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Molecules 2019, 24(4), 728; https://doi.org/10.3390/molecules24040728

A Novel Dantrolene Sodium-Loaded Mixed Micelle Containing a Small Amount of Cremophor EL: Characterization, Stability, Safety and Pharmacokinetics

1
State Key Laboratory of Bioactive Substance and Function of Natural Medicines & Beijing Key laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
2
Chinese Pharmaceutical Association, Beijing 100022, China
*
Author to whom correspondence should be addressed.
Co-first author.
Received: 7 January 2019 / Revised: 11 February 2019 / Accepted: 13 February 2019 / Published: 18 February 2019
(This article belongs to the Section Nanochemistry)
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Abstract

Dantrolene sodium (DS) is the only drug specifically used for the treatment of malignant hyperthermia. Nevertheless, its clinical application is significantly restricted due to its aqueous insolubility and the limited formulations available in clinical practice. In order to solve these problems, a novel mixed micelle composed of phospholipid and Cremophor EL was designed and evaluated. The mixed micelle was prepared using a stirring- ultrasonic method. The Dynamic Light Scattering (DLS) results showed that the micelle was small in size (12.14 nm) and narrowly distributed (PdI = 0.073). Transmission Electron Microscopy (TEM) images showed that the micelle was homogeneous and spherical. The stability study indicated that the system was stable for storage and dilution with distilled water, while the safety testing showed that the micelle was safe for intravenous administration with low hemolysis rates and low allergic reaction rates. In the pharmaceutics study, the Cmax and AUC0-t of the DS-loaded micelle were 4- and 4.5- folds higher than that of the DS. Therefore, the constructed phospholipid-Cremophor EL mixed micelle is a promising drug delivery system for DS. View Full-Text
Keywords: mixed micelle; dantrolene sodium; Cremophor EL; drug safety; pharmacokinetics mixed micelle; dantrolene sodium; Cremophor EL; drug safety; pharmacokinetics
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Jin, W.; Tan, X.; Wen, J.; Meng, Y.; Zhang, Y.; Li, H.; Jiang, D.; Song, H.; Zheng, W. A Novel Dantrolene Sodium-Loaded Mixed Micelle Containing a Small Amount of Cremophor EL: Characterization, Stability, Safety and Pharmacokinetics. Molecules 2019, 24, 728.

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