Identification of permeability-related hurdles in oral delivery of curcumin using the Caco-2 cell model

Wahlang, Banrida; Pawar, Yogesh B.; Bansal, Arvind K.

doi:10.1016/j.ejpb.2010.12.006

Cited by 222 publications

(175 citation statements)

References 28 publications

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“…According to these results, the use of microemulsion for DOX can be leaded to an enhancement of permeated drug concentration. A similar result concerning the release of a submicron lipid emulsion formulation was also observed (15,16 …”

Section: Permeability Studies For Dox Microemulsion and Solutionsupporting

confidence: 59%

Radioactive Permeability Studies of Doxycycline Hyclate from Microemulsion and Solution

İlem-Özdemir¹,

Gündoğdu²,

Ekinci³

et al. 2016

Marmara Pharm J

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Doxycycline Hyclate (DOX) is an antibacterial drug which is member of the second tetracycline group and the absorption of DOX is reduced about 20% in the presence of skimmed milk. Therefore new drug delivery system can be advisable for DOX to reduce the food and drug interaction and improve the bioavailability. The aim of the present study is to prepare a microemulsion system of DOX which could result in reducing in food interaction and an improvement of oral bioavailability by increasing the drug's permeability. For this purposes, DOX was radiolabeled with 99m Tc. radiochemical purity was determined with radioactive thin layer chromatography (rTlc) studies. Tc-DOX-s. Based on the in vitro cell culture studies, this dosage form is a promising formulation as an alternative for oral drug delivery of DOX. Permeability of DOX from

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Section: Permeability Studies For Dox Microemulsion and Solutionsupporting

confidence: 59%

Radioactive Permeability Studies of Doxycycline Hyclate from Microemulsion and Solution

İlem-Özdemir¹,

Gündoğdu²,

Ekinci³

et al. 2016

Marmara Pharm J

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“…The cumulative amount of the drug that permeated through the monolayers measured in the receiver compartment was plotted against the sampling time. The apparent permeability coefficient was calculated according to the following equation (27).…”

Section: Transport Across the Caco-2 Monolayersmentioning

confidence: 99%

Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin

et al. 2013

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Abstract. Novel self-microemulsifying floating tablets were developed to enhance the dissolution and oral absorption of the poorly water-soluble tetrahydrocurcumin (THC). Their physicochemical properties and THC permeability across Caco-2 cell monolayers were assessed. The self-microemulsifying liquid containing THC was adsorbed onto colloidal silicon dioxide, mixed with HPMC, gas-generating agents (sodium bicarbonate and tartaric acid), lactose and silicified-microcrystalline cellulose and transformed into tablets by direct compression. The use of different types/concentrations of HPMC and sodium bicarbonate in tablet formulations had different effects on the floating characteristics and in vitro THC release. The optimum tablet formulation (F2) provided a short floating lag time (∼23 s) together with a prolonged buoyancy (>12 h). About 72% of THC was released in 12 h with an emulsion droplet size in aqueous media of 33.9±1.0 nm while that of a self-microemulsifying liquid was 29.9±0.3 nm. The tablet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. The THC released from the self-microemulsifying liquid and tablet formulations provided an approximately three-to fivefold greater permeability across the Caco-2 cell monolayers than the unformulated THC and indicated an enhanced absorption of THC by the formulations. The self-microemulsifying floating tablet could provide a dosage form with the potential to improve the oral bioavailability of THC and other hydrophobic compounds.

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“…Curcumin is ineffectively transported across the intestinal mucosa into the circulation (Holder et al, 1978;Wahlstrom and Blennow, 1978;Ravindranath and Chandrasekhara, 1980;Cheng et al, 2001;Sharma et al, 2001Sharma et al, , 2004Garcea et al, 2004Garcea et al, , 2005Yang et al, 2007a;Vareed et al, 2008;Villegas et al, 2008;Suresh and Srinivasan, 2010;Wahlang et al, 2011;Berginc et al, 2012). Furthermore, the curcumin molecules that bypass transport hurdles and escape biotransformation in the intestinal mucosa (Ireson et al, 2002;Hoehle et al, 2007;Wahlang et al, 2011;Berginc et al, 2012;Dempe et al, 2012), i.e., by definition the first pass effect for orally administered curcumin, and manage to reach the circulation instantaneously become susceptible to chemical modification in blood ; uptake and biotransformation by the liver (second pass effect), kidneys, and other organs (Holder et al, 1978;Wahlstrom and Blennow, 1978;Pan et al, 1999;Asai and Miyazawa, 2000;Garcea et al, 2004;Hoehle et al, 2006;Tamvakopoulos et al, 2007b;Vareed et al, 2008;Marczylo et al, 2009), and excretion via the biliary or urinary system, albeit the latter occurs to a limited extent (Holder et al, 1978;Ravindranath and Chandrasekhara, 1980;Sharma et al, 2004;Marczylo et al, 2009;Suresh and Srinivasan, 2010). These phenomena are further elaborated in the context of biological curcumin metabolite...…”

Section: A Curcumin Pharmacokinetics and Pharmacodynamicsmentioning

confidence: 99%

“…The enzymatic source responsible for the reduction of curcumin is, however, strictly cytosolic, whereas the reduction of hexahydrocurcumin to octahydrocurcumin occurs in both the cytosol and microsomes (Ireson et al, 2002). In Caco-2 cell transport experiments, Wahlang et al (2011) showed that itraconazole-mediated inhibition of cytochrome P450 CYP3A4, an isozyme that is replete Cancer Pharmacology of Curcumin in the liver and intestines (Yokose et al, 1999) and capable of detoxifying certain drugs by reduction (Shahrokh et al, 2012), results in an increased curcumin permeability coefficient (Wahlang et al, 2011). This finding is suggestive of alterations in reductive biotransformation of curcumin by CYP3A4, which manifests itself in differential curcumin transport kinetics as a result of a shifted curcumin:reduced curcumin equilibrium and corollary effects on transporter activity.…”

Section: Pharmacokinetics and Pharmacodynamic Implications Of Curcmentioning

confidence: 99%

The Molecular Basis for the Pharmacokinetics and Pharmacodynamics of Curcumin and Its Metabolites in Relation to Cancer

Golen²,

et al. 2013

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Identification of permeability-related hurdles in oral delivery of curcumin using the Caco-2 cell model

Cited by 222 publications

References 28 publications

Radioactive Permeability Studies of Doxycycline Hyclate from Microemulsion and Solution

Radioactive Permeability Studies of Doxycycline Hyclate from Microemulsion and Solution

Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin

The Molecular Basis for the Pharmacokinetics and Pharmacodynamics of Curcumin and Its Metabolites in Relation to Cancer

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