title: Drug delivery strategies for poorly water-soluble drugs: the industrial perspective.
abstract: BACKGROUND
  For poorly soluble compounds, a good bioavailability is typically needed to assess the therapeutic index and the suitability of the compound for technical development. In industry, the selection of the delivery technology is not only driven by technical targets, but also by constraints, such as production costs, time required for development and the intellectual property situation.
  
  
  METHODS
  This review covers current developments in parenteral and oral delivery technologies and products for poorly water-soluble compounds, such as nano-suspensions, solid dispersions and liposomes. In addition, the use of biorelevant dissolution media to assess dissolution and solubility properties is described. Suggestions are also included to systematically address development hurdles typical of poorly water-soluble compounds intended for parenteral or oral administration.
  
  
  CONCLUSIONS
  A holistic assessment is recommended to select the appropriate delivery technology by taking into account technical as well as intellectual property considerations. Therefore, first and foremost, a comprehensive physico-chemical characterization of poorly water-soluble compounds can provide the key for a successful selection and development outcome. In this context, the identified physical form of the compound in the formulation is used as a guide for a risk-benefit assessment of the selected oral delivery technology. The potential of nano-suspensions for intravenous administration is unclear. In the case of oral administration, nano-suspensions are mainly used to improve the oral absorption characteristics of micronized formulations. The development of an in situ instantaneous solubilization method, based on stable, standardized liposomes with low toxicity, opens new avenues to solubilize poorly water-soluble compounds.
authors: Phares AG, Muttenz, Switzerland.
authors: Peter
authors: P
authors: van Hoogevest
authors: Xiangli
authors: X
authors: Liu
authors: Alfred
authors: A
authors: Fahr
mesh_terms: D000818:Animals; D001702:Biopharmaceutics / Q000639:trends; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004655:Emulsions; D006801:Humans; D018973:Intellectual Property; D008081:Liposomes; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D012492:Salts / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D013535:Suspensions
chemical_list: D004655:Emulsions; D008081:Liposomes; D004364:Pharmaceutical Preparations; D012492:Salts; D013535:Suspensions