What is the True Solubility Advantage for Amorphous Pharmaceuticals?

By Bruno C. Hancock, Michael Parks. Pharmaceutical Research, 2000

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Nanocrystal technology, drug delivery and clinical applications (2008, methodology): “The polymorphic modifi cation I has a solubility of 0.13, the high energy modifi cation II a solubility of 0.43 and the amorphous material of 1.6 mg/ml (Hancock and Parks 2000; Chong-Hui and Grant 2001).”
Strategies to Address Low Drug Solubility in Discovery and Development (2013, background): “…the “equilibrium” solubility of a thermodynamically unstable amorphous material, such that spontaneous crystallization results in underestimation of the initial (kinetic) solubility properties of the amorphous form (Hancock and Parks, 2000; Bhugra and Pikal, 2008; Murdande et al., 2010a,b, 2011a).”
Maltodextrin/pectin microparticles by spray drying as carrier for nutraceutical extracts (2011, background): “This behaviour may be explained by an increase of the microparticle–water interaction due to both amorphous physical state of the powders, leading to an improving of solubility (Hancock and Parks, 2000), and the smallest dimensions (3.”