Understanding Critical Quality Attributes for Nanocrystals from Preparation to Delivery

Poor solubility of active pharmaceutical ingredients (APIs) is a great challenge for the pharmaceutical industry and, hence, drug nanocrystals are widely studied as one solution to overcome these solubility problems. Drug nanocrystals have comparatively simple structures which make them attractive f...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2015-12, Vol.20 (12), p.22286-22300
Main Authors: Peltonen, Leena, Strachan, Clare
Format: Article
Language:English
Subjects:
bioavailability
Chemistry, Pharmaceutical - methods
Crystals
Dissolution
drug nanocrystals
Excipients - chemistry
Formulations
Nanocrystals
Nanoparticles - chemistry
permeation
Pharmaceutical industry
Pharmaceutical Preparations - chemistry
Pharmaceuticals
Precipitates
precipitation
Quality management
Review
Solubility
stability
Supersaturation
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Summary:Poor solubility of active pharmaceutical ingredients (APIs) is a great challenge for the pharmaceutical industry and, hence, drug nanocrystals are widely studied as one solution to overcome these solubility problems. Drug nanocrystals have comparatively simple structures which make them attractive for the formulation for poorly soluble drugs, and their capability to improve the dissolution in vitro is easily demonstrated, but turning the in vitro superior properties of nanocrystals to success in vivo, is often demanding: controlled (including enhanced) drug dissolution followed by successful permeation is not guaranteed, if for example, the dissolved drug precipitates before it is absorbed. In this review critical quality attributes related to nanocrystal formulations from production to final product performance in vivo are considered. Many important parameters exist, but here physical stability (aggregation tendency and solid state form), solubility properties influencing dissolution and supersaturation, excipient use to promote the maintenance of supersaturation, and finally the fate of nanocrystals in vivo are the main subjects of our focus.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules201219851