Microcrystalline cellulose-carboxymethyl cellulose sodium as an effective dispersant for drug nanocrystals: A case study

Carbohydr Polym. 2016 Jan 20:136:499-506. doi: 10.1016/j.carbpol.2015.09.048. Epub 2015 Sep 16.

Abstract

This study is aimed at seeking an alternative dispersant for spray drying of drug nanosuspensions. The ideal dispersant is not only able to prevent the agglomeration of drug nanocrystals in the suspension state, but also it is able to preserve redispersibility of drug nanocrystals after drying. An active pharmaceutical ingredient (API) was used as a model drug. API nanosuspensions were prepared by homogenization and converted into nanocrystals powder (API-NP) with microcrystalline cellulose-carboxymethyl cellulose sodium (MCCS) via spray drying. It was found that MCCS was able to prevent the aggregation of API-NP in the suspension state and the agglomeration during spray-drying process, possibility due to its high Zeta potential and steric barrier from network structure, and reduction of API size at nanoscale and incorporation into MCCS network structure did not affect the solid state of API as evidenced by DSC and XRD analysis. The spray-dried API-NP/MCCS powders exhibited excellent sphere-shape performance, and could easily redispersed to API-NC suspensions state. Dissolution of the spray-dried API-NP was distinctly superior to those of the crude powder and physical mixture, respectively. Within 30 min, approximate 85.87% of API was dissolved from the API-NP/MCCS. MCCS was demonstrated to be an effective dispersant for spray-dried drug nanocrystals and preservation of the nanocrystals associated with excellent redispersibility.

Keywords: Microcrystalline cellulose-carboxymethyl cellulose sodium; Nanocrystals; Redispersibility; Spray-drying.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aerosols / chemistry
  • Carboxymethylcellulose Sodium / chemistry*
  • Cellulose / chemistry*
  • Desiccation
  • Drug Carriers / chemistry
  • Nanoparticles / chemistry*

Substances

  • Aerosols
  • Drug Carriers
  • Cellulose
  • Carboxymethylcellulose Sodium
  • microcrystalline cellulose