Determination of the passive absorption through the rat intestine using chromatographic indices and molar volume

Genty, Muriel; González, Gustavo; Clere, Christian; Desangle-Gouty, Valérie; Legendre, Jean-Yves

doi:10.1016/s0928-0987(00)00175-5

Cited by 67 publications

(33 citation statements)

References 24 publications

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“…39 Among others, everted and noneverted intestinal sac models in rats have commonly been employed to study drug absorption. [40][41][42] Genty et al 43 have compared permeability values of some actively and passively transported molecules through both everted and non-everted sacs. They reported that the permeability was higher for actively transported molecules when the sacs were everted.…”

Section: Ex Vivo Intestinal Permeation Studiesmentioning

confidence: 99%

“…These results suggested that passive permeability of actively transported molecules can be determined through non-everted rat gut sacs. 43 The non-everted sac model utilized in this work exhibited reported advantages over the everted sac model, including simplicity, need for less test sample, and amenability for successive collection of serosal samples with less intestinal morphological changes. 44 The well-known limitations of the everted gut sac model are morphological damages to intestinal tissue while everting, 45 presence of muscularis mucosa, and small closed serosal compartment.…”

Section: Ex Vivo Intestinal Permeation Studiesmentioning

confidence: 99%

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Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Freag¹,

Elnaggar²,

Abdallah³

2013

IJN

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Diosmin (DSN) is an outstanding phlebotonic flavonoid with a tolerable potential for the treatment of colon and hepatocellular carcinoma. Being highly insoluble, DSN bioavailability suffers from high inter-subject variation due to variable degrees of permeation. This work endeavored to develop novel DSN loaded phytosomes in order to improve drug dissolution and intestinal permeability. Three preparation methods (solvent evaporation, salting out, and lyophilization) were compared. Nanocarrier optimization encompassed different soybean phospholipid (SPC) types, different solvents, and different DSN:SPC molar ratios (1:1, 1:2, and 1:4). In vitro appraisal encompassed differential scanning calorimetry, infrared spectroscopy, particle size, zeta potential, polydispersity index, transmission electron microscopy, drug content, and in vitro stability. Comparative dissolution studies were performed under sink versus non-sink conditions. Ex vivo intestinal permeation studies were performed on rats utilizing noneverted sac technique and high-performance liquid chromatography analysis. The results revealed lyophilization as the optimum preparation technique using SPC and solvent mixture (Dimethyl sulphoxide:t-butylalchol) in a 1:2 ratio. Complex formation was contended by differential scanning calorimetry and infrared data. Optimal lyophilized phytosomal nanocarriers (LPNs) exhibited the lowest particle size (316 nm), adequate zeta-potential (-27 mV), and good in vitro stability. Well formed, discrete vesicles were revealed by transmission electron microscopy, drug content, and in vitro stability. Comparative dissolution studies were performed. LPNs demonstrated significant enhancement in DSN dissolution compared to crude drug, physical mixture, and generic and brand DSN products. Permeation studies revealed 80% DSN permeated from LPNs via oxygenated rat intestine compared to non-detectable amounts from suspension. In this study, LPNs (99% drug loading) could be successfully tailored for DSN with improved dissolution and permeation characteristics, which is promising for lowering the influence of exogenous factors and increasing drug delivery.

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Section: Ex Vivo Intestinal Permeation Studiesmentioning

confidence: 99%

Section: Ex Vivo Intestinal Permeation Studiesmentioning

confidence: 99%

Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Freag¹,

Elnaggar²,

Abdallah³

2013

IJN

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“…Chem. 30,2011were derived from the Henderson-Hasselbalch equation and provide an indication of the degree of ionization; the compound is 50% ionized when (pK a -pH) or (pH-pK a ) ¼ 0. All acidic compounds show a similar positive relationship between log k IAM and (pK a -pH); however, the relationship is compound-dependent.…”

Section: Log K Iam Values For the Oecd Reference Compoundsmentioning

confidence: 99%

Database of published retention factors for immobilized artificial membrane HPLC and an assessment of the effect of experimental variability

Ledbetter

Gutsell

Hodges

et al. 2011

Enviro Toxic and Chemistry

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A database was collated of published experimental logarithmic values for the relative retention factors (log k(IAM)) measured using an immobilized artificial membrane column and high-performance liquid chromatography (IAM HPLC). Log k(IAM) is an alternative measure of hydrophobicity to the octanol/water partition coefficient (log K(OW)). While there are several accepted methods to measure log K(OW), no standardized method exists to determine log k(IAM). The database of collated log k(IAM) values includes 13 key experimental parameters and contains 1,686 values for 555 compounds, which are predominantly polar organic compounds and include drug molecules and surfactants. These compounds are acidic, basic, and neutral and both ionized and un-ionized under the conditions of analysis. The data compiled demonstrated experimental variability for each experimental parameter considered, including column stationary phase, pH, temperature, and mobile phase. Reducing the experimental variability allowed for greater consistency in the datasets.

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“…In general, larger molecules have a lower aqueous solubility than smaller molecules (Potts and Guy, 1993;Genty et al, 2001). The particle size may affect the solubility to a certain extent.…”

Section: Molecular and Particle Sizementioning

confidence: 99%

Solubility of Pharmaceutical Solids

Wiser

Gao

Jasti

et al. 2011

Oral Bioavailability

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Determination of the passive absorption through the rat intestine using chromatographic indices and molar volume

Cited by 67 publications

References 24 publications

Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

Database of published retention factors for immobilized artificial membrane HPLC and an assessment of the effect of experimental variability

Solubility of Pharmaceutical Solids

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