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TALANTA · 2017 · IF 4.162

Nano-encapsulant of ascorbic acid-loaded apoferritin-assisted photoelectrochemical sensor for protease detection

Jiexia Chen,Guang-Chao Zhao

A signal-on photoelectrochemical (PEC) biosensor based on nano-encapsulant of ascorbic acid-loaded apoferritin - assisted for protease detection is described. The loaded ascorbic acid could be released from the central cavity of apoferritin into the buffer solution as sacrificial electron donor to capture the photo-generated holes of CdTe quantum dots when light is turned on. In this system, the biosensor relied on monitoring the photocurrent intensity as a result of enzymatic substrate proteolysis in the homogeneous aqueous solution. A low detection limit of 2.7   ng   mL −1 for trypsin in the linear range from 30 to 450   ng   mL −1 is achieved. We believe that such a sensing system not only holds the potential ability as a probe for trypsin activity assay, but also could be used for the corresponding inhibitor-screening. It might provide a potentially feasible alternative tool for determining trypsin in human serum in a clinical laboratory. The established method could open a different perspective for PEC enzyme detection and provide a new platform for future development of PEC analysis with other clinically important proteins.

研究领域: 生物传感 · 分析化学 · 生物医学工程
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APPLIED SURFACE SCIENCE · 2014 · IF 2.538

Beta-cyclodextrins conjugated magnetic Fe3O4 colloidal nanoclusters for the loading and release of hydrophobic molecule

Shaonan Lv,Yubei Song,Yaya Song,Zhigang Zhao,Changjing Cheng

Herein, we report a facile method to prepare beta-cyclodextrin (β-CD)-conjugated magnetic Fe 3 O 4 colloidal nanocrystal clusters (Fe 3 O 4 @GLY-CD) using (3-glycidyloxypropyl) trimethoxysilane (GLY) as the intermediate linker. The resulting Fe 3 O 4 @GLY-CD was characterized by several methods including Fourier transform infrared (FT-IR) spectroscopy, field-emission scanning electron microscopy (SEM), transmission electron microscopy (TEM), dynamic light scattering (DLS), X-ray diffraction (XRD), thermogravimetric analysis (TGA) and vibrating sample magnetometer (VSM). In addition, the loading and release properties of the synthesized Fe 3 O 4 @GLY-CD for the hydrophobic molecule 8-anilino-1-naphthalenesulfonic acid ammonium salt (ANS) were also investigated. The results show that the Fe 3 O 4 @GLY-CD has a spherical structure with an average diameter of 186   nm and high saturated magnetism of 51.2   emu/g. The grafting of β-CD onto Fe 3 O 4 colloidal nanocrystal clusters can markedly increase the loading capacity of ANS because of β-CD/ANS inclusion complex formation. The in vitro delivery profile shows that the release of ANS from the Fe 3 O 4 @GLY-CD nanosystem exhibits an initial burst followed by a slow and steady release. Moreover, Fe 3 O 4 @GLY-CD also demonstrates a temperature-dependent release behavior for ANS owing to the effect of temperature on the association constants of β-CD/ANS inclusion complexes. The developed magnetic hybrid nanomaterial is expected to find potential applications in several fields including separation science and biomedicine.

CAS / MDL: 10025-77-1 68037-40-1
研究领域: 材料科学 · 生物医学工程 · 药物递送
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2017 · IF 4.159

Enhanced encapsulation and bioavailability of breviscapine in PLGA microparticles by nanocrystal and water-soluble polymer template techniques

Hong Wang,Guangxing Zhang,Xueqin Ma,Yanhua Liu,Jun Feng,Kinam Park,Wenping Wang

Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents . In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine . Breviscapine nanocrystals were prepared using a precipitation-ultrasonication method and further loaded into PLGA microparticles by casting in a mold from a water-soluble polymer. The obtained disc-like particles were then characterized and compared with the spherical particles prepared by an emulsion-solvent evaporation method. X-ray powder diffraction (XRPD) and confocal laser scanning microscopy (CLSM) analysis confirmed a highly-dispersed state of breviscapine inside the microparticles. The drug form, loading percentage and fabrication techniques significantly affected the loading capacity and efficiency of breviscapine in PLGA microparticles, and their release performance as well. Drug loading was increased from 2.4% up to 15.3% when both nanocrystal and template methods were applied, and encapsulation efficiency increased from 48.5% to 91.9%. But loading efficiency was reduced as the drug loading was increased. All microparticles showed an initial burst release, and then a slow release period of 28   days followed by an erosion-accelerated release phase, which provides a sustained delivery of breviscapine over a month. A relatively stable serum drug level for more than 30   days was observed after intramuscular injection of microparticles in rats. Therefore, PLGA microparticles loaded with nanocrystals of poorly soluble drugs provided a promising approach for long-term therapeutic products characterized with preferable in vitro and in vivo performance.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物医学工程
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Chemical Engineering and Processing-Process Intensification · 2024 · IF 3.8

Supercritical carbon dioxide as solvent for manufacturing of ibuprofen loaded gelatine sponges with enhanced performance

Senlin Li,Yifan Zheng,Zhihao Zhang,Shengao Xu,Yuan Pu,Dan Wang

Supercritical carbon dioxide was used as the solvent for manufacturing of ibuprofen loaded gelatine sponges with high loading capacity and fast release performance toward healthcare materials in the treatment of postoperative dental pain. The solubility of ibuprofen in supercritical CO 2 was first determined at 313 K under different pressure conditions. The micronisation of ibuprofen drugs were successfully adsorbed onto the surface of network pore system of gelatine sponges via supercritical CO₂ processing. The loading capacity of ibuprofen in gelatine sponges obtained by using supercritical CO₂ as the solvent can be up to 19.86 wt%, which was double that of the sample prepared by direct soaking in ethanol. The dissolution of ibuprofen was determined and higher instantaneous dissolution rate was observed for the ibuprofen loaded gelatine sponges synthesized by supercritical CO₂ processing.

CAS / MDL: 15687-27-1
研究领域: 制药工程 · 材料科学 · 药物递送
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International Journal of Nanomedicine · 2023 · IF 8

A facile doxorubicin-dichloroacetate conjugate nanomedicine with high drug loading for safe drug delivery

Conglian Yang,Tingting Wu,Yuting Qin,Yan Qi,Yu Sun,Miao Kong,Xue Jiang,Xianya Qin,Yaqi Shen,Zhiping Zhang

Background Doxorubicin (DOX) is an effective chemotherapeutic agent but severe side effects limit its clinical application. Nanoformulations can reduce the toxicity while still have various limitations, such as complexity, low drug loading capability and excipient related concerns.Methods An amphiphilic conjugate, doxorubicin-dichloroacetate, was synthesized and the corresponding nanoparticles were prepared. The in vitro cytotoxicity and intracellular uptake, in vivo imaging, antitumor effects and systemic toxicities of nanoparticles were carried out to evaluate the therapeutic efficiency of tumor.Results Doxorubicin-dichloroacetate conjugate can self-assemble into nanoparticles with small amount of DSPE-PEG2000, leading to high drug loading (71.8%, w/w) and diminished excipient associated concerns. The nanoparticles exhibited invisible systemic toxicity and high maximum tolerated dose of 75 mg DOX equiv./kg, which was 15-fold higher than that of free DOX. It also showed good tumor targeting capability and enhanced antitumor efficacy in murine melanoma model.Conclusion This work provides a promising strategy to simplify the drug preparation process, increase drug loading content, reduce systemic toxicity as well as enhance antitumor efficiency.

研究领域: 药剂学 · 肿瘤学 · 纳米医学
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Materials Today Nano · 2024 · IF 8.2

Iron ion driven remote loading of galloylated cabazitaxel prodrugs for synergistic ferroptosis and chemotherapy

Baoyue Zhang,Jiang Yu,Ruiping Huang,Jianying Ye,Fanlin Meng,Zhaochu Xu,Wenwen Cui,Jia Song,Siqi Wang,Yanjun Du,Qingzhi Lv,Wanling Zhu,Dan Liu,Yongjun Wang

Liposomes, particularly those designed for remote drug loading, have achieved remarkable success as drug-delivery vehicles in clinical settings. However, the lack of ionizable or coordinative groups prevents many promising drugs from being remotely loaded into liposomes for cancer therapy. Herein, to provide a universal remote loading approach, we chose cabazitaxel (CTX) as a model drug to modify galloyl group bridged by different lengths of alkyl chain. Fortunately, all the synthesized prodrugs could be actively loaded into liposomes via Fe 3+ gradient with high encapsulation efficiency and loading capacity. As the intraliposomal aqueous phase, Fe 3+ was not only served as the driving force of prodrugs remote loading, but also regarded as an exogenous replenishment to strengthen iron-dependent ferroptosis for multimodal therapy. The length of linkage between CTX and galloyl group played a crucial role in the chemical stability of prodrugs, in vitro drug release rate and in vivo pharmacokinetics behavior of prodrug liposomes. Among three prodrug liposomes, only decylene glycol-bridged CTX-gallic acid (CTX-DC-GA) liposomes kept a good balance between drug leakage during circulation and specific drug release under tumor microenvironment. Ultimately, CTX-DC-GA liposomes displayed optimal antitumor efficacy with good safety. We proposed Fe 3+ -based galloylated prodrug liposomes give new horizons for achieving the combination of ferroptosis and chemotherapy.

研究领域: 药剂学 · 肿瘤学 · 生物化学
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Nature Communications · 2024 ·Vol. 15 ·期 1 ·1-11 · IF 14.7

One-step formation of polymorphous sperm-like microswimmers by vortex turbulence-assisted microfluidics

Tan Rong,Yang Xiong,Lu Haojian,Shen Yajing

Microswimmers are considered promising candidates for active cargo delivery to benefit a wide spectrum of biomedical applications. Yet, big challenges still remain in designing the microswimmers with effective propelling, desirable loading and adaptive releasing abilities all in one. Inspired by the morphology and biofunction of spermatozoa, we report a one-step formation strategy of polymorphous sperm-like magnetic microswimmers (PSMs) by developing a vortex turbulence-assisted microfluidics (VTAM) platform. The fabricated PSM is biodegradable with a core-shell head and flexible tail, and their morphology can be adjusted by vortex flow rotation speed and calcium chloride solution concentration. Benefiting from the sperm-like design, our PSM exhibits both effective motion ability under remote mag/netic actuation and protective encapsulation ability for material loading. Further, it can also realize the stable sustain release after alginate-chitosan-alginate (ACA) layer coating modification. This research proposes and verifies a new strategy for the sperm-like microswimmer construction, offering an alternative solution for the target delivery of diverse drugs and biologics for future biomedical treatment. Moreover, the proposed VTAM could also be a general method for other sophisticated polymorphous structures fabrication that isn’t achievable by conventional laminar flow.

研究领域: 生物医学工程 · 材料科学 · 纳米医学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2015 · IF 2.858

Preparation and characterization of vanillin-crosslinked chitosan therapeutic bioactive microcarriers

Qin Zou,Junfeng Li,Yubao Li

Chitosan microspheres with diameter of 14.3–48.5   μm were prepared by emulsion method and using natural vanillin as cross-linking agent. The surface morphology and microstructure of the microspheres were characterized by scanning electron microscopy, X-ray diffraction and Fourier-transform infrared spectroscopy, etc. The hollow microspheres showed a well-defined spherical shape with median diameter of 30.3   μm and possessed a uniform surface with micro-wrinkles, which is in favor of the drug release. Interpenetrating network cross-linking mechanism might result from the Schiff base reaction and the acetalization of hydroxyl and carbonyl between chitosan and vanillin. Berberine, as a model drug, was loaded in the microspheres and released in a sustainable manner. The drug loading ratio could change from 9.16% to 29.70% corresponding to the entrapment efficiency of 91.61% to 74.25%. In vitro cell culture study using MG63 cells and in vivo implantation clearly showed that the microspheres could provide favorable cell attachment and biocompatibility. The results confirm that the drug-loaded vanillin-crosslinked chitosan microspheres could be a worthy candidate either as carriers of drugs and cells, or as therapeutic matrix for bone repair and regeneration.

CAS / MDL: 111-30-8 121-33-5
研究领域: 生物材料学 · 药物递送系统 · 组织工程学
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Chemistry-An Asian Journal · 2025 · IF 3.3

Dual-Drug Loaded γ-Polyglutamic Acid Hydrogel with Hydrophilic Doxorubicin and Hydrophobic Camptothecin for Enhanced Tumor Therapy

Xiaoqing Jia,Yingfeng Wei,Xinyuan Zhang,Qiuping Gu,Youshun Liu,Shige Wang,Chunping Zhu

A dual-drug-loaded γ-polyglutamic acid (γ-PGA) hydrogel was synthesized, integrating third-generation dendrimers (G3) as cross-linkers for the simultaneous encapsulation of hydrophilic doxorubicin (DOX) and hydrophobic camptothecin (CPT). This hydrogel, formed via an efficient EDC/NHS-mediated reaction, demonstrated a biocompatible, porous, and pH-responsive network. The hydrophobic core of G3 significantly enhanced CPT loading, while γ-PGA facilitated effective DOX incorporation. Controlled drug release was observed, with DOX releasing faster in acidic tumor-like environments, optimizing therapeutic impact at the tumor site. In vitro studies highlighted the hydrogel's high biocompatibility and synergistic anticancer efficacy, reducing CT26 colon cancer cell viability more effectively than single-drug systems. In vivo experiments confirmed substantial tumor suppression, prolonged survival, and the absence of systemic toxicity in murine models. These results underscore the potential of this dual-drug delivery platform as a robust, multifunctional system for cancer therapy. The biocompatibility, degradability, and tailored drug release characteristics make this hydrogel a promising candidate for clinical translation, offering a novel solution for enhancing cancer treatment efficacy while minimizing side effects.

研究领域: 生物材料 · 药物递送 · 肿瘤学 · 生物医学工程
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POLYMER · 2012 · IF 3.438

Revisiting the time for removing the unloaded drug by dialysis method based on a biocompatible and biodegradable polymer vesicle

Liang Sun,Jianzhong Du

Polymer vesicles have been widely explored as drug delivery carriers. However, there are still several notable problems in the determination of the drug loading content (DLC) and the drug loading efficiency (DLE) of the drug delivery vehicles . Presented in this paper is the reconsideration of various important factors in the measurement of the DLC and DLE based on an ‘instant’ biocompatible and biodegradable polymer vesicle which can be directly dissolved in water, with a focus on the study on the time for removing the free drug. Firstly, an anti-cancer drug, doxorubicin (DOX), was successfully encapsulated into a highly biocompatible and biodegradable poly( ε -caprolactone)- block -poly[2-(methacryloyloxy)ethyl phosphorylcholine] (PCL- b -PMPC) diblock copolymer vesicle. Secondly, a specific methodology for removing the unencapsulated drug by dialysis method before the drug release experiment has been established to verify the DLC and the DLE of DOX. A number of important factors have been investigated, such as the period of time for removing the free drug, the temperature and the volume of water outside the dialysis tube, etc. Finally, the DOX release experiment was carried out at pH 5.0 and pH 7.4 with the cumulative release percentages of 55% and 35% after 24 h when the DOX feeding was 1.0 mg. As PCL- b -PMPC vesicles absorb UV light, the DOX encapsulated in polymer vesicles was calculated by subtracting the UV absorbance of vesicle solution from the UV absorbance of DOX-loaded vesicle solution at different DOX feedings of 1.0, 3.0 and 5.0 mg. We also found the appropriate calibration curves at different solution conditions were of great significance for the calculation of DLC and DLE.

研究领域: 药剂学 · 生物材料学
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Nanomaterials · 2018 ·Vol. 8 ·期 6 ·446 · IF 3.504

MIL-100(Al) Gels as an Excellent Platform Loaded with Doxorubicin Hydrochloride for pH-Triggered Drug Release and Anticancer Effect

Yuge Feng,Chengliang Wang,Fei Ke,Jianye Zang,Junfa Zhu

Slow and controlled release systems for drugs have attracted increasing interest recently. A highly efficient metal-organic gel (MOGs) drug delivery carrier, i.e., MIL-100(Al) gel, has been fabricated by a facile, low cost, and environmentally friendly one-pot process. The unique structure of MIL-100(Al) gels has led to a high loading efficiency (620 mg/g) towards doxorubicin hydrochloride (DOX) as a kind of anticancer drug. DOX-loaded MOGs exhibited high stability under physiological conditions and sustained release capacity of DOX for up to three days (under acidic environments). They further showed sustained drug release behavior and excellent antitumor effects in in vitro experiments on HeLa cells, in contrast with the extremely low biotoxicity of MOGs. Our work provides a promising way for anticancer therapy by utilizing this MOGs-based drug delivery system as an efficient and safe vehicle.Keywords:metal-organic gels;doxorubicin loading and release;pH-responsiveness;anticancer effect

研究领域: 材料科学 · 肿瘤学 · 药物递送
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Materials Science & Engineering C-Materials for Biological Applications · 2015 · IF 3.088

Comparison of bare and amino modified mesoporous silica@poly(ethyleneimine)s xerogel as indomethacin carrier: Superiority of amino modification

Jing Li,Lu Xu,Hongyu Wang,Baixue Yang,Hongzhuo Liu,Weisan Pan,Sanming Li

The purpose of this study was to facilely develop amino modified mesoporous silica xerogel synthesized using biomimetic method (B-AMSX) and to investigate its potential ability to be a drug carrier for loading poorly water-soluble drug indomethacin (IMC). For comparison, mesoporous silica xerogel without amino modification (B-MSX) was also synthesized using the same method. The changes of characteristics before and after IMC loading were systemically studied using fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), small angle X-ray scattering (SAXS) and nitrogen adsorption/desorption analysis. The results showed that B-MSX and B-AMSX were spherical nanoparticles with mesoporous structure. Compared with B-MSX, IMC loading capacity of B-AMSX was higher because more drug molecules can be loaded through stronger hydrogen bonding force. DSC and SAXS analysis confirmed the amorphous state of IMC after being loaded into B-MSX and B-AMSX. The in vitro drug release study revealed that B-MSX and B-AMSX improved IMC release significantly, and B-AMSX released IMC a little faster than B-MSX because of larger pore diameter of IMC-AMSX. B-MSX and B-AMSX degraded gradually in dissolution medium evidenced by color reaction and absorbance value, and B-AMSX degraded slower than B-MSX due to amino modification. In conclusion, B-AMSX with superiority of higher loading capacity and enhanced dissolution release can be considered to be a good candidate as drug carrier for IMC.

CAS / MDL: 919-30-2 681-84-5
研究领域: 药剂学 · 材料科学
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