Felix Ditzinger1,2, Daniel J Price3,4, Alexandra-Roxana Ilie5,6, Niklas J Köhl5, Sandra Jankovic1,2, Georgia Tsakiridou7,8, Simone Aleandri2, Lida Kalantzi7, René Holm6, Anita Nair3, Christoph Saal3, Brendan Griffin5, Martin Kuentz2. 1. Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland. 2. Institute of Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, Muttenz, Switzerland. 3. Analytics Healthcare, Merck KGaA, Darmstadt, Germany. 4. Goethe University, Frankfurt, Germany. 5. School of Pharmacy, University College Cork, Cork, Ireland. 6. Drug Product Development, Janssen Research and Development, Johnson and Johnson, Beerse, Belgium. 7. Product Design & Evaluation, Pharmathen SA, Athens, Greece. 8. Faculty of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece.
Abstract
OBJECTIVES: This review highlights aspects of drug hydrophobicity and lipophilicity as determinants of different oral formulation approaches with specific focus on enabling formulation technologies. An overview is provided on appropriate formulation selection by focussing on the physicochemical properties of the drug. KEY FINDINGS: Crystal lattice energy and the octanol-water partitioning behaviour of a poorly soluble drug are conventionally viewed as characteristics of hydrophobicity and lipophilicity, which matter particularly for any dissolution process during manufacturing and regarding drug release in the gastrointestinal tract. Different oral formulation strategies are discussed in the present review, including lipid-based delivery, amorphous solid dispersions, mesoporous silica, nanosuspensions and cyclodextrin formulations. SUMMARY: Current literature suggests that selection of formulation approaches in pharmaceutics is still highly dependent on the availability of technological expertise in a company or research group. Encouraging is that, recent advancements point to more structured and scientifically based development approaches. More research is still needed to better link physicochemical drug properties to pharmaceutical formulation design.
OBJECTIVES: This review highlights aspects of drug hydrophobicity and lipophilicity as determinants of different oral formulation approaches with specific focus on enabling formulation technologies. An overview is provided on appropriate formulation selection by focussing on the physicochemical properties of the drug. KEY FINDINGS: Crystal lattice energy and the octanol-water partitioning behaviour of a poorly soluble drug are conventionally viewed as characteristics of hydrophobicity and lipophilicity, which matter particularly for any dissolution process during manufacturing and regarding drug release in the gastrointestinal tract. Different oral formulation strategies are discussed in the present review, including lipid-based delivery, amorphous solid dispersions, mesoporous silica, nanosuspensions and cyclodextrin formulations. SUMMARY: Current literature suggests that selection of formulation approaches in pharmaceutics is still highly dependent on the availability of technological expertise in a company or research group. Encouraging is that, recent advancements point to more structured and scientifically based development approaches. More research is still needed to better link physicochemical drug properties to pharmaceutical formulation design.
Authors: Felix Ditzinger; Daniel J Price; Anita Nair; Johanna Becker-Baldus; Clemens Glaubitz; Jennifer B Dressman; Christoph Saal; Martin Kuentz Journal: Pharmaceutics Date: 2019-11-04 Impact factor: 6.321
Authors: Fiona Macintyre; Hanu Ramachandruni; Jeremy N Burrows; René Holm; Anna Thomas; Jörg J Möhrle; Stephan Duparc; Rob Hooft van Huijsduijnen; Brian Greenwood; Winston E Gutteridge; Timothy N C Wells; Wiweka Kaszubska Journal: Malar J Date: 2018-11-01 Impact factor: 2.979