A pH-Responsive Hydrogel for the Oral Delivery of Ursolic Acid: A Pentacyclic Triterpenoid Phytochemical DOI Creative Commons
Carlos D. Gutierrez, Rosana L. Aranzábal, Ana M. Lechuga

et al.

Gels, Journal Year: 2024, Volume and Issue: 10(9), P. 602 - 602

Published: Sept. 22, 2024

In this study, poly(HEMA-PEGxMEM-IA) hydrogels were prepared by radical copolymerization of poly(ethylene glycol) methyl ether methacrylate (PEGxMEM), 2-hydroxyethyl (HEMA), and itaconic acid (IA). The reaction was carried out in ethanolic solution using N,N′-methylenebisacrylamide (MBA) as a crosslinking agent 1-hydroxycyclohexyl phenyl ketone (HCPK) photo-initiator. (HGx) evaluated delivery system for ursolic (UA), phytochemical extracted from the plant Clinopodium revolutum, “flor de arena”. characterized Fourier-transform infrared spectroscopy (FTIR-ATR), Raman spectroscopy, X-Ray diffraction (XRD), thermogravimetric analysis (TGA), scanning electron microscopy (SEM). swelling behavior studied buffer solutions pH 2 to 10, specifically at 2.2 (gastric environment) 7.4 (intestinal environment). It found that showed sensitivity pH. At 2.2, degree HG5 HG9 0.45 0.93 (g water/g hydrogel), respectively. 7.4, 1.97 2.64 SEM images show variation pore size function pH, UA crystals pores can also be observed. vitro release data best fit Korsmeyer–Peppas kinetic model diffusion exponent indicates mechanism is governed Fickian diffusion.

Language: Английский

Development and in vitro evaluation of ursolic acid-loaded poly(lactic-co-glycolic acid) nanoparticles in cholangiocarcinoma DOI Creative Commons

Pornpattra Maphanao,

Yaowaret Phothikul,

Cherdpong Choodet

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(34), P. 24828 - 24837

Published: Jan. 1, 2024

Cholangiocarcinoma (CCA), an epithelial biliary tract malignancy, is a significant health concern in the Greater Mekong Subregion, particularly northeastern Thailand. Prior to development of advanced stages, CCA typically asymptomatic, thereby limiting treatment options and chemotherapeutic effectiveness. Ursolic acid (UA), triterpenoid derived from plants, was previously discovered inhibit cell growth through induction apoptosis. Nevertheless, therapeutic effectiveness UA limited by its poor solubility water low bioavailability; therefore, dimethyl sulfoxide (DMSO) utilized as solvent treat with cells. Enhancing cellular uptake reducing toxicity, utilization polymeric nanoparticles (NPs) proves beneficial. In this study, UA-loaded PLGA (UA-PLGA NPs) were synthesized using nanoprecipitation characterized silico formation analysis, average particle size, surface functional groups ζ-potential measurements, electron microscopic imaging, drug loading efficiency release studies, stability, hemo- biocompatibility, cytotoxicity assays. Molecular dynamics simulations validated into via hydrogen bonding. The UA-PLGA NPs had spherical shape size 240 nm, negative ζ-potential, good great bio-compatibility encapsulation 98%. exhibited characteristic simple diffusion-controlled Fickian process, predicted Peppas-Sahlin kinetic model. cytotoxic effects on KKU-213A KKU-055 cells even when dispersed media without organic solvent, i.e., DMSO, highlighting ability overcome UA. Rhodamine 6G (R6G) loaded same approach NPs, demonstrating effective delivery dye These findings suggest that showed promise potential phytochemical system for treatment.

Language: Английский

Citations

3
The Potential of Ursolic Acid Nanoformulations As Drug Delivery Systems in Alzheimer's Disease Therapy and Research DOI
Aditi Kaushik,

Ram Mor,

Sushila Kaura

et al.

International Journal of Latest Technology in Engineering Management & Applied Science, Journal Year: 2025, Volume and Issue: 14(4), P. 795 - 800

Published: May 17, 2025

Abstract: Scientific studies have demonstrated that Nanoparticles become a promising contributor towards Alzheimer’s disease (AD) research prospects offering significant advantages in imaging diagnostics as well therapy. These particles offer better terms of solubility, permeability and bioavailability due to their nanoscale size which enables effective drug delivery particular brain areas while reducing off-target side-effects. Ursolic acid (UA), bioactive compound with therapeutic properties, faces challenges clinical applications its poor solubility low bioavailability. To address these limitations, UA was encapsulated using three different polymer-based nanoparticle formulations: Gum Acacia (UGNPs), Eudragit (UE-NPs), Ghatti (UAGG-NPs). This study compares the physicochemical loading efficiency, release profiles, antioxidant activities UA-loaded nanoparticles. All formulations encapsulation sustained release, notable variations stability, activity, enzyme inhibition. The findings suggest nanoparticles significantly enhance UA’s potential, each formulation exhibiting distinct advantages. Further analysis unravels comparative benefits systems, highlighting implications for oxidative stress-related neurodegenerative disorders. UA-Nps strong acetylcholinesterase (AChE) inhibition, suggesting potential role highlights Eudragit-based enhanced also recognizing formulations. safety, effectiveness long-term consequences nanotechnology-based AD treatment management require further research. initial step same direction has been taken throughout this investigation analysis.

Language: Английский

Citations

0
Nanoencapsulation of vitamin B2 using chitosan‐modified poly(lactic‐co‐glycolic acid) nanoparticles: Synthesis, characterization, and in vitro studies on simulated gastrointestinal stability and delivery DOI Creative Commons

Siriratchakorn Sathiensathaporn,

Anna Solé‐Porta, Duangkamon Baowan

et al.

Journal of Food Science, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 28, 2024

Abstract Vitamin B 2 , or riboflavin, is essential for maintaining healthy cellular metabolism and function. However, its light sensitivity, poor water solubility, gastrointestinal barriers limit storage, delivery, absorption. Selecting suitable nanomaterials encapsulating vitamin crucial to overcoming these challenges. This study employed chitosan‐coated poly(lactic‐ co ‐glycolic acid) nanoparticles (CS‐PLGA NPs) as a novel delivery system enhance the bioavailability of food fortification nutraceutical applications. The nanoparticles, with sizes below 200 nm, exhibited greater stability than PLGA NPs after freeze‐drying in simulated body fluids. Encapsulation improved photostability under ultraviolet prolonged release fluids compared non‐encapsulated . Furthermore, CS‐PLGA demonstrated higher uptake intestinal epithelial cells (Caco‐2), indicating enhanced transport potential use fortified systems. These findings underscore promise delivering food, nutraceutical, pharmaceutical Practical Application offers promising solution bioavailability, especially individuals absorption issues. formulation improves stability, controlled release, uptake, which can lead more effective supplementation strategies It could benefit patients deficiencies, such those malabsorption disorders, by ensuring efficient through tract. Additionally, this approach be applied other water‐soluble vitamins bioactive compounds, offering versatile platform improving efficacy oral supplements.

Language: Английский

Citations

1
A pH-Responsive Hydrogel for the Oral Delivery of Ursolic Acid: A Pentacyclic Triterpenoid Phytochemical DOI Creative Commons
Carlos D. Gutierrez, Rosana L. Aranzábal, Ana M. Lechuga

et al.

Gels, Journal Year: 2024, Volume and Issue: 10(9), P. 602 - 602

Published: Sept. 22, 2024

In this study, poly(HEMA-PEGxMEM-IA) hydrogels were prepared by radical copolymerization of poly(ethylene glycol) methyl ether methacrylate (PEGxMEM), 2-hydroxyethyl (HEMA), and itaconic acid (IA). The reaction was carried out in ethanolic solution using N,N′-methylenebisacrylamide (MBA) as a crosslinking agent 1-hydroxycyclohexyl phenyl ketone (HCPK) photo-initiator. (HGx) evaluated delivery system for ursolic (UA), phytochemical extracted from the plant Clinopodium revolutum, “flor de arena”. characterized Fourier-transform infrared spectroscopy (FTIR-ATR), Raman spectroscopy, X-Ray diffraction (XRD), thermogravimetric analysis (TGA), scanning electron microscopy (SEM). swelling behavior studied buffer solutions pH 2 to 10, specifically at 2.2 (gastric environment) 7.4 (intestinal environment). It found that showed sensitivity pH. At 2.2, degree HG5 HG9 0.45 0.93 (g water/g hydrogel), respectively. 7.4, 1.97 2.64 SEM images show variation pore size function pH, UA crystals pores can also be observed. vitro release data best fit Korsmeyer–Peppas kinetic model diffusion exponent indicates mechanism is governed Fickian diffusion.

Language: Английский

Citations

0