Epalrestat (EPL) is a water-insoluble drug (14μM) that inhibits aldose reductase. This study investigated the interactions between β-cyclodextrin (CD) derivatives and EPL to determine the solubilizing effect on EPL from phase solubility diagrams. We improved the solubility of EPL in water by adding β-CD derivatives. Moreover, the solubility of EPL mixed with β-CD derivatives by cogrinding in a ball mill method was about 2-3 times higher than those of EPL with the same CD concentration (5mM) calculated from phase solubility diagrams. In addition, we investigated the effect of β-CD derivatives on in vitro percutaneous absorption of EPL through hairless mouse skin. Among the coground mixtures of EPL and β-CD derivatives, the mixture containing methyl (ME)-β-CD showed the strongest enhancement of EPL skin permeation. Furthermore, adding 10wt% urea as a skin permeation enhancer after cogrinding with ME-β-CD improved the flux of EPL 300 times compared to the flux of EPL alone. This result indicates the ME-β-CD ground mixture system with urea has potential as a new transdermal drug delivery system of EPL for diabetic neuropathy.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejps.2017.05.047 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Ionic-liquid-supported copper-promoted synthesis of 3,5-disubstituted-1,2,4-triazoles.
Org Biomol Chem
January 2025
Department of Chemistry, Rabindranath Tagore University, Hojai 782435, Assam, India.
The synthesis of triazoles plays an important role in drug discovery research. 1,2,4-triazoles are considered significant scaffolds among several bioactive heterocycles due to their extensive use in the pharmaceutical and agrochemical sectors. Consequently, the importance of the synthesis of 1,2,4-triazoles a sustainable method has increased.
View Article and Find Full Text PDFProbing the Self-Aggregation of l-Tryptophan into Spherical Microstructures and Their Selective Interactions with Bilirubin.
ACS Appl Bio Mater
January 2025
Department of Chemistry, Indian Institute of Technology Palakkad, Palakkad, Kerala 678 623, India.
The aggregation of proteins, peptides and amino acids has been a keen subject of interest owing to their implications in metabolic disorders. In this work, we investigated the self-aggregation of the unmodified aromatic amino acid l-tryptophan (Trp) into unusual spherical microstructures. Using fluorescence spectroscopy and field emission scanning electron microscopy (FE-SEM), we detail the time-dependent transformation of monomeric tryptophan into spherical aggregates with distinct fluorescence characteristics (λ = 345 nm, λ = 430 nm) compared to the monomer.
View Article and Find Full Text PDFExternal Validation of the Walter Index for Posthospitalization Mortality Prediction in Older Adults.
JAMA Netw Open
January 2025
Division of Geriatrics, School of Medicine, University of California San Francisco.
Importance: The Walter Index is a widely used prognostic tool for assessing 12-month mortality risk among hospitalized older adults. Developed in the US in 2001, its accuracy in contemporary non-US contexts is unclear.
Objective: To evaluate the external validity of the Walter Index in predicting posthospitalization mortality risk in Brazilian older adult inpatients.
Boswellic acid exerts anti-tumor effect in oral squamous cell carcinoma by inhibiting PI3K/AKT1 mediated signaling pathway.
Minerva Dent Oral Sci
January 2025
Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences (SIMATS), Saveetha University, Chennai, India.
Background: Boswellic acid (BA) is a bioactive compound derived from Boswellia trees. This study aims to investigate the anti-cancer properties of BA against KB oral squamous cancer cells and elucidate the underlying mechanisms.
Methods: Escalating doses of BA were administered to KB cells, and various analyses were conducted using bioinformatic tools such as GEO, GEO2R, and STITCH database.
Conventional periodontal probing versus salivary biomarkers in diagnosis and evaluation of chronic periodontitis in type 2 diabetes mellitus.
Minerva Dent Oral Sci
January 2025
Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences (SIMATS), Saveetha University, Chennai, India -
Chronic periodontitis is a prevalent inflammatory condition that affects both the oral health and systemic well-being of individuals, particularly those with type 2 diabetes mellitus (T2DM). Accurate diagnosis and evaluation of periodontal status are crucial for effective management of the disease. This narrative review aimed to compare the diagnostic and evaluative capabilities of conventional periodontal probing and salivary biomarkers in chronic periodontitis among individuals with T2DM.
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!