NDLI: Fabrication of Carvedilol Nanosuspensions Through the Anti-Solvent Precipitation–Ultrasonication Method for the Improvement of Dissolution Rate and Oral Bioavailability

Content Provider	Springer Nature Link
Author	Liu, Dandan Xu, Heming Tian, Baocheng Yuan, Kun Pan, Hao Ma, Shilin Yang, Xinggang Pan, Weisan
Copyright Year	2012
Abstract	The present study aims to prepare carvedilol (CAR) nanosuspensions using the anti-solvent precipitation–ultrasonication technique to improve its dissolution rate and oral bioavailability. Alpha-tocopherol succinate (VES) was first used as a co-stabilizer to enhance the stability of the nanosuspensions. The effects of the process parameters on particle size of the nanosuspensions were investigated. The optimal values of the precipitation temperature, power inputs, and the time length of ultrasonication were selected as 10°C, 400 W, and 15 min, respectively. Response surface methodology based on central composite design was utilized to evaluate the formulation factors that affect the size of nanosuspensions, i.e., the concentration of CAR and VES in the organic solution, and the level of sodium dodecyl sulfate in the anti-solvent phase, respectively. The optimized formulation showed a mean size of 212 ± 12 nm and a zeta potential of −42 ± 3 mV. Scanning electron microscopy revealed that the nanosuspensions were flaky-shaped. Powder X-ray diffraction and differential scanning calorimetry analysis confirmed that the nanoparticles were in the amorphous state. Fourier transform infrared analysis demonstrated that the reaction between CAR and VES is probably due to hydrogen bonding. The nanosuspension was physically stable at 25°C for 1 week, which allows it to be further processing such as drying. The dissolution rate of the nanosuspensions was markedly enhanced by reducing the size. The in vivo test demonstrated that the C $_{max}$ and AUC$_{0–36}$ values of nanosuspensions were approximately 3.3- and 2.9-fold greater than that of the commercial tablets, respectively.
Starting Page	295
Ending Page	304
Page Count	10
File Format	PDF
Journal	AAPS PharmSciTech
Volume Number	13
Issue Number	1
e-ISSN	15309932
Language	English
Publisher	Springer US
Publisher Date	2012-01-13
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Biochemistry Pharmacy Biotechnology Pharmacology/Toxicology
Content Type	Text
Resource Type	Article

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