Preparation of stable colloidal suspensions of superdisintegrants via wet stirred media milling--颗粒学报PARTICUOLOGY

Azad, M. A., Afolabi, A., Patel, N., Davé, R., & Bilgili, E. (2014). Preparation of stable colloidal suspensions of superdisintegrants via wet stirred media milling. Particuology, 14, 76–82. https://doi.org/10.1016/j.partic.2013.07.008

Preparation of stable colloidal suspensions of superdisintegrants via wet stirred media milling

Mohammad A. Azad, Afolawemi Afolabi, Nikita Patel, Rajesh Davé, Ecevit Bilgili^*

Otto H. York Department of Chemical, Biological, and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark, NJ, USA

10.1016/j.partic.2013.07.008

Volume 14, June 2014, Pages 76-82

Received 31 March 2013, Revised 18 June 2013, Accepted 20 July 2013, Available online 27 September 2013.

E-mail: bilgece@njit.edu

Highlights

• Colloidal suspensions of superdisintegrants were prepared via wet media mill.

• The superdisintegrants used were crospovidone (CP) and sodium starch glycolate (SSG).

• Stabilizers used were hydroxypropyl cellulose (HPC) and sodium dodecyl sulfate (SDS).

• Extensive breakage of the superdisintegrant particles occurred during milling.

• SSG suspensions were stable w/o HPC–SDS, whereas CP suspensions required HPC–SDS.

Abstract

Superdisintegrants are cross-linked polymers that can be used as dispersants for fast release of drug nanoparticles from nanocomposite microparticles during in vitro and in vivo dissolution. Currently available superdisintegrant particles have average sizes of approximately 5–130 μm, which are too big for drug nanocomposite applications. Hence, production of stable superdisintegrant suspensions with less than 5 μm particles is desirable. Here, we explore the preparation of colloidal suspensions of anionic and nonionic superdisintegrants using a wet stirred media mill and assess their physical stability. Sodium starch glycolate (SSG) and crospovidone (CP) were selected as representative anionic and nonionic superdisintegrants, and hydroxypropyl cellulose (HPC) and sodium dodecyl sulfate (SDS) were used as a steric stabilizer and a wetting agent/stabilizer, respectively. Particle sizing, scanning electron microscopy, and zeta potential measurements were used to characterize the suspensions. Colloidal superdisintegrant suspensions were prepared reproducibly. The extensive particle breakage was attributed to the swelling-induced softening in water. SSG suspensions were stable even in the absence of stabilizers, whereas CP suspensions required HPC–SDS for minimizing particle aggregation. These findings were explained by the higher absolute (negative) zeta potential of the suspensions of the anionic superdisintegrant (SSG) as compared with those of the nonionic superdisintegrant (CP).

Graphical abstract

Keywords

Colloidal suspensions; Dispersants; Physical stability; Superdisintegrants; Swelling; Wet stirred media milling

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