Lipophilicity and hydrophobicity considerations in bio‐enabling oral formulations approaches – a PEARRL review
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Authors
Price, Daniel
Ilie, Alexandra Roxana
Koehl, Niklas
Tsakiridou, Georgia
Aleandri, Simone
Kalantzi, Lida
Holm, Rene
Nair, Anita
Author (Corporation)
Publication date
08/2018
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Type
01A - Journal article
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Parent work
Journal of Pharmacy and Pharmacology
Special issue
DOI of the original publication
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Series
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Volume
71
Issue / Number
Pages / Duration
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Publisher / Publishing institution
Wiley
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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.
Keywords
crystal lattice energy, hydrophobicity, lipophilicity, modern formulation approaches, poorly water-soluble drug
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ISBN
ISSN
0022-3573
2042-7158
2042-7158
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
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Citation
Ditzinger, F., Price, D., Ilie, A. R., Koehl, N., Jankovic, S., Tsakiridou, G., Aleandri, S., Kalantzi, L., Holm, R., Nair, A., Saal, C., Griffin, B., & Kuentz, M. (2018). Lipophilicity and hydrophobicity considerations in bio‐enabling oral formulations approaches – a PEARRL review. Journal of Pharmacy and Pharmacology, 71. https://doi.org/10.1111/jphp.12984