Manufacturing Different Types of Solid Dispersions of BCS Class IV Polyphenol (Daidzein) by Spray Drying: Formulation and Bioavailability

Daidzein (DZ) is a polyphenolic compound belonging to Biopharmaceutical Classification System class IV, which shows that it may have limited therapeutic effects due to its low solubility and poor bioavailability. This study aimed to obtain high-purity DZ and prepare and characterize different types of solid dispersions (SDs) in order to enhance aqueous solubility and bioavailability. Excipients were investigated in order to manufacture different types of solid dispersions (SDs). Second-generation solid dispersions (SG), third-generation solid dispersions (TG), and second- and third-generation pH-modulated solid dispersions (SD and TG pHM-SD) were produced via spray drying. The SDs were characterized and tested for in vitro DZ release and oral bioavailability. SDs have shown increased aqueous solubility and in vitro release rate. Solid-state characterization showed that DZ was in an amorphous state in most of the formulations. The enhanced aqueous solubility of TG-pHM SD was reflected by an increase in oral bioavailability, which significantly increased the maximum plasma concentration approximately 20-fold and decreased the time to reach the maximum plasma concentration. The production of pHM SDs that contain DZ via spray drying is a simple and effective approach for oral drug delivery, which has the potential to greatly reduce the dose and enhance therapeutics effects

Preparation of Spray-Dried Soy Isoflavone-Loaded Gelatin Microspheres for Enhancement of Dissolution: Formulation, Characterization and in Vitro Evaluation

The most bioactive soy isoflavones (SI), daidzein (DAI) and genistein (GEN) have poor water solubility, which reduces their bioavailability and health benefits and limits their use in industry. The goal of this study was to develop and characterize a new gelatin matrix to microencapsulate DAI and GEN from soy extract (SE) by spray drying, in order to obtain solid dispersions to overcome solubility problems and to allow controlled release. The influences of 1:2 (MP2) and 1:3 (MP3) SE/polymer ratios on the solid state, yield, morphology, encapsulation efficiency, particle size distribution, release kinetics and cumulative release were evaluated. Analyses showed integral microparticles and high drug content. MP3 and MP2 yield were 43.6% and 55.9%, respectively, with similar mean size (p > 0.05), respectively. X-ray diffraction revealed the amorphous solid state of SE. In vitro release tests showed that dissolution was drastically increased. The results indicated that SE microencapsulation might offer a good system to control SI release, as an alternative to improve bioavailability and industrial applications

<i>In vitro</i> antioxidant potential and <i>in vivo</i> effects of <i>Schinus terebinthifolia</i> Raddi leaf extract in diabetic rats and determination of chemical composition by HPLC-ESI-MS/MS

<p>The present study investigated the <i>in vitro</i> and <i>in vivo</i> antioxidant potential and phytochemical composition of <i>Schinus terebinthifolia</i>, which is widely used in folk medicine for various therapeutic purposes. The <i>in vitro</i> analyses indicated that the hydroethanolic extract (HE) had 312.50 ± 0.50 mg GAE/g of total phenols. It also presented anti-DPPH• and anti-ABTS•⁺ activity, reduced phosphomolybden and metal ions and blocked the bleaching of β-carotene. The HE at concentrations of 3.0 and 2.0 μg/mL had TRAP values of 2.223 ± 0.018 and 1.894 ± 0.026 μM Trolox, respectively. The HE increased the availability of antioxidants in plasma in treated animals <i>in vivo</i>. HPLC-ESI-MS/MS indicated the presence of 11 phenols: cumaric acid, (+)-catechin, myricetin-3-<i>O</i>-glicuronide, kaempferol-3-<i>O</i>-glucoside, myricetin, myricitrin, quercetin, gallic acid, methyl galate, pentagalloyl glucose and ethyl galate. Thus, <i>S. terebinthifolia</i> has potential for the prevention or treatment of diseases that are related to oxidative stress, such as diabetes mellitus.</p