The objective of this study was to obtain detailed information on the mechanism of drug release from mixed-film of pectin-chitosan/Eudragit RS. Pellets (710-840 microm in diameter) containing 60% theophylline and 40% microcrystalline cellulose were prepared by extrusion-spheronization method. Eudragit L100-55 enteric coating capsules included film-coated pellets of theophylline in theoretical coating weight gains of 10, 15, and 20%, with pectin-chitosan complex contents of 5, 10, 15, and 20% for each level of weight gain were prepared and subjected to in vitro drug release. Drug release from this system showed a bimodal release profile characteristic with the drug release enhancement, being triggered (burst release) in the colonic medium. The reason for burst drug release may be due to the enzymatic degradation of pectin via pectinolytic enzymes in the simulated colonic medium. The mechanism of drug release from each formulation was evaluated in the terms of zero-order, first-order, Higuchi and Korsmeyer-Peppas models. It was observed that none of the enteric coating capsules showed any drug release in the simulated gastric medium (phase I). The analysis of release profiles showed that zero-order kinetics was found as the better fitting model for all formulations in the simulated small intestine (phase II) and it could be due to the pectin-chitosan swelling and subsequent formation of aqueous channels. In the colonic medium (phase III), due to degradation of pectin and its leaching from the mixed-film, there was a modification in drug release kinetics from swelling-controlled at phase II to anomalous at phase III. It also was found that both zero-order and Higuchi models contributed in colonic drug release from most of the formulations.
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PLoS One
January 2025
Chakri Naruebodindra Medical Institute, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Samut Prakan, Thailand.
Cadmium is a non-essential element and neurotoxin that causes neuroinflammation, which leads to neurodegenerative diseases and brain cancer. To date, there are no specific or effective therapeutic agents to control inflammation and alleviate cadmium-induced progressive destruction of brain cells. Fluoroquinolones (FQs), widely used antimicrobials with effective blood-brain barrier penetration, show promise in being repurposed as anti-inflammatory drugs.
View Article and Find Full Text PDFACS Biomater Sci Eng
January 2025
Institute of Biomedical Engineering, University of Toronto, Toronto, Ontario M5S 3E3, Canada.
Restenosis remains a long-standing limitation to effectively maintain functional blood flow after percutaneous transluminal angioplasty (PTA). While the use of drug-coated balloons (DCBs) containing antiproliferative drugs has improved patient outcomes, limited tissue transfer and poor therapeutic targeting capabilities contribute to off-target cytotoxicity, precluding adequate endothelial repair. In this work, a DCB system was designed and tested to achieve defined arterial delivery of an antirestenosis therapeutic candidate, cadherin-2 (N-cadherin) mimetic peptides (NCad), shown to selectively inhibit smooth muscle cell migration and limit intimal thickening in early animal PTA models.
View Article and Find Full Text PDFInflammation
January 2025
Research Center for Food and Cosmetic Safety and Center for Drug Research and Development, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan.
Atopic dermatitis (AD) is a multifaceted inflammatory skin condition characterized by the involvement of various cell types, such as keratinocytes, macrophages, neutrophils, and mast cells. Research indicates that flavonoids possess anti-inflammatory properties that may be beneficial in the management of AD. However, the investigation of the glycoside forms for anti-AD therapy is limited.
View Article and Find Full Text PDFNano Lett
January 2025
Faculty of Hepato-Pancreato-Biliary Surgery, The First Medical Center of Chinese People's Liberation Army (PLA) General Hospital, Beijing 100853, P. R. China.
Portal vein tumor thrombus (PVTT) is a poor prognostic factor for hepatocellular carcinoma (HCC) patients, highlighting the need for an oral drug delivery system that combines convenience, simplicity, biosafety, and improved patient compliance. Leveraging the unique anatomy of the portal vein and insights from single-cell RNA sequencing of the PVTT tumor microenvironment, we developed oral pellets using CaCO@PDA nanoparticles (NPs) encapsulating both doxorubicin hydrochloride and low molecular weight heparin. These NPs target the tumor thrombus microenvironment, aiming to break down the thrombus barrier and turn the challenge of portal vein blockage into an advantage by enhancing drug delivery efficiency through oral administration.
View Article and Find Full Text PDFJ Mater Chem B
January 2025
Department of Gastrointestinal Surgery, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200127, China.
Hypoxia, a condition that enhances tumor invasiveness and metastasis, poses a significant challenge for diverse cancer therapies. There is a pressing demand for hypoxia-responsive nanoparticles with integrated photodynamic functions in order to address the aforementioned issues and overcome the reduced efficacy caused by tumor hypoxia. Here, we report a hypoxia-responsive supramolecular nanoparticle SN@IR806-CB consisting of a dendritic drug-drug conjugate (IR806-Azo-CB) and anionic water-soluble [2]biphenyl-extended-pillar[6]arene modified with eight ammonium salt ions (AWBpP6) the synergy of π-π stacking interaction, host-guest complexation, and hydrophobic interactions for synergistic photothermal therapy (PTT), photodynamic therapy (PDT), and chemotherapy (CT; , PTT-PDT-CT).
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