The purpose of this work is to investigate the effect of the genipin/hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex on the intestinal absorption of genipin and identify its mechanism of action. The phase solubility profile was classified as A(L) type, indicating the formulation of a 1:1 stoichiometry inclusion complex. Fourier transform infrared spectroscopy, Differential scanning calorimetry, X-ray powder diffractometry, and (1)H nuclear magnetic resonance (NMR) and two-dimensional (2D) (1)H rotating-frame Overhauser enhancement (ROESY) NMR spectroscopies further confirmed the formulation of the inclusion complex with superior dissolution properties than the drug alone. The results of single-pass intestinal perfusion showed that the intestinal absorption of genipin was affected by P-glycoprotein (Pgp). The absorption rate and permeability value of the inclusion complex were significantly higher than the free drug, suggesting that its enhancing effect was involved in its solubilizing effect and Pgp inhibitory effect. The mechanisms of HP-β-CD on Pgp inhibition were demonstrated by restraining the Pgp ATPase activity rather than changing the fluidity of the cell membrane.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jf202712y | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Measuring mechanical stress in living tissues.
Nat Rev Phys
May 2020
Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute for Science and Technology (BIST), Barcelona, Spain.
Living tissues are active multifunctional materials capable of generating, sensing, withstanding and responding to mechanical stress. These capabilities enable tissues to adopt complex shapes during development, to sustain those shapes during homeostasis, and to restore them during healing and regeneration. Abnormal stress is associated with a broad range of pathologies, including developmental defects, inflammatory diseases, tumor growth and metastasis.
View Article and Find Full Text PDFImproving stabilization of α-tocopherol and α-tocopheryl acetate against oxidation, light and UV radiation by complexation with β-cyclodextrin and starch.
J Food Sci Technol
January 2025
Agricultural Biochemistry Department, Faculty of Agriculture, Ain-Shams University, P.O. Box 68, Hadayek Shoubra, Cairo 11241 Egypt.
Unlabelled: Despite the remarkably high antioxidant activity of tocopherols, their applications in the food industry are limited because of their instability under various conditions. Complexes of α-tocopherol (α-TQ) or α-tocopheryl acetate (α-TQA) with β-cyclodextrin (β-CD) or starch were prepared and characterized by UV-vis, IR and thermal analysis. Oxidative stability of α-TQ and α-TQA against HO was 74.
View Article and Find Full Text PDFFetal radiation during acetabular and pelvic ring fixation: Which injury patterns dictate dangerous levels of fluoroscopic cumulative dose.
J Clin Orthop Trauma
March 2025
Department of Orthopaedic Surgery, Mercy St. Vincent Medical Center, 2213 Cherry St., Toledo, OH, 43608, USA.
Background: Gravid females with pelvic fractures are rarely encountered by the orthopaedic trauma surgeon. The initial injury can be detrimental to the pregnant patient, but an unnecessary "second hit" from surgery could also contribute to the outcome of the fetus. Understanding the surgical risks for this unique patient population requires knowledge about the negative effects of anesthesia, surgical exposures, and radiation.
View Article and Find Full Text PDFEthical dilemmas surrounding patients´ "unwise" treatment preferences and suboptimal decision quality: case series of three renal cell carcinoma patients who developed local recurrences after non-guideline-concordant care choices.
Pan Afr Med J
October 2024
College of Medicine, Qatar University, Doha, Qatar.
Patient engagement and shared decision-making (SDM) between patients and clinicians is the foundation of patient-centered care. It aims to reach a treatment option that fits the patient's preference and is guideline-concordant. We sought to evaluate the possible causes and outcomes of patient's non-guideline-concordant care choices.
View Article and Find Full Text PDFChondroitin Sulphate-Chitosan Based Nanogels Loaded with Naringenin-β-Cyclodextrin Complex as Potential Tool for the Treatment of Diabetic Retinopathy: A Formulation Study.
Int J Nanomedicine
January 2025
Department of Drug Sciences, University of Pavia, Pavia, 27100, Italy.
Purpose: The main purpose of the study was the formulation development of nanogels (NHs) composed of chondroitin sulfate (CS) and low molecular weight chitosan (lCH), loaded with a naringenin-β-cyclodextrin complex (NAR/β-CD), as a potential treatment for early-stage diabetic retinopathy.
Methods: Different formulations of NHs were prepared by varying polymer concentration, lCH ratio, and pH and, then, characterized for particle size, zeta potential, particle concentration (particles/mL) and morphology. Cytotoxicity and internalization were assessed in vitro using Human Umbilical Vein Endothelial Cells (HUVEC).
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!