AI Article Synopsis
- Oxyberberine (OBB) shows strong anti-hyperuricemic effects, but its use is limited due to poor water solubility and low plasma levels.
- Researchers developed an OBB-HP-β-CD supersaturated drug delivery system (SDDS) to improve these properties, utilizing ultrasonic-solvent evaporation and characterizing the system.
- Results indicated that the OBB-HP-β-CD SDDS significantly enhanced the solubility, dissolution rate, and bioavailability of OBB, making it 5-10 times more effective against hyperuricemia compared to raw OBB.
Article Abstract
Propose: Oxyberberine (OBB), one of the main metabolites of berberine derived from intestinal and erythrocyte metabolism, exhibits appreciable anti-hyperuricemic activity. However, the low water solubility and poor plasma concentration-effect relationship of OBB hamper its development and utilization. Therefore, an OBB-hydroxypropyl-β-cyclodextrin (HP-β-CD) supersaturated drug delivery system (SDDS) was prepared and characterized in this work.
Methods: OBB-HP-β-CD SDDS was prepared using the ultrasonic-solvent evaporation method and characterized. Additionally, the in vitro and in vivo release experiments were conducted to assess the release kinetics of OBB-HP-β-CD SDDS. Subsequently, the therapeutic efficacy of OBB-HP-β-CD SDDS on hyperuricemia (HUA) was investigated by means of histopathological examination and evaluation of relevant biomarkers.
Results: The results of FT-IR, DSC, PXRD, NMR and molecular modeling showed that the crystallized form of OBB was transformed into an amorphous OBB-HP-β-CD complex. Dynamic light scattering indicated that this system was relatively stable and maintained by formation of nanoaggregates with an average diameter of 23 nm. The dissolution rate of OBB-HP-β-CD SDDS was about 5 times higher than that of OBB raw material. Furthermore, the of OBB-HP-β-CD SDDS (10.882 μg/mL*h) was significantly higher than that of the raw OBB counterpart (0.701 μg/mL*h). The oral relative bioavailability of OBB-HP-β-CD SDDS was also enhanced by 16 times compared to that of the raw material. Finally, in vivo pharmacodynamic assay showed the anti-hyperuricemic potency of OBB-HP-β-CD SDDS was approximately 5-10 times higher than that of OBB raw material.
Conclusion: Based on our findings above, OBB-HP-β-CD SDDS proved to be an excellent drug delivery system for increasing the solubility, dissolution, bioavailability, and anti-hyperuricemic potency of OBB.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11164094 | PMC |
| http://dx.doi.org/10.2147/IJN.S464994 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Vehicle effect on in-vitro and in-vivo performance of spray-dried dispersions.
J Pharm Sci
January 2025
Synthetic Molecule Pharmaceutical Sciences, Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
In early drug development, amorphous spray-dried dispersions (SDDs) applied to enhance the bioavailability of poorly water-soluble compounds are typically administered to preclinical species via oral gavage in the form of suspensions. The liquid formulations are usually prepared on the same day of dosing to minimize the exposure of the amorphous material to the aqueous vehicle, thereby reducing the risk of crystallization. Dose-ability (e.
View Article and Find Full Text PDFAssociation of subretinal drusenoid deposits and cardiovascular disease.
Sci Rep
October 2024
Ophthalmology Department, Hadassah Medical Center, Jerusalem, Israel.
Article Synopsis
- * A total of 597 AMD patients were analyzed, with 332 having SDDs and 265 without, using optical coherence tomography (SD-OCT) and reviewing electronic medical records.
- * Results showed that AMD patients with SDDs are significantly more likely to be diagnosed with CVD and have procedures such as percutaneous transluminal coronary angioplasty (PTCA), suggesting a possible shared mechanism between SDDs and severe cardiovascular conditions.
Update review on SUDEP: Risk assessment, background & seizure detection devices.
Epilepsy Behav
November 2024
Academic Center for Epileptology Kempenhaeghe, Heeze, The Netherlands; Eindhoven University of Technology, Eindhoven, The Netherlands; Department of Neurology, Ghent University Hospital, Ghent, Belgium.
Article Synopsis
- The review examines sudden unexpected death in epilepsy (SUDEP), focusing on risk factors, scoring systems to assess risk, and mechanisms behind SUDEP occurrences.
- Key risk factors include the presence and frequency of generalized tonic-clonic seizures (GTC), with odds ratios indicating significant risk, particularly in specific contexts like bedroom sharing.
- Four main SUDEP risk scoring systems are discussed, highlighting their different designs and the need for further validation in general epilepsy populations, along with proposed mechanisms of SUDEP involving brainstem dysfunction and potential roles of adenosine and serotonin.
prominin-1-null Xenopus laevis develop subretinal drusenoid-like deposits, cone-rod dystrophy and RPE atrophy.
J Cell Sci
November 2024
The University of British Columbia, Faculty of Medicine, Department of Ophthalmology and Visual Sciences, Vancouver, BC V5Z 0A6, Canada.
Prominin-1 (PROM1) variants are associated with inherited, non-syndromic vision loss. We used CRISPR/Cas9 to induce prom1-null mutations in Xenopus laevis and then tracked retinal disease progression from the ages of 6 weeks to 3 years. We found that prom1-null-associated retinal degeneration in frogs was age-dependent and involved retinal pigment epithelium (RPE) dysfunction preceding photoreceptor degeneration.
View Article and Find Full Text PDFAccelerated discovery and miniaturization of novel single-stranded cytidine deaminases.
Nucleic Acids Res
October 2024
College of Animal Sciences, Jilin University, Changchun 130062, China.
Cytidine base editors (CBEs) hold significant potential in genetic disease treatment and in breeding superior traits into animals. However, their large protein sizes limit their delivery by adeno-associated virus (AAV), given its packing capacity of <4.7 kb.
View Article and Find Full Text PDFWant 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!