Enhanced transport of a novel anti-HIV agent—cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers

Udata, Chandrasekhar; Patel, J. R.; Pal, Dhananjay; Hejchman, Elżbieta; Cushman, Mary; Mitra, Ashim K.

doi:10.1016/s0378-5173(02)00523-9

Cited by 28 publications

(18 citation statements)

References 24 publications

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“…Arima et al (2001) reported the enhancing effect of dimethyl-␤-CD on the oral bioavailability of tacrolimus in Caco-2 cells. In addition, dimethyl-␤-CD and HP-␤-CD exhibited 22-and 19-fold permeability coefficient enhancement of cosalane (a potent inhibitor of HIV), respectively (Udata et al, 2003). The authors concluded that CDs can promote transport by altering membrane fluidity with a minimal disruption of cellular bar- rier.…”

Section: Discussionmentioning

confidence: 99%

Effects of γ- and Hydroxypropyl-γ-cyclodextrins on the Transport of Doxorubicin across an in Vitro Model of Blood-Brain Barrier

Monnaert¹,

Betbeder²,

Fénart³

et al. 2004

J Pharmacol Exp Ther

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Association between doxorubicin (DOX) and ␥-cyclodextrin (␥-CD) or hydroxypropyl-␥-CD (HP-␥-CD) has been examined to increase the delivery of this antitumoral agent to the brain. The stoichiometry and the stability constant of ␥-CD or HP-␥-CD and DOX complexes were determined in physiological medium by UV-visible spectroscopy. By using an in vitro model of the blood-brain barrier (BBB), endothelial permeability and toxicity toward the brain capillary endothelial cells of DOX, ␥-CD, and HP-␥-CD were performed. For each CD, endothelial permeability was relatively low and a disruption of the BBB occurred at 20 M, 20 mM, and 50 mM DOX, ␥-CD, and HP-␥-CD, respectively. Increasing amounts of CDs were added to a fixed DOX concentration. Addition of ␥-CD or HP-␥-CD, up to 15 and 35 mM, respectively, decreased the DOX delivery, probably due to the low complex penetration across the BBB and the decrease in free DOX concentration. Higher CD concentrations increased the DOX delivery to the brain, but this effect is due to a loss of BBB integrity. In contrast to what was observed on Caco-2 cell model with various drugs, CDs are not able to increase the delivery of DOX across our in vitro model of BBB.

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Section: Discussionmentioning

confidence: 99%

Effects of γ- and Hydroxypropyl-γ-cyclodextrins on the Transport of Doxorubicin across an in Vitro Model of Blood-Brain Barrier

Monnaert¹,

Betbeder²,

Fénart³

et al. 2004

J Pharmacol Exp Ther

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“…Arima et al (2001) reported the enhancing effect of dimethyl-β-CD on the oral bioavailability of tacrolimus in Caco-2 cells. In addition, dimethyl-β-CD and HP-β-CD exhibited 22-fold and 19-fold permeability coefficient enhancement of cosalane (a potent inhibitor of HIV) respectively (Udata et al, 2003). The authors concluded that CDs can promote transport by altering membrane fluidity with a minimal disruption of cellular barrier.…”

Section: Discussionmentioning

confidence: 99%

DMEM (Dulbecco’s Modified Eagle’s Medium)

2006

Cold Spring Harb Protoc

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“…Both positive and negative outcomes have been achieved with the complexation of drugs with cyclodextrins in relation to the in vitro permeability (32)(33)(34)(35)(36)(37). To investigate if the complexation may also affect the in vitro intestinal permeability of thalidomide, transport experiments were performed on Caco-2 cells.…”

Section: In Vitro Permeability Datamentioning

confidence: 99%

Preparation, Characterization, and In Vitro Intestinal Permeability Evaluation of Thalidomide–Hydroxypropyl-β-Cyclodextrin Complexes

et al. 2011

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Abstract. Thalidomide is emerging as a therapeutic agent with renewed clinical importance, presenting anti-inflammatory, immunomodulatory, and antineoplasic properties. In this work, we studied the complexation of thalidomide with cyclodextrins as a strategy to circumvent the poor aqueous solubility of the drug. Thalidomide-hydroxypropyl-β-cyclodextrin complexes were obtained by kneading method and were characterized by differential scanning calorimetry, powder X-ray diffractometry, and scanning electronic microscopy. The aqueous solubility and in vitro dissolution of thalidomide were significantly improved through the complexation. Physicochemical analysis of the complexes in solid state revealed a decreased crystallinity of the complexed drug in comparison with free thalidomide. Thalidomide was able to dissociate from the complexes and permeates across intestinal epithelial Caco-2 cells with a favorable high permeability profile equivalent to that of the free drug. In summary, the present results suggest that thalidomide-hydroxypropyl-β-cyclodextrin complexes could be regarded as a promising strategy for improving the gastrointestinal absorption of thalidomide.

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Enhanced transport of a novel anti-HIV agent—cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers

Cited by 28 publications

References 24 publications

Effects of γ- and Hydroxypropyl-γ-cyclodextrins on the Transport of Doxorubicin across an in Vitro Model of Blood-Brain Barrier

Effects of γ- and Hydroxypropyl-γ-cyclodextrins on the Transport of Doxorubicin across an in Vitro Model of Blood-Brain Barrier

DMEM (Dulbecco’s Modified Eagle’s Medium)

Preparation, Characterization, and In Vitro Intestinal Permeability Evaluation of Thalidomide–Hydroxypropyl-β-Cyclodextrin Complexes

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