Open AccessLipophilicity and hydrophobicity considerations in bio‐enabling oral formulations approaches – a PEARRL review
Author(s) -
Ditzinger Felix,
Price Daniel J.,
Ilie AlexandraRoxana,
Köhl Niklas J.,
Jankovic Sandra,
Tsakiridou Georgia,
Aleandri Simone,
Kalantzi Lida,
Holm René,
Nair Anita,
Saal Christoph,
Griffin Brendan,
Kuentz Martin
Publication year - 2019
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.12984
Subject(s) - lipophilicity , pharmaceutics , biochemical engineering , drug , mesoporous silica , pharmaceutical formulation , nanotechnology , drug delivery , pharmaceutical sciences , chemistry , materials science , computer science , pharmacology , organic chemistry , mesoporous material , medicine , chromatography , engineering , catalysis
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.