Chitosan composite microparticles: A promising gastroadhesive system for taxifolin

Moura, Fernanda Cristina Stenger; Perioli, Luana; Pagano, Cinzia; Vivani, Riccardo; Ambrogi, Valeria; Bresolin, Tania Mari Bellé; Ricci, Maurizio; Schoubben, Aurelie Marie Madeleine

doi:10.1016/j.carbpol.2019.04.075

Cited by 20 publications

(16 citation statements)

References 68 publications

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“…The use of Tax polymorphs, characterized by a better solubilization rate than Pristine-Tax, would consent to improve its efficacy and eventually extend its application field without the necessity of using excipients. In fact, reviewing the literature, several papers disclose the use of excipients as a strategy to increase Tax bioavailability [ 56 , 57 , 58 , 59 , 60 ].…”

Section: Resultsmentioning

confidence: 99%

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

et al. 2021

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Taxifolin, also known as dihydroquercetin, possesses several interesting biological properties. The purpose of the study was to identify polymorphs of taxifolin prepared using crystallization in different solvents. Data from X-ray powder diffraction, differential scanning calorimetry, and thermogravimetry enabled us to detect six different crystalline phases for taxifolin. Besides the already known fully hydrated phase, one partially hydrated phase, one monohydrated phase, two anhydrous polymorphs, and one probably solvated phase were obtained. The unit cell parameters were defined for three of them, while one anhydrous polymorph was fully structurally characterized by X-ray powder diffraction data. Scanning electron microscopy and hot stage microscopy were also employed to characterize the crystallized taxifolin powders. The hydrate and anhydrous forms showed remarkable stability in drastic storage conditions, and their solubility was deeply evaluated. The anhydrous form converted into the hydrate form during the equilibrium solubility study and taxifolin equilibrium solubility was about 1.2 mg/mL. The hydrate taxifolin intrinsic dissolution rate was 56.4 μg cm−2 min−1. Using Wood’s apparatus, it was not possible to determine the intrinsic dissolution rate of anhydrous taxifolin that is expected to solubilize more rapidly than the hydrate form. In view of its high stability, its use can be hypothesized.

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Section: Resultsmentioning

confidence: 99%

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

et al. 2021

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“…It is obtained from crustacea shells, insect cuticles, and cell walls of some fungi and is straight-chain amino polysaccharide (poly- 1,4-D-glucosamine) with many features which are favorable for its use in drug delivery 9. It is being highly explored for its application in oral delivery 10. Not only chitosan, but its derivatives like glycol chitosan, thiolated chitosan, arginine-chitosan, carboxymethyl chitosan, aminated chitosan are also being explored for the drug delivery application 11,12.…”

Section: Introductionmentioning

confidence: 99%

<p>Ionically Cross-Linked Chitosan Nanoparticles for Sustained Delivery of Docetaxel: Fabrication, Post-Formulation and Acute Oral Toxicity Evaluation</p>

Mahmood¹,

Madni²,

Rehman³

et al. 2019

IJN

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IntroductionPolymeric nanoparticles are potential carriers for the efficient delivery of hydrophilic and hydrophobic drugs due to their multifaceted applications. Docetaxel is relatively less hydrophobic and twice as potent as paclitaxel. Like other taxane chemotherapeutic agents, docetaxel is not well tolerated and shows toxicity in the patients. Nanoencapsulation of potent chemotherapeutic agents has been shown to improve tolerability and therapeutic outcome. Therefore, the present study was designed to fabricate chitosan and sodium tripolyphosphate (STPP) based on ionically cross-linked nanoparticles for sustained release of docetaxel.MethodsNanoparticles were prepared by the ionic-gelation method by dropwise addition of the STPP solution into the chitosan solution in different ratios. CNPs were characterized for post-formulation parameters like size, zeta potential, scanning electron microscope (SEM), FTIR, DSC/TGA, pXRD, and in-vitro drug release, as well as for acute oral toxicity studies in Wistar rats.Results and discussionThe optimized docetaxel loaded polymeric nanoparticles were in the size range (172.6nm–479.65 nm), and zeta potential (30.45–35.95 mV) required to achieve enhanced permeation and retention effect. In addition, scanning electron microscopy revealed rough and porous surface, whereas, FTIR revealed the compatible polymeric nanoparticles. Likewise, the thermal stability was ensured through DSC and TG analysis, and powder X-ray diffraction analysis exhibited solid-state stability of the docetaxel loaded nanoparticles. The in-vitro drug release evaluation in phosphate buffer saline (pH 7.4) showed sustained release pattern, i.e. 51.57–69.93% within 24 hrs. The data were fitted to different release kinetic models which showed Fickian diffusion as a predominant release mechanism (R2= 0.9734–0.9786, n= 0.264–0.340). Acceptable tolerability was exhibited by acute oral toxicity in rabbits and no abnormality was noted in growth, behavior, blood biochemistry or histology and function of vital organs.ConclusionIonically cross-linked chitosan nanoparticles are non-toxic and biocompatible drug delivery systems for sustained release of chemotherapeutic agents, such as docetaxel.

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“…Inclusion complexes of the phenolic extracts (i.e., M2, M5, and E) and Syloid ® AL-1 (30:70, w : w ) were prepared using the solvent evaporation method [ 17 , 18 ]. In particular, the phenolic extract was solubilized in 10 mL ethanol, and Syloid ® AL-1 was then added to the solution that was left under magnetic stirring for 2 h. Ethanol was successively evaporated under vacuum, and the powder obtained was recovered and stored in a desiccator until further use.…”

Section: Methodsmentioning

confidence: 99%

“…An amount of inclusion complex was further processed to coat it with a lipid mixture (lauric acid:stearic acid, 77:33, w:w) characterized by a melting temperature of 37 °C. Briefly, the lipid mixture was melted at 40 °C, and the inclusion complex was added and stirred for 10 min [ 18 , 19 ]. The lipid:inclusion complex weight ratio was 1.1:1.…”

Section: Methodsmentioning

confidence: 99%

Exploiting Food-Grade Mesoporous Silica to Preserve the Antioxidant Properties of Fresh Olive Mill Wastewaters Phenolic Extracts

et al. 2021

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Fresh olive mill wastewaters phenolic extracts are of great interest as preservatives or fortifying ingredients but are characterized by limited stability. The purpose of this study was to use mesoporous silica to enhance their stability and preserve their antioxidant properties. The phenolic extracts were characterized for their composition by HPLC-DAD and included in a mesoporous matrix with or without a lipid coating. The inclusion complexes were characterized in terms of total phenolic content, radical scavenging capacity and in vitro antioxidative activity and cell compatibility. Besides, inclusion complex stability under different storage conditions (22 and 37 °C, 75% relative humidity, 1 month) was evaluated. The inclusion process was nearly quantitative and modified neither the total phenolic content nor the total antioxidant capacity. None of the inclusion complex concentrations assayed on the HT29 cell line showed toxicity. Moreover, HT29 cells treated with the inclusion complex exhibited a significant antioxidant effect, while the lipid coating impaired the antioxidant activity. The complexes without lipid were stable under all the investigated conditions, while the lipid-coated products were less stable under the more drastic conditions. Overall, inclusion complexes in mesoporous silica have suitable characteristics to be used for different applications, including food supplementation.

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Chitosan composite microparticles: A promising gastroadhesive system for taxifolin

Cited by 20 publications

References 68 publications

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

<p>Ionically Cross-Linked Chitosan Nanoparticles for Sustained Delivery of Docetaxel: Fabrication, Post-Formulation and Acute Oral Toxicity Evaluation</p>

Exploiting Food-Grade Mesoporous Silica to Preserve the Antioxidant Properties of Fresh Olive Mill Wastewaters Phenolic Extracts

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