Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

Abstract

The aim of our research was to improve the solubility and antioxidant activity of pterostilbene (PTR) by developing a novel amorphous solid dispersion (ASD) with Soluplus® (SOL). DSC analysis and mathematical models were used to select the three appropriate PTR and SOL weight ratios. The amorphization process was carried out by a low-cost and green approach involving dry milling. An XRPD analysis confirmed the full amorphization of systems in 1:2 and 1:5 weight ratios. One glass transition (Tg) observed in DSC thermograms confirmed the complete miscibility of the systems. The mathematical models indicated strong heteronuclear interactions. SEM micrographs suggest dispersed PTR within the SOL matrix and a lack of PTR crystallinity, and showed that after the amorphization process, PTR-SOL systems had a smaller particle size and larger surface area compared with PTR and SOL. An FT-IR analysis confirmed that hydrogen bonds were responsible for stabilizing the amorphous dispersion. HPLC studies showed no decomposition of PTR after the milling process. PTR’s apparent solubility and antioxidant activity after introduction into ASD increased compared to the pure compound. The amorphization process improved the apparent solubility by ~37-fold and ~28-fold for PTR-SOL, 1:2 and 1:5 w/w, respectively. The PTR-SOL 1:2 w/w system was preferred due to it having the best solubility and antioxidant activity (ABTS: IC50 of 56.389 ± 0.151 µg·mL−1 and CUPRAC: IC0.5 of 82.52 ± 0.88 µg·mL−1).

Myricetin Amorphous Solid Dispersions—Antineurodegenerative Potential

“…Amorphous materials lack long-range order in their atomic arrangement, while crystalline materials exhibit a regular and repeating pattern. Confirming the amorphous/crystalline nature of a substance is crucial as it affects its physical and chemical properties, including solubility, stability, and bioavailability [ 46 , 47 , 48 , 50 , 55 , 56 , 59 ].…”

“…Research studies provide that the lack of melting effect and the appearance of T g confirm full amorphization [ 48 , 50 , 64 ]. For example, amorphous polyphenol-PVP dispersions for which the melting point of polyphenol disappeared were presented for curcumin [ 62 ], daidzein [ 44 ], genistein [ 45 ], naringenin + hesperetin [ 56 ], and wogonin [ 65 ].…”

“…The use of ASD technology allows for the creation of a stable, amorphous structure that enhances the dissolution properties of polyphenols, thereby increasing their bioavailability. Over the past years, the preparation of ASDs of curcumin [ 41 , 42 , 43 ], daidzein [ 44 ], genistein [ 45 ], hesperidin [ 46 , 47 ], hesperetin [ 47 , 48 ], myricetin [ 32 , 34 ], naringenin [ 49 ], pterostilbene [ 50 ], quercetin [ 51 , 52 , 53 ], resveratrol [ 42 ], and sinapic acid [ 54 ] has been confirmed. These works confirm that the amorphization process makes it possible to significantly improve the solubility and/or biological activity of polyphenols.…”

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

“…At specific time intervals, 2.0 mL of the sample was taken out and immediately replaced with an equal amount of fresh medium at the same temperature. The percentage cumulative cannabinoid release (% CBD, CBDA, and CBC) was measured at different time points (5,10,15,30,45,60,90,120, and 180 min) for each formulation. The samples were then passed through a filter with a pore size of 0.22 µm and analyzed using high-performance liquid chromatography (HPLC).…”

“…Two systems of the HiE with Neusilin US2, and Sol prepared in a 1:1 mass ratio (extract weight: carrier) using a solvent-evaporation technique, were enrolled in the dissolution study. The percentage cumulative cannabinoid release (% CBD, CBDA, and CBC) was measured at different time points (5,10,15,30,45,60,90,120, and 180 min) for each system.…”