scholarly journals In vivo dissolution of poorly water-soluble drugs: Proof of concept based on fluorescence bioimaging

2020 ◽  
Author(s):  
Yinqian Yang ◽  
Yongjiu Lv ◽  
Chengying Shen ◽  
Tingting Shi ◽  
Haisheng He ◽  
...  
Keyword(s):  
Water Soluble ◽  
Proof Of Concept ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Fluorescence Bioimaging ◽  
Poorly Water Soluble ◽  
In Vivo Dissolution

Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: Studies with halofantrine

2004 ◽  
Vol 93 (5) ◽  
pp. 1110-1121 ◽  
Author(s):  
Christopher J.H. Porter ◽  
Ann Marie Kaukonen ◽  
Agnes Taillardat-Bertschinger ◽  
Ben J. Boyd ◽  
Jacquelyn M. O'Connor ◽  
...  
Keyword(s):  
Water Soluble ◽  
Lipid Digestion ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Lipid Formulations

scholarly journals Development of a New Ex Vivo Lipolysis-Absorption Model for Nanoemulsions

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 164 ◽  
Author(s):  
Lu Xiao ◽  
Ying Liu ◽  
Tao Yi
Keyword(s):  
Ex Vivo ◽  
Water Soluble ◽  
Absorption Model ◽  
Poorly Water Soluble Drugs ◽  
Everted Gut Sac ◽  
In Vivo Absorption ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

The use of lipid-based formulations (LBFs) in improving the absorption of poorly water-soluble drugs has now well established. Because the in vivo evaluation of LBFs is labor-intensive, in vitro or ex vivo approaches could provide advantages. In this study, a new ex vivo lipolysis-absorption model (evLAM) composed of an intestinal digestion system and an intestinal tissue system was developed to evaluate and predict the in vivo absorption performances of LBFs. Model factors, including the pH of the system and concentrations of d-glucose and pancreatic lipase, were investigated and optimized by a Box-Behnken design. To evaluate this new model, a lipid formulation of indomethacin, which was chosen based on preliminary studies of pseudo-ternary phase diagrams, emulsion droplets, and solubility, was further investigated by an in vivo pharmacokinetic study of rats, the everted gut sac model, and the evLAM, respectively. The absorption percentages obtained from the evLAM were much more similar to the data of rats in vivo than those from the everted gut sac model, showing a preferable in vitro-in vivo correlation (r = 0.9772). Compared with the conventional in vitro and in vivo methods, the evLAM, which allowed precise insights into the in vivo absorption characteristics without much time or a complicated process, could be a better tool for assessing LBFs of poorly water-soluble drugs.

Beta-casein nanocarriers of celecoxib for improved oral bioavailability

2014 ◽  
Vol 6 (4) ◽  
Author(s):  
Hadas Perlstein ◽  
Yaelle Bavli ◽  
Tanya Turovsky ◽  
Abraham Rubinstein ◽  
Dganit Danino ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Water Soluble ◽  
Proof Of Concept ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Beta Casein ◽  
Poorly Water Soluble

AbstractBeta-casein (bCN) micelles were developed as a platform for improved oral bioavailability (BA) of poorly water-soluble drugs. Here we demonstrate a proof-of-concept using the NSAID celecoxib (Cx) loaded into bCN micelles (Cx/bCN). In a crossover pharmacokinetic (PK) study in pigs (n=4), dosed intraduodenally with either the commercial Cx formulation Celebra

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