Hepatocellular carcinoma (HCC) is a prevalent liver cancer representing the fourth most lethal cancer worldwide. Trans-Resveratrol (T-R) possesses a promising anticancer activity against HCC. However, it suffers from poor bioavailability because of the low solubility, chemical instability, and hepatic metabolism. Herein, we developed T-R-loaded nanocochleates using a simple trapping method. Nanocarriers were optimized using a comprehensive in-vitro characterization toolset and evaluated for the anticancer activity against HepG2 cell line. T-R-loaded nanocochleates demonstrated monodispersed cylinders (163.27 ± 2.68 nm and 0.25 ± 0.011 PDI) and -46.6 mV ζ-potential. They exhibited a controlled biphasic pattern with minimal burst followed by sustained release for 72 h. Significant enhancements of Caco-2 transport and ex-vivo intestinal permeation over liposomes, with 1.8 and 2.1-folds respectively, were observed. Nanocochleates showed significant reduction of 24 h IC values compared to liposomes and free T-R. Moreover, an efficient knockdown of anti-apoptotic (Bcl-2) and cancer stemness (NANOG) genes was demonstrated. To the best of our knowledge, we are the first to develop T-R loaded nanocochleates and scrutinize its potential in suppressing NANOG expression, 2-folds lower, compared to free T-R. According to these auspicious outcomes, nanocochleates represent a promising nanoplatform to enhance T-R oral permeability and augment its anticancer efficacy in the treatment of HCC.
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http://dx.doi.org/10.1016/j.ejpb.2021.08.020 | DOI Listing |
Front Endocrinol (Lausanne)
December 2024
Department of Endocrinology and Metabolism, Lanzhou University Second Hospital, Lanzhou, Gansu, China.
Although pituitary tumors (PTs) are mostly benign, some PTs are characterized by low surgical resection rates, high recurrence rates, and poor response to conventional treatments and profoundly affect patients' quality of life. Everolimus (EVE) is the only FDA-approved mTOR inhibitor, which can be used for oral treatment. It effectively inhibits tumor cell proliferation and angiogenesis.
View Article and Find Full Text PDFEur J Pharm Biopharm
December 2024
School of Pharmaceutical Sciences, Beijing Advanced Innovation Center for Structural Biology, and Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Tsinghua University, Beijing 100084, PR China. Electronic address:
Oral delivery of peptide drugs remains one of the most formidable challenges in the frontier of pharmaceutical research. Peptide drugs typically suffer from exceptionally low oral bioavailability, primarily attributed to rigorous enzymatic degradation within the gastrointestinal (GI) tract, limited ability to traverse the enterocyte barrier, and significant first-pass hepatic metabolism. Absorption of peptide drugs via the lymphatic route could potentially bypass intracellular lysosome degradation and hepatic first-pass metabolism.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
School of Health Science and Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China; National Grain Industry (Urban Grain and Oil Security) Technology Innovation Center, Shanghai 200093, China. Electronic address:
Oral delivery of macromolecular drugs is often hampered by the harsh gastrointestinal environment, which makes the drugs have poor bioavailability. Insulin, the most used drug for diabetes, also faces the same challenge for oral administration. Hence, we decorated microbial metabolite propionate on chitosan (CS) to fabricate insulin-loaded propionate-modified CS hydrogel nanoparticles (IN-CS/PA HNPs).
View Article and Find Full Text PDFMajor depressive disorder (MDD) is one of the most common diseases affecting millions of people worldwide. The use of existing antidepressants in many cases does not allow achieving stable remission, probably due to insufficient understanding of pathological mechanisms. This indicates the need for the development of more effective drugs based on in-depth understanding of MDD's pathophysiology.
View Article and Find Full Text PDFCryst Growth Des
December 2024
School of Chemical and Process Engineering, University of Leeds, Woodhouse Lane, Leeds LS2 9JT, U.K.
Waxes comprise a diverse set of materials from lubricants and coatings to biological materials such as the intracuticular wax layers on plant leaves that restrict water loss to inhibit dehydration. Despite the often mixed hydrocarbon chain lengths and functional groups within waxes, they show a propensity for ordering into crystalline phases, albeit with a wealth of solid solution behavior and disorder modes that determine chemical transport and mechanical properties. Here, we reveal the microscopic structure and heterogeneity of replica leaf wax models based on the dominant wax types in the plant, namely CH and CHOH and their binary mixtures.
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