Poor water solubility for many drugs and drug candidates remains a major obstacle to their development and clinical application. Conventional formulations to improve solubility suffer from low ...bioavailability and poor pharmacokinetics, with some carriers rendering systemic toxicities (e.g. Cremophor
® EL). In this review, several major nanonization techniques that seek to overcome these limitations for drug solubilization are presented. Strategies including drug nanocrystals, nanoemulsions and polymeric micelles are reviewed. Finally, perspectives on existing challenges and future opportunities are highlighted.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The interactions of nanoparticles with the soft surfaces of biological systems like cells play key roles in executing their biomedical functions and in toxicity. The discovery or design of new ...biomedical functions, or the prediction of the toxicological consequences of nanoparticles in vivo, first require knowledge of the interplay processes of the nanoparticles with the target cells. This article focusses on the cellular uptake, location and translocation, and any biological consequences, such as cytotoxicity, of the most widely studied and used nanoparticles, such as carbon‐based nanoparticles, metallic nanoparticles, and quantum dots. The relevance of the size and shape, composition, charge, and surface chemistry of the nanoparticles in cells is considered. The intracellular uptake pathways of the nanoparticles and the cellular responses, with potential signaling pathways activated by nanoparticle interactions, are also discussed.
The cellular uptake, location and translocation, and biological consequence of nanoparticles are reviewed with regard to the size, shape, composition, charge, and surface chemistry of the nanoparticles in cells.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
Nanomaterial-biology interaction is the critical step in the fate of biomedical nanomedicines, influencing the consequent biological outcomes. Herein, we present two-dimensional carbon-based ...nanomaterials–graphdiyne oxide (GDYO) nanosheets that interact with an intracellular protein corona consisting of signal transducer and activator of transcription 3 (STAT3), inducing the reeducation of immunosuppressive macrophages. The interaction at the GDYO–STAT3 interface, driven by structure matching, hydrogen bonding, and salt bridges, simultaneously triggers the immune response in the tumor microenvironment, facilitating cancer immunotherapy. For the first time, our data reveal an interaction mechanism between the nanoparticle–protein interfaces inevitably formed inside the cells that determines the macrophage phenotype. Our results suggest that GDYO nanosheets could be applied for local immunomodulation due to their function and structural organization of the intracellular protein corona occurred inside macrophages.
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IJS, KILJ, NUK, PNG, UL, UM
Inorganic nanoparticles have shown promising potentials as novel biomedical imaging agents with high sensitivity, high spatial and temporal resolution. To translate the laboratory innovations into ...clinical applications, their potential toxicities are highly concerned and have to be evaluated comprehensively both in vitro and in vivo before their clinical applications. In this review, we first summarized the in vivo and in vitro toxicities of the representative inorganic nanoparticles used in biomedical imagings. Then we further discuss the origin of nanotoxicity of inorganic nanomaterials, including ROS generation and oxidative stress, chemical instability, chemical composition, the surface modification, dissolution of nanoparticles to release excess free ions of metals, metal redox state, and left-over chemicals from synthesis, etc. We intend to provide the readers a better understanding of the toxicology aspects of inorganic nanomaterials and knowledge for achieving optimized designs of safer inorganic nanomaterials for clinical applications.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The paper aimed to evaluate the effects of dietary inclusion of green tea powder (GTP) on laying performance, egg quality, and blood biochemical parameters of laying hens. A total of 240 Jingfen No. ...6 laying hens (age, 24 wk) were randomly allocated into 4 groups: control group (CON, basal diet), GTP0.5, GTP0.75, and GTP1.0 (basal diet included 0.5, 0.75, and 1.0% GTP, respectively). Each group has 5 replicates with 12 birds each. The feeding trial lasted 8 wk. The results showed that the hen-day egg production rate in GTP0.5 and GTP 0.75 group was higher than that of GTP1.0 group (P < 0.05), hen-day egg production rate in the GTP1.0 group was lower compared to the CON group (P > 0.05), the feed conversion ratio (FCR) in the GTP0.75 group was lower than that in CON and GTP 1.0 group (P < 0.05) during the entire experimental period. Albumen height and Haugh unit were higher in the GTP0.75 and GTP1.0 group compared to the CON group at d 56 (P < 0.05). At the end of experiment, plasma TG content in the GTP0.75 and GTP1.0 group was lower than that in the CON group (P < 0.05), the T-CH concentration in the GTP0.5 and GTP0.75 group was lower compared to the CON group (P < 0.05), plasma LDL-C and CORT concentrations were decreased by dietary GTP supplementation (P < 0.05), the HDL-C and BUN concentrations in the GTP0.75 and GTP1.0 group were higher than that in the CON group (P < 0.05). The antibody titers of H5N1 in the GTP0.75 and GTP1.0 group, and H7N9 in the GTP1.0 group were lower than that in the CON group (P < 0.05). In conclusion, dietary GTP inclusion could affect laying performance, regulate lipid metabolism, and have no favorable influence on antibody titers of H5N1 and H7N9, herein, dietary 0.5% GTP inclusion is suggested for Jingfen No. 6 laying hens during the peak laying period.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
The purpose of this study was to construct microemulsion-base hydrogel formulation for topical delivery of ibuprofen. Ethyl oleate (EO) was screened as the oil phase of microemulsions, due to a good ...solubilizing capacity of the microemulison systems and excellent skin permeation rate of ibuprofen. The pseudo-ternary phase diagrams for microemulsion regions were constructed using ethyl oleate as the oil, Tween 80 as the surfactant, propylene glycol as the cosurfactant. Various microemulsion formulations were prepared and the abilities of various microemulsions to deliver ibuprofen through the skin were evaluated in vitro using Franz diffusion cells fitted with porcine skins. The in vitro permeation data showed that microemulsions increased the permeation rate of ibuprofen 5.72–30.0 times over the saturated solution. The optimum formulation consisted of 3% ibuprofen, 6% EO, 30% Tween 80/PG (2:1) and water, showed a high permeation rate of 38.06
μg
cm
−2
h
−1. Xanthan gum as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The studied microemulsion-based hydrogel showed a good stability. These results indicate that the studied microemulsion-based hydrogel may be a promising vehicle for topical delivery of ibuprofen.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Fullerenol is one of the main precursors of fullerene-based materials, which is promising for various biological applications because of its unusual biocompatibility and biofunctionality. However, ...the functional groups, acidity and reducibility, which substantialize the applications of fullerenols, remain open questions. Using density functional theory calculations, we investigated reaction mechanisms underlying the acidity and reducibility of C
60
fullerenols. On the basis of theoretical insights combined with synthesis, IR and NMR structural characterization of
13
C-labeled C
60
fullerenols, we identified the functional groups and developed and verified a structural model for C
60
fullerenols. The results show a strong dependence of acidity and reducibility on the hydroxyl distributions of fullerenols. Fullerenols with stable π-electron configurations on C
60
cores, in which no double bonds have to be placed in conjugated pentagonal rings when drawing their Kekulé structures, have low acidities and reducibilities. Contrarily, fullerenols with unstable π-electron configurations have high acidities and reducibilities. For fullerenols with different hydroxyl distributions, the calculated acid dissociation constants range from −17.55 to 15.21, and the calculated redox potentials range from −0.87 to 1.32 V. Hydroxyls with high acidities and reducibilities unlikely survive in fullerenols synthesized using alkali, oxidizing conditions. Instead, they exist as the corresponding conjugate bases or oxidized products. This structural prediction agrees with our NMR results and the previous experiments. The proposed structural model is able to interpret the main IR and NMR spectroscopic and electronically paramagnetic properties of C
60
fullerenols without the disadvantages of the previous models.
An explicit structural model was developed and verified for fullerenols.
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IJS, KILJ, NUK, UL, UM, UPUK
The purpose of this study was to evaluate solid lipid nanoparticles as the topical carrier for epidermal targeting of podophyllotoxin (POD). The high pressure homogenization was employed to prepare ...drug-loaded solid lipid nanoparticles. The POD-loaded SLN stabilized by 0.5% poloxamer 188 and 1.5% soybean lecithin (P-SLN) and 2% polysorbate 80 (T-SLN) was characterized by photon correlation spectroscopy (PCS). P-SLN showed an average diameter of 73.4 nm and a zeta potential of −48.36 mV. The imaging of AFM indicated that the P-SLN had a spherical shape. DSC and X-ray diffraction analysis showed that POD was dispersed in SLN in an amorphous state. The in vitro permeation study showed that P-SLN increased the accumulative amount of POD in porcine skin 3.48 times over 0.15% tincture. But T-SLN with a diameter of 123.1 nm and a zeta potential of −17.4 mV did not show a high accumulative amount of POD when compared with P-SLN, though both P-SLN and T-SLN could avoid the systemic uptake of POD. Because of the fluorescence property of POD, fluorescence microscopy imaging was employed to visualize the penetration of POD into skin from SLN. The penetration of POD from P-SLN seemed to follow two pathways along the stratum corneum and hair follicle route. The imaging revealed that P-SLN had a strong localization of POD within epidermis. The penetration of P-SLN with low particle size into stratum corneum along the skin surface ‘furrow’ and the consequent controlled release of POD might lead to the epidermal targeting. P-SLN provides a good epidermal targeting effect and may be a promising carrier for topical delivery of POD.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
In this work, a hydrogel-thickened microemulsion (HTM) was investigated for delivering an extremely low concentration of drug molecule. The pseudo-ternary phase diagrams were constructed using ...isopropyl myristate (IPM), Tween 80, propylene glycol and water. The various HTM were prepared and characterized. We described that HTM has the combination of o/w microstructure of microemulsion and the three-dimensional gel network of hydrogel in continuous phase using transmission electron microscope. The stability tests showed that HTM had good stability. The influence of the addition of hydrogel into microemulsions on the viscosity and permeation ability is investigated. The abilities of HTM to deliver an extremely low concentration of triptolide as a model drug were evaluated using the in vitro permeation studies. The permeation rates of triptolide from various HTM were 2.2–3.6 times over that from the control hydrogel. The addition of 2% menthol into HTM consisting of 3% IPM, 30% Tween 80, 15% propylene glycol, 0.75% carbomer 940 resulted in the highest permeation rate of 0.105
±
0.006
μg
cm
−2
h
−1, which was 5.8 times over control gel. The powerful permeation enhancing ability of HTM with a suitable viscosity makes it promising alternative carrier for transdermal administration of drug molecule at an extremely low concentration.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Carbon nanotubes (CNTs) have attracted great interdisciplinary interest due to their peculiar structural, mechanical and electronic properties. Applications of CNTs in biomedical research are being ...actively explored by many scientists worldwide. However, manipulation of CNTs is impeded by several problems, such as 1) formation of complex and entangled bundles; 2) very low solubility of CNTs in organic solvents and water; 3) inert properties of pristine CNTs under many chemical reaction conditions, etc. Chemical modification of CNTs has partly solved the above issues and is still one of the most effective means of manipulating and processing CNTs. Many bioapplications of CNTs rely on successful outer/inner surface functionalizations. This Feature Article is comprised of two main parts. In the first part, we briefly review the covalent surface chemistry for the CNT functionalization; in the second part, we focus on the biomedical applications of surface chemistry for CNTs, in particular, the chemistry for controlling biomedical functions and meanwhile lowering nanotoxicity of CNTs. We also analyze the underlying factors that led to the controversy in the previous experimental data of safety studies of CNTs.
