Dry amorphisation of mangiferin, a poorly water-soluble compound, using mesoporous silica

Baán, Adrienn; Adriaensens, Peter; Lammens, Joris; Hernández, René Delgado; Berghe, Wim Vanden; Pieters, Luc; Vervaet, Chris; Kiekens, Filip

doi:10.1016/j.ejpb.2019.05.026

Cited by 14 publications

(4 citation statements)

References 25 publications

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“…Similarly, our results further suggest that MGF has potential value to be used as adjuvant phytotherapeutic treatment against CRC to reduce adverse toxicity and to mitigate outcome of colon cancer treatment. To further develop its application in clinical practice, more molecular combination studies with different MGF formulations ( du Plessis-Stoman et al, 2011 ; Morozkina et al, 2021 ; Baán et al, 2019 ) as well as uniformly controlled clinical trials are needed.…”

Section: Discussionmentioning

confidence: 99%

Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism

et al. 2021

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In spite of the current advances and achievements in cancer treatments, colorectal cancer (CRC) persists as one of the most prevalent and deadly tumor types in both men and women worldwide. Drug resistance, adverse side effects and high rate of angiogenesis, metastasis and tumor relapse remain one of the greatest challenges in long-term management of CRC and urges need for new leads of anticancer drugs. We demonstrate that CRC treatment with the phytopharmaceutical mangiferin (MGF), a glucosylxanthone present in Mango tree stem bark and leaves (Mangifera Indica L.), induces dose-dependent tumor regression and decreases lung metastasis in a syngeneic immunocompetent allograft mouse model of murine CT26 colon carcinoma, which increases overall survival of mice. Antimetastatic and antiangiogenic MGF effects could be further validated in a wound healing in vitro model in human HT29 cells and in a matrigel plug implant mouse model. Interestingly, transcriptome pathway enrichment analysis demonstrates that MGF inhibits tumor growth, metastasis and angiogenesis by multi-targeting of mitochondrial oxidoreductase and fatty acid β-oxidation metabolism, PPAR, SIRT, NFκB, Stat3, HIF, Wnt and GP6 signaling pathways. MGF effects on fatty acid β-oxidation metabolism and carnitine palmitoyltransferase 1 (CPT1) protein expression could be further confirmed in vitro in human HT29 colon cells. In conclusion, antitumor, antiangiogenic and antimetastatic effects of MGF treatment hold promise to reduce adverse toxicity and to mitigate therapeutic outcome of colorectal cancer treatment by targeting mitochondrial energy metabolism in the tumor microenvironment.

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Section: Discussionmentioning

confidence: 99%

Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism

et al. 2021

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“…The amorphous form of several drugs, including ibuprofen, griseofulvin, indomethacin, simvastatin, nifedipine, ezetimibe, and celecoxib, can be physically stabilized by using mesoporous materials [10,[20][21][22]. Interestingly, a recent study revealed that mangiferin, a promising therapeutic polyphenol, can be transformed into its amorphous form by balling milling with mesoporous silica [23].…”

Section: Nano-confinement Effect On Molecular Dynamicsmentioning

confidence: 99%

Mesoporous Drug Delivery System: From Physical Properties of Drug in Solid State to Controlled Release

Wang

Xin

et al. 2023

Molecules

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Mesoporous materials, which exhibit great potential in the control of polymorphs and delivery of poorly water-soluble drugs, have obtained considerable attention in the field of pharmaceutical science. The physical properties and release behaviors of amorphous or crystalline drugs may be affected by formulating them into mesoporous drug delivery systems. In the past few decades, an increasing amount of papers have been written about mesoporous drug delivery systems, which play a crucial role in improving the properties of drugs. Herein, mesoporous drug delivery systems are comprehensively reviewed in terms of their physicochemical characteristics, control of polymorphic forms, physical stability, in vitro performance, and in vivo performance. Moreover, the challenges and strategies of developing robust mesoporous drug delivery systems are also discussed.

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“…The XRD diffractogram of mangiferin showed characteristic peaks of diffraction [34,35], and the developed mangiferin-loaded formulation also has diffraction peaks, but the intensity of the peak is less as compared to mangiferin peaks, as mentioned in Figure 7. The intensity of the peak was very low in the mangiferin-loaded formulation, indicating the uniform distribution of the mangiferin in the developed nanocrystals [36]. To ascertain whether the generated particles were crystalline or amorphous, X-ray diffraction examinations on raw and processed samples were conducted.…”

Section: X-ray Diffraction (Xrd) Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

Sarwar,

Iqbal,

Jamil

et al. 2023

Molecules

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Making nanoscale drug carriers could boost the bioavailability of medications that are slightly water soluble. One of the most promising approaches for enhancing the chemical stability and bioavailability of a variety of therapeutic medicines is liquid nanocrystal technology. This study aimed to prepare nanocrystals of mangiferin for sustained drug delivery and enhance the pharmacokinetic profile of the drug. The fractional factorial design (FFD) was used via a selection of independent and dependent variables. The selected factors were the concentration of mangiferin (A), hydroxypropyl methyl cellulose (HPMC) (B), pluronic acid (C), tween 80 (D), and the ratio of antisolvent to solvent (E). The selected responses were the particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. The nanocrystals were further evaluated for mangiferin release, release kinetics, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), particle size, zeta potential, and scanning electron microscopy (SEM). The stability studies of developed nanocrystals were performed for 6 months and pharmacokinetics on albino rabbits. The value of entrapment efficiencies ranged from 23.98% to 86.23%. The percentage release of mangiferin varied from 62.45 to 99.02%. FTIR and DSC studies showed the stability of mangiferin in the nanocrystals. The particle size of the optimized formulation was almost 100 nm and −12 mV the value of the zeta potential. The results of stability studies showed that the nanocrystals of mangiferin were stable for a period of six months. The peak plasma concentration of mangiferin from nanocrystals and suspension of mangiferin were 412 and 367 ng/mL, respectively. The value of AUC0−t of nanocrystals and suspension of mangiferin was 23,567.45 ± 10.876 and 18,976.12 ± 9.765 µg×h/mL, respectively, indicating that the nanocrystals of mangiferin showed greater availability of mangiferin compared to the suspension of the formulation. The developed nanocrystals showed a good release pattern of mangiferin, better stability studies, and enhanced the pharmacokinetics of the drug.

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Dry amorphisation of mangiferin, a poorly water-soluble compound, using mesoporous silica

Cited by 14 publications

References 25 publications

Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism

Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism

Mesoporous Drug Delivery System: From Physical Properties of Drug in Solid State to Controlled Release

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

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