Article
Biochemistry & Molecular Biology
Quanpeng Qiu, Gang Guo, Xiaolong Guo, Xiake Hu, Tianyu Yu, Gaixia Liu, Haowei Zhang, Yinnan Chen, Junjun She
Summary: Barrett's esophagus (BE) is a precancerous lesion of esophageal adenocarcinoma (EAC) characterized by the replacement of squamous epithelium with columnar epithelium. Loss of P53 is a risk factor for the progression of BE. In this study, P53-deficient esophageal epithelial cells were exposed to acidic bile salt treatment, which resulted in reduced P53 protein expression and enhanced cell survival. Acidic bile salt exposure also impaired cell adhesion through repression of the JAK/STAT signaling pathway and activation of VEGFR/AKT in P53-deficient esophageal cells. Furthermore, the expression levels of P53, ICAM1, STAT3, and VEGFR were correlated in clinical samples of EAC, providing potential therapeutic targets for EAC.
Article
Pharmacology & Pharmacy
Muhammad Embaby, Gamal M. El Maghraby, Mohamed A. Osman, Amal A. Sultan
Summary: This study investigates the regional difference in linagliptin intestinal membrane transport and the effects of carvedilol, atorvastatin, and bile salts on intestinal absorption of linagliptin. The results show incomplete absorption of linagliptin from the explored intestinal segments, with absorption decreasing as movement progresses distally through the small intestine before increasing at the ascending colon. P-glycoprotein (P-gp) efflux is identified as a possible mechanism for reduced linagliptin intestinal absorption. Co-perfusion with carvedilol, atorvastatin, or bile salts significantly enhances linagliptin absorption, suggesting P-gp efflux inhibition as one possible mechanism for enhanced linagliptin intestinal membrane transport.
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2023)
Article
Biology
Weiyin Huang, Shuang Chen, Lin Sun, Hubin Wwang, Hongqun Qiao
Summary: The study investigated the intestinal permeability of lamivudine using Caco-2 cells monolayer and single-pass intestinal perfusion, revealing a passive diffusion absorption mechanism possibly related to efflux transporters. Lamivudine was classified as a moderate-permeability drug in the Biopharmaceutics Classification System.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2022)
Article
Chemistry, Medicinal
Noemi Lupo, Christian Steinbring, Julian David Friedl, Bao Le-Vinh, Andreas Bernkop-Schnuerch
Summary: Bile salts and fatty acids have a significant impact on the physical characteristics and drug release behavior of self-emulsifying drug delivery systems, leading to decreased size, improved stability, and accelerated drug release.
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2021)
Article
Food Science & Technology
Dorota Dulko, Robert Staron, Lukasz Krupa, Neil M. Rigby, Alan R. Mackie, Krzysztof Gutkowski, Andrzej Wasik, Adam Macierzanka
Summary: Human bile can potentially facilitate the hydrolysis of proteins resistant to gastric digestion in the small intestine, with the concentration of bile salts playing a key role in increasing proteolysis rate. This study suggests that simple mixtures of bile salts and phosphatidylcholine can serve as relevant substitutes for human bile in in vitro proteolysis studies.
FOOD RESEARCH INTERNATIONAL
(2021)
Article
Pharmacology & Pharmacy
Sapir Ifrah, Arik Dahan, Nir Debotton
Summary: Self-double emulsifying drug delivery systems have been shown to enhance the intestinal permeability of Biopharmaceutics Classification System (BCS) class III drugs. This study developed an innovative oral formulation for zanamivir using a self-double nanoemulsifying Winsor delivery system (SDNE-WDS), which successfully increased the permeability of zanamivir and demonstrated the effectiveness of SDNE-WDS in overcoming intestinal permeability barriers.
Article
Pharmacology & Pharmacy
David J. Brayden, Vivien Stuettgen
Summary: Bile salts have been found to enhance permeation in intestinal and buccal models, showcasing moderate efficacy and low toxicity similar to established permeation enhancers in clinical trials. However, their non-specific mechanism of action and potential toxicity necessitate cautious usage. At moderate concentrations, bile salts can impact cell parameters without causing significant damage to cell tissue and function.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Physical
Paresh Y. Parekh, Vijay I. Patel, Mehul R. Khimani, Pratap Bahadur
Summary: This communication provides an overview of the self-assembly of bile salts, focusing on their mixed aggregates with various amphiphiles. The authors explore the interactions between bile salts and surfactants, phospholipids, ionic liquids, drugs, and polymers through a literature survey. The study highlights the potential of bile salts to alter the size/shape of aggregates and use them for solubility improvement and smart delivery vehicles for important compounds and drugs.
ADVANCES IN COLLOID AND INTERFACE SCIENCE
(2023)
Article
Nanoscience & Nanotechnology
Santosh Bashyal, Jo-Eun Seo, Taekwang Keum, Gyubin Noh, Shrawani Lamichhane, Jeong Hwan Kim, Chang Hyun Kim, Young Wook Choi, Sangkil Lee
Summary: The study successfully demonstrated enhanced permeability of insulin through buccal administration using hydrophobic ion-pairing (HIP) nanocomplexes, providing a promising strategy for the delivery of this life-saving peptide hormone.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Chemistry, Analytical
Weiwei Tang, Yuejie Zhang, Ping Li, Bin Li
Summary: In this study, an integrated strategy combining quadruple single-pass intestinal perfusion (Q-SPIP) technique and matrix-assisted laser desorption ionization mass spectrometry imaging (MALDI MSI) was developed for in situ visualization and assessment of drug absorption and interaction in rat intestines. The Q-SPIP model enabled simultaneous perfusion of four individual segments of each rat intestine, providing rich data for analysis. The optimized MALDI MSI approach accurately visualized the drug distribution and absorption in rat intestinal tissue. The findings demonstrate the utility and versatility of Q-SPIP coupled with MALDI MSI in studying transporter-mediated intestinal drug absorption and interaction.
ANALYTICAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Carlynne Choy, Lee Yong Lim, Lai Wah Chan, Zhixiang Cui, Shirui Mao, Tin Wui Wong
Summary: This review examines the potential of targeting intestinal receptors to improve the oral delivery of nanoinsulin. While promising, further research and optimization are needed.
PHARMACOLOGICAL REVIEWS
(2022)
Article
Chemistry, Analytical
Weiwei Tang, Yuejie Zhang, Ping Li, Bin Li
Summary: Visualization and characterization of intestinal membrane transporter-mediated drug absorption and interaction are challenging. A new integrated strategy using quadruple single-pass intestinal perfusion (Q-SPIP) technique coupled with matrix-assisted laser desorption ionization mass spectrometry imaging (MALDI MSI) was developed for in situ visualization and assessment of drug absorption and interaction in rat intestines. The utility and versatility of this strategy were demonstrated through the examination of P-glycoprotein (P-gp)-mediated intestinal absorption of berberine (BBR) and its combination with natural products possessing inhibitory potency against P-gp.
ANALYTICAL CHEMISTRY
(2023)
Article
Food Science & Technology
Karol Parchem, Monika Baranowska, Anna Koscielak, Ilona Klosowska-Chomiczewska, M. Rosario Domingues, Adam Macierzanka, Agnieszka Bartoszek
Summary: This study evaluated the effect of lipoxygenase-induced phospholipid (PL) oxidation on the rate of PL hydrolysis and its toxicity towards HT29 cell line. The results showed that the degradation products of PL hydroperoxides inhibited the activity of pancreatic phospholipase A2 (PLA2). The exposure of cells to simulated intestinal fluid (SIF) with bile salts (BSs) decreased cell viability and damaged cellular DNA, but this genotoxic effect was reversed in the presence of PL samples. The decline in PLA2 activity caused by PL oxidation products may be a protective mechanism against the rapid release of oxidized fatty acids with high cytotoxicity towards intestinal epithelium cells.
FOOD RESEARCH INTERNATIONAL
(2023)
Article
Pharmacology & Pharmacy
Zhixiang Liu, Tong An, Rui Yuan, Maoxiong Tian, Linlin Yuan, Tong Zhang, Gang Cheng
Summary: This study investigated the applicability of mPEG-PR as a novel non-absorbable indicator in the in situ single-pass intestinal perfusion (SPIP) experiment. The results showed that mPEG-PR was a stable and accurate method for correcting water flux and predicting the fraction dose absorbed in human.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Pharmacology & Pharmacy
David Dahlgren, Tobias Olander, Markus Sjoblom, Mikael Hedeland, Hans Lennernas
Summary: Paracellular permeation enhancers were found to increase the mucosal permeability of hydrophilic peptides with low molecular mass compared to those with a transcellular mechanism-of-action. Additionally, luminal hypotonicity primarily affects paracellular solute transport in the mucosal crypt region.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Biochemistry & Molecular Biology
Qingxiang Guan, Dandan Sun, Guangyuan Zhang, Cheng Sun, Miao Wang, Danyang Ji, Wei Yang
Article
Chemistry, Multidisciplinary
Dandan Sun, Miao Wang, Danyang Ji, Jin Qiao, Tong He, Xin Liu, Qingxiang Guan
CHINESE CHEMICAL LETTERS
(2018)
Article
Pharmacology & Pharmacy
Lichun Zhao, Dandan Sun, Haibin Lu, Bing Han, Guangyuan Zhang, Qingxiang Guan
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2018)
Article
Multidisciplinary Sciences
Qingxiang Guan, Guangyuan Zhang, Dandan Sun, Yue Wang, Kun Liu, Miao Wang, Cheng Sun, Zhuo Zhang, Bingjin Li, Jiayin Lv
Review
Pharmacology & Pharmacy
Dandan Sun, Jian Zhang, Limei Wang, Zhuo Yu, Caitriona M. O'Driscoll, Jianfeng Guo
DRUG DISCOVERY TODAY
(2021)
Article
Biochemistry & Molecular Biology
Jianfeng Guo, Zhuo Yu, Dandan Sun, Yifang Zou, Yun Liu, Leaf Huang
Summary: This study demonstrates the concept of successful FOLFOX-associated CRC and HCC therapies through the combination of two nano delivery systems. Further optimization in dosing and timing has the potential to enhance the clinical efficacy of this combination strategy.
Article
Pharmacology & Pharmacy
Yifang Zou, Fang Xiao, Liu Song, Bingxue Sun, Dandan Sun, Di Chu, Limei Wang, Shulan Han, Zhuo Yu, Caitriona M. O'Driscoll, Jianfeng Guo
Summary: The study demonstrated that the modified CD nanoparticles could enhance the combined efficacy of docetaxel and siRNA in the treatment of colorectal cancer, offering a promising therapeutic strategy.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Dandan Sun, Yifang Zou, Liu Song, Shulan Han, Hao Yang, Di Chu, Yun Dai, Jie Ma, Caitriona M. O'Driscoll, Zhuo Yu, Jianfeng Guo
Summary: This study confirms the potential of ginsenoside Rg3 as an inducer of immunogenic cell death (ICD) against colorectal cancer (CRC) cells. The effectiveness of Rg3 in inducing ICD is significantly enhanced when combined with quercetin (QTN) that induces reactive oxygen species (ROS). A targeted nanoparticle formulation, co-encapsulating Rg3 and QTN, is developed to improve the in vivo delivery and shows enhanced tumor targeting and prolonged blood circulation in a CRC mouse model. The combination of this nanoparticle formulation with anti-PD-L1 leads to significantly longer survival in animals.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Engineering, Biomedical
Xuefang Hao, Weiwei Gai, Feng Ji, Jiadi Zhao, Dandan Sun, Fan Yang, Haixia Jiang, Yakai Feng
Summary: The development of platelet membrane cloaked gene complexes based on natural bovine serum albumin and polyethyleneimine has shown promising results in promoting VEGF expression in vascular endothelial cells, enhancing migration and proliferation of VECs, and inhibiting neointimal hyperplasia.
ACTA BIOMATERIALIA
(2022)
Review
Nanoscience & Nanotechnology
Hao Yang, Liu Song, Yifang Zou, Dandan Sun, Limei Wang, Zhuo Yu, Jianfeng Guo
Summary: The skin is crucial for protecting the body, detecting environmental changes, and maintaining physiological balance. Hyaluronic acids play key roles in cell differentiation, proliferation, and migration, making them potential candidates for treating skin damage and injury. Advanced strategies are needed for addressing the complexity of the healing process in order to improve treatment outcomes.
ACS APPLIED BIO MATERIALS
(2021)
Article
Pharmacology & Pharmacy
Xuezhi Zhuo, Vito Fodera, Per Larsson, Zarah Schaal, Christel A. S. Bergstrom, Korbinian Lobmann, Aleksei Kabedev
Summary: Our previous work demonstrated that beta-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for over 12 months. We further investigated the stabilization mechanisms by testing five other drug molecules and using experimental techniques and molecular dynamics simulations. The results showed that steric confinement, hydrogen bonding, and the glass transition temperature of the drug molecule play important roles in stabilizing ASDs with high drug loadings.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Sebastian Schmidt, Ulrike Holzgrabe
Summary: The binding of drugs to plasma proteins, such as human serum albumin (HSA), is crucial for determining pharmacokinetic parameters. This study investigated the enantioselective binding of S- and R-ketamine to HSA. It was found that ketamine has weak affinity to HSA, with no significant differences in binding behavior between the individual enantiomers and the racemate. The aromatic ring and N-methyl group were identified as the most strongly involved structural moieties in the binding of ketamine to HSA.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Yuchen Zhao, Han Wang, Lin Jin, Ziwei Zhang, Lianghu Liu, Mengqi Zhou, Xianzheng Zhang, Lingling Zhang
Summary: Interleukins (ILs) are important for communication between immune cells and non-immune cells, but dysregulation of ILs expression is a characteristic of autoinflammatory diseases. Drugs targeting ILs have significant clinical benefits, but may also cause adverse reactions. Fusion protein technology, with its ability to enhance therapeutic efficacy, has been explored for developing anti-inflammatory drugs. This review discusses the efficacy of fusion protein drugs developed with ILs or their receptors in treating autoinflammatory diseases, highlighting the potential of this technology in future anti-inflammatory drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Serena Bertoni, Elena Simone, Stefano Sangiorgi, Beatrice Albertini, Nadia Passerini
Summary: This study investigated the correlation between the structure and release properties of solid lipid microparticles (MPs) with different liquid additives. The additives accelerated the conversion of the unstable alpha-form of tristearin to the stable beta-polymorph and caused structural modifications in the MPs. The presence of additives prolonged the drug release in water and resulted in higher release profiles in biorelevant media. The findings suggest that the release behavior can be influenced by the polymorphism and supramolecular-level structural modification of lipid formulations containing crystal modifiers.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Juulia Jarvinen, Ahmed B. Montaser, Santosh Kumar Adla, Jukka Leppanen, Marko Lehtonen, Kati-Sisko Vellonen, Tuomo Laitinen, Aaro Jalkanen, William F. Elmquist, Juri Timonen, Kristiina M. Huttunen, Jarkko Rautio
Summary: This study attempted to alter the brain distribution pattern of Palbociclib by creating and assessing two novel prodrugs. Although the prodrug design did not significantly improve Palbociclib brain delivery, the study provides valuable insights for future prodrug development and drug delivery strategies targeting specific transporters.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Review
Pharmacology & Pharmacy
Miao Wang, Xinyu Ma, Shiyu Zong, Yaqiong Su, Rui Su, Hong Zhang, Yang Liu, Chunliu Wang, Ye Li
Summary: This article discusses the potential and limitations of nasal administration in central nervous system drug delivery. Nasal gel viscosity can alleviate the impact of nasal mucociliary clearance on drug delivery, and materials such as gellan gum, chitosan, carbomer, cellulose, and poloxamer can be used to prepare nasal gels.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Bjarke Strom Larsen, Eric Kissi, Liebert Parreiras Nogueira, Natalja Genina, Ingunn Tho
Summary: This study investigates the influence of drug load and polymer molecular weight on the structure of 3D printed tablets. The results show that drug load and polymer molecular weight have a significant impact on the porosity and size of the tablets, while the effect of drug load on the total porosity of the tablets is minimal.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Zhentao Qiao, Fuhang Wang, Dongjian Han, Yuansong Zhuang, Qingjiao Jiang, Yi Zhang, Miaomiao Liu, Quanxu An, Zhiwei Wang, Deliang Shen
Summary: In this study, it was demonstrated that periadventitial delivery of rapamycin-fibrin glue (RPM-FG) can inhibit intimal hyperplasia (IH) in a rat carotid artery injury model without compromising re-endothelialization. This provides a promising direction for the future development of a safe, effective, and minimally invasive perivascular drug delivery method to treat vascular disease.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Neele Puhlmann, Rodrigo Vidaurre, Klaus Kuemmerer
Summary: Active pharmaceutical ingredients and their metabolites and transformation products are pollutants that can harm human and environmental health. Designing greener APIs is an effective strategy to address this issue. The drug discovery and development process can incorporate environmental parameters to achieve this design, and this process is highly flexible.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)