Abstract
The solubility-permeability interplay deals with the question: what is the concomitant effect on the drug's apparent permeability when increasing the apparent solubility with a solubility-enabling formulation? The solubility and the permeability are closely related, exhibit certain interplay between them, and ongoing research throughout the past decade shows that treating the one irrespectively of the other may be insufficient. The aim of this article is to provide an overview of the current knowledge on the solubility-permeability interplay when using solubility-enabling formulations for oral lipophilic drugs, highlighting active permeability aspects. A solubility-enabling formulation may affect the permeability in opposite directions; the passive permeability may decrease as a result of the apparent solubility increase, according to the solubility-permeability tradeoff, but at the same time, certain components of the formulation may inhibit/saturate efflux transporters (when relevant), resulting in significant apparent permeability increase. In these cases, excipients with both solubilizing and e.g. P-gp inhibitory properties may lead to concomitant increase of both the solubility and the permeability. Intelligent development...Continue Reading
Citations
Mar 31, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xu ZhangMancang Gu
May 6, 2019·Pharmaceutics·Kohsaku Kawakami
Jul 28, 2019·Journal of Microencapsulation·Ran LiXi-Ming Xu
Mar 25, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sidney J StohsHarry G Preuss
Nov 12, 2020·Soft Matter·Nathan P AlexanderStephanie R Dungan
Aug 28, 2020·Expert Opinion on Drug Delivery·Alejandro Ruiz-PicazoMarta González-Álvarez
Dec 30, 2020·Nutrition in Clinical Practice : Official Publication of the American Society for Parenteral and Enteral Nutrition·Joseph I Boullata
Nov 5, 2019·Biochimica Et Biophysica Acta. Reviews on Cancer·Urvi H GalaRobert O Williams
Jan 31, 2021·Pharmaceutics·Marika RuponenRiikka Laitinen
Feb 3, 2021·AAPS PharmSciTech·Bhakti Mahendra PawarTamilvanan Shunmugaperumal
Jan 27, 2021·International Journal of Pharmaceutics·Noa Fine-ShamirArik Dahan
Apr 4, 2021·Pharmaceutics·Kazuya SugitaEtsuo Yonemochi
Jun 12, 2021·Cancer Chemotherapy and Pharmacology·Morgan J HomanBernard L Marini
May 24, 2019·Molecular Pharmaceutics·Noa Fine-Shamir, Arik Dahan
Aug 27, 2021·AAPS PharmSciTech·Mercy OkezueKari Clase
Aug 18, 2020·Journal of Chemical Information and Modeling·Xiting WangTao Lu
Oct 2, 2021·AAPS PharmSciTech·Gayathri Ramachandran, M S Sudheesh