Pharmaceutical Research

, Volume 23, Issue 2, pp 429–437

Dense Gas Processing of Micron-Sized Drug Formulations Incorporating Hydroxypropylated and Methylated Beta-Cyclodextrin

  • Raffaella Mammucari
  • Fariba Dehghani
  • Neil R. Foster
Research Paper
  • 115 Downloads

Purpose

Because of their importance in pharmaceutical applications, hydroxypropyl-β-cyclodextrin and methyl-β-cyclodextrin have been selected to study the formation of micronized complexes incorporating active pharmaceutical ingredients (APIs) and cyclodextrins (CDs) by dense gas (DG) processing.

Methods

A single-step DG technique was used as an alternative to conventional methods for the manufacturing of API/CD complexes. The DG technology is highly attractive in the pharmaceutical industry because of its potential to generate micronized particles with controlled particle size distributions at moderate operating conditions. The effect of the aerosol solvent extraction system (ASES) processing on the dissolution performance of naproxen (NPX) was examined.

Results

The CDs were produced as microspheres smaller than 3 μm. The coprecipitation of each CD with NPX resulted in the production of microparticles with enhanced dissolution rates.

Conclusions

The ASES was operated under mild conditions and generated micron-sized spherical particles that could be of particular interest in formulations for pulmonary delivery.

Particular advantages of the technique are that (1) nontoxic solvents are used, and (2) it is suitable for the processing of thermally labile compounds. The proposed process can create opportunities to improve current administration routes and exploit novel delivery systems for drug formulations incorporating CDs.

Key Words

carbon dioxide cyclodextrin dense gases pulmonary drug delivery supercritical fluids 

Abbreviations

API

active pharmaceutical ingredient

ASES

aerosol solvent extraction system

CD

cyclodextrin

DELOS

depressurization of an expanded liquid organic solution

HP-β-CD

hydroxypropyl-β-cyclodextrin

M-β-CD

methyl-β-cyclodextrin

NPX

naproxen

PGSS

particles from gas-saturated solutions

SAA

supercritical assisted atomization

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Copyright information

© Springer Science + Business Media, Inc. 2006

Authors and Affiliations

  • Raffaella Mammucari
    • 1
  • Fariba Dehghani
    • 1
  • Neil R. Foster
    • 1
  1. 1.School of Chemical Engineering and Industrial ChemistryThe University of New South WalesSydneyAustralia

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