Nanomedicine
·
2025
·
IF 3.9
Xiaolin Zeng,Baoyan Chen,Peng Qian,Dongjun Jiang,Xianwei Wu,Shiqi Wei,Yangchen Xing,Yuxin Chen,Qianyu Zhang,Huali Chen
Aim To develop an enteric sustained-release nanoparticle formulations of aspirin for applicability to a broader population.Methods Aspirin-loaded nanoparticles were prepared using poly(lactic-co-glycolic acid) (PLGA) and the enteric polymer Eudragit L100–55 through an optimized oil-in-water emulsification solvent evaporation method. The nanoparticles were subjected to comprehensive physicochemical characterization, including particle size, zeta potential, and morphological analysis. Additionally, their stability, in vitro drug release profile, cytotoxicity, intestinal absorption, and in vivo pharmacokinetics were systematically evaluated.Results The nanoparticles exhibited well-defined spherical morphology, uniform particle size, and favorable surface charge, demonstrating excellent biocompatibility. In the in vitro drug release study, AS-PLGA@NPs exhibited pronounced enterolysis effect. The morphology of the nanoparticles was confirmed by scanning electron microscopy (SEM) at different release stages. In vivo intestinal absorption and pharmacokinetic studies in rats demonstrated that AS-PLGA-EL@NPs enhanced drug absorption, prolonged drug release, and showed higher bioavailability compared to conventional enteric-coated tablets.Conclusion The development and preparation of an oral enteric sustained-release nanoparticle delivery system for aspirin has the potential to serve a broader population, with promising applications in various therapeutic contexts.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2024
·Vol. 25
·期 23
·12825
·
IF 4.9
Lijun Ding,Xiao Luo,Qingyue Xian,Sishi Zhu,Weijia Wen
Fucoxanthin (FN), a carotenoid derived from brown seaweed and algae, offers significant health benefits. However, its unique structure leads to challenges in stability and bioavailability. To overcome these issues, we successfully encapsulated fucoxanthin in solid lipid nanoparticles (SLNs) utilizing health-safe materials, achieving remarkable results. SLNs exhibited a nanoscale size of 248.98 ± 4.0 nm, along with an impressive encapsulation efficiency of 98.30% ± 0.26% and a loading capacity of 5.48% ± 0.82% in lipid. The polydispersity index (PDI) was measured at 0.161 ± 0.03, indicating a narrow size distribution, while the high negative zeta potential of −32.93 ± 1.2 mV suggests excellent stability. Pharmacokinetic studies conducted in Sprague–Dawley rats revealed an exceptional oral bioavailability of 2723.16% compared to fucoxanthin crystals, likely attributed to the enhanced stability and improved cellular uptake of the SLNs. To further improve bioavailability, we creatively applied enteric coatings to the freeze-dried SLNs, effectively protecting fucoxanthin from gastric degradation, which is supported by in vitro digestion results. These findings underscore the potential of SLNs as a superior delivery system for fucoxanthin, significantly enhancing its therapeutic efficacy and broadening its application in the food and pharmaceutical industries.
研究领域:
药剂学
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食品科学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Nanoscale
·
2021
·Vol. 13
·期 7
·4278-4294
·
IF 7.79
Ruo-Yun Zhang,Kai Cheng,Yang Xuan,Xiao-Quan Yang,Jie An,Yong-Guo Hu,Bo Liu,Yuan-Di Zhao
Colorectal cancer is one of the malignant tumors with high morbidity and lethality. Its efficient diagnosis and treatment has important significance. In this study, the orthotopic cancer model mouse, which could perfectly simulate clinical inflammatory colorectal cancer, was constructed by chemical induction. Based on this model, a new pH/ultrasonic dual-response, step-targeting and precisely controlled-release enteric-coated granule was designed for the combined sonodynamic (SDT)-chemotherapy. The enteric-coated granule was fabricated by enwrapping carboxymethyl chitosan (CMC) on folic acid-modified phospholipid (SLB-FA) encapsulating mesoporous silicon-coated gold nanoparticles loaded with chlorin (Ce6) and doxorubicin hydrochloride (DOX), titled as Au@mSiO2/Ce6/DOX/SLB-FA@CMC (GMCDS-FA@CMC). The diameter of the Au@mSiO2/Ce6/DOX/SLB-FA (GMCDS-FA) nanoprobe was 61.21 nm and that of the GMCDS-FA@CMC enteric-coated granule was 1.1 μm. MTT results showed that the cell survival rate was still as high as 76.55 ± 1.27% when the concentration of GMCDS-FA was up to 200 μg mL−1, which can indicate the low cytotoxicity of the nanoprobe. According to CT imaging, the enteric-coated granule had the highest concentration in the colorectum of the orthotopic cancer mouse after 7–9 h with oral administration, and was nearly metabolized out of the body after 24 h. The in vitro and in vivo experiments showed that the targeting enteric-coated granule had the best effect of treatment and desired prognosis after combined SDT-chemotherapy.
研究领域:
肿瘤学
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药剂学
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医学影像学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2013
·Vol. 14
·期 12
·24305-24319
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IF 2.464
Jian Chen,Gui-Dong Huang,Si-Rong Tan,Jiao Guo,Zheng-Quan Su
This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS) enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%), plasticisers (TEC and DBS), dosage of plasticiser (10%, 20% and 30%) and coating weight (2%, 3% and 5%) were evaluated for drug release characteristics. Thein vitrorelease was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8) revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.
研究领域:
药剂学
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药物递送系统
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DOI
高影响因子
Arabian Journal of Chemistry
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2024
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IF 5.3
Shengan Hu,Chongmei Xu,Yinghui Zhang,Yue Du,Jinbao Tang,Lu Chen
In this study, the enteric swelling layer of capsules was prepared by optimizing the ratio of pullulan to gellan gum. The enteric-coating solution was prepared by dissolving polyacrylic acid resin III in 85 % ethanol, and the two were combined to form pullulan enteric-coated capsules (PECs). To elaborate further, Pullulan enteric-coated thin films (PEFs) were fabricated using the casting method, and their oxygen permeability (OP) and water vapor permeability (WVP) were assessed. Enteric capsules were prepared employing a secondary impregnation method. The cap gap and surface roughness of the capsules were characterized using Scanning Electron Microscopy (SEM) and Atomic Force Microscopy (AFM). The water content and hygroscopicity of the capsules were examined by employing the drying weight loss method. The pullulan-based enteric capsules (PECs) exhibited attributes such as low water content, hygroscopicity, brittleness, leakage resistance, and high impermeability. Finally, the in vitro release of aspirin from the enteric capsules was investigated. Results demonstrated the excellent combination of the enteric-coating layer and the swelling layer in the PECs. Compared with Gelatin enteric-coated capsules (GECs) on the market, it had a smaller cap gap, lower brittleness, weaker moisture absorption, and a good dissolution effect. Thus, it met the requirements of Chinese pharmacopeia, i.e., the ability to maintain integrity for 2 h in simulated gastric fluid and a drug-release rate reaching 80 % within 30 min in simulated intestinal fluid. This capsule also exhibited certain characteristics of a pulsatile drug-delivery system. This work proposed a potential method of preparing enteric hard capsules by using pullulan combined with polyacrylic acid resin III.
研究领域:
药剂学
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材料科学
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产品关联
DOI
高影响因子
Asian Journal of Pharmaceutical Sciences
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2014
·
IF 0
Shuling Kan,Jing Lu,Jianping Liu,Junlin Wang,Yi Zhao
The study aims to prepare naproxen enteric-coated pellets (NAP-ECPs) by fluid-bed coating using QbD principle. Risk assessment was firstly performed by using failure mode and effect analysis (FMEA) methodology. A Plackett–Burman design was then used for assessment of the most important variables affecting enteric-coated pellets characteristics. A Box–Behnken design was subsequently used for investigating the main, interactive, and quadratic effects of these variables on the response. By FMEA we discovered that eight factors should be considered to be high/important risk variables as compared with others. The responses of acid resistance and cumulative drug release were taken as critical quality attributes (CQAs). Pareto ranking analyses indicated that the coating weight gain (X 7 ), triethyl citrate percentage (X 1 ) and glycerol monostearate percentage (X 2 ) were the most significant factors affecting the selected responses out of the eight high-risk variables. Optimization with response surface method (RSM) further fully clarified the relationship between X 7 , X 1 , X 2 and CQAs, and design space was established based on the constraints set on the responses. Due to the extreme coincidence of the predicted value generated by model with the observed value, the accuracy and robustness of the model were confirmed. It could be concluded that a promising NAP-ECPs was successfully designed using QbD approach in a laboratory scale.
研究领域:
药剂学
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药物研发
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产品关联
DOI
Nature Nanotechnology
·
2024
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IF 38.1
Wu Ziyu,Chen Lin,Guo Wenyan,Wang Jun,Ni Haiya,Liu Jianing,Jiang Wentao,Shen Jian,Mao Chun,Zhou Min,Wan Mimi
Mitochondrial transplantation is an important therapeutic strategy for restoring energy supply in patients with ischaemic heart disease (IHD); however, it is limited by the invasiveness of the transplantation method and loss of mitochondrial activity. Here we report successful mitochondrial transplantation by oral administration for IHD therapy. A nitric-oxide-releasing nanomotor is modified on the mitochondria surface to obtain nanomotorized mitochondria with chemotactic targeting ability towards damaged heart tissue due to nanomotor action. The nanomotorized mitochondria are packaged in enteric capsules to protect them from gastric acid erosion. After oral delivery the mitochondria are released in the intestine, where they are quickly absorbed by intestinal cells and secreted into the bloodstream, allowing delivery to the damaged heart tissue. The regulation of disease microenvironment by the nanomotorized mitochondria can not only achieve rapid uptake and high retention of mitochondria by damaged cardiomyocytes but also maintains high activity of the transplanted mitochondria. Furthermore, results from animal models of IHD indicate that the accumulated nanomotorized mitochondria in the damaged heart tissue can regulate cardiac metabolism at the transcriptional level, thus preventing IHD progression. This strategy has the potential to change the therapeutic strategy used to treat IHD.
研究领域:
心脏病学
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纳米技术
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药学
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产品关联
DOI
PubMed
高影响因子
ACS Nano
·
2025
·
IF 16
Xinyue Zhang,Chen Peng,Wen Zhang,Nan Wang,Jiaxin Li,Wei He,Junping Xiao,Guanghui Ouyang,Yan Li
Oral administration of insulin for diabetes mellitus treatment has always been challenging due to a series of physiological barriers in the gastrointestinal tract. Herein, we developed glucose-responsive polyzwitterionic nanoparticles (NPs) for oral delivery of insulin, which were loaded into enteric capsules to overcome the barriers in the stomach. Glucose could bind with phenylboronic acid (PBA) of NPs to increase their negative charge density, thereby achieving glucose-responsive insulin release in a hyperglycemic environment. It was proven that NPs with polyzwitterionic poly[2-(methacryloyloxy)ethyl choline phosphate] (PMCP) could overcome the mucus barrier. In particular, polyzwitterionic PMCP could promote the NPs across the epithelial cell layer, which was attributed to the targeting and specific CP–PC interaction between polyzwitterionic PMCP and the epithelial cell membrane. The NPs in enteric capsules could significantly enhance the oral bioavailability of insulin to 14.2% in streptozotocin-induced type 1 diabetic mice, which resulted in a good hypoglycemic effect after single or continuous oral administration. Importantly, the NPs in enteric capsules did not induce any observable increase in terms of pro-inflammatory cytokines or pathological change of the small intestines. Therefore, this work provides a promising insulin oral delivery system for the safe and efficient treatment of diabetes mellitus.
研究领域:
药剂学
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纳米技术
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药物递送
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生物医学工程
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糖尿病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2024
·
IF 4.4
Chen Mingjun,Feng Yang,Luo Dan,Zhang Chen,Zhou Jing,Dai Hengheng,Lin Mingxiong,Tong ZhanQi
Purpose: Wuwei Kushen Changrong capsule (Composite Sophora Colon-soluble Capsule, CSCC) is a Chinese patent medicine developed to treat ulcerative colitis. Studies highlight CSCC potential efficacy for ulcerative colitis (UC) but unclear mechanism limits its widely treatment for patients. We aimed to investigate the anti-colitis efficacy of CSCC and explore the mechanism by which GPR43 inhibits the NLRP3/STAT3 signaling pathway, thereby mediating the protective effects of CSCC on the intestinal barrier.Methods: The protective effects of CSCC were evaluated in a murine ulcerative colitis model induced by 3% DSS. Assessments included body weight, Disease Activity Index (DAI) score, colon length, and histopathological score. Colon tissue, cell function, and immune-inflammatory status were evaluated using immunohistochemistry, immunofluorescence, ELISA, and real-time fluorescence quantitative PCR (RT-PCR). Protein expression levels of relevant pathways and receptors were measured using Western blot. All experiments were repeated.Results: CSCC protected mice from DSS-induced colitis by upregulating Gpr43, promoting the expression of ZO-1 and Occludin tight junction proteins. Mechanistically, CSCC inhibits the MEK4/JNK1/STAT3 activation pathway, consequently suppressing the STAT3/NLRP3/IL-1β pathway and inhibiting the production of inflammatory factors such as IL-17A.Conclusion: The mechanisms through which CSCC protects against DSS-induced colitis may include upregulating Gpr43, inhibiting the STAT3/NLRP3 pathway, and suppressing inflammation factors like IL-17A. These findings highlight the mechanisms underlying CSCC’s anti-colitis effects and suggest its potential as a therapeutic candidate for managing the progression of UC.
研究领域:
药理学
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免疫学
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胃肠病学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Donghao Gu,Yun Liu,Li Liu,Jinshuai Lan,Zhe Li,Ruifeng Zeng,Yue Ding,Weisan Pan
Oral nano-drug delivery systems offering combination therapy have garnered significant interest in colon cancer treatment due to their precision in targeting tumors and minimizing peripheral tissue exposure. However, challenges such as the complex gastrointestinal environment and effective retention of nanoparticles in the colon have impeded further advancement. We developed a novel oral drug delivery system designed for localized treatment of colon cancer via chemotherapy and photothermal therapy (PTT). This system utilized mesoporous polydopamine (MPDA) as a photothermal carrier for doxorubicin hydrochloride (DOX), with surface modification using folic acid (FA) to enhance systemic tumor targeting. Additionally, to ensure gastrointestinal retention and precise colon localization, the nanoparticles were coated with an enteric-soluble material, ES100, resulting in the formulation MPDA-FA-DOX/ES100. This formulation exhibited high photothermal conversion efficiency, robust photothermal stability, and responsive drug release under near-infrared (NIR) laser stimulation. FA modification significantly enhanced the cellular uptake of nanoparticles by CT26 cells, promoting greater cytotoxic effects through combined chemotherapy and PTT. In vivo , MPDA-FA-DOX/ES100 demonstrated superior accumulation in colon tumor tissues and substantial photothermal effects, and notably, the CT/PTT group demonstrated significant tumor growth inhibition along with excellent biocompatibility. Collectively, these findings highlight the clinical potential of MPDA-FA-DOX/ES100 as an effective platform for localized and synergistic CT/PTT of colon cancer.
研究领域:
药学
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癌症治疗
·
纳米技术
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
ADVANCED FUNCTIONAL MATERIALS
·
2024
·
IF 18.5
Jingwen Han,Jiamin Ye,Jiacheng Shi,Yueyue Fan,Xue Yuan,Ruiyan Li,Gaoli Niu,Muhammad Abubakar,Yong Kang,Xiaoyuan Ji
Given the unique anatomy and location of inflammatory bowel disease (IBD), oral pharmacological treatment is the mainstay for managing IBD because of its convenience and direct accessibility to the gastrointestinal tract. However, efficient delivery systems must be designed to navigate the harsh gastrointestinal environment during application. Here, an innovative oral drug delivery system was proposed using nanomotor (NM)-loaded soluble microcapsules for treating IBD. MnO 2 -Au-mSiO 2 NMs incorporate partially encapsulated MnO 2 antennas that convert reactive oxygen species into oxygen, autonomously propelling the NMs. Astaxanthin (AST), known for its anti-inflammatory properties, is loaded into the mesoporous silica (mSiO 2 ) of NMs (AST@NMs). AST effectively reduces inflammation and shifts macrophages from a proinflammatory (M1) phenotype to an anti-inflammatory (M2) phenotype. To protect the nanomotors from harsh digestive conditions and achieve intestinal-responsive release, using photocurable 3D printing, we fabricated enteric-coated oral microcapsules (MCs). Additionally, to prevent leakage of AST@NMs, a calcium alginate shell was cured in situ on the surface of the microcapsules (AST@NMs@MCs). In vitro and in vivo, AST@NMs@MCs effectively reduced inflammation, repaired the intestinal barrier, and modulated the gut microbiota. These findings underscore the protective effects of the microcapsules on AST@NM, highlighting their potential as a promising strategy for treating colitis.
研究领域:
药学
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纳米技术
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生物医学工程
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胃肠病学
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2024
·
IF 10.5
Pandi Peng,Tao Feng,Xue Yang,Rui Ding,Junru Wang,Pengyu Chen,Yuxin Guo,Peng Li
Inflammatory bowel disease (IBD) is closely associated with dysregulated immune response, gut mucosal barrier, and microbiota. Conventional treatments suffer from inferior bioavailability and inadequate efficiency. Herein, we present a synergistic therapeutic strategy based on multifunctionalized probiotics to mitigate IBD through single oral administration. The probiotic ( Escherichia coli Nissle 1917) is bioorthogonally conjugated with immunomodulators and subsequently encapsulated by an enteric coating. The viability and bioactivity of probiotics are not affected by the modifications. And the armored probiotics are able to resist the harsh environment of the stomach and shed their enteric coating in the intestinal tract, exposing immunomodulators to polarize pro-inflammatory M1-type macrophages into anti-inflammatory M2-type. In a mouse colitis model, orally administered multifunctionalized probiotics cooperatively alleviate IBD with increased body weight to 1.13 folds and decreased disease activity index to 0.43 folds, through downregulating the pro-inflammatory cytokines expression, upregulating the epithelial tight junction-associated proteins levels to restore the intestinal barrier, and increasing the microbiota richness and abundance. This work exhibits a feasible approach to construct functionalized orally administered probiotics for enhanced synergistic therapy of IBD.
研究领域:
药学
·
生物技术
·
免疫学
·
胃肠病学
✓ 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）