Lepid transport across the intestinal epithelial cell

Arreaza-Plaza, C.A.; Bosch, Virgilio; Otayek, M.A.

doi:10.1016/0005-2760(76)90150-8

Cited by 23 publications

(3 citation statements)

References 20 publications

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“…However, it has been clearly demonstrated that anomalies in CF exist in the intracellular movement of the CFTR itself. Various physiochemical conditions, such as low temperatures [233] or chemical agents [235], are able to increase the stability of the mutated CFTR protein and avoid its abnormal retention in the ER [236,237]. The latter would, in part, be attributable to a defective interaction between the CFTR and certain PLs that play the role of lipid chaperones.…”

Section: Enterocyte Phase Abnormalitiesmentioning

confidence: 99%

Mechanisms of lipid malabsorption in Cystic Fibrosis: the impact of essential fatty acids deficiency

et al. 2005

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Transport mechanisms, whereby alimentary lipids are digested and packaged into small emulsion particles that enter intestinal cells to be translocated to the plasma in the form of chylomicrons, are impaired in cystic fibrosis. The purpose of this paper is to focus on defects that are related to intraluminal and intracellular events in this life-limiting genetic disorder. Specific evidence is presented to highlight the relationship between fat malabsorption and essential fatty acid deficiency commonly found in patients with cystic fibrosis that are often related to the genotype. Given the interdependency of pulmonary disease, pancreatic insufficiency and nutritional status, greater attention should be paid to the optimal correction of fat malabsorption and essential fatty acid deficiency in order to improve the quality of life and extend the life span of patients with cystic fibrosis.

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Section: Enterocyte Phase Abnormalitiesmentioning

confidence: 99%

Mechanisms of lipid malabsorption in Cystic Fibrosis: the impact of essential fatty acids deficiency

et al. 2005

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“…Natural long-chain TGs are normally absorbed into the blood circulation by the lymphatic system. To verify that the TG-like prodrugs could mimic the absorption pathway of natural TG, colchicine (5 mg/kg), an inhibitor of lymphatic transport, was used to inhibit the secretion of chylomicrons from enterocytes [55 , 56] . After the intraperitoneal injection of colchicine, the CTX plasma concentrations after oral administration of the three TG-like prodrug SNEDDS decreased significantly, while those after oral administration of the CTX solution were not affected ( Fig.…”

Section: Resultsmentioning

confidence: 99%

Fine-tuning the activation behaviors of ternary modular cabazitaxel prodrugs for efficient and on-target oral anti-cancer therapy

Zhang,

Miao,

Zhao

et al. 2024

Asian Journal of Pharmaceutical Sciences

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“…Colchicine, which is known as an inhibitor of chylomicron synthesis, dissolved in PBS (pH 7.4) was intravenously administered at a dose of 5 mg/kg body weight. [9][10][11] One hour after colchicine injection, each lipid-based formulation including SG was orally administered. Blood was then withdrawn and a plasma sample was obtained as described above.…”

Section: Evaluation Of Intestinal Absorption Of Lipid-based Formulationsmentioning

confidence: 99%

Disposition of Lipid-Based Formulation in the Intestinal Tract Affects the Absorption of Poorly Water-Soluble Drugs

Iwanaga

Kubota

Miyazaki

et al. 2006

Biological & Pharmaceutical Bulletin

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Recently, drug discovery strategies, based on the technology of combinatorial chemistry and high throughput screening, have often produced compounds with poor water-solubility.1,2) Most of those compounds will drop out as candidates at the pre-formulation or formulation study stage because of their low intestinal absorption despite their high pharmacological activity in vitro. Therefore, the investigation of new dosage formulations for poorly water-soluble compounds will contribute to drug development.Since a new oral dosage formulation for an immunosuppressant drug (cyclosporine A), named "Neoral R ", was developed and used clinically, 3) lipid-based formulations 4,5) to improve the oral absorption of poorly water-soluble drugs have received considerable attention in the pharmaceutical industry. Neoral R contains various ingredients to form an emulsion in the intestinal tract and works as a Self-microemulsifying drug delivery system (SMEDDS).6) This system is regarded as an advanced system of lipid-based formulations. As SMEDDS generally consists of lipid(s) and surfactant(s), these components may affect the absorption mechanism of poorly water-soluble drugs. However, the disposition of lipidbased formulation components in the intestinal tract has not yet been clarified.In this study, we investigated the role of lipid-based formulation components for the intestinal absorption of poorly water-soluble drug by focusing on the disposition of the formulation after oral administration. , the mixture of saturated polyglycolized glyceride and mono-or di-fatty acid esters of polyethylene glycol (Lauroyl macrogol-32 glycerides), was a kind gift from Gattefosse (Gennevilliers Cedex, France). All other chemicals used were of analytical grade. MATERIALS AND METHODS MaterialsPreparation of Lipid-Based Formulations SG (M.W. 418.5), an anthraquinone derivative, was used as a poorly water-soluble model compound. This compound is a poorly water-soluble dye, and its logP value was 7.40. Soybean oil emulsion was prepared by the conventional method. 7) Briefly, 3 mg of SG was added to 0.5 ml of soybean oil preheated at 60°C in a hot water bath and dissolved completely. 0.25 ml of Tween 80 and 4.25 ml of distilled water were added to the oil and sonicated at 20 W for 5 min using an Ultrasonic Disrupter UD-201, Tomy Co. (Tokyo, Japan). For SMEDDS, 3 mg of SG was dissolved in 5 ml of Gelucire 44/14 R preheated at 60°C in a hot water bath. It was then cooled down immediately before use because Gelucire 44/14 R becomes semi-solid at room temperature.In Vivo Oral Administration to Rats All animal experiments were approved by the Animal Experimentation Committee of Osaka University of Pharmaceutical Sciences. Male Wistar rats weighing 300-350 g were obtained from Japan SLC, Inc. (Shizuoka, Japan). The day before the experiment, the rats were lightly anesthetized with ether, and were implanted surgically with a combination of Phicon (Fuji Systems Ltd., Tokyo, Japan) and PE50 (Clay Adams, Parsippany, NJ, U.S.A.) in a catheter, which was ins...

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Lepid transport across the intestinal epithelial cell

Cited by 23 publications

References 20 publications

Mechanisms of lipid malabsorption in Cystic Fibrosis: the impact of essential fatty acids deficiency

Mechanisms of lipid malabsorption in Cystic Fibrosis: the impact of essential fatty acids deficiency

Fine-tuning the activation behaviors of ternary modular cabazitaxel prodrugs for efficient and on-target oral anti-cancer therapy

Disposition of Lipid-Based Formulation in the Intestinal Tract Affects the Absorption of Poorly Water-Soluble Drugs

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