Oral supplementation of solvent-free kynurenic acid/cyclodextrin nanosponges complexes increased its bioavailability

Monfared, Yousef Khazaei; Pedrazzo, Alberto Rubin; Mahmoudian, M.R.; Caldera, Fabrizio; Zakeri–Milani, Parvin; Valizadeh, Hadi; Cavalli, Roberta; Matencio, Adrián; Trotta, Francesco

doi:10.1016/j.colsurfb.2022.113101

Cited by 6 publications

(8 citation statements)

References 39 publications

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“…Results demonstrated insignificant changes in the measured parameters for all tested groups compared to normal healthy control mice ( p ≥ 0.05), suggesting the safety of the developed formulations. Our results were in accordance with many reported articles describing the safety and biocompatibility of ß-CD-NS [ 68 , 69 ].…”

Section: Resultssupporting

confidence: 93%

“…Despite the extensive reports on the nephroprotective role of FS [ 70 ], the renal tissue was the most affected by FS suspension ( Figure 11 C(c)). Since this was only obvious based on histopathological but not biochemical analysis, the slight changes observed could be attributed to different factors, including mice physiological state and other effects on nutrients uptake, among others [ 68 ]. Interestingly, renal tissues showed no symptoms of toxicity for FS-NS formulations ( Figure 11 C(d,e)).…”

Section: Resultsmentioning

confidence: 99%

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Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer

Aboushanab,

El-Moslemany,

El-Kamel

et al. 2023

Pharmaceutics

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Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to develop lactoferrin-coated FS-loaded β-cyclodextrin nanosponges (LF-FS-NS) for targeted FS delivery to breast cancer. NS formation through cross-linking of β-cyclodextrin by diphenyl carbonate was confirmed by FTIR and XRD. The selected LF-FS-NS showed good colloidal properties (size 52.7 ± 7.2 nm, PDI < 0.3, and ζ-potential 24 mV), high loading efficiency (96 ± 0.3%), and sustained drug release of 26 % after 24 h. Morphological examination using SEM revealed the mesoporous spherical structure of the prepared nanosponges with a pore diameter of ~30 nm, which was further confirmed by surface area measurement. Additionally, LF-FS-NS enhanced FS oral and IP bioavailability (2.5- and 3.2-fold, respectively) compared to FS suspension in rats. Antitumor efficacy evaluation in vitro on MDA-MB-231 cells and in vivo on an Ehrlich ascites mouse model demonstrated significantly higher activity and targetability of LF-FS-NS (30 mg/kg) compared to the free drug and uncoated formulation. Consequently, LF-FS-NS could be addressed as a promising formulation for the effective management of breast cancer.

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Section: Resultssupporting

confidence: 93%

Section: Resultsmentioning

confidence: 99%

Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer

Aboushanab,

El-Moslemany,

El-Kamel

et al. 2023

Pharmaceutics

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“…The kneading process presents some advantages because it is scalable, easy and efficient [ 13 ]. The 5% of loading (1:0.05 w/w ratio) is considerably lower than several complexes prepared [ 7 , 12 ] suggesting (i) that all the VitD3 will enter completely in the cavities and (ii) the high quantity of βNS-CDI (1:4) will control the release equilibrium. Figure 1 A shows the FTIR-ATR spectra of the VitD3, βNS-CDI (1:4), physical mixture and inclusion complex.…”

Section: Resultsmentioning

confidence: 88%

“…On the other hand, the thermostability study demonstrated a greater loss of VitD3 in the physical mixture, due to the non-formation of the inclusion complex. It is widely known that the formation of the inclusion complex is capable of protecting and increasing the stability of the drug inside it [ 12 ]. In addition, all these vitamin D forms were also tested mimicking oral human administration in vitro to explore their biological effectiveness.…”

Section: Discussionmentioning

confidence: 99%

“…In addition, nanosponges have been reported to be able to increase the stability of drugs and reduce their degradation [ 9 ]. Recent reviews [ 7 , 10 ] point to their wide potential and minimal negligible toxicity [ 11 , 12 ], increasing their bio-capacities in several applications including the ability to (i) increase or improve the apparent solubility of poorly soluble drugs, (ii) modulate the drug release and activity, (iii) protect drugs against several agents, (iv) enhance bioactivities, (v) absorb contaminants or deliver the drug, etc.…”

Section: Introductionmentioning

confidence: 99%

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Developing New Cyclodextrin-Based Nanosponges Complexes to Improve Vitamin D Absorption in an In Vitro Study

Uberti

Pagliaro

Bisericaru

et al. 2023

IJMS

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Vitamin D plays an important role in numerous cellular functions due to the ability to bind the Vitamin D receptor (VDR), which is present in different tissues. Several human diseases depend on low vitamin D3 (human isoform) serum level, and supplementation is necessary. However, vitamin D3 has poor bioavailability, and several strategies are tested to increase its absorption. In this work, the complexation of vitamin D3 in Cyclodextrin-based nanosponge (CD-NS, in particular, βNS-CDI 1:4) was carried out to study the possible enhancement of bioactivity. The βNS-CDI 1:4 was synthesized by mechanochemistry, and the complex was confirmed using FTIR-ATR and TGA. TGA demonstrated higher thermostability of the complexed form. Subsequently, in vitro experiments were performed to evaluate the biological activity of Vitamin D3 complexed in the nanosponges on intestinal cells and assess its bioavailability without cytotoxic effect. The Vitamin D3 complexes enhance cellular activity at the intestinal level and improve its bioavailability. In conclusion, this study demonstrates for the first time the ability of CD-NS complexes to improve the chemical and biological function of Vitamin D3.

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