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Title: Preparation and characterization of spironolactone nanoparticles by antisolvent precipitation
Authors: Dong, Y.
Ng, W.K.
Shen, S.
Kim, S.
Tan, R.B.H. 
Keywords: Antisolvent precipitation
Dissolution rate
Oral bioavailability
Issue Date: 22-Jun-2009
Citation: Dong, Y., Ng, W.K., Shen, S., Kim, S., Tan, R.B.H. (2009-06-22). Preparation and characterization of spironolactone nanoparticles by antisolvent precipitation. International Journal of Pharmaceutics 375 (1-2) : 84-88. ScholarBank@NUS Repository.
Abstract: Due to low aqueous solubility and slow dissolution rate, spironolactone, a synthetic steroid diuretic, has a low and variable oral bioavailability. Nanoparticles were thus prepared by antisolvent precipitation in this work for accelerating dissolution of this kind of poorly water-soluble drugs. Effects of surfactant type/concentration and feed drug concentration on the precipitated particle size were evaluated. It was found that introduction of spironolactone solution in N-methyl-2-pyrrolidone (NMP) to the antisolvent water can produce the particles in the submicron range with hydroxypropyl methylcellulose (HPMC) as the stabilizer. The particle size decreased with the increase of HPMC concentration from 0 to 0.125% (w/v), further increase of which did not affect the size significantly. Increasing feed drug concentration from 10 to 100 mg/ml resulted in the particle size decrease. In comparison with raw drug, the chemical structure of nanosized spironolactone was not changed but the crystallinity was reduced. Dissolution of spironolactone nanoparticles in 0.1 M HCl was 2.59 times faster than raw drugs in 60 min. © 2009 Elsevier B.V. All rights reserved.
Source Title: International Journal of Pharmaceutics
ISSN: 03785173
DOI: 10.1016/j.ijpharm.2009.03.013
Appears in Collections:Staff Publications

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