NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
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2026
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IF 4
Morsy Wafaa A.,Heibashy Dina M. I.,Eissa Shimaa M.,Elshafiey Sara H.
Pulmonary fibrosis is a progressive and fatal lung disease characterized by excessive extracellular matrix deposition. Bleomycin (BLM)-induced pulmonary fibrosis is a widely used experimental model that replicates key pathological features of the human disease. Berberine (Brb), a natural phytochemical, exhibits anti-inflammatory and immunomodulatory properties. However, its clinical application is restricted by poor bioavailability. Nano-formulation of Brb (Nano-Brb) may enhance its therapeutic potential. Therefore, this study aimed to evaluate the protective effects of Nano-Brb against BLM-induced pulmonary fibrosis in rats and to elucidate the underlying biochemical, histopathological, immunohistochemical, and molecular mechanisms. Thirty adult male albino rats were randomly assigned into six groups: control, Brb-treated (100 mg/kg body weight), Nano-Brb-treated (100 mg/kg body weight), BLM-treated (single intratracheal dose of 5 mg/kg body weight), BLM + Brb, and BLM + Nano-Brb. Nano-Brb significantly attenuated BLM-induced pulmonary fibrosis, as evidenced by reduced pro-inflammatory cytokines, including interleukin-1β (IL-1β), interleukin-4 (IL-4), interleukin-13 (IL-13), and tumor necrosis factor-alpha (TNF-α), as well as decreased matrix metalloproteinases (MMPs). It also modulated nuclear factor kappa B (NF-κB) and transforming growth factor-beta (TGF-β) signaling and reduced collagen type I (Col-I) and collagen type III (Col-III), connective tissue growth factor (CTGF), and neutrophil elastase (NE). Histopathological, histochemical, and immunohistochemical investigations confirmed marked improvement in lung architecture. Furthermore, Nano-Brb reduced transforming growth factor-beta 1 (TGF-β1) expression and upregulated pulmonary sirtuin 3 (SIRT3) gene expression. The present results suggest that Nano-Brb enhanced the lung’s architecture and functional performance by modulating inflammatory cytokines, oxidative stress, gene expression, and histopathological damage. Graphical Created in https://BioRender.com . Schematic representation of the experimental design: rats were administered bleomycin to induce pulmonary fibrosis, followed by treatment with berberine or nano-berberine. The study assessed oxidative stress markers, inflammatory cytokines, histopathological and immunohistochemical changes, and gene expression related to fibrosis and inflammation. The nano-formulation demonstrated superior therapeutic efficacy.
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Materials Today Bio
·
2025
·
IF 10.2
Si Shen,Wang Shen,Lu Wang,Bin Sun,Yongli Zhang,Yong Zhang,Ruoyang Jia,Yang Wu,Xue Chen,Keang Cao,Yuqing Fang,Hongmei Xia
Psoriasis is a common immune-mediated squamous skin disease, primarily characterized by the over proliferation of keratinocytes and a significant thickening of the stratum corneum. Traditional systemic drug delivery therapies often fall short due to low drug bioavailability and significant toxic side effects. Topical medications, while capable of achieving local or systemic treatment via transdermal routes, face limitations in psoriasis patients due to the abnormal thickening of the epidermis, which reduces skin permeability and hampers drug penetration efficiency. Hydrogel microneedles, as an emerging transdermal drug delivery technology, offer significant advantages such as high permeability, ease of use, low toxicity and side effects, and controlled release. Therefore, this study developed a liposome-hydrogel microneedle delivery system for the administration of berberine hydrochloride. We successfully prepared berberine hydrochloride-loaded liposomes (Ber-LPs) with high encapsulation efficiency and good stability, and integrated them into hydrogel microneedles crosslinked with PVA and PEGDA (Ber-LPs-PEGDA&PVA MNs) through a photocuring method. These microneedles exhibit an intact structure, high mechanical strength, and effective skin penetration. In vivo studies on anti-psoriatic effects showed that, compared to the model group, Ber-LPs-PEGDA&PVA MNs significantly alleviated imiquimod-induced psoriasis-like symptoms in mice, reduced skin epidermal thickness, decreased the expression levels of inflammatory cytokines, and lowered the expression of CD31 and VEGF, demonstrating excellent therapeutic efficacy. Additionally, the microneedles exhibited good drug release properties, antioxidant capacity, and biocompatibility. The novel hydrogel microneedle drug delivery system developed in this study offers a safe and effective solution for the treatment of psoriasis, with significant potential for clinical application.
研究领域:
药剂学
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皮肤病学
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生物医学工程
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Regenerative Biomaterials
·
2024
·
IF 5.6
Wang Qiuyu,Zhang Sai,Jiang Jiayi,Chen Shaojuan,Ramakrishna Seeram,Zhao Wenwen,Yang Fan,Wu Shaohua
A dressing patch made of radially oriented poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanofibers was successfully manufactured with a modified electrospinning strategy. The as-electrospun PHBV radially oriented nanofiber dressing patch exhibited uniform and bead-free nanofibrous morphology and innovative radially oriented arrangement, which was demonstrated to possess obviously improved mechanical property, increased surface hydrophilicity, and enhanced biological properties compared to the PHBV nanofiber dressing patch control with traditionally randomly oriented pattern. Interestingly, it was found that the radially oriented pattern could induce the cell migration from the periphery to the center along the radially oriented nanofibers in a rapid manner. In order to further improve the bio-function of PHBV radially oriented nanofiber dressing patch, berberine (Beri, an isoquinoline alkaloid) with two different concentrations were encapsulated into PHBV nanofibers during electrospinning, which were found to present a sustained drug release behavior for nearly one month. Importantly, the addition of Beri could impart the dressing patch with excellent anti-inflammatory property by significantly inhibiting the secretion of pro-inflammatory factors of M1 macrophages, and also showed an additive influence on promoting the proliferation of human dermal fibroblasts (HDFs), as well as inhibiting the growth of E. coli, S. aureus, and C. albicans, compared with the Beri-free dressing patch. In the animal studies, the electrospun PHBV radially oriented nanofiber dressing patch loading with high Beri content was found to obviously accelerate the healing process of diabetic mouse full-thickness skin wound with shortened healing time (100% wound closure rate after 18 days’ treatment) and improved healing quality (improved collagen deposition, enhanced re-epithelialization and neovascularization, and increased hair follicles). In all, this study reported an innovative therapeutic strategy integrating the excellent physical cues of electrospun PHBV radially oriented nanofiber dressing patch with the multiple biological cues of Beri for the effective treatment of hard-to-heal diabetic wounds.
研究领域:
生物医学工程
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材料科学
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伤口愈合
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药学
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组织工程
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JOURNAL OF MOLECULAR STRUCTURE
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2025
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IF 4.7
Yangsheng Yu,Yijing Wang,Xuening Zhang,Dawei Yang,Bangming Cao
Myocardial infarction (MI) remains a leading cause of mortality, primarily due to ischemia/reperfusion injury and the limited regenerative capacity of cardiomyocytes. To overcome the limitations of free berberine (BBR)—such as low bioavailability, poor myocardial targeting, and rapid systemic clearance—we developed a multifunctional nanoplatform (1-CS@Zn-CPs@BBR) integrating chitosan, Zn(II)-based coordination polymers, and BBR. The design rationale was guided by recent advances in nanocarrier engineering and supported by literature evidence highlighting the importance of responsive delivery and biointerface stability under oxidative conditions. The constructed system demonstrates dual pH/ROS-responsive release, favorable electrochemical properties for real-time monitoring, and excellent biocompatibility. In vitro studies confirmed enhanced cardioprotective efficacy compared with free BBR, indicating improved delivery precision and cellular protection. Collectively, this work provides a well-supported and literature-informed strategy for integrating targeted delivery and electrochemical monitoring into a single nanoplatform, representing a promising and efficient alternative to conventional therapeutic approaches for myocardial injury.
研究领域:
纳米医学
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心血管药理学
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药物递送系统
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生物医学工程
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY
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2018
·Vol. 410
·期 25
·6489-6495
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IF 3.307
Wen Aoli,Peng Xiaoxiao,Zhang Pingping,Long Yunfei,Gong Huiming,Xie Qingru,Yue Ming,Chen Shu
Berberine hydrochloride (BHC), a natural isoquinoline alkaloid, is widely applied as a an agent in traditional Chinese medicine. Almost all the traditional methods for BHC detection require complicated preprocessing steps or expensive instruments. In this article, we report a simple, rapid, sensitive, and selective method for BHC detection using fluorescent gold nanoclusters (F-AuNCs) as the fluorescent probe with a large Stokes shift of 237 nm. The F-AuNCs prepared with citrate-stabilized stannous chloride and hydrogen tetrachloroaurate(III) as raw materials in an aqueous medium display strong and stable fluorescence at 566 nm. When F-AuNCs are mixed with BHC, the fluorescence of F-AuNCs is effectively quenched. Under optimized conditions, this method allows sensitive and selective measurements of BHC in a concentration ranging from 1.0 × 10 -6 to 1.0 × 10 -4 mol L -1 with a detection limit of 7.5 × 10 -8 mol L -1 , which is relatively low among reported spectral methods. This method provides excellent selectivity for the detection of BHC against inorganic anions and natural amino acids. In addition, the BHC content in two different types of berberine tablets was successfully determined by this method and the results showed high accuracy.
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研究领域:
分析化学
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药学
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纳米科技
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高影响因子
International Journal of Nanomedicine
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2022
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IF 7.033
Yuying Xu,Jintao Huang,Yapei Fan,Haiyue Long,Minting Liang,Qunjie Chen,Zhiping Wang,Chaoxi Wu,Yifei Wang
Aim This study focuses on constructing of an anti-inflammatory drug delivery system by encapsulation of berberine in the β-glucan nanoparticles and evaluates its effect on treating ulcerative colitis. Methods β-Glucan and the anti-inflammatory drug berberine (BER) are self-assembled into nanoparticles to construct a drug delivery system (GLC/BER). The interaction between the drug and the carrier was characterized by circular dichroism, ultraviolet-visible spectroscopy, and dynamic light scattering. The anti-inflammatory effect of the GLC/BER was evaluated through a lipopolysaccharide (LPS)-induced RAW264.7 macrophage inflammation model and a sodium sulfate (DSS)-induced C57BL/6 mouse ulcerative colitis model. Results The GLC/BER nanoparticles have a particle size of 80–120 nm and a high encapsulation efficiency of 37.8±4.21%. In the LPS-induced RAW264.7 macrophage inflammation model, GLC/BER significantly promoted the uptake of BER by RAW264.7 cells. RT-PCR and ELISA assay showed that it could significantly inhibit the inflammatory factors including IL-1β, IL-6 and COX-2. Furthermore, GLC/BER shows inhibiting effect on the secretion of pro-inflammatory factors such as IL-1β and IL-6, down-regulating the production of nitrite oxide; in animal studies, GLC/BER was found to exert a relieving effect on mice colitis. Conclusion The study found that GLC/BER has an anti-inflammatory effect in vitro and in vivo, and the GLC carrier improves the potency and bioavailability of BER, providing a new type of nanomedicine for the treatment of colitis.
研究领域:
药学
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纳米技术
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炎症研究
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胃肠病学
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Scientific Reports
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2021
·Vol. 11
·期 1
·1-12
·
IF 4.38
Ma Lan,Yu Yijun,Liu Hanxiao,Sun Weibin,Lin Zitong,Liu Chao,Miao Leiying
The repair of skeletal defects in maxillofacial region remains an intractable problem, the rising technology of bone tissue engineering provides a new strategy to solve it. Scaffolds, a crucial element of tissue engineering, must have favorable biocompatibility as well as osteoinductivity. In this study, we prepared berberine/polycaprolactone/collagen (BBR/PCL/COL) scaffolds with different concentrations of berberine (BBR) (25, 50, 75 and 100 μg/mL) through electrospinning. The influence of dosage on scaffold morphology, cell behavior and in vivo bone defect repair were systematically studied. The results indicated that scaffolds could release BBR stably for up to 27 days. Experiments in vitro showed that BBR/PCL/COL scaffolds had appropriate biocompatibility in the concentration of 25–75 μg/mL, and 50 and 75 μg/mL scaffolds could significantly promote osteogenic differentiation of dental pulp stem cells. Scaffold with 50 μg/mL BBR was implanted into the critical bone defect of rats to evaluate the ability of bone repair in vivo. It was found that BBR/PCL/COL scaffold performed more favorable than polycaprolactone/collagen (PCL/COL) scaffold. Overall, our study is the first to evaluate the capability of in vivo bone repair of BBR/PCL/COL electrospun scaffold. The results indicate that BBR/PCL/COL scaffold has prospective potential for tissue engineering applications in bone regeneration therapy.
研究领域:
生物医学工程
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组织工程
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再生医学
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JOURNAL OF CONTROLLED RELEASE
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2020
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IF 7.727
Yuanna Shen,Yiqing Zou,Xiaonan Chen,Pengyu Li,Yiqin Rao,Xuan Yang,Yingying Sun,Haiyan Hu
The prevalence of infections with Helicobacter pylori ( H. pylori ) has progressively increased worldwide, which demonstrated to be closely correlated to its biofilm formation. H. pylori biofilms protect the bacteria by significantly decreasing their sensitivity to antibiotics. Moreover, H. pylori colonizes on the gastrointestinal tract epithelium which is covered by mucus layer, acting as another barrier to prevent antibacterial agents from reaching the colonization sites. Herein, we prepared four types of versatile self-assembled nanodrugs (BD/RHL NDs) containing lipophilic alkyl berberine derivatives (BDs) and rhamnolipids (RHL) to overcome the dual obstructions of both mucus layer and biofilms. Molecular dynamics simulations estimated that the driving forces for self-assembly of BD/RHL NDs were electrostatic and hydrophobic interactions. BD/RHL NDs, characterized by appropriate size, negative charge and enhanced hydrophilicity, successfully penetrated through mucus layer without interacting with mucins. In in vitro experiments, BD/RHL NDs exhibited substantial ability to eradicate H. pylori biofilms by destroying their extracellular polymeric substances (EPS) and killing planktonic H. pylori . Furthermore, BD/RHL NDs inhibited the adherence of H. pylori on both biotic and abiotic surfaces, therefore cut off the critical step of the biofilm re-formation which was associated with the recrudescence of infections. In an H. pylori- infected mice model, C10-BD/RHL NDs group showed 40 folds less remnant H. pylori and greater mucosal protection compared with the conventional clinical triple therapy. In conclusion, BD/RHL NDs could penetrate through mucus layer and effectively eradicate H. pylori biofilms in vitro and in vivo , providing a novel strategy for clinical treatment of biofilm-related infections.
研究领域:
药学
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微生物学
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纳米技术
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传染病学
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COLLOIDS AND SURFACES B-BIOINTERFACES
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2020
·
IF 4.389
Jia Jin,Ming Xu,Yixuan Liu,Zhixiao Ji,Kaili Dai,Lun Zhang,Lei Wang,Fei Ye,Gang Chen,Zhengbing Lv
It is important to develop effective, biocompatible, easily stored and affordable hemostats for controlling bleeding and preventing infection in prehospital trauma. In this study, we synthesized a series of alginate-based composite microspheres coated by different amounts of berberine (SCC-1B, SCC-5B and SCC-10B), which were further characterized using scanning electron microscopy (SEM), viscometer, particle analyzer and Fourier transform infrared (FT-IR) spectroscopy. The in vitro and vivo results demonstrated that compared to control group (SCC, Composite polysaccharide microspheres without berberine, and CMPHP, Commercial hemostatic agent), SCC-10B with proper content berberine (7%), not only exhibited inherent excellent antibacterial activity, but also enhanced hemostatic effect by increasing adhesion and aggregation of blood cells, which could be considered as synergistic effects. More importantly, through inserting berberine into the cross-linked network, biodegradability and biocompatibility of SCC-10B were also improved. Taken together, SCC-10B could be a candidate for emergency hemostatic and antibacterial treatment in prehospital trauma.
研究领域:
材料科学
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生物医学工程
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药剂学
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Frontiers in Pharmacology
·
2020
·
IF 4.225
Zhao Junli,Wang Yaqian,Gao Jie,Jing Yang,Xin Wenkuan
Previous studies showed that berberine, an alkaloid from Coptis Chinensis Franch, might exert a positive inotropic effect on the heart. However, the underlying mechanisms were unclear. Here, we reported that berberine at 10–20 µM increased the left ventricular (LV) developed pressure and the maximal rate of the pressure rising, and it increased the maximal rate of the pressure descending at 20 µM in Langendorff-perfused isolated rat hearts. These effects diminished with the concentration of berberine increasing to 50 µM. In the concentration range of 50–300 µM, berberine increased the isometric tension of isolated left ventricular muscle (LVM) strips with or without electrical stimulations, and it (30–300 µM) also increased the intracellular Ca2+ level in the isolated LV myocytes. The removal of extracellular Ca2+ hindered the berberine-induced increases in the tension of LVM strips and the intracellular Ca2+ level of LV myocytes. These suggested that berberine might exert its positive inotropic effects via enhancing Ca2+ influx. The blockade of L-type Ca2+ channels (LTCCs) with nifedipine significantly attenuated 300 μM berberine-induced tension increase in LVM strips but not the increase in the intracellular Ca2+ level. Berberine (300 μM) further increased the LVM tension following the treatment with the LTCC opener FPL-64716 (10 μM), indicating an LTCC-independent effect of berberine. Lowering extracellular Na+ attenuated the berberine-induced increases in both the tension of LVM strips and the intracellular Ca2+ level of LV myocytes. In conclusion, berberine might exert a positive inotropic effect on the isolated rat heart by enhancing the Ca2+ influx in LV myocytes; these were extracellular Na+-dependent.
研究领域:
药理学
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心血管生理学
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Haofeng Hu,Fulin Luo,Qian Zhang,Ming Xu,Xin Chen,Zhihao Liu,Haodong Xu,Lei Wang,Fei Ye,Kui Zhang,Bin Chen,Song Zheng,Jia Jin
In wound treatment, severe bleeding and infection are always primary challenges. Therefore, it is highly desired to develop novel dressing with both hemostatic and antibacterial capability. Herein, a series of biocomposite hemostatic films (BHFs) based alginate/chitosan/collagen-berberine have been prepared and well characterized for further biofunctional study. We have demonstrated that the hemostatic and antibacterial activities were significantly enhanced by calcium/berberine dual-crosslinking system in the film. Through the synergistic effects, BHF-6B exhibited a shorter in vivo clotting and wound healing time than that of commercial dressing in rat tail amputation and full-thickness skin defect models. Additionally, BHF-6B showed excellent bacteriostatic activity with long-term effects. Moreover, hemolysis and cytotoxicity tests in vitro illustrated the prominent biocompatibility of the composite films. Notably, BHF-6B could be degraded quickly and completely in vivo . Overall, the present work indicated that the functionalized BHF-6B has great potential as an absorbable biomaterial for wound treatment.
研究领域:
生物材料
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组织工程
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伤口愈合
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药学
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PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2022
·
IF 5.589
Zhe Wang,Xin Chen,Duanxiu Li,Enhe Bai,Hailu Zhang,Yanwen Duan,Yong Huang
Co-amorphous technology is an emerging approach for pharmaceutical engineering of drugs and drug leads with improved physicochemical properties and bioavailability. Platensimycin (PTM) is a promising natural antibiotic lead that acts on bacterial fatty acid synthase and exhibits excellent antibacterial activity . Despite great strides to improve its poor pharmacokinetics by medicinal chemistry and nanotechnology, there are no convenient oral delivery systems developed. Here, a co-amorphous system of PTM and berberine chloride (BCL) was developed for oral delivery of PTM. Co-amorphous PTM-BCL was prepared by rotary vacuum evaporation method, and systematically characterized by powder X-ray diffraction, temperature modulated differential scanning calorimetry , Fourier transform infrared spectroscopy (FTIR), and X-ray photoelectron spectroscopy (XPS). Compared with PTM or BCL alone, the equilibrium solubility and dissolution rate of both of them in the co-amorphous systems decreased significantly, showing the characteristics of sustained release . The molecular interactions between PTM and BCL were mediated by strong charged-mediated hydrogen bonds , based on FTIR, XPS, and NMR-based techniques. The co-amorphous PTM-BCL system showed excellent physiochemical stability at room and elevated (40 °C) temperature under dry conditions. The combination of PTM and BCL showed increased killing of a clinical isolated methicillin-resistant Staphylococcus aureus strain in killing checkerboard assays. Finally, co-amorphous PTM-BCL exhibited 2- or 3-fold longer half-life in rats than that of crystalline and amorphous PTM upon oral administration, respectively. Our study suggests a rational approach to realize the full potential of potent antibiotic PTM, which may be conveniently adapted for engineering of other important pharmaceutics.
研究领域:
药学
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生物医学工程
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PubMed
高影响因子
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