Intestinal permeability enhancement of levothyroxine sodium by straight chain fatty acids studied in MDCK epithelial cell line

Pabla, Dimple; Akhlaghi, Fatemeh; Zia, Hossein

doi:10.1016/j.ejps.2010.05.002

Cited by 41 publications

(32 citation statements)

References 31 publications

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“…Lauric acid, myristic acid and linoleic acid, show the highest impact on absorption of caffeic acid in transport studies using Caco-2 cell monolayers. Capric acid, lauric acid and oleic acid are known to increase the permeability of polar drugs in other cell monolayers [13]. Lauric acid, myristic acid and capric acid are among the major fatty acids present in coconut oil.…”

Section: Resultsmentioning

confidence: 99%

“…Capric acid (C10), lauric acid (C12) and oleic acid (C18) significantly increase levothyroxine sodium transport and the order of enhancement was C12≈C18 > C10. This increase in transport and the reductions in transepithelial electrical resistance (TEER) values indicate opening of tight junctions to improve the paracellular permeability [13]. Sodium caprate induced increased permeability to polysucrose and opening of the tight junctions was visualized by transmission electron microscopy [11].…”

Section: Introductionmentioning

confidence: 99%

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Effect of three edible oils on the intestinal absorption of caffeic acid: An in vivo and in vitro study

et al. 2017

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Polyphenolic antioxidants are mainly absorbed through passive paracellular permeation regulated by tight junctions. Some fatty acids are known to modulate tight junctions. Fatty acids resulting from the digestion of edible oils may improve the absorption of polyphenolic antioxidants. Therefore, we explored the effect of three edible oils on the intestinal absorption of caffeic acid. Rats were fed with soybean oil and caffeic acid dissolved in distilled water. Caffeic acid contents in the plasma collected up to 1 hr were quantified. The experiment was repeated with coconut oil and olive oil. Component fatty acids of the oils were individually tested in vitro for their effect on permeability of caffeic acid using Caco-2 cell monolayers. Highest absorption of caffeic acid was observed in animals fed with coconut oil. In vitro transport percentages of caffeic acid in 2.5 mmol/L solutions of fatty acids were 22.01±0.12 (lauric), 15.30 ± 0.25 (myristic acid), 13.59 ± 0.35 (linoleic acid), 3.70 ± 0.09 (oleic acid) and 0.10–2.0 (all other fatty acids). Lauric acid and myristic acid are the two major fatty acids present in coconut oil. Therefore, these fatty acids may contribute to the higher absorption of caffeic acid in the presence of coconut oil.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effect of three edible oils on the intestinal absorption of caffeic acid: An in vivo and in vitro study

et al. 2017

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“…Pabla et al (2010) studied the permeability enhancing properties of various medium chain fatty acids including capric acid (C10), lauric acid (C12) and unsaturated long chain fatty acids such as oleic acid (C18) on levothyroxine sodium, a BCS Class III drug. The results were consistent with previous literature findings that fatty acids increase the permeability of a series of hydrophilic drugs by dilating the tight junctions and/or changing the cytoskeleton of the intestinal epithelial cells without pronounced cytotoxicity.…”

Section: Fatty Acidsmentioning

confidence: 99%

Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs

Baki

Chaudhari²,

Gaudana

et al. 2015

Excipient Applications in Formulation Design and Drug Delivery

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Active agents have been considered the main ingredients of any therapeutic product since the early ages of formulation technology. However, the importance of the inactive ingredients has been realized during the last three decades. With the development and manufacturing of more intelligent and multifunction excipients, new ways became available for formulation technologists to increase the beneficial effects of drugs on human body. Many modern active agents have internal characteristics that significantly decrease their potential and theoretical bioavailability; however, today we have the widest variety of inactive ingredients that we can utilize in order to change these properties. The careful and educated selection of excipients might significantly influence the effect of the drugs, including hastening or delaying their onset of action, increasing their bioavailability by changing their physicochemical characteristics, and increasing their stability. In this chapter, we focus primarily on the factors determining and influencing bioavailability as well as the selection of excipients for formulating new dosage forms with enhanced therapeutic efficacy, based on the physicochemical properties of drugs. We will provide some examples from the scientific literature to demonstrate the achievements in this multidisciplinary area.

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“…Različiti literaturni podaci i in silico predviđene vrednosti za oktanol/voda particioni koeficijent (logP iznosi od 1.15 do 2.39) ukazuju na lipofilnu prirodu ove supstance [14][15][16]. Iako bi se na osnovu lipidne prirode očekivalo da levotiroksin lako prolazi kroz intestinalnu membranu, visokopolarna cviter-jonska struktura bočnog lanca koji sadrži ostatak aminokiseline alanina (slika 3) sprečava prolaz molekula kroz hidrofobni unutrašnji lipidni dvosloj membrane, što dovodi do smanjene permeabilnosti [17]. In vitro ispitivanjem na MDCK ćelijama dobijena je vrednost za efektivnu permeabilnost od 0.54 ± 0.06 x 10 -6 cm/min, dok je in silico predviđena vrednost za humanu efektivnu permeabilnost na osnovu strukture molekula 1.34 ± 10 -4 cm/s [16,17].…”

Section: Fizičko-hemijske I Biofarmaceutske Osobineunclassified

“…Iako bi se na osnovu lipidne prirode očekivalo da levotiroksin lako prolazi kroz intestinalnu membranu, visokopolarna cviter-jonska struktura bočnog lanca koji sadrži ostatak aminokiseline alanina (slika 3) sprečava prolaz molekula kroz hidrofobni unutrašnji lipidni dvosloj membrane, što dovodi do smanjene permeabilnosti [17]. In vitro ispitivanjem na MDCK ćelijama dobijena je vrednost za efektivnu permeabilnost od 0.54 ± 0.06 x 10 -6 cm/min, dok je in silico predviđena vrednost za humanu efektivnu permeabilnost na osnovu strukture molekula 1.34 ± 10 -4 cm/s [16,17]. S obzirom da koeficijent permeabilnosti za metoprolol, koji se smatra visoko permeabilnom supstancom i referentnim standardom za procenu stepena permeabilnosti, iznosi 1.4 ± 10 -4 cm/s, može se zaključiti da se levotiroksin nalazi na samoj granici između supstanci niske i visoke permeabilnosti [15].…”

Section: Fizičko-hemijske I Biofarmaceutske Osobineunclassified

Biopharmaceutical characterization of levothyroxine sodium immediate-release tablets

Kocić¹

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Intestinal permeability enhancement of levothyroxine sodium by straight chain fatty acids studied in MDCK epithelial cell line

Cited by 41 publications

References 31 publications

Effect of three edible oils on the intestinal absorption of caffeic acid: An in vivo and in vitro study

Effect of three edible oils on the intestinal absorption of caffeic acid: An in vivo and in vitro study

Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs

Biopharmaceutical characterization of levothyroxine sodium immediate-release tablets

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