Chitosan modified poly (lactic acid) nanoparticles increased the ursolic acid oral bioavailability

Antônio, Emilli; Antunes, Osmar dos Reis; Marcano, Rossana Gabriela Del Jesús Vásquez; Diedrich, Camila; Santos, Juliane da Silva; Machado, Christiane Schineider; Khalil, Najeh Maissar; Mainardes, Rubiana Mara

doi:10.1016/j.ijbiomac.2021.01.041

Cited by 32 publications

(17 citation statements)

References 66 publications

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“…Meticulous literature research to find UA-based polymer formulations as possible antimicrobial agents revealed to us that, while there are numerous articles on the in vitro antimicrobial activity of unformulated UA or its derivatives, articles regarding the in vitro antimicrobial activity of UA-based polymer formulations are practically absent. Most of the previously prepared NPs loaded with UA have, in fact, been studied for their anti-inflammatory [57,58] or antitumor activity [59][60][61][62]. To the best of our knowledge, except for our previous article on UA-loaded dendrimer NPs whose antibacterial activity was not attributable to UA [55], the only article on the antimicrobial activity of a UAliquid crystalline systems-based formulation established the improvement of the antifungal activity of UA [63].…”

Section: Determination Of Mics Of Ua-g4k and Uamentioning

confidence: 99%

Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

et al. 2021

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Ursolic acid (UA), a pentacyclic triterpenoid acid found in many medicinal plants and aromas, is known for its antibacterial effects against multi-drug-resistant (MDR) Gram-positive bacteria, which seriously threaten human health. Unfortunately, UA water-insolubility, low bioavailability, and systemic toxicity limit the possibilities of its application in vivo. Consequently, the beneficial activities of UA observed in vitro lose their potential clinical relevance unless water-soluble, not cytotoxic UA formulations are developed. With a nano-technologic approach, we have recently prepared water-soluble UA-loaded dendrimer nanoparticles (UA-G4K NPs) non-cytotoxic on HeLa cells, with promising physicochemical properties for their clinical applications. In this work, with the aim of developing a new antibacterial agent based on UA, UA-G4K has been tested on different strains of the Enterococcus genus, including marine isolates, toward which UA-G4K has shown minimum inhibitory concentrations (MICs) very low (0.5–4.3 µM), regardless of their resistance to antibiotics. Time-kill experiments, in addition to confirming the previously reported bactericidal activity of UA against E. faecium, also established it for UA-G4K. Furthermore, cytotoxicity experiments on human keratinocytes revealed that nanomanipulation of UA significantly reduced the cytotoxicity of UA, providing UA-G4K NPs with very high LD50 (96.4 µM) and selectivity indices, which were in the range 22.4–192.8, depending on the enterococcal strain tested. Due to its physicochemical and biological properties, UA-G4K could be seriously evaluated as a novel oral-administrable therapeutic option for tackling difficult-to-treat enterococcal infections.

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Section: Determination Of Mics Of Ua-g4k and Uamentioning

confidence: 99%

Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

et al. 2021

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“…Previous studies on UA-loaded chitosan focused on organic, acid-modified chitosan nanoparticles. Chitosan modified poly (lactic acid) nanoparticles by the emulsionsolvent evaporation method, which was used extensively to improve the bioavailability of UA [14]. The folate-chitosan nanoparticles loaded with UA could increase the solubility of UA [15].…”

Section: Introductionmentioning

confidence: 99%

Effects of Different Drying Methods on the Characterization, Dissolution Rate and Antioxidant Activity of Ursolic Acid-Loaded Chitosan Nanoparticles

Zhao

Duan

Cao

et al. 2021

Foods

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To improve the water solubility of ursolic acid (UA), UA-loaded chitosan nanoparticles were firstly prepared by the ionotropic gelation method and dried by freeze drying (FD), microwave freeze drying (MFD) and spray drying (SD). The characterization of UA-loaded chitosan nanoparticles was performed with particle size, drug loading (DL), scanning electron microscope (SEM), fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), dissolution studies and antioxidant activity. The results demonstrated that UA was successfully encapsulated into chitosan nanoparticles using sodium tripolyphosphate (TPP) as a cross-linker, with a 79% encapsulation efficiency. The spray-dried, UA-loaded chitosan nanoparticles had the lowest drug loading (11.8%) and the highest particle size (496.9 ± 11.20 nm). The particle size of UA-loaded chitosan nanoparticles dried by MFD and FD was lower, at 240.8 ± 12.10 nm and 184.4 ± 10.62 nm, respectively, and their antioxidant activity was higher than those nanoparticles dried by SD. Moreover, the drying time and energy consumption of UA-loaded chitosan nanoparticles dried by MFD and SD were lower than that of FD. The dissolution rates of UA-loaded chitosan nanoparticles prepared by FD and MFD were 60.6% and 57.1%, respectively, in a simulated gastric fluid, which was a greater value than SD (55.9%). Therefore, the UA-loaded chitosan nanoparticles encapsulation method, combined with MFD technology, showed a promising potential to improve the water solubility of UA.

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“…First of all, bioavailability is the rate and extent to which a drug is absorbed into the circulation of the body, which is affected by the chemical structure, solubility, hydrophilic lipophilicity, stability, dosage form characteristics and other factors of the drug molecule ( Tjandrawinata et al, 2018 ). The stability, surface modification and the development of preparation technology of nanoformulations have greatly improved the bioactivity and bioavailability of UA molecules ( Yang et al, 2012 ; Antonio et al, 2021 ). Studies have confirmed that the area under the plasma drug concentration-time curve (AUC) and the peak concentration ( C max ) that can be achieved after administration of UA nanoformulations in vivo are 2–3 times that of the original UA molecules ( Pi et al, 2016 ; Qiu et al, 2019 ).…”

Section: Current Situation and Future Prospects Of Ua Nanoformulationsmentioning

confidence: 99%

Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule

et al. 2021

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Background: Ursolic acid (UA) is a natural pentacyclic triterpene derived from fruit, herb, and other plants. UA can act on molecular targets of various signaling pathways, inhibit the growth of cancer cells, promote cycle stagnation, and induce apoptosis, thereby exerting anticancer activity. However, its poor water-solubility, low intestinal mucosal absorption, and low bioavailability restrict its clinical application. In order to overcome these deficiencies, nanotechnology, has been applied to the pharmacological study of UA.Objective: In this review, we focused on the absorption, distribution, and elimination pharmacokinetics of UA in vivo, as well as on the research progress in various UA nanoformulations, in the hope of providing reference information for the research on the anticancer activity of UA.Methods: Relevant research articles on Pubmed and Web of Science in recent years were searched selectively by using the keywords and subheadings, and were summarized systematically.Key finding: The improvement of the antitumor ability of the UA nanoformulations is mainly due to the improvement of the bioavailability and the enhancement of the targeting ability of the UA molecules. UA nanoformulations can even be combined with computational imaging technology for monitoring or diagnosis.Conclusion: Currently, a variety of UA nanoformulations, such as micelles, liposomes, and nanoparticles, which can increase the solubility and bioactivity of UA, while promoting the accumulation of UA in tumor tissues, have been prepared. Although the research of UA in the nanofield has made great progress, there is still a long way to go before the clinical application of UA nanoformulations.

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Chitosan modified poly (lactic acid) nanoparticles increased the ursolic acid oral bioavailability

Cited by 32 publications

References 66 publications

Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

Effects of Different Drying Methods on the Characterization, Dissolution Rate and Antioxidant Activity of Ursolic Acid-Loaded Chitosan Nanoparticles

Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule

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