JOURNAL OF MICROENCAPSULATION
·
2019
·
IF 2.04
Tingting Chen,Shunying Li,Wenting Zhu,Zhi Liang,Qingbing Zeng
Polyelectrolyte complexes (PEC) provide new opportunities for controlled release system of drugs, and have potentials to address challenges on the way to effective oral insulin delivery. Here, an innovative pH-sensitive PEC for insulin oral administration was developed, which was formed by self-assembly of two oppositely charged nanoparticles (chitosan-coated nanoparticles and alginate-coated nanoparticles) through electrostatic interaction via optimised double emulsion method. The encapsulation efficiency of insulin-loaded alginate-coated and chitosan-coated nanoparticles were 81.5 ± 7.4% and 55.2 ± 7.0%, respectively, and the particle size of these nanoparticles were in 200–300 nm range. The pH-dependent morphology of PEC was observed by transmission electron microscopy. The PEC exhibited insulin release profile triggered by pH in vitro and was non-cytotoxicity against Caco-2 cell. The insulin-loaded PEC could decrease blood glucose levels effectively and prolong insulin release after oral administration to diabetic rats. The results illustrated that the as-prepared PEC may be employed as a potential oral insulin delivery system.
研究领域:
药学
·
纳米技术
·
药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
·
2025
·
IF 4
Huilin Deng,Yaozhong Zheng,Qiongyao Wang,Jiaqi Peng,Weibin Bai,Lingmin Tian,Zouyan He,Rui Jiao
Mangiferin (MGF), a C-glycosyl xanthone from the mango plant, offers various health benefits but has low absorption, mostly remaining in the gut where it interacts with microbes. This study examines MGF's effects on human gut microbiota and metabolite profiles after in vitro digestion and fermentation with feces. Findings indicate MGF had limited permeability (under 2 %) across the Caco-2 monolayer, with most being fermented by microbes. MGF utilization increased post-digestion and fermentation, significantly altering gut metabolite profiles by boosting lipid and benzenoid abundance while reducing organic acids. It also promoted beneficial bacteria like Bacteroides and Bifidobacterium , decreasing harmful genera such as Sutterella . Metabolomic analysis revealed enhanced pathways for unsaturated fatty acid synthesis and longevity, primarily through oleic and linolenic acids, highlighting MGF's role in modulating gut health.
研究领域:
胃肠科学
·
微生物学
·
营养生物化学
·
代谢组学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2014
·
IF 3.785
Yuliang Xiao,Pingli Li,Yanna Cheng,Xinke Zhang,Juzheng Sheng,Decai Wang,Juan Li,Qian Zhang,Chuanqing Zhong,Rui Cao,Fengshan Wang
The purpose of this report was to demonstrate the effect of amphiphilic polysaccharides-based self-assembling micelles on enhancing the oral absorption of low molecular weight chondroitin sulfate (LMCS) in vitro and in vivo , and identify the transepithelial transport mechanism of LMCS micelles across the intestinal barrier. α-Linolenic acid-low molecular weight chondroitin sulfate polymers(α-LNA–LMCS) were successfully synthesized, and characterized by FTIR, 1 HNMR, TGA/DSC, TEM, laser light scattering and zeta potential . The significant oral absorption enhancement and elimination half-life ( t 1/2 ) extension of LNA–LMCS2 in rats were evidenced by intragastric administration in comparison with CS and LMCS. Caco-2 transport studies demonstrated that the apparent permeability coefficient ( P app ) of LNA–LMCS2 was significantly higher than that of CS and LMCS ( p < 0.001), and no significant effects on the overall integrity of the monolayer were observed during the transport process. In addition, α-LNA–LMCS micelles accumulated around the cell membrane and intercellular space observed by confocal laser scanning microscope (CLSM). Furthermore, evident alterations in the F-actin cytoskeleton were detected by CLSM observation following the treatment of the cell monolayers with α-LNA–LMCS micelles, which further certified the capacity of α-LNA–LMCS micelles to open the intercellular tight junctions rather than disrupt the overall integrity of the monolayer. Therefore, LNA–LMCS2 with low cytotoxicity and high bioavailability might be a promising substitute for CS in clinical use, such as treating osteoarthritis , atherosclerosis , etc.
研究领域:
药剂学
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药理学
·
生物药剂学
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药物递送系统
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药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Pei Zhang,Zhongqin Chen,Longjian Zhou,Jialong Gao,Huina Zheng,Haisheng Lin,Guoping Zhu,Xiaoming Qin,Wenhong Cao
An oyster peptide (OPs)-loaded composite nanogel based on carboxymethyl cellulose and carboxymethyl chitosan (CMC@CMCS@OPs) was prepared, and the characterization, absorption and transport mechanism were further investigated. CMC@CMCS@OPs, a dense spherical microstructure with a diameter of ∼64 nm, which enhanced the thermal and digestive stabilities of individual OPs and improved its retention rate of hypoglycemic activity in vitro . The swelling response and in-vitro release profiles showed that CMC@CMCS@OPs could help OPs achieve targeted and controlled release in the intestine. In addition, CMC@CMCS@OPs had no cytotoxicity on Caco-2 cells, and its apparent permeability coefficients increased 4.70–7.45 times compared with OPs, with the absorption rate increased by 129.38 %. Moreover, the transcytosis of CMC@CMCS@OPs nanogel occurred primarily through the macropinocytosis pathway, endocytosis pathway and intestinal efflux transporter-mediated efflux. Altogether, these results suggested that CMC@CMCS@OPs nanogel could be as an effective OPs delivery device for enhancing its stability and absorption.
研究领域:
纳米技术
·
药学
·
食品科学
·
生物技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food & Function
·
2024
·
IF 5.1
Zhengming Xu,Kseniya Hileuskaya,Aliaksandr Kraskouski,Yujiao Yang,Zhe Huang,Zhengang Zhao
A diet containing natural active compounds that can inhibit the hydrolytic activity of α-glucosidase on carbohydrates and intestinal glucose absorption is an effective means of controlling postprandial hyperglycemia. Phlorizin and polydatin as phenolic glycosides had a high affinity to the catalytic site of α-glucosidase, but exhibited unsatisfactory competitive inhibitory capacity, with IC50 of 0.97 and > 2 mM, respectively. However, dodecyl-acylated derivatives of phlorizin and polydatin exerted α-glucosidase inhibitory capacity, with IC50 of 55.10 and 70.95 µM, respectively, which were greatly enhanced and much stronger than that of acarbose with IC50 of 2.46 mM. Both dodecyl phlorizin and dodecyl polydatin reduced the catalytic ability of α-glucosidase by reversible noncompetitive and uncompetitive mixed inhibition, which bind noncovalently to the allosteric site 2 through hydrogen bonds and hydrophobic interactions, thereby inducing the secondary structure unfolding and intrinsic fluorescence quenching of α-glucosidase. Confocal microscopy detection visually showed the significant inhibitory effects on FITC-labeled glucose uptake in intestinal Caco-2 cells by phlorizin, polydatin, dodecyl phlorizin and dodecyl polydatin. In addition, based on the differentiated Caco-2 cell monolayer model, dodecyl phlorizin and dodecyl polydatin suppressed intestinal glucose transport more effectively than phlorizin and polydatin, suggesting that they were promising in vivo hypoglycemic active compounds.
研究领域:
药理学
·
生物化学
·
分子生物学
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营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Particuology
·
2025
·
IF 4.3
Mingyang Hu,Rui Zheng,Qi Pan,Chen Peng,Xinyue Zhang,Wei He,Wenlong Yao,Yan Li
Compared to intravenous injection, oral administration is attractive due to its many advantages for cancer therapy. Taken physiological barriers and other profiles of oral anticancer drug carriers into consideration, targeted and pH-sensitive polyzwitterionic liposomes (ZL) based on zwitterionic poly(carboxybetaine) (PCB) were constructed for oral delivery of doxorubicin hydrochloride (DOX·HCl) for cancer therapy. The DOX-ZL with 40% trehalose had good lyophilization stability, which would be packaged into enteric capsules to enhance their stability in stomach. In addition, DOX-ZL exhibited good storage stability and serum stability. The DOX-ZL could achieve controlled release of DOX·HCl at the endosomal pH 5.0 due to the pH-sensitive of zwitterionic PCB. Importantly, DOX-ZL could targeted deliver DOX·HCl to Caco-2 cells to cross the intestinal epithelial cell layer. The empty ZL had good biocompatibility, while DOX-ZL significantly inhibited tumor cells growth due to their high cellular uptake and controlled drug release ability. Therefore, this work provided a promising approach for oral cancer therapy.
研究领域:
药学
·
生物医学工程
·
癌症治疗
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药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
ADVANCED FUNCTIONAL MATERIALS
·
2024
·
IF 18.5
Hanxiao Pan,Bingyu Ding,Zhijiang Jiang,Jie Wang,Dingwei Li,Fengnan Yu,Lifen Wang,Sunkuan Hu,Yingzheng Zhao,Helin Xu
Ulcerative colitis (UC) is associated with the shedding of the gut mucus. Decellularized porcine small intestinal submucosa (SIS-ECM) contains numerous active forms of extracellular matrix as well as growth factors. Herein, a mucus-mimetic hydrogel (MAG) is designed as a barrier therapy by integrating SIS-ECM with hyaluronic acid and epigallocatechin-3-gallate. MAG not only presented the viscoelastic behaviors with G' of 4000 Pa but also good thixotropy. Moreover, MAG as a physical shielding is effective to hinder E. coli invasion. Besides, the good repairing effect on the injured Caco-2 cells is presented by MAG. When MAG as a biomimetic mucus is rectally administrated to colitis mouse, it alleviated effectively the colitis symptoms and improved the colonic shorting. Moreover, expression of IL-1β, IL-6, and TNF-α at the laminae propria is substantially inhibited by MAG. Besides, the colonic epitheliums are well rearranged, and the tight junction proteins (ZO-1, Occludin-1, Claudin-5) between them are greatly upregulated after MAG treatment. Meanwhile, the mucus secretion of goblets cells is effectively repaired by MAG treatment. The repairing mechanism of intestinal mucosa barriers is associated with promoting the proliferation and differentiation of intestinal stem cells. Collectively, MAG might be a promising strategy of barrier therapy for UC.
研究领域:
胃肠病学
·
生物材料
·
组织工程
·
炎症性肠病
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Yinghuan Jing,Kangyu Wang,Tianxiang Pi,Zefan Chen,Tianhong Liu,Xinyu Liu,Hangyu Ye,Xinxing Xu,Yuanhui Zhao
Low molecular weight chondroitin sulfate (CS) has gained considerable attention for its superior bioactivity compared to native CS. In this study, the mechanisms of low molecular weight chondroitin sulfate from hybrid sturgeon cartilage (LMSCS), prepared using the H 2 O 2 /Vc system, on the remission of osteoarthritis (OA) were investigated both in in vitro and in vivo . A Caco-2/SW1353 co-culture cell model and a monosodium iodoacetate (MIA)-induced OA mouse model were used to validate its inhibited apoptosis, anti-inflammatory effects, and intestinal flora modulation. LMSCS was found to effectively alleviate inflammation, decrease chondrocyte apoptosis, and reduce MMP-13 levels by inhibiting the activation of NF-κB and MAPK signaling pathways. Notably, in vivo experiments, LMSCS exhibited significant anti-inflammatory effects compared to SCS. This trend, however, was not observed in vitro , which could be largely attributed to LMSCS' ability to regulate intestinal flora. Compared to SCS, LMSCS enhanced the abundance of beneficial bacteria, particularly, the Prevotellaceae_NK3B31_group and Akkermansia , and increased the levels of short-chain fatty acids such as butyrate and propionate. The effectiveness of LMSCS in mitigating inflammatory responses in vivo is thus largely due to its intestinal flora modulation, providing for its development and application.
研究领域:
药理学
·
风湿病学
·
免疫学
·
微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMATERIALS
·
2011
·
IF 7.883
Yun Jin,Yupin Song,Xi Zhu,Dan Zhou,Chunhui Chen,Zhirong Zhang,Yuan Huang
The present study was to demonstrate the effects of goblet cell-targeting nanoparticles on the oral absorption of insulin in vitro , ex vivo and in vivo , and identify the targeting mechanism as well as the influence of mucus. The insulin loaded nanoparticles were prepared using trimethyl chitosan chloride (TMC) modified with a CSKSSDYQC (CSK) targeting peptide. Compared with unmodified nanoparticles, the CSK peptide modification could facilitate the uptake of nanoparticles in villi, enhance the permeation of drugs across the epithelium, meanwhile, induce a significantly higher internalization of drugs via clathrin and caveolae mediated endocytosis on goblet cell-like HT29-MTX cells. In transport studies across Caco-2/HT29-MTX co-cultured cell monolayer (simulating intestinal epithelium), the CSK peptide modification also showed enhanced transport ability, even if the targeting recognition was partially affected by mucus. Moreover, it was found the existence of mucus was propitious to the transport of insulin from both modified and unmodified nanoparticles. In the pharmacological and pharmacokinetic studies in diabetic rats, the orally administrated CSK peptide modified nanoparticles produced a better hypoglycemic effect with a 1.5-fold higher relative bioavailability compared with unmodified ones. In conclusion, CSK peptide modified TMC nanoparticles showed sufficient effectiveness as goblet cell-targeting nanocarriers for oral delivery of insulin.
研究领域:
药学科学
·
纳米技术
·
药物递送系统
·
糖尿病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2021
·Vol. 46
·期 3
·1295-1307
·
IF 3.591
Zhi-Gang Yin,Xiong-Wei Liu,Hui-Juan Wang,Min Zhang,Xiong-Li Liu,Ying Zhou
A highly efficient synthesis of structurally diverse ortho-acylphenol–diindolylmethane hybrids 3 using carboxylic acid-activated chromones as versatile synthetic building blocks is reported here for the first time, through 1,4-nucleophilic addition and followed by a decarboxylation and pyrone ring opening reaction process. The newly synthesized compounds were evaluated for their in vitro anticancer activity, and most of the compounds displayed good anticancer activities against four tested tumor cells (A549, PC-3, NCI-H1299, Caco-2). Among these compounds, compound 3t displayed the most potent and broad-spectrum anti-proliferative inhibition against the tested cell lines, especially A549 cells, and was more potent than arundine and cisplatin drugs, and had selectivity in cancer cells compared to MRC-5 and HK-2 normal cells. Preliminary mechanism studies showed that compound 3t exerted an anti-tumor effect in A549 cells by inhibiting the proliferation, colony formation and migration of A549 cells, and inducing cycle arrest at the G0/G1 phase and apoptosis. Furthermore, treatment of A549 cells with compound 3t caused increased ROS content and induced MMP collapse; western blot analysis showed that the expression level of p53 was significantly increased; Bax/Bcl-2 ratio and Cyt c were increased, and caspase-9, -3, and PARP were cleaved. These studies showed that compound 3t could induce apoptosis of A549 cells through the mitochondrial pathway, which was related to the activation of p53 and the generation of ROS. Thus, our results indicate that compound 3t may be used as a promising skeleton for the development of new anti-tumour drugs.
研究领域:
药物化学
·
肿瘤学
·
药学
·
细胞生物学
✓ 已验证
DOI
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2024
·
IF 7
Yue Su,Zhengying Cui,Xinyan Yang,Yujun Jiang,Wei Zhang,Yu Zhang,Chaoxin Man
Ulcerative colitis (UC) is an immune-mediated intestinal disease without a comprehensive cure, and the alleviation of UC has become an urgent problem. The results showed that JY062 with its EPS group (JEC) alleviated the intestinal barrier damage caused by LPS. After JEC intervention on Caco-2 cells, resulted in upregulation of ZO-1, Claudin-1, Occludin and MUC2 transcript levels and decreased mRNA expression of Claudin-2 (p < 0.05). JEC effectively attenuated the inflammatory response in UC mice and restoration of immunoglobulin levels (IgG, IgM and IgA), which resulted in shortening and swelling of the colon, disappearance of goblet cells, infiltration of inflammatory cells and mucosal damage were alleviated in mice. Similarly, changes in the expression of MUC2 and tight junction proteins after JEC intervention also occurred in UC mice. Administration of JEC significantly inhibited the differentiation of pro-inflammatory Th17 cells in the thymus and peripheral blood, promoted the differentiation of CD4+ T cells to Treg cells, and effectively regulated DSS-induced macrophage imbalance, which was manifested by the polarization of pro-inflammatory M1 macrophages to anti-inflammatory M2 macrophages. This study clearly demonstrates that JEC could significantly prevent intestinal barrier on DSS-induced experimental colitis and could be applied as a potential symbiotic strategy to assist in the alleviation of UC.
研究领域:
微生物学
·
免疫学
·
胃肠病学
·
药理学
✓ 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）