Toward successful cyclodextrin based solubility-enabling formulations for oral delivery of lipophilic drugs: solubility–permeability trade-off, biorelevant dissolution, and …

N Fine-Shamir, A Beig, M Zur, D Lindley… - Molecular …, 2017 - ACS Publications
The purpose of this work was to investigate key factors dictating the success/failure of
cyclodextrin-based solubility-enabling formulations for oral delivery of low-solubility drugs …

Understanding the relationship between solubility and permeability of γ-cyclodextrin-based systems embedded with poorly aqueous soluble benznidazole

J Ndayishimiye, T Kumeria, A Popat… - International Journal of …, 2022 - Elsevier
When administered orally, the bioavailability of drugs is strongly influenced by their aqueous
solubility and permeability. Although solubility-enabling excipients can improve the aqueous …

Oral delivery of lipophilic drugs: the tradeoff between solubility increase and permeability decrease when using cyclodextrin-based formulations

A Beig, R Agbaria, A Dahan - PLoS One, 2013 - journals.plos.org
The purpose of this study was to investigate the impact of oral cyclodextrin-based
formulation on both the apparent solubility and intestinal permeability of lipophilic drugs. The …

[HTML][HTML] Dissolution/permeation of albendazole in the presence of cyclodextrin and bile salts: a mechanistic in vitro study into factors governing oral bioavailability

JB Eriksen, SB Christensen, A Bauer-Brandl… - Journal of …, 2022 - Elsevier
We aimed to understand the impact of the interplay between bile salts and cyclodextrins on
the dissolution-permeation of poorly soluble drug compounds with a moderate-strong …

Predicting the solubility–permeability interplay when using cyclodextrins in solubility-enabling formulations: model validation

JM Miller, A Dahan - International journal of pharmaceutics, 2012 - Elsevier
Although the extraordinary solubility advantage afforded by cyclodextrins has led to their
widespread use as pharmaceutical solubilizers, several reports have emerged that …

A win–win solution in oral delivery of lipophilic drugs: supersaturation via amorphous solid dispersions increases apparent solubility without sacrifice of intestinal …

JM Miller, A Beig, RA Carr, JK Spence… - Molecular …, 2012 - ACS Publications
Recently, we have revealed a trade-off between solubility increase and permeability
decrease when solubility-enabling oral formulations are employed. We have shown this …

Solubility-enabling formulations for oral delivery of lipophilic drugs: considering the solubility-permeability interplay for accelerated formulation development

N Fine-Shamir, A Dahan - Expert Opinion on Drug Delivery, 2024 - Taylor & Francis
Introduction Tackling low water solubility of drug candidates is a major challenge in today's
pharmaceutics/biopharmaceutics, especially by means of modern solubility-enabling …

Segmental-dependent solubility and permeability as key factors guiding controlled release drug product development

M Markovic, M Zur, N Fine-Shamir, E Haimov… - Pharmaceutics, 2020 - mdpi.com
The main factors influencing the absorption of orally administered drugs are solubility and
permeability, which are location-dependent and may vary along the gastrointestinal tract …

Ethanol-based solubility-enabling oral drug formulation development: Accounting for the solubility-permeability interplay

N Fine-Shamir, A Dahan - International Journal of Pharmaceutics, 2024 - Elsevier
The aim of the current work was to investigate the key factors that govern the success/failure
of an ethanol-based solubility-enabling oral drug formulation, including the effects of the …

Modeling the influence of cyclodextrins on oral absorption of low‐solubility drugs: I. Model development

ED Gamsiz, L Miller, AG Thombre… - Biotechnology and …, 2010 - Wiley Online Library
The ability to quantitatively predict the influence of a solubilization technology on oral
absorption would be highly beneficial in rational selection of drug delivery technology and …