Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

Abstract

The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME were evaluated using morphologic, chromatographic, thermic, spectroscopic, and diffractometric assays. The flow, wettability, and dissolution rate of HME powders were also assessed. Both CE and its marker theobromine proved to be stable under heating according to thermal analysis and Arrhenius plot under isothermal conditions. Physicochemical analysis confirmed the stability of CE HME preparations and provided evidence of drug–polymer interactions. Improvements in the functional characteristics of CE were observed after the extrusion process, particularly in dissolution and flow properties. In addition, the use of a mixture design allowed the identification of synergic effects by excipient combination. The optimized combination of polymers obtained considering four different aspects showed that a mixture of the Soluplus, Plasdone S630, and Eudragit E in equal proportions produced the best results (flowability index 88%; contact angle 47°; dispersibility 7.5%; and dissolution efficiency 87%), therefore making the pharmaceutical use of CE more feasible.

3D Printed Drug Delivery Systems Based on Natural Products

“…Nevertheless, FDM possesses the potential to become a suitable candidate to manufacture drug delivery systems containing natural products. Although no work has been found employing FDM for natural products, as mentioned in Section 2.2 , some researchers have clearly demonstrated the feasibility of HME to develop filaments made of natural products [ 49 , 50 , 51 , 52 ]. Seeing HME as a previous step of FDM, it is reasonable to consider FDM as alternative to PAM.…”

“…The 3D printed medicines containing natural products as API have not been developed yet. Nevertheless, there are some studies that employ plant extracts to manufacture filaments by hot-melt extrusion [ 49 , 50 , 51 , 52 ]. The possibility of obtaining filaments loaded with plant extracts offers a valuable potential for the preparation of 3D printed drug delivery systems containing natural APIs by FDM.…”

“…Pinho et al [ 49 ] produced filaments containing cocoa extracts (CE) obtained from Theobroma cacao . This natural product, commonly employed in the food industry, also shows therapeutic potential, because of its cardioprotective and anti-inflammatory actions [ 53 ].…”

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

“…The compressibility (%) was determined in triplicate using a powder characteristic tester, PT-N (Hosokawa Micron Powder Systems, Summit, NJ, USA), based on the values of aerated density (δa) and packed density (δt) using the following equation [ 31 ]: compressibility (%) = 100 × (δt − δa)/δt, for samples that could not be analyzed due to their high cohesiveness, a compressibility value equal to 40% obtained for cohesive materials was assigned for model analysis purposes.…”

Bio- Fortification of Angelica gigas Nakai Nano-Powder Using Bio-Polymer by Hot Melt Extrusion to Enhance the Bioaccessibility and Functionality of Nutraceutical Compounds

“…The spectra are presented in (Figure 5), which shows that the splitting peak is in the range 1700−3500 cm −1 in polymer-mediated extrudate AGNC; however, no splitting peak was observed in FAGN in the same range. The changes in the FTIR spectra of the AGNC formulations are mainly related to the intensity and position of some bands corresponding to the formation of new functional groups, suggesting an interaction of secondary metabolites with the polymeric matrix [45]. In the HP-mediated extrudate AGNC, there is a new peak in the wavelength of 3315 and 2929 cm −1 , which corresponds to O-H and CH 2 stretching.…”