Abstract
In this study, a novel ternary complex system (TCS) composed of baicalein, phospholipids, and Soluplus was prepared to improve the flowability and dissolution for baicalein phospholipid complex (BPC). TCS was characterized using differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The flowability, solubility, oil–water partition coefficient, in vitro dissolution, and in vivo pharmacokinetics of the system were also evaluated. DSC, IR, PXRD, and SEM data confirmed that the crystal form of baicalein disappeared in BPC and TCS. Furthermore, the angle of repose of TCS of 35° indicated an improvement in flowability, and solubility increased by approximately eight-fold in distilled water when TCS was compared with BPC (41.00 ± 4.89 μg/mL vs. 5.00 ± 0.16 μg/mL). Approximately 91.24% of TCS was released at the end of 60 min in 0.5% SDS (pH = 6.8), which suggested that TCS could improve the dissolution velocity and extent. Moreover, TCS exhibited a considerable enhancement in bioavailability with higher peak plasma concentration (25.55 μg/mL vs. 6.05 μg/mL) and increased AUC0–∞ (62.47 μg·h/mL vs. 50.48 μg·h/mL) with 123.75% relative bioavailability compared with BPC. Thus, Soluplus achieved the purpose of improving the flowability and solubility of baicalein phospholipid complexes. The application of Soluplus to phospholipid complexes has great potential.
Highlights
Baicalein (Figure 1A) is a bioactive ingredient of Radix Scutellariae
A novel ternary complex system (TCS) composed of baicalein, phospholipids, and Soluplus was successfully
A novel TCS composed of baicalein, phospholipids, and Soluplus was successfully developed
Summary
Baicalein (Figure 1A) is a bioactive ingredient of Radix Scutellariae. Baicalein has been reported with various pharmacological effects, such as anti-cancer [1], anti-tumor [2], anti-inflammatory [3], anti-pathogen [4], and antioxidant functions [5]. Ma’s research showed that baicalein plays a vital role in suppressing metastasis of breast cancer cells through downregulation of both SATB1 and. Baicalein could regulate bone formation via the mTORCI pathway [7]. Wu reported that baicalein is a Biopharmaceuticals Classification System (BCS) class IV compound because of its low solubility (solubility of 0.052 mg/mL in water) and poor lipophilicity (Papp = 0.037 × 10−6 cm/s) [8]. The poor solubility and permeability of baicalein limit its oral absorption and bioavailability.
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
