Current Nanoscience
·
2023
·Vol. 21
·期 2
·319-332
·
IF 1.5
Yongshi Chen,Hao Wu,Geng Lu,Yi Zhu,Junfeng Ban,Xiaofang Li
BackgroundInfection is the main reason for the failure of the clinical application of guided tissue regeneration (GTR).ObjectiveThe aim of this study is to develop a membrane containing nanoparticles incorporated with the antimicrobial drug metronidazole (MTZ-NPs Membrane) to enhance drug permeation delivery into cells and promote periodontal tissue recovery and regeneration.MethodsWe prepared membranes containing nanoparticles incorporated with metronidazole (MTZ-NPs Membrane) and characterized the properties, such as mechanical properties, physicochemical properties, and release. Coumarin-6 was used to prepare a membrane containing nanoparticles incorporated with Coumarin-6 (C6-NPs Membrane) to evaluate the efficiency of the nanoparticles-loaded membranes on transmembrane entry into cells. Moreover, in vivo experiments were conducted to assess the effectiveness of the membrane.ResultsMTZ-NPs membrane had suitable mechanical strength; the drug was released by diffusion. Fourier Transform Infrared Spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) results showed the existence of metronidazole might be in the amorphous state in the membrane and had good compatibility with polymers. The in vitro cytotoxicity assays showed that the MTZ-NPs membrane was biocompatible. Cellular uptake of the C6-NPs membrane was significantly higher than that of the C6 membrane (p < 0.0001), signifying that encapsulating the drug in nanoparticles increases drug permeability and improves drug transport efficiency across the cellular membrane. The histological analysis showed that the MTZ-NPs membrane could promote periodontal tissue recovery.ConclusionMTZ-NPs membrane can improve drug penetration delivery into the cells and has a good prospect for the treatment of periodontal disease.
研究领域:
生物材料学
·
口腔医学
·
药剂学
✓ 已验证
DOI
高影响因子
Research
·
2023
·
IF 11
Bitao Lu,Enling Hu,Weiwei Ding,Wenyi Wang,Ruiqi Xie,Kun Yu,Fei Lu,Guangqian Lan,Fangyin Dai
Efficient hemostasis during emergency trauma with massive bleeding remains a critical challenge in prehospital settings. Thus, multiple hemostatic strategies are critical for treating large bleeding wounds. In this study, inspired by bombardier beetles to eject toxic spray for defense, a shape-memory aerogel with an aligned microchannel structure was proposed, employing thrombin-carrying microparticles loaded as a built-in engine to generate pulse ejections for enhanced drug permeation. Bioinspired aerogels, after contact with blood, can rapidly expand inside the wound, offering robust physical barrier blocking, sealing the bleeding wound, and generating a spontaneous local chemical reaction causing an explosive-like generation of CO2 microbubbles, which provide propulsion thrust to accelerate burst ejection from arrays of microchannels for deeper and faster drug diffusion. The ejection behavior, drug release kinetics, and permeation capacity were evaluated using a theoretical model and experimentally demonstrated. This novel aerogel showed remarkable hemostatic performance in severely bleeding wounds in a swine model and demonstrated good degradability and biocompatibility, displaying great potential for clinical application in humans.
研究领域:
生物医学工程
·
材料科学
·
创伤急救
✓ 已验证
DOI
高影响因子
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
·
2022
·Vol. 47
·期 5
·639-652
·
IF 2.569
Guan Chi,Yang Yingxin,Tian Dong,Jiang Zhiqiang,Zhang Huiying,Li Yali,Yan Jiaxiu,Zhang Congman,Chen Chun,Zhang Junhua,Wang Jing,Wang Yu,Du Hongwen,Zhou Hongyu,Wang Tao
Background and Objective Oral bioavailability ( F ) is one of the key factors that need to be determined in drug discovery. This factor is determined by the permeability and solubility of new molecule entities (NMEs) according to the biopharmaceutics classification system (BCS). Methods In the present study, we evaluated the permeability of 22 drugs in rat intestinal tissues using an Ussing chamber system and correlated the permeability with data on human intestinal absorption ( F a ) and intestinal availability ( F a × F g ) reported in the literature. Results The rat intestinal permeability data were better correlated with the combined effect of the absorbed fraction ( F a ) and the fraction escaping intestinal metabolism ( F g ) than F a itself. Clear regional dependent absorption was observed for most of the test drugs, and ileal P app was generally higher than that in other segments. Finally, the function of the efflux transporter P-glycoprotein (P-gp) with regard to oral absorption of substrates was evaluated with an Ussing chamber. We also demonstrated that the rat intestinal stability of the three cytochrome P450 (CYP) substrates was consistent with the human data. Conclusion An Ussing chamber system incorporating rat intestinal tissue would be a valuable tool to predict human intestinal absorption and metabolism for molecules with various physicochemical properties.
研究领域:
药理学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Xiaoyuan Yang,Yujia Tang,Meng Wang,Yixuan Wang,Wenxiu Wang,Meilu Pang,Yuehong Xu
Psoriasis is an immune-mediated skin disorder that affects populations worldwide. Methotrexate (MTX) is a cytotoxic drug with powerful anti-proliferative and anti-inflammatory effects that has gained prominence in treating inflammatory diseases including psoriasis. However, low solubility and side effects through oral administration hinder its systemic application. In this study, we developed a novel niosomes based on ceramide (cerosomes) to co-deliver MTX and nicotinamide (NIC), i.e., MTX/NIC cerosomes, for topically treating psoriasis with the aim to enhancing the efficacy and reducing the toxicity. NIC significantly solublized MTX by forming hydrogen bonds with MTX. In vitro and in vivo permeation studies showed that the cerosomes significantly promoted drug permeation through and retention in the skin, and the enhancing mechanism was clarified by Fourier transform infrared and Raman spectroscopy. MTX/NIC cerosomes exhibited strong anti-proliferation effect on lipopolysaccharide- irritated HaCaT cells by arresting the cell cycle at S phase and inducing apoptosis. Importantly, compared to MTX oral administration, topical application of MTX/NIC cerosomes on imiquimod (IMQ)-induced psoriatic mouse model exhibited a superior performance in ameliorating skin lesions, reducing spleen index and epidermal thickness, and downregulating the mRNA expression levels of proinflammatory cytokines including TNFα, IL-23, IL-17A, IL-6, IL-1β, and IL-22. Taken together, MTX/NIC cerosomes is a promising approach for psoriasis topical treatment.
研究领域:
药剂学
·
皮肤病学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
ACS Nano
·
2017
·
IF 13.942
Tianjiao Ji,Jiayan Lang,Jing Wang,Rong Cai,Yinlong Zhang,Feifei Qi,Lijing Zhang,Xiao Zhao,Wenjing Wu,Jihui Hao,Zhihai Qin,Ying Zhao,Guangjun Nie
During pancreatic tumor development, pancreatic stellate cells (PSCs) proliferate exuberantly to secrete extracellular matrix (ECM) in the tumor stroma, which presents major barriers for drug delivery and penetration in tumor tissue. Thus, down-regulating ECM levels via regulation of the PSCs may allow enhanced penetration of therapeutic drugs and thereby enhancing their therapeutic efficacy. To regulate the PSCs, a matrix metalloproteinase-2 (MMP-2) responsive peptide-hybrid liposome (MRPL) was constructed via coassembly of a tailor-designed MMP-2 responsive amphiphilic peptide and phospholipids. By utilizing the MMP-2-rich pathological environment, the pirfenidone (PFD) loaded MRPL (MRPL-PFD) can specifically release PFD at the pancreatic tumor site and down-regulate the multiple components of ECM expressed by the PSCs. This resulted in a significant increase in the penetration of gemcitabine into the tumor tissue and enhanced the efficacy of gemcitabine for pancreatic tumor. Our design tailored for antifibrosis of pancreatic cancer may provide a practical approach to build functional liposomes through supramolecular assembly, and regulation of ECM may be a promising adjuvant therapeutic strategy for pancreatic and other ECM-rich tumors.
研究领域:
药学
·
肿瘤学
·
生物材料
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Advanced Healthcare Materials
·
2019
·Vol. 8
·期 21
·1900898
·
IF 6.27
Ailin Hou,Guilan Quan,Beibei Yang,Chao Lu,Minglong Chen,Dan Yang,Lili Wang,Hu Liu,Xin Pan,Chuanbin Wu
The precise delivery of traditional dissolving microneedles (TDMNs) is often limited by the incomplete insertion due to the skin deformation, and the topical irritation is inevitable after long application, which ultimately results in compromised therapeutic efficacy. The aim of this study is to develop a rapidly separating dissolving microneedles (RSDMNs) system to achieve precise drug delivery. Therapeutic molecules are concentrated in the needle tip, while the blank separating part allows it to counteract skin indentation and rapidly separate from the base part. For rational design of an ideal separating part, and the molecular interactions between polymer and sugar are explored to make a good balance between mechanical performance and disintegration rate. The optimal RSDMNs can rapidly disintegrate in the mimic skin within 30 s, and the generated micropores in the skin reseal quickly. The ex vivo drug permeation of RSDMNs is significantly higher than that of TDMNs due to the complete needle imbed aided by the separating part. Furthermore, RSDMNs exhibit excellent in vivo anti-inflammation effect by remarkably down regulating the expression of TNF-α, IL-1β, and IL-6. In conclusion, the RSDMNs can reach precise drug delivery in a short time, which are more reliable for the self-administration strategy in the future.
研究领域:
药学
·
生物医学工程
·
药物递送系统
·
透皮给药
✓ 已验证
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Yi Xiang,Jing Liang,Lili Liu,Fei Wang,Lianfu Deng,Wenguo Cui
Electrospun fibers are excellent drug carriers and tissue engineering scaffolds. However, approaches to promote drug permeation in tissues with such carriers remain of great interest. Here, we propose a Quality-by-Design strategy to enhance drug permeation with self-nanoemulsifying electrospun fibers. Owing to the nanoemulsion which formed spontaneously when the polymer contacts aqueous solution such as body fluid, the resulting drug-laden fibrous membrane exhibits an outstanding drug permeation and therapeutic enhancement effect in a Franz cell experiment with ex vivo abdomen skin of rats, an artificial connective tissue model, and an in vivo rheumatoid arthritis model in rats. Meanwhile, the material also shows the capacity of rational regulation on the rate of drug release. These features of the present strategy establish our material as a new efficient approach for various clinical conditions calling for cure.
研究领域:
药剂学
·
药物递送系统
·
组织工程
·
材料科学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）