BIOMEDICINE & PHARMACOTHERAPY
·
2021
·
IF 6.53
Mariana Carolina Di Santo,Cecilia Luciana D’ Antoni,Ana Paula Domínguez Rubio,Agustina Alaimo,Oscar Edgardo Pérez
Plant-based polyphenols are natural compounds, present in fruits and vegetables. During recent years, polyphenols have gained special attention due to their nutraceutical and pharmacological activities for the prevention and treatment of human diseases. Nevertheless, their photosensitivity and low bioavailability, rapid metabolism and short biological half-life represent the major limitations for their use, which could be overcome by polyphenols encapsulation (flavonoids and non-flavonoids) into chitosan (CS)-tripolyphosphate (TPP) based nanoparticles (NP). In this review, we particularly focused on the ionic gelation method for the NP design. This contribution exhaustively discusses and compares results of scientific reports published in the last decade referring to ionic gelation applied for the protection, controlled and site-directed delivery of polyphenols. As a consequence, CS-TPP NP would constitute true platforms to transport polyphenols, or a combination of them, to be used for the designing of a new generation of drugs or nutraceuticals.
研究领域:
药剂学
·
生物技术
·
纳米技术
·
食品科学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
Carbohydrate Polymer Technologies and Applications
·
2025
·
IF 6.5
Yao Fu,Shuwen Tan,Xiaojia Xu,Wenlong Xing,Qi He,Yi Lu,Jia Tang,Xiaoyan Liu,Yu Fang
Natural polysaccharides are widely used in biomedical and pharmaceutical applications due to their biocompatibility and biodegradability. In this study, alginate-based Poly( N -vinylcaprolactam)- co -sodium alginate (P(VCL- co -SA)) microgel particles with different mass ratios of VCL/SA were synthesized and employed as stabilizers for curcumin-loaded Pickering emulsions. The obtained P(VCL- co -SA) microgels display a uniform, spherical morphology with low polydispersity. Moreover, the microgels demonstrated high interfacial activity at the dodecane/water interface, enabling the stabilization of dodecane-in-water emulsions across a broad pH range (3–9) at 25°C. At an elevated temperature (55°C), the emulsions remained stable at pH 6 and 9 (above the p K a of alginate, ∼3.5), while phase separation was observed at pH 3 below the p K a . The emulsion stability was further enhanced by optimizing Ca 2+ ion concentration. Furthermore, high internal phase soybean oil-in-water emulsions stabilized by P(VCL 83 - co -SA 17 ) microgels were successfully developed for curcumin encapsulation. The emulsions provided excellent protection for curcumin at room temperature. When incubated at 37°C, curcumin retention was significantly enhanced after the addition of Ca 2+ ions. Compared to previously reported systems that encapsulate curcumin in emulsions, the present approach exhibits superior performance, such as, encapsulation efficiency and retention rate. These findings provide insights into the development of high-performance Pickering emulsions that are stabilized by natural products and highlight their potential applications in food technology and the pharmaceutical industry.
研究领域:
食品科学与技术
·
药学
·
胶体与界面化学
·
高分子材料
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
·
2025
·
IF 3.4
Ling Chen,Xiao-Qin Ma,Hai-Li Wu,Shun Zhang,Jie-Feng Chen,Ning Lin,Qing Chen
Glioblastoma is a highly aggressive brain tumor with a poor prognosis and limited treatment options. Resveratrol (RES) and temozolomide (TMZ) both showed significant antitumor activity in GBM therapy. However, they are limited by poor solubility and stability, respectively. This study reports the first successful development of a resveratrol–temozolomide (RES–TMZ) cocrystal. The cocrystal significantly improved the solubility of RES and stability of TMZ, while it exhibited enhanced oral bioavailability in rats. In vitro cytotoxicity assays revealed that the RES–TMZ cocrystal showed superior inhibitory effects on U87 glioma cell proliferation and induced a higher apoptosis rate compared to that of monotherapy or physical mixtures. Mechanistic studies further demonstrated that the cocrystal exerts its effects through the mitochondrial-dependent apoptotic pathway, characterized by the upregulation of the proapoptotic protein Bax, downregulation of the antiapoptotic protein Bcl-2, activation of the caspase-3 pathway, and collapse of mitochondrial membrane potential coupled with a burst of intracellular reactive oxygen species. This work establishes pharmaceutical cocrystallization as a viable strategy to develop improved combination therapies for glioblastoma by overcoming drug limitations while potentiating therapeutic effects.
研究领域:
药学
·
肿瘤学
·
药物递送
·
晶体工程
·
凋亡研究
✓ 已验证
产品关联
DOI
高影响因子
Acta Pharmaceutica Sinica B
·
2025
·
IF 14.6
Haiyan Wang,Zhichao Sun,Chunlei Dai,Ran Liao,Ran Lin,Liying Wang,Wenjun Fu,Ruhe Zhang,Danwen Zheng,Zhongde Zhang,Jun Wu,Yuntao Liu
Acute respiratory distress syndrome (ARDS) is a life-threatening disease. In the clinical management of ARDS, current treatments such as glucocorticoids and protease inhibitors encounter significant challenges due to their high toxicity, limited administration routes, or poor targeting. These limitations highlight the urgent need for innovative therapeutic strategies. Songorine (Son), a compound derived from the herb Aconitum carmichaelii Debeaux, possesses good antioxidant and anti-inflammatory properties, exhibiting great potential for treating ARDS. However, its clinical application is partially constrained by low aqueous solubility and uncertain efficacy for ARDS. In this study, we developed a lung-targeted lipid nanomedicine by encapsulating Son in dipalmitoyl phosphatidylcholine (DPPC) liposomes (Son@liposome, Son-lipo). In a lipopolysaccharide-induced ARDS mouse model, we demonstrated that Son-lipo effectively targeted inflamed lung tissues with commendable biocompatibility. Further, Son-lipo significantly alleviated multiple ARDS phenotypes such as endothelial barrier damage, lung edema, pulmonary dysfunction, and alveolar lesion, which involved uncontrolled inflammation, oxidative stress, and cell apoptosis. RNA sequencing and Western blotting analyses revealed that Son-lipo inhibited the activation of the TLR4/NF- κ B/NLRP3 pathway responsible for ARDS. In conclusion, our study successfully developed an inhalable lipid-nanomedicine (Son-lipo) as a novel therapeutic strategy for ARDS. It elucidates the compound's ability to mitigate ARDS by repairing the endothelial barrier and reversing the inflammatory microenvironment, thereby providing a promising candidate drug for improving clinical management of ARDS.
研究领域:
纳米医学
·
呼吸系统疾病
·
药学
·
炎症研究
·
药物递送
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Yusong Zhang,Wei Shi,Huanlin Li,Lei Yang,Lei Hou,Cheng Ma
Enantiomers often exhibit significant differences or even diametrically opposed effects in pharmacological activity, toxicological properties, and metabolic behavior. Single-enantiomer drugs frequently demonstrate distinct advantages over the racemate. Therefore, accurately distinguishing between enantiomers and racemate is particularly crucial in the fields of chemistry and biomedicine. Racemates, as mixtures of equal amounts of the enantiomers (levorotating and dextrorotating), exist in two forms: racemic mixtures and racemic compounds. Racemic compounds exhibit differences from their enantiomers in absorption spectra, whereas racemic mixtures do not. This study investigates the absorption spectra of ( S )-(+)-2-phenylpropionic acid, ( R )-(-)-2-phenylpropionic acid, and their racemates using terahertz time-domain spectroscopy technology. Experimental results indicate that the enantiomer exhibits absorption peaks similar to those of the racemic mixture, but with a significant difference in absorption intensity. Further combined with density functional theory (DFT), theoretical spectral calculations were performed on the solid state and solution enantiomers based on single molecule and unit cell models respectively. It was found that the enantiomeric simulation spectra were highly consistent. After the sample transitioned from solid to solution state, changes in hydrogen bonds would change its molecular vibration characteristics and intermolecular interaction patterns.
研究领域:
物理化学
·
光谱学
·
手性化学
·
药学
·
计算化学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Man Zhang,Yuanpeng Wang
Transdermal insulin delivery using microneedle (MN) systems provides a promising, patient-friendly alternative to conventional subcutaneous injections. In this study, we developed a citric acid crosslinked carboxymethyl cellulose hydrogel microneedle (CMC-CA HMN) system capable of efficient insulin loading and rapid, pH-triggered release. Thermal esterification produced a CMC-CA hydrogel enriched with abundant carboxyl groups, facilitating electrostatic insulin loading under acidic conditions and immediate release at physiological pH. Fourier transform infrared (FTIR) spectroscopy confirmed successful ester crosslinking. The optimized hydrogel exhibited a high insulin loading capacity (8.7 mg g −1 ) driven primarily by electrostatic interactions. Mechanical tests demonstrated sufficient needle strength for reliable skin penetration, and ex vivo tests on porcine skin verified effective insertion and rapid insulin diffusion into dermal layers. In diabetic rats, a 0.6 IU insulin‑loaded HMN patch yielded glucose‑lowering and pharmacokinetic profiles closely matching those of a 0.2 IU subcutaneous injection, while 0.3 IU produced a smaller effect. Histological analyses further confirmed excellent biocompatibility. The developed CMC-CA HMN platform thus represents a scalable, safe, and efficient strategy for transdermal insulin delivery, substantially advancing the clinical potential of microneedle-mediated protein therapies.
研究领域:
药学
·
药物递送
·
生物材料
·
纳米医学
·
糖尿病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMACROMOLECULES
·
2025
·
IF 5.4
Yu Sun,Li Cui,Wanqiu Peng,Rong Chen,Xueneng Guan,Jiangyun Liu
Parkinson’s disease (PD) is difficult to treat clinically and lacks an effective treatment. The aim of this study was to synthesize and characterize butyrate-modified hyaluronic acid (HA-But), validate its therapeutic efficacy, and elucidate its mechanisms of action in PD. Behavioral tests, including the open field test, Y-maze, and elevated plus maze test, demonstrated that HA-But significantly alleviated motor dysfunction in PD mice. ELISA results indicated a marked reduction in pro-inflammatory cytokine levels following the HA-But treatment. In addition, immunohistochemistry, immunofluorescence, and Western blot analyses revealed that HA-But improved dopaminergic neuron survival and reduced α-synuclein aggregation. Furthermore, HA-But activated PINK1/Parkin-mediated mitophagy, modulated gut microbiota composition, and increased short-chain fatty acid (SCFA) levels, especially butyric acid. Combining HA-But with gastrodin further improved the PD symptoms in mice. These findings suggested the potential of HA-But as a novel approach for PD treatment.
研究领域:
神经科学
·
药学
·
分子生物学
·
肠脑轴
·
神经退行性疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2025
·
IF 8.1
Yang Wang,Yanan Fu,Meiying Wu,Haoqiang Wan,Xinchun Chen,Lanlan Ge,Chenyan Shi,Yangfan Li,Xiaobin Zeng,Tianqi Wang
The chemotherapeutic drug doxorubicin (DOX) has been demonstrated to trigger pyroptosis in tumor cells at exceptionally high concentrations. Nevertheless, the administration of DOX at suprapharmacological doses could cause acute off-target cytotoxicity and severe adverse effects. Herein, a biflavonoid derivative, F24, was found to improve the sensitivity of hepatocellular carcinoma (HCC) cells to low-dose DOX and reduce the adverse effects of DOX. We demonstrated that F24 synergized with low-dose DOX to increase pyroptosis and autophagy in HCC cells through dual-target CDK6 inhibition/p53 activation at a proper ratio. To achieve this synergistic effect, nanodiscs with large hydrophobic cavities were selected to codeliver the low-dose hydrophobic drugs DOX and F24 (DOX-F24@Nanodisc, DF@N), which improved the tumor accumulation of the two drugs and ensured precise drug ratio integrity within the tumor cells. DF@N can trigger gasdermin-E (GSDME)-based pyroptosis in tumor cells, accompanied by the cleavage of caspase-3. Strikingly, knocking out GSDME or caspase-3 redirected DF@N-driven cellular death from the pyroptosis pathway to the apoptotic pathway. Furthermore, DF@N administration suppressed tumor growth and activated pyroptosis in a Huh7 mouse xenograft tumor model. Overall, F24 was found to induce autophagy by targeting CDK6 and had a synergistic effect on DOX-induced pyroptosis. These results indicate that the pyroptosis-induced DF@N nanodisc system provides an effective and secure therapeutic strategy for treating HCC.
研究领域:
肿瘤学
·
药学
·
分子生物学
·
纳米医学
·
癌症治疗
·
细胞死亡机制
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD SCIENCE
·
2025
·Vol. 90
·期 12
·e70725
·
IF 3.4
Jing Jing,Huizhen Li,Cheng Li,Mengjie Xu,Yana Zhao,Jianlan Cui,Zhijun Zhang
The leaves of Hemerocallis citrina Baroni ( H. citrina Baroni) are a promising source of bioactive polysaccharides (HCLP). However, the presence of abundant pigments in crude HCLP complicates subsequent purification and analysis, making an effective decolorization step essential. A model of decolorization conditions of HCLP was established using single factor and response surface methodology (RSM), and the optimal decolorization conditions were obtained. Subsequently, the HCLP-0.1 was successfully isolated via DEAE-52 cellulose column. Structural characterization revealed that HCLP-0.1 has a molecular weight ( M w ) of 8317.64 Da, composed of Man, GlcN, Rha, GlcA, GalA, Glc, Gal, Xyl, and Ara. Furthermore, HCLP-0.1 was characterized by α- and β-pyranose configurations, crystallinity, and an irregular triple-helical structure. Thermal analysis demonstrated excellent thermal stability. Antioxidant assays revealed that HCLP-0.1 possesses significant concentration-dependent (0.1–2.0 mg/mL) scavenging capacity against ABTS, hydroxyl, and DPPH radicals. These results support the potential of HCLP as a natural antioxidant, providing a solid basis for its future application in functional foods or pharmaceuticals.
研究领域:
生物化学
·
天然产物化学
·
食品科学与技术
·
药学
·
多糖研究
·
抗氧化研究
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2025
·
IF 8.2
Shiting Xu,Wenhao Gao,Shuang Lin,Bingkun Kang,Xiaoting Shi,Da Zheng,Longyun Xiao,Lingjun Zeng,Qian Zhang,Wenjun Tian,Hongtao Song
Ferroptosis, a newly recognized mode of regulated cell death characterized by iron-mediated accumulation of lipid peroxides, represents a viable treatment strategy for metastatic colorectal cancer (CRC). Nonetheless, the clinical effectiveness of single-agent ferroptosis inducers is constrained by the adaptive and self-repair capabilities of tumor cells. To address this limitation, this study proposes a self-amplifying ferroptosis nanodrug SOR/QUE@HSA, which is engineered by coencapsulating sorafenib (SOR) and quercetin (QUE) within human serum albumin (HSA). SOR/QUE@HSA offers a uniform structure, improved stability, and enhanced drug delivery efficiency. The released SOR and QUE impeded the uptake of glutamine (Gln) and cysteine (Cys) by targeting solute carrier family 7 member 11 (SLC7A11) and solute carrier family 1 member 5 (SLC1A5), respectively. This dual inhibition consequently disrupts the synthesis of glutathione (GSH), resulting in a marked downregulation of glutathione peroxidase 4 (GPX4), ultimately enhancing ferroptosis in CRC. Additionally, QUE inhibits hexokinase-II (HK-II), which results in decreased ATP production and lactate (LA) generation, thereby impeding tumor metastasis. In summary, our findings unveil a plausible role for the therapeutic potential of QUE as a ferroptosis-inducing anticancer agent, and the synergistic combination of QUE and SOR within this nanoplatform presents an option for treating metastatic CRC.
研究领域:
肿瘤学
·
纳米医学
·
分子生物学
·
药学
·
细胞死亡研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2025
·
IF 4.5
Yanzhi Wang,Shanshan Sun,Mengqian Liu,Sai Zhang,Jiaxin Zheng,Hongmin Liu
Paclitaxel (PTX) is a widely used chemotherapeutic agent, but its clinical utility is limited by poor solubility, systemic toxicity, and inadequate tumor targeting. To address these challenges, we developed a novel glycyrrhetinic acid–biguanide conjugate (GABG) capable of forming self-assembling, carrier-free nanoparticles. GABG’s amphiphilic and self-emulsifying properties enable efficient PTX encapsulation and targeted delivery. PTX-loaded GABG nanoparticles (PTX@GABG NPs) significantly enhanced cytotoxicity against multiple tumor cell lines, improving cellular uptake and selective tumor accumulation. Molecular dynamics simulations confirmed stable PTX–GABG interactions, supporting the structural integrity of the nanocomplex. In vivo biodistribution studies revealed strong liver tropism following intraperitoneal administration, with tumor-targeting efficiency comparable to intravenous delivery. The cellular uptake of GABG nanoparticles in H22 cells was shown to be governed by GA receptor-mediated endocytosis, with both caveolae- and clathrin-dependent pathways contributing to their efficient internalization. Therapeutic evaluations demonstrated that PTX@GABG NPs induced superior tumor inhibition compared to free PTX, driven by enhanced apoptosis and ROS-mediated cytotoxicity. Notably, the antitumor efficacy of intraperitoneal administration was comparable to that of intravenous injection, highlighting its potential as a less invasive yet effective delivery route. Given its dual functionality in drug encapsulation and liver targeting, GABG presents a promising platform for hepatic tumor therapy. Its cationic biguanide groups may further enable encapsulation of biopharmaceuticals such as RNA, underscoring its versatility in precision nanomedicine.
研究领域:
纳米医学
·
药学
·
癌症治疗
·
药物递送
·
分子药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2025
·
IF 3.8
Chen Biqing,Gao Jiayin,Sun Haizhu,Zhao Yinghan,Liu Yan,Lv Xinpeng,Qiu Xiaohong,Li Yang
Chemotherapy remains a cornerstone in the treatment of multiple solid and gynecologic malignancies, including endometrial cancer, ovarian cancer, and breast cancer. Carboplatin, epirubicin, gemcitabine, paclitaxel, topotecan, and docetaxel are widely used in combination regimens; however, there is still a lack of sensitive, rapid, and multiplex technologies for real-time monitoring of chemotherapeutic drug concentrations. In this study, we developed a carboxyl-polyethylene glycol (PEG)-modified magnetite (Fe₃O₄@PEG) nanoplatform combined with artificial intelligence (AI)-driven spectral analysis to achieve ultra-sensitive and multiplex detection of six chemotherapeutic drugs. Fe₃O₄ nanoparticles were synthesized by co-precipitation and subsequently functionalized with carboxyl-PEG to enhance drug capture efficiency and resistance to matrix interference. Using a confocal Raman imaging system, SERS spectra of single and mixed drug systems were collected, and convolutional neural networks (CNNs) were employed for automated feature extraction and classification to enable qualitative and quantitative analysis. The constructed SERS platform achieved 10⁻⁷–10⁻⁸ milligrams per milliliter (mg/mL) detection limits for all six drugs in serum matrices, with classification accuracies exceeding 95% in multiplex mixtures. For improved quantitative accuracy and normalization, the 2078 cm⁻ 1 Raman peak of deuterated methanol (CD₃OD) was employed as an internal standard to correct for potential fluctuations in laser intensity and sample concentration. Within the simulated therapeutic concentration range, quantitative regression yielded R 2 ≥ 0.98. This AI-SERS platform offers advantages of multiplex detection, trace-level sensitivity, and strong anti-matrix interference, holding great promise for pharmacokinetic monitoring and individualized chemotherapy optimization across a broad range of solid tumors. Graphical abstract Schematic illustration of an AI-integrated Fe 3 O 4 @PEG–SERS nanoplatform for multiplex detection of six chemotherapeutic agents (carboplatin, epirubicin, gemcitabine, paclitaxel, topotecan, and docetaxel). Carboxyl-PEG–modified magnetite nanoparticles enhance drug adsorption and stability, while convolutional neural networks enable accurate qualitative and quantitative spectral analysis for personalized chemotherapy optimization.
研究领域:
肿瘤学
·
纳米技术
·
分析化学
·
生物医学工程
·
药学
·
人工智能
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）