Amphiphilic amino acid copolymers as stabilizers for the preparation of nanocrystal dispersion

The recent advance of particle size engineering in nanometer ranges has widened the formulation opportunities of relatively water-insoluble drugs. However, the ‘nanoformulation’ suffers from a lack of systematic understanding about the requirements of polymeric stabilizers. Furthermore, the polymers...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmaceutical sciences 2005-04, Vol.24 (5), p.441-449
Main Authors: Lee, Jonghwi, Lee, Soo-Jeong, Choi, Ji-Yeun, Yoo, Ji Youn, Ahn, Cheol-Hee
Format: Article
Language:English
Subjects:
Amino Acids - administration & dosage
Amino Acids - chemistry
Biological and medical sciences
Dispersion
Drug Stability
General pharmacology
Hydrophobic and Hydrophilic Interactions
Insoluble drug
Medical sciences
Nanocrystals
Nanoparticles
Nanostructures
Particle engineering
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polymers - administration & dosage
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The recent advance of particle size engineering in nanometer ranges has widened the formulation opportunities of relatively water-insoluble drugs. However, the ‘nanoformulation’ suffers from a lack of systematic understanding about the requirements of polymeric stabilizers. Furthermore, the polymers that can be used for the preparation of nanocrystals are so limited that finding a proper stabilizer for a given formulation is often difficult. In this study, amino acid copolymers whose properties can systematically be tailored are developed, and their morphological and compositional effects are investigated. Copolymers containing lysine (K) as their hydrophilic segments, and phenylalanine (F) or leucine (L) as their hydrophobic segments successfully produce stable nanocrystals (200–300 nm) in water, while copolymers of K and alanine (A) could not generate nanosized particles. Not the morphology but the hydrophobicity of copolymers seems to be a critical parameter in the preparation of drug nanocrystals by wet comminution. The effective stabilization performance of copolymers requires the hydrophobic moiety content to be higher than 15 mol%. Comminution for only 5 min is long enough for nanocrystal preparation, and the crystallinity of drug is found intact after the processing.
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2004.12.010