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Molecules 2017, 22(5), 776; doi:10.3390/molecules22050776

Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex

1
School of Pharmacy, Nanjing Medical University, Nanjing 211166, China
2
Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese, Nanjing 210028, China
3
Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, China
4
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 211198, China
*
Authors to whom correspondence should be addressed.
Academic Editors: Guy Van den Mooter, Holger Grohganz and Korbinian Löbmann
Received: 29 March 2017 / Revised: 3 May 2017 / Accepted: 8 May 2017 / Published: 11 May 2017
(This article belongs to the Collection Poorly Soluble Drugs)
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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. View Full-Text
Keywords: baicalein; phospholipid complex; soluplus baicalein; phospholipid complex; soluplus
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Fan, J.; Dai, Y.; Shen, H.; Ju, J.; Zhao, Z. Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex. Molecules 2017, 22, 776.

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