesized Eu-MTN nanoparticles was demonstrated with a breast cancer cell line (i.e., BT-20). High biocompatibility and strong luminescence of the Eu-MTNs show great potential in biomedical applications.
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