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1.
Int J Biol Macromol ; 273(Pt 1): 132777, 2024 Jun 02.
Article in English | MEDLINE | ID: mdl-38834113

ABSTRACT

In this work, a bio-based material (CGP) is obtained by combing chitosan, gelatin and polyvinyl alcohol through a simple solution mixing to simultaneously address polylactic acid film (PLA)' flammability and poor barrier, toughness and antibacterial properties by soaking. The results of open fire testing show that modified PLA films can effectively prolong the combustion time, improve the thermal stability and reduce the release of heat in the cone calorimeter test. For the PLA sample after soaking for 5 times (PLA-5) in particular, it can reduce the peak heat release rate (pHRR) and total heat release (THR) values to 85.8 kW/m2 and 1.3 MJ/m2 from the values of 129.5 kW/m2 and 1.8 MJ/m2 for PLA, respectively. Structural analysis suggests that CGP primarily operates in the condensed phase by forming physical barriers. Meanwhile, the modified PLA films can exhibit superior barrier effects, which indicate the oxygen transmission rate value of PLA-5 decreases to 0.9 cm3/(m2·day) from the 392.5 cm3/(m2·day) of raw PLA film. Moreover, the PLA-5 also have excellent toughness (the value increased to 200.5 % from 31.0 %) and persistent antibacterial effects (it still has 100 % sterilization after 500 days).

2.
Molecules ; 29(9)2024 May 03.
Article in English | MEDLINE | ID: mdl-38731612

ABSTRACT

Organic dyes are widely used in many important areas, but they also bring many issues for water pollution. To address the above issues, a reconstructed kaolinite hybrid compound (γ-AlOOH@A-Kaol) was obtained from raw kaolinite (Kaol) in this work. The product was then characterized by X-ray diffraction (XRD), Fourier-transform infrared (ATR-FTIR), Brunauer-Emmett-Teller (BET), and scanning electron microscopy (SEM), and the absorption properties of γ-AlOOH@A-Kaol for congo red were further studied. The results demonstrated that flower-like γ-AlOOH with nanolamellae were uniformly loaded on the surface of acid-treated Kaol with a porous structure (A-Kaol). In addition, the surface area (36.5 m2/g), pore volume (0.146 cm3/g), and pore size (13.0 nm) of γ-AlOOH@A-Kaol were different from those of A-Kaol (127.4 m2/g, 0.127 cm3/g, and 4.28 nm, respectively) and γ-AlOOH (34.1 m2/g, 0.315 cm3/g, and 21.5 nm, respectively). The unique structure could significantly enhance the sorption capacity for congo red, which could exceed 1000 mg/g. The reasons may be ascribed to the abundant groups of -OH, large specific surface area, and porous structure of γ-AlOOH@A-Kaol. This work provides an efficient route for comprehensive utilization and production of Kaol-based compound materials that could be used in the field of environmental conservation.

3.
Molecules ; 29(10)2024 May 16.
Article in English | MEDLINE | ID: mdl-38792212

ABSTRACT

Lignanoids are an active ingredient exerting powerful antioxidant and anti-inflammatory effects in the treatment of many diseases. In order to improve the efficiency of the resource utilization of traditional Chinese medicine waste, Magnolia officinalis Rehder & E.H.Wilson residue (MOR) waste biomass was used as raw material in this study, and a series of deep eutectic solvents (ChUre, ChAce, ChPro, ChCit, ChOxa, ChMal, ChLac, ChLev, ChGly and ChEG) were selected to evaluate the extraction efficiency of lignanoids from MORs. The results showed that the best conditions for lignanoid extraction were a liquid-solid ratio of 40.50 mL/g, an HBD-HBA ratio of 2.06, a water percentage of 29.3%, an extract temperature of 337.65 K, and a time of 107 min. Under these conditions, the maximum lignanoid amount was 39.18 mg/g. In addition, the kinetics of the extraction process were investigated by mathematic modeling. In our antioxidant activity study, high antioxidant activity of the lignanoid extract was shown in scavenging four different types of free radicals (DPPH, ·OH, ABTS, and superoxide anions). At a concentration of 3 mg/mL, the total antioxidant capacity of the lignanoid extract was 1.795 U/mL, which was equal to 0.12 mg/mL of Vc solution. Furthermore, the antibacterial activity study found that the lignanoid extract exhibited good antibacterial effects against six tested pathogens. Among them, Staphylococcus aureus exerted the strongest antibacterial activity. Eventually, the correlation of the lignanoid extract with the biological activity and physicochemical properties of DESs is described using a heatmap, along with the evaluation of the in vitro hypoglycemic, in vitro hypolipidemic, immunomodulatory, and anti-inflammatory activity of the lignanoid extract. These findings can provide a theoretical foundation for the extraction of high-value components from waste biomass by deep eutectic solvents, as well as highlighting its specific significance in natural product development and utilization.


Subject(s)
Antioxidants , Biomass , Magnolia , Magnolia/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Deep Eutectic Solvents/chemistry , Lignin/chemistry , Lignin/pharmacology , Lignin/isolation & purification , Plant Extracts/chemistry , Plant Extracts/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Animals
4.
Molecules ; 29(3)2024 Feb 05.
Article in English | MEDLINE | ID: mdl-38338480

ABSTRACT

To increase the effectiveness of using typical biomass waste as a resource, iridoids, chlorogenic acid, and flavonoids from the waste biomass of Eucommia ulmoides leaves (EULs) were extracted by deep eutectic solvents (DESs) in conjunction with macroporous resin. To optimize the extract conditions, the experiment of response surface was employed with the single-factor of DES composition molar ratio, liquid-solid ratio, water percentage, extraction temperature, and extraction time. The findings demonstrated that the theoretical simulated extraction yield of chlorogenic acid (CGA), geniposidic acid (GPA), aucubin (AU), geniposide (GP), rutin (RU), and isoquercetin (IQU) were 42.8, 137.2, 156.7, 5.4, 13.5, and 12.8 mg/g, respectively, under optimal conditions (hydrogen bond donor-hydrogen bond acceptor molar ratio of 1.96, liquid-solid ratio of 28.89 mL/g, water percentage of 38.44%, temperature of 317.36 K, and time of 55.59 min). Then, 12 resins were evaluated for their adsorption and desorption capabilities for the target components, and the HPD950 resin was found to operate at its optimum. Additionally, the HPD950 resin demonstrated significant sustainability and considerable potential in the recyclability test. Finally, the hypoglycemic in vitro, hypolipidemic in vitro, immunomodulatory, and anti-inflammatory effects of EUL extract were evaluated, and the correlation analysis of six active components with biological activity and physicochemical characteristics of DESs by heatmap were discussed. The findings of this study can offer a theoretical foundation for the extraction of valuable components by DESs from waste biomass, as well as specific utility benefits for the creation and development of natural products.


Subject(s)
Eucommiaceae , Flavonoids , Flavonoids/chemistry , Solvents/chemistry , Chlorogenic Acid/chemistry , Eucommiaceae/chemistry , Deep Eutectic Solvents , Plant Extracts/chemistry , Water , Iridoids
5.
ACS Omega ; 9(1): 1723-1737, 2024 Jan 09.
Article in English | MEDLINE | ID: mdl-38222590

ABSTRACT

Aucubin (AU) is an active ingredient that exerts strong antioxidant and anti-inflammatory effects in the treatment of several diseases. In order to improve the efficiency of resource utilization of traditional biomass waste, Eucommia ulmoides seed-draff (EUSD) waste biomass was used as the raw material, and a series of deep eutectic solvents were selected to evaluate the extraction efficiency of aucubin from EUSD. A response surface experiment was designed based on a single-factor experiment to optimize the extract conditions. The results showed that the best conditions for aucubin extraction were an HBD-HBA ratio of 2.18, a liquid-solid ratio of 46.92 mL/g, a water percentage of 37.95%, a temperature of 321.03 K, and an extraction time of 59.55 min. The maximum amount of aucubin was 156.4 mg/g, which was consistent with the theoretical value (156.8 mg/g). Then, the performance of 12 resins for adsorption and desorption was contrasted. The results revealed that HPD950 resin exhibited the best performance, with an adsorption capacity of 95.2% and a desorption capacity of 94.3%. Additionally, the pseudo-second-order model provided the best match to the kinetics data, the Langmuir model provided the best fit to the isotherm data, and adsorption was a beneficial, spontaneous, exothermic, and physical process. In the recyclability test, the HPD950 resin had great potential and excellent sustainability in aucubin recovery. In the antioxidant activity study, the aucubin extract exerted a strong antioxidant ability with scavenging capabilities for four free radicals. Furthermore, the antifungal activity study found that the aucubin extract exhibited a good antifungal effect against 5 tested pathogens. The research results can provide a theoretical basis for the extraction of high-value components from waste biomass by deep eutectic solvent and a certain application value for the development and utilization of natural aucubin products.

6.
Sheng Wu Gong Cheng Xue Bao ; 39(8): 3520-3529, 2023 Aug 25.
Article in Chinese | MEDLINE | ID: mdl-37622377

ABSTRACT

"Biochemical Engineering Experiment" is a compulsory curriculum for the concentrated practical teaching of biotechnology majors in Hunan University of Science and Engineering. It is also an experimental curriculum for improving the overall quality of bioengineering students under the context of "Emerging Engineering Education". The course includes comprehensive experiments and designable experiments, and the contents of which are designed by combining the local characteristic resources of Yongzhou, the research platform and the characteristics of the talents with engineering background. In the teaching practice, methods such as heuristic teaching, research cases-embedded teaching and interactive teaching are comprehensively used to boost students' interest in learning and stimulate their innovative thinking and application capability. Through curriculum examination and post-class investigation, it was found that the students' abilities of knowledge transfer and application were significantly improved, and they achieved excellent performances in discipline competitions and approved project proposals. The practice and continuous improvement of this course may facilitate fostering high-level innovative and application-oriented talents of biotechnology majors.


Subject(s)
Curriculum , Students , Humans , Learning , Bioengineering , Biomedical Engineering
7.
Mater Today Bio ; 21: 100721, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37502829

ABSTRACT

Development of lysosomes and mitochondria dual-targeting photosensitizer with the virtues of near-infrared (NIR) emission, highly efficient reactive oxygen generation, good phototoxicity and biocompatibility is highly desirable in the field of imaging-guided photodynamic therapy (PDT) for cancer. Herein, a new positively charged amphiphilic organic compound (2-(2-(5-(7-(4-(diphenylamino)phenyl)benzo[c][1,2,5]thiadiazol-4-yl)thiophen-2-yl)vinyl)-3-methylbenzo[d]thiazol-3-ium iodide) (ADB) based on a D-A-π-A structure is designed and comprehensively investigated. ADB demonstrates special lysosomes and mitochondria dual-organelles targeting, bright NIR aggregation-induced emission (AIE) at 736 â€‹nm, high singlet oxygen (1O2) quantum yield (0.442), as well as good biocompatibility and photostability. In addition, ADB can act as a two-photon imaging agent for the elaborate observation of living cells and blood vessel networks of tissues. Upon light irradiation, obvious decrease of mitochondrial membrane potential (MMP), abnormal mitochondria morphology, as well as phagocytotic vesicles and lysosomal disruption in cells are observed, which further induce cell apoptosis and resulting in enhanced antitumor activity for cancer treatment. In vivo experiments reveal that ADB can inhibit tumor growth efficiently upon light exposure. These findings demonstrate that this dual-organelles targeted ADB has great potential for clinical imaging-guided photodynamic therapy, and this work provides a new avenue for the development of multi-organelles targeted photosensitizers for highly efficient cancer treatment.

8.
Int J Biol Macromol ; 225: 266-276, 2023 Jan 15.
Article in English | MEDLINE | ID: mdl-36336155

ABSTRACT

In this work, a biomass composite material (CS@NC@PA-Na) was prepared from chitosan (CS), nano-cellulose (NC) and sodium phytate (PA-Na). The prepared products were characterized by scanning electron microscopy (SEM), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectrometry (XPS) and X-ray diffraction (XRD). The fire/water safety and antimicrobial properties of the CS@NC@PA-Na were fully studied. The results indicated CS@NC@PA-Na (50 mg) could effectively reduce the concentration of methyl orange by 85 % under 30 min adsorption. Meanwhile, only 5 wt% CS@NC@PA-Na could increase the limiting oxygen index (LOI) value of epoxy resin composite from 24.5 to 30.1 %, and decrease the peak heat/smoke release rate by 29.5 and 33.3 %, respectively. Moreover, CS@NC@PA-Na also exhibited excellent antibacterial effect. This work provides an efficient, feasible and eco-friendly route for large-scale production of multi-functional CS-based biomass materials that could be used in the fields of fire safety and environmental conservation.


Subject(s)
Chitosan , Water Purification , Chitosan/pharmacology , Chitosan/chemistry , Biomass , Cellulose , Anti-Bacterial Agents/pharmacology , Spectroscopy, Fourier Transform Infrared
9.
Heliyon ; 8(10): e10765, 2022 Oct.
Article in English | MEDLINE | ID: mdl-36267368

ABSTRACT

Aucubin (AU) is an active ingredient exerting strong antioxidant and anti-inflammatory effects in treating several diseases. This study evaluated the extraction of AU from Eucommia ulmoides seed-draff (EUSD) waste biomass using a series of solvents (methanol, ethanol, i-propanol, n-propanol, n-butanol, n-pentanol and cyclohexane) assisted with microwave and ultrasound, and proposed the optimized method for extraction. Five factors were investigated by Box-Behnken design (BBD) and response surface methodology (RSM). The optimized extraction conditions were as follows: liquid-solid ratio of 46.37 mL/g, methanol percentage of 89.56%, ultrasonic (extraction) time of 59.95 min, microwave power of 306.73 W, and microwave (extraction) time of 18.93 s. To this end, the AU extraction reached the maximum value (149.1 mg/g), which was consistent with the theoretical value (149.3 mg/g). Furthermore, the kinetics of extraction process were investigated by mathematic modeling. The extraction process analysis was also explored by 1H nuclear magnetic resonance (1H-NMR) spectroscopy, Fourier transform infrared (FTIR) spectroscopy and COSMOtherm program. This study found out that methanol provided better extraction efficiency than the conventional solvents (water, ethanol, i-propanol, n-propanol, n-butanol, n-pentanol, cyclohexane) due to possible interactions by the formation of hydrogen bond between AU and methanol, and ultrasound and microwave could significantly enhance mass transfer, which exhibited higher extraction efficiency and lower energy consumptions (149.1 mg/g and 0.102 kW·h vs. 73.4 mg/g and 0.700 kW·h for Soxhlet extraction). In the antibacterial activity study, the AU extract exerted strong antibacterial ability against 4 tested pathogens, and the antibacterial effect followed the order of: Staphylococcus aureus (35.9 ± 1.32 mm) > Escherichia coli (30.7 ± 1.38 mm) > Bacillus subtilis (20.5 ± 1.36 mm) > Salmonella (15.9 ± 1.39 mm) with the AU concentration of 40 mg/mL. Therefore, the development of this study will help to deepen the further understanding of natural product extraction by methanol-based ultrasonic and microwave, and has certain application value for the development and utilization of natural iridoid glycosides product.

10.
ACS Appl Mater Interfaces ; 13(46): 54783-54793, 2021 Nov 24.
Article in English | MEDLINE | ID: mdl-34763423

ABSTRACT

Photosensitizers play a critical role in photodynamic therapy (PDT). Multifunctional organic nanoparticles (NPs) that possess bright fluorescence in aggregates, high singlet oxygen (1O2) quantum yield, near-infrared (NIR) absorption and emission, large Stokes shift, two-photon bioimaging, specific organelle targeting, high PDT efficiency, as well as good biocompatibility and photostability are ideal candidate photosensitizers for image-guided PDT. Due to its enhanced fluorescence and high 1O2 generation efficiency in aggregate states, photosensitizers with aggregation-induced emission (AIE) characteristics have attracted increasing interest in PDT. In this study, a new AIE-active Schiff base 5-(((5-(7-(4-(diphenylamino)phenyl)benzo[c][1,2,5]thiadiazol-4-yl)thiophen-2-yl)methylene)amino)-3-methylthiophene-2,4-dicarbonitrile (TBTDC) based on a D-A-π-A skeleton has been designed and synthesized, and it can be readily encapsulated by Pluronic F-127 to form uniform nanoparticles. TBTDC NPs exhibit bright NIR emission at 825 nm with a Stokes shift up to 300 nm, impressive two-photon bioimaging capability with tissue penetration deep into 300 µm, high 1O2 generation quantum yield (0.552), specific targeting to lysosome, as well as good biocompatibility and photostability. Furthermore, TBTDC NPs present remarkable cytotoxicity for tumor cells and suppression of tumor growth in nude mice through reactive oxygen species generation upon white light irradiation. These results reveal that TBTDC NPs have great potential to become excellent candidates for multifunctional organic photosensitizers for two-photon bioimaging and image-guided PDT and are promising in future clinical applications.


Subject(s)
Antineoplastic Agents/pharmacology , Optical Imaging , Photochemotherapy , Photosensitizing Agents/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Density Functional Theory , Drug Screening Assays, Antitumor , Humans , Infrared Rays , Mammary Neoplasms, Experimental/diagnostic imaging , Mammary Neoplasms, Experimental/drug therapy , Mice , Mice, Inbred BALB C , Mice, Nude , Molecular Structure , Nanoparticles/chemistry , Particle Size , Photosensitizing Agents/chemical synthesis , Photosensitizing Agents/chemistry , Poloxamer/chemistry , Poloxamer/pharmacology , Schiff Bases/chemical synthesis , Schiff Bases/chemistry , Schiff Bases/pharmacology
11.
Appl Microbiol Biotechnol ; 104(11): 4757-4770, 2020 Jun.
Article in English | MEDLINE | ID: mdl-32291487

ABSTRACT

Ceaseless growth in human population led to high demand in everything. Currently, the world largely depends on petroleum-based "all material synthesis" scheme. On the other hand, depletion of fossil-based resources and their huge impact on environmental pollution have forced us to search for sustainable and eco-friendly alternative resources. In this context, the notion to utilize waste biomass could possibly provide environmental and economic benefits. This study was carefully designed to critically review state of the art in the transformation of waste biomass into value-added products. Even though extensive reviews on biomass utilization have been published in the past few years, the current study basically focused on new trends and prospective in this area. Here, global biomass potential, research developments and practices, novel biomass transformation approaches, and future perspectives were broadly discussed. More importantly, in addition to revising published researches, already implemented and ongoing large-scale projects on valorization of waste biomass have been assessed. Therefore, this study is believed to give crucial information on the current status and future direction of waste biomass utilization so as to accomplish the quest towards green economy.Key Points • Huge biomass potential and dramatically increase in R&D trends on waste biomass.• Selection of appropriate waste biomass valorization techniques. • Development of efficient and feasible waste biomass transformation technology. • Coproduction of low-value, high-volume and high-value, low volume products.


Subject(s)
Biomass , Biotechnology/methods , Biotransformation , Waste Products , Biofuels , Biotechnology/trends , Research/trends
12.
RSC Adv ; 11(1): 15-22, 2020 Dec 21.
Article in English | MEDLINE | ID: mdl-35423018

ABSTRACT

The mechanofluorochromic properties of three C6-unsubstituted tetrahydropyrimidines (THPs), namely, diethyl 1,2,3-triphenyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (1), dimethyl 1,2,3-tri(4-trifluoromethylphenyl)-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (2), and dimethyl 1,2,3-tri(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (3), with aggregation-induced emission (AIE) characteristics were investigated. The blue-green/cyan emissions of the three THPs can be switched reversibly by a grinding-fuming/heating process, with the change in maximum emission wavelength (λ em) up to 57 nm and the decrease of fluorescence quantum yields (Φ F). Interestingly, the green or cyan fluorescence of the ground powder (λ em is located at 481, 470 and 477 nm for 1b, 2 and 3, respectively) can spontaneously recover to the original blue (λ em is located at 434, 442 and 436 nm for 1b, 2 and 3, respectively) in 1-2 d at room temperature without any external stimulation. X-ray single-crystal diffraction, powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC) studies demonstrate that the conversion between the molecular packing modes is the main reason for the mechanofluorochromism and the spontaneously recoverable mechanofluorochromism relates to intermolecular hydrogen bonds. The sensitively and/or spontaneously recoverable mechanofluorochromism of these THPs is expected to have great potential in sensing, optical recording and self-healing fluorescent materials.

13.
Eur J Med Chem ; 151: 294-303, 2018 May 10.
Article in English | MEDLINE | ID: mdl-29627724

ABSTRACT

Therapeutic effects of photodynamic therapy (PDT) are limited by the selectivity of photosensitizer (PS). Herein, a novel tumor-targeted drug-PS conjugate (Gan-ZnPc) which integrated with zinc phthalocyanine (ZnPc) and Ganetespib has been developed. ZnPc is a promising PS with remarkable photosensitization ability. Ganetespib is a heat shock protein 90 (Hsp90) inhibitor with preferential tumor selectivity and conjugated to ZnPc as a tumor-targeted ligand. The multifunctional small molecule conjugate, Gan-ZnPc, could be bound to extracellular Hsp90 and then selectively internalized into the tumor cells, followed by the generation of abundant intracellular reactive oxygen species (ROS) upon irradiation. Besides, Gan-ZnPc can arrest cell proliferation and induce apoptosis by the inhibition of Hsp90. Herein, with combination of the inhibition of Hsp90 and the generation of cytotoxic ROS, Gan-ZnPc implements tumor selectivity, concentrated PDT and chemotherapy in a synergistic manner, which results in highly effective anti-tumor activity in vitro and in vivo.


Subject(s)
Indoles/therapeutic use , Mammary Neoplasms, Experimental/drug therapy , Organometallic Compounds/therapeutic use , Photosensitizing Agents/therapeutic use , Triazoles/therapeutic use , Animals , Breast Neoplasms/drug therapy , Breast Neoplasms/metabolism , Breast Neoplasms/pathology , Cell Line , Cell Line, Tumor , Drug Delivery Systems , Drug Synergism , Female , HSP90 Heat-Shock Proteins/metabolism , Humans , Indoles/chemistry , Indoles/pharmacology , Isoindoles , Mammary Neoplasms, Experimental/metabolism , Mammary Neoplasms, Experimental/pathology , Mice , Mice, Inbred BALB C , Organometallic Compounds/chemistry , Organometallic Compounds/pharmacology , Photochemotherapy , Photosensitizing Agents/chemistry , Photosensitizing Agents/pharmacology , Reactive Oxygen Species/metabolism , Triazoles/chemistry , Triazoles/pharmacology , Zinc Compounds
14.
RSC Adv ; 8(2): 785-791, 2018 Jan 02.
Article in English | MEDLINE | ID: mdl-35538981

ABSTRACT

The Ca-Al and Ca-Al-X (X = F-, Cl- and Br-) catalysts were prepared via thermal decomposition of Ca-Al layered double hydroxides (LDHs), and tested for methanolysis of propylene carbonate (PC) to produce dimethyl carbonate (DMC). The catalytic performance of these catalysts increased in the order of Ca-Al-Br- < Ca-Al < Ca-Al-Cl- < Ca-Al-F-, which was consistent with the strong basicity of these materials. The recyclability test results showed that the addition of Al and halogens (F-, Cl- and Br-) not only stabilized the CaO but also improved the recyclability of the catalysts. Particularly, the Ca-Al-F- catalyst exerted the highest stability after 10 recycles. These catalysts have an important value for the exploitation of DMC synthesis by transesterification of PC with methanol.

15.
Int J Pharm ; 516(1-2): 352-363, 2017 Jan 10.
Article in English | MEDLINE | ID: mdl-27887884

ABSTRACT

Because of the peculiarity of the bone microstructure, the uptake of chemotherapeutics often happens at non-targeted sites, which induces side effects. In order to solve this problem, we designed a bone-targeting drug delivery system that can release drug exclusively in the nidus of the bone. Alendronate (ALN), which has a high ability to target to hydroxyapatite, was used to fabricate double ALN-conjugated poly (ethylene glycol) 2000 material (ALN-PEG2k-ALN). The ALN-PEG2k-ALN was characterized using 1H NMR and 31P NMR and FTIR. ALN-PEG2k-ALN-modified calcium phosphate nanoparticles (APA-CPNPs) with an ALN targeting moiety and hydrophilic poly (ethylene glycol) arms tiled on the surface was prepared for bone-targeted drug delivery. The distribution of ALN-PEG2k-ALN was tested by X-ray photoelectron spectroscopy. Isothermal titration calorimetry data indicated that similar to free ALN, both ALN-PEG2k-ALN and APA-CPNPs can bind to calcium ions. The bone-binding ability of APA-CPNPs was verified via ex vivo imaging of bone fragments. An in vitro release experiment demonstrated that APA-CPNPs can release drug faster in an acid environment than a neutral environment. Cell viability experiments indicated that blank APA-CPNPs possessed excellent biocompatibility with normal cells. Methotrexate (MTX) loaded APA-CPNPs have the same ability to inhibit cancer cells as free drug at high concentrations, while they are slightly weaker at low concentrations. All of these experiments verified the prospective application of APA-CPNPs as a bone-targeting drug delivery system.


Subject(s)
Alendronate/chemistry , Bone Neoplasms/drug therapy , Calcium Phosphates/chemistry , Methotrexate/administration & dosage , Alendronate/metabolism , Animals , Antimetabolites, Antineoplastic/administration & dosage , Antimetabolites, Antineoplastic/pharmacokinetics , Antimetabolites, Antineoplastic/pharmacology , Bone Neoplasms/secondary , Cell Line , Cell Line, Tumor , Cell Survival/drug effects , Drug Carriers/chemistry , Drug Delivery Systems , Durapatite/metabolism , Female , Humans , Methotrexate/pharmacokinetics , Methotrexate/pharmacology , Mice , Nanoparticles , Photoelectron Spectroscopy , Polyethylene Glycols/chemistry , Rats , Rats, Sprague-Dawley , Tissue Distribution
16.
Carbohydr Polym ; 147: 415-425, 2016 08 20.
Article in English | MEDLINE | ID: mdl-27178948

ABSTRACT

Agomelatine (AGM), is efficacious in both the acute phase and the continuation phase of depression. However, its poor water-solubility, low bioavailability and polymorphism limit its pharmacological effects. To address these problems, agomelatine-hydroxypropyl-ß-cyclodextrin inclusion complex (AGM/HPß-CD) was prepared successfully by freeze-drying. The products was evaluated by structural characterization, solubilization test, in-situ absorption of rat intestinal tract and pharmacokinetic study. In addition, thermodynamic studies were performed, the results indicated that the inclusion process was enthalpy-determined and exothermic nature of complexation, signifying the role of steric interactions in complex formation. Molecular docking of AGM with HPß-CD has been conducted as well to verify the experimental findings and predict the stable molecular structure of the inclusion complex. The in vivo data showed that, AGM was mainly absorbed in duodenum and jejunum by passive diffusion. AGM/HPß-CD inclusion complex displayed earlier Tmax and higher Cmax, and the AUC0-12h was approximately twice larger than its physical mixture. These results suggested that AGM/HPß-CD inclusion complex was established with 1:1 stoichiometry through the naphthalene group of AGM and it was deeply inserted into the cavity of HPß-CD, and the inclusion complex could significantly enhance the oral bioavailability of AGM.


Subject(s)
2-Hydroxypropyl-beta-cyclodextrin/chemistry , Acetamides/administration & dosage , Acetamides/pharmacokinetics , Acetamides/chemistry , Animals , Area Under Curve , Calorimetry, Differential Scanning , Freeze Drying , Intestinal Mucosa/metabolism , Molecular Docking Simulation , Rats , Solubility
17.
J Mater Chem B ; 3(26): 5249-5260, 2015 Jul 14.
Article in English | MEDLINE | ID: mdl-32262600

ABSTRACT

Lymphatic metastasis plays an important role in tumour recurrence. The applications of nanoparticles in the treatment of lymphatic metastatic tumours have been limited by targeting inefficiency and nonselective toxicity. Hence, in this report, we have developed lipid-coated ZnO nanoparticles (LZnO NPs) in an attempt to solve these issues. Using the microreactor method, we have fabricated ultrasmall (∼30 nm) core-shell-structured nanoparticles loaded with 6-mercaptopurine (6-MP). In vivo results show that the lipid shell induces a remarkable improvement in lymphotropism and biocompatibility compared to ZnO nanoparticles. Furthermore, the ZnO core exhibits not only pH-responsive behaviour to guarantee effective drug delivery, but also a strong preferential ability to kill cancerous cells, as a consequence of the generation of higher inducible levels of reactive oxygen species in rapidly dividing cells. Furthermore, LZnO NPs enhance the cytotoxicity of 6-MP, resulting from the improved internalization of nanoparticles through endocytosis. These findings indicate that LZnO NPs are a promising candidate for use as lymphatic-targeted drug carriers.

18.
Int J Nanomedicine ; 9: 4867-78, 2014.
Article in English | MEDLINE | ID: mdl-25364245

ABSTRACT

Layered double hydroxide (LDH) has attracted considerable attention as a drug carrier. However, because of its poor in vivo behavior, polyethylene glycolylated (PEGylated) phospholipid must be used as a coformer to produce self-assembled core-shell nanoparticles. In the present study, we prepared a PEGylated phospholipid-coated LDH (PLDH) (PEG-PLDH) delivery system. The PEG-PLDH nanoparticles had an average size of 133.2 nm. Their core-shell structure was confirmed by transmission electron microscopy and X-ray photoelectron spectroscopy. In vitro liposome-cell-association and cytotoxicity experiments demonstrated its ability to be internalized by cells. In vivo studies showed that PEGylated phospholipid membranes greatly reduced the blood clearance rate of LDH nanoparticles. PEG-PLDH nanoparticles demonstrated a good control of tumor growth and increased the survival rate of mice. These results suggest that PEG-PLDH nanoparticles can be a useful drug delivery system for cancer therapy.


Subject(s)
Antineoplastic Agents/pharmacology , Antineoplastic Agents/pharmacokinetics , Drug Carriers/chemistry , Hydroxides/chemistry , Nanoparticles/chemistry , Animals , Antineoplastic Agents/blood , Antineoplastic Agents/chemistry , Blood Proteins/chemistry , Body Weight/drug effects , Cell Survival/drug effects , Drug Carriers/toxicity , HeLa Cells , Humans , Hydroxides/toxicity , Methotrexate/blood , Methotrexate/chemistry , Methotrexate/pharmacokinetics , Methotrexate/pharmacology , Mice , Nanoparticles/toxicity , Particle Size , Phospholipids/chemistry , Phospholipids/toxicity , Polyethylene Glycols/chemistry , Polyethylene Glycols/toxicity , Rats, Sprague-Dawley , Xenograft Model Antitumor Assays
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