Redispersible fast dissolving nanocomposite microparticles of poorly water-soluble drugs

Anagha Bhakay, Mohammad Azad, Ecevit Bilgili, Rajesh Dave

Research output: Contribution to journalArticlepeer-review

51 Scopus citations

Abstract

Enhanced recovery/dissolution of two wet media-milled, poorly water-soluble drugs, Griseofulvin (GF) and Azodicarbonamide (AZD), incorporated into nanocomposite microparticles (NCMPs) via fluidized bed drying (FBD) and spray-drying (SD) was investigated. The effects of drying method, drug loading, drug aqueous solubility/wettability as well as synergistic stabilization of the milled suspensions on nanoparticle recovery/dissolution were examined. Drug nanoparticle recovery from FBD and SD produced NCMPs having high drug loadings was evaluated upon gentle redispersion via optical microscopy and laser diffraction. During wet-milling, hydroxypropyl cellulose (HPC) alone stabilized more wettable drug (AZD) nanoparticles with slight aggregation, but could not prevent aggregation of the GF nanoparticles. In contrast, well-dispersed, stable nanosuspensions of both drugs were produced when sodium dodecyl sulfate (SDS) and HPC were combined. The FBD and SD NCMPs without SDS exhibited incomplete nanoparticle recovery, causing slower dissolution for GF, but not for AZD, likely due to higher aqueous solubility/wettability of AZD. For high active loaded NCMPs (FBD ∼50 wt%, SD ∼80 wt%) of either drug, HPC-SDS together owing to their synergistic stabilization led to fast redispersibility/ dissolution, corroborated via optical microscopy and particle sizing. These positive attributes can help development of smaller, high drug-loaded dosage forms having enhanced bioavailability and better patient compliance.

Original languageEnglish (US)
Pages (from-to)367-379
Number of pages13
JournalInternational Journal of Pharmaceutics
Volume461
Issue number1-2
DOIs
StatePublished - Jan 30 2014

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • Fast dissolution
  • Fluidized bed coating
  • Nanoparticles
  • Redispersion
  • Spray drying
  • Wet media milling

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