TY - JOUR
TI - Lipophilicity and hydrophobicity considerations in bio-enabling oral formulations approaches – a PEARRL review
AU - Ditzinger, F.
AU - Price, D.J.
AU - Ilie, A.-R.
AU - Köhl, N.J.
AU - Jankovic, S.
AU - Tsakiridou, G.
AU - Aleandri, S.
AU - Kalantzi, L.
AU - Holm, R.
AU - Nair, A.
AU - Saal, C.
AU - Griffin, B.
AU - Kuentz, M.
JO - The Journal of pharmacy and pharmacology
PY - 2019
VL - 71
TODO - 4
SP - 464-482
PB - Wiley-Blackwell Publishing Ltd
SN - null
TODO - 10.1111/jphp.12984
TODO - cyclodextrin;  drug;  lipid;  mesoporous silica;  octanol;  silicon dioxide;  unclassified drug;  water;  drug, amorphous solid dispersion;  crystal lattice energy;  drug design;  drug dosage form;  drug formulation;  drug manufacture;  drug release;  drug solubility;  energy;  gastrointestinal tract;  hydrophobicity;  lipophilicity;  molecular interaction;  nanosuspension;  oral drug administration;  physical chemistry;  Review;  theoretical study;  chemical phenomena;  chemistry;  drug delivery system;  drug design;  drug development;  human;  medicinal chemistry;  oral drug administration;  procedures;  solubility, Administration, Oral;  Chemistry, Pharmaceutical;  Drug Delivery Systems;  Drug Design;  Drug Development;  Drug Liberation;  Humans;  Hydrophobic and Hydrophilic Interactions;  Pharmaceutical Preparations;  Solubility
TODO - 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. © 2018 Royal Pharmaceutical Society
ER -