An Enhanced Water Solubility and Stability of Anthocyanins in Mulberry Processed with Hot Melt Extrusion

Mulberry fruits are rich sources of anthocyanins that exhibit beneficial biological activity. These anthocyanins become instable in an aqueous media, leading to their low bioavailability. In this study, a colloidal dispersion was produced by processing mulberry samples with hot-melt extrusion. In this process, hydrophilic polymer matrices were used to disperse the compound in an aqueous media. Mulberry samples were processed with hot-melt extrusion and in the presence of an ionization agent and sodium alginate to form mulberry-extrudate solid formulations. The particle size of mulberry-extrudate solid formulations decreased, while the total phenol content, the total anthocyanin content, and solubility increased. Fourier transform infrared spectroscopy (FT-IR) revealed that mulberry-extrudate solid formulations now contained new functional groups, such as –COOH group. We investigated whether mulberry-extrudate solid formulations had a positive impact on the stability of anthocyanins. The non-extrudate mulberry sample and mulberry-extrudate solid formulations were incubated with a simulated gastric fluid system and an intestinal fluid system. The number of released anthocyanins was determined with HPLC. We found that anthocyanins were released rapidly from non-extrudate mulberry extract. Mulberry-extrudate solid formulations contained a large number of available anthocyanins even after being incubated for 180 min in the intestinal fluid system. Thus, hot-melt extrusion enhanced water solubility and stability of anthocyanins with the prolonged release.

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Vacuum Compression Molding as a Screening Tool to Investigate Carrier Suitability for Hot-Melt Extrusion Formulations

Pharmaceutics ◽

10.3390/pharmaceutics12111019 ◽

2020 ◽

Vol 12 (11) ◽

pp. 1019

Author(s):

Gauri Shadambikar ◽

Thomas Kipping ◽

Nicole Di-Gallo ◽

Alessandro-Giuseppe Elia ◽

Anja-Nadine Knüttel ◽

...

Keyword(s):

Screening Tool ◽

Drug Carriers ◽

Hot Melt Extrusion ◽

Compression Molding ◽

Simulated Gastric Fluid ◽

Formulation Development ◽

Melt Extrusion ◽

Scanning Calorimetry ◽

Production Scale ◽

Hot Melt

Hot-melt extrusion (HME) is the most preferred and effective method for manufacturing amorphous solid dispersions at production scale, but it consumes large amounts of samples when used for formulation development. Herein, we show a novel approach to screen the polymers by overcoming the disadvantage of conventional HME screening by using a minimum quantity of active pharmaceutical ingredient (API). Vacuum Compression Molding (VCM) is a fusion-based method to form solid specimens starting from powders. This study aimed to investigate the processability of VCM for the creation of amorphous formulations and to compare its results with HME-processed formulations. Mixtures of indomethacin (IND) with drug carriers (Parteck® MXP, Soluplus®, Kollidon® VA 64, Eudragit® EPO) were processed using VCM and extrusion technology. Thermal characterization was performed using differential scanning calorimetry, and the solid-state was analyzed via X-ray powder diffraction. Dissolution studies in the simulated gastric fluid were performed to evaluate the drug release. Both technologies showed similar results proving the effectiveness of VCM as a screening tool for HME-based formulations.

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Evaluation of hot-melt extrusion technique in the preparation of HPC matrices for prolonged release

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2013.10.014 ◽

2014 ◽

Vol 52 ◽

pp. 77-85 ◽

Cited By ~ 28

Author(s):

Giulia Loreti ◽

Alessandra Maroni ◽

Maria Dorly Del Curto ◽

Alice Melocchi ◽

Andrea Gazzaniga ◽

...

Keyword(s):

Hot Melt Extrusion ◽

Prolonged Release ◽

Melt Extrusion ◽

Hot Melt

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IMPROVING SOLUBILITY AND DISSOLUTION OF A NATURAL PRODUCT APIGENIN VIA PREPARATION OF SOLID DISPERSION BY HOT MELT EXTRUSION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021.v13s3.10 ◽

2021 ◽

pp. 47-52

Author(s):

SOFI N. STIANI ◽

TAOFIK RUSDIANA ◽

ANAS SUBARNAS

Keyword(s):

Solid Dispersion ◽

Water Solubility ◽

Practical Method ◽

Hot Melt Extrusion ◽

Raw Material ◽

Melt Extrusion ◽

Scanning Calorimetry ◽

Twin Screw ◽

Hot Melt

Objective: Hot Melt Extrusion (HME) is one of the techniques for preparing a solid dispersion hydrophilic excipient known as a no solvents practical method to increase the solubility of drugs. Apigenin (APG) has properties that thermal stable with melting point 345-350 °C but very low solubility in the water around 1,35 µg/ml. The polymer is stable in the HME method are Soluplus and Kollidon VA 64. The study aims to optimize the kind of polymer in HME formulae to improve the solubility and dissolution rate of apigenin by solid dispersion using hot-melt extrusion. Methods: Apigenin 10–50% w/w and Kollidon®VA 64 or Soluplus® and combination of Kollidon®VA 64 and Soluplus® were mixed, and the resulting blends extruded using a twin-screw extruder (Teach-Line ZK25T). Characterization of apigenin extrudates conducted using scanning electron microscopy, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffractometry, and dissolution. Results: Solubility studies presented enhancement in apigenin of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 (90%); and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% increased more than 18,25; 16,18-and 8,52-fold in water, respectively. Furthermore dissolution studies showed enhancement in apigenin percent release of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 90%; and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% tablet apigenin HME up to 34,29%; 69,75% and 30,69%, respectively. Conclusion: The formulation of 10% w/w Apigenin and 90% Soluplus® using hot-melt extrusion able to increase water solubility approximately 18,25-fold than raw material apigenin.

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Development of a Polymer-Mediated Soybean Nanocomposite by Hot Melt Extrusion to Improve Its Functionality and Antioxidant Properties

Foods ◽

10.3390/foods8020041 ◽

2019 ◽

Vol 8 (2) ◽

pp. 41 ◽

Cited By ~ 3

Author(s):

Md Azad ◽

Won Kim ◽

Cheng Jin ◽

Wie Kang ◽

Cheol Park ◽

...

Keyword(s):

Water Solubility ◽

Hydroxypropyl Methylcellulose ◽

Antioxidant Properties ◽

Food Products ◽

Hot Melt Extrusion ◽

Total Phenolic ◽

Melt Extrusion ◽

Antioxidant Power ◽

Soybean Food ◽

Hot Melt

The poor bioaccessibility of the phenolic compounds of soybeans is a key challenge to developing functional food products. Therefore, a novel hydrophilic food-grade hydroxypropyl methylcellulose (HPMC) polymer was added to soybean to prepare a soybean food composite (SFC), in order to improve the soybean’s functionality. The SFC was prepared with soybean (95%) plus HPMC (5%) (w/w) mixes (HSE), as well as 100% soybean extrudate (SE), at 80 °C and 130 °C by a hot melt extrusion (HME) process. A non-extrudate 100% soybean material was considered as a control. It is observed that water solubility was significantly increased (35.18%), and particle size reached to nano-size (171.5 nm) in HSE at 130 °C compared to the control (7.14% and 1166 nm, respectively). The total phenolic, flavonoid, and single isoflavones content, including daidzin, daidzein, glycitein, genistein, and genistin was significantly increased in HSE at 130 °C compared to the control. The antioxidant properties were also significantly increased in HSE at 130 °C compared to the control, measured by 2,2-diphenyl-1 picryl hydrazyl (DPPH), a ferric reducing antioxidant power assay (FRAP), and the phosphomolybdenum method (PPMD). Finally, it is concluded that the HPMC polymer could be used as a novel excipient to develop nanocomposite via HME, in order to improve the functionality of soybean food products.

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