Cyclodextrins in drug delivery

Loftsson, Þorsteinn; Jarho, Pekka; Másson, Már; Järvinen, Tomi

doi:10.1517/17425247.2.1.335

Cited by 692 publications

(459 citation statements)

References 108 publications

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“…When the complex is first order with respect to CDs then A L -type phase-solubility (linear increase in solubility of the compound as a function of CDs concentration) profiles are obtained. If the complex is first order with respect to therapeutic agent, but second or higher order with respect to the CDs then A Ptype curve is obtained (positive deviation from linearity with increasing concentration of CDs) (33,34). Phase-solubility studies demonstrate that HPβCD, RMβCD, and SβCD, through their ability to form inclusion complexes, dramatically improved the solubility of Δ 8 -THC (Fig.…”

Section: Discussionmentioning

confidence: 98%

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Enhanced Solubility, Stability, and Transcorneal Permeability of Delta-8-Tetrahydrocannabinol in the Presence of Cyclodextrins

et al. 2011

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Abstract. The purpose of this study was to investigate the effect of cyclodextrins (CDs) on aqueous solubility, stability, and in vitro corneal permeability of delta-8-tetrahydrocannabinol (Δ 8 -THC). Phase solubility of Δ 8 -THC was studied in the presence of 2-hydroxypropyl-β-cyclodextrin (HPβCD), randomly methylated-β-cyclodextrin (RMβCD) and sulfobutyl ether-β-cyclodextrin sodium salt (SβCD). Stability of Δ 8 -THC in 5% w/v aqueous CD solutions, as a function of pH, was studied following standard protocols. In vitro corneal permeation of Δ 8 -THC (with and without CDs) across excised rabbit cornea was also determined. Phase-solubility profile of Δ 8 -THC in the presence of both HPβCD and RMβCD was of the A P type, whereas, with SβCD an A L type was apparent. Aqueous solubility of Δ 8 -THC increased to 1.65, 2.4, and 0.64 mg/mL in the presence of 25% w/v HPβCD, RMβCD, and SβCD, respectively. Significant degradation of Δ 8 -THC was not observed within the study period at the pH values studied, except for at pH 1.2. Transcorneal permeation of Δ 8 -THC was dramatically improved in the presence of CDs. The results demonstrate that CDs significantly increase aqueous solubility, stability, and transcorneal permeation of Δ 8 -THC. Thus, topical ophthalmic formulations containing Δ 8 -THC and modified beta CDs may show markedly improved ocular bioavailability.

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Section: Discussionmentioning

confidence: 98%

“…Effect of increasing concentration of CDs on aqueous solubility of the therapeutic agent is usually determined using phase-solubility studies according to the method of Higuchi and Connors (33,34). A-type phase-solubility profiles are obtained when apparent solubility of the therapeutic agent increases with increasing concentration of CDs.…”

Section: Discussionmentioning

confidence: 99%

Enhanced Solubility, Stability, and Transcorneal Permeability of Delta-8-Tetrahydrocannabinol in the Presence of Cyclodextrins

et al. 2011

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“…The binding constant (K), which reflects the strength of the binding interaction, can be determined from the solubility diagram using the slope and the drug initial solubility (S0), i.e. drug solubility when no BSA is present (Loftsson et al, 2005):…”

Section: Solubility Studiesmentioning

confidence: 99%

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Khoder

Abdelkader

ElShaer

et al. 2016

International Journal of Pharmaceutics

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Please cite this article as: Khoder, Mouhamad, Abdelkader, Hamdy, ElShaer, Amr, Karam, Ayman, Najlah, Mohammad, Alany, Raid G., Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin.International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2016.11.019 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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“…Hydrophilic cyclodextrins 40 can increase the drug transport only if the resistance of UWL on 41 donor side is equal or higher than the resistance of membrane barrier Masson et al, 1999). According to this 43 mechanism, the complexed drug is carried to the membrane where 44 the complex dissociates and only the free drug molecule penetrates 45 through the membrane (Loftsson et al, 2005). In silico simulations 46 confirmed that bCD and bCD-involved assemblies confronting large 47 energy barriers to go across the membrane (Ren et al, 2015).…”

Section: Introductionmentioning

confidence: 98%

Endocytosis of fluorescent cyclodextrins by intestinal Caco-2 cells and its role in paclitaxel drug delivery

Réti-Nagy

Malanga

Fenyvesi

et al. 2015

International Journal of Pharmaceutics

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Chemical compounds studied in this article: Cyclodextrins are widely used excipients in pharmaceutical formulations. They are mainly utilized as solubilizers and absorption enhancers, but recent results revealed their effects on cell membranes and pharmacological barriers. In addition to the growing knowledge on their interaction with plasma membranes, it was confirmed that cyclodextrins are able to enter cells by endocytosis. The number of the tested cyclodextrins was limited, and the role of this mechanism in drug absorption and delivery is not known. Our aim was to examine the endocytosis of fluorescently labeled hydroxypropyl-b-cyclodextrin, random methyl-b-cyclodextrin and soluble b-cyclodextrin polymer, and the cellular uptake of the fluorescent paclitaxel derivative-random methyl-b-cyclodextrin complex. The studied cyclodextrin derivatives were able to enter Caco-2 intestinal cells and localized in vesicles in the cytoplasm, while their permeability was very limited through Caco-2 monolayers. We demonstrated for the first time that the fluorescent paclitaxel derivative and rhodamine-labeled random methyl-b-cyclodextrin were detected in the same intracellular vesicles after treating cells with their inclusion complex. These results indicate that the endocytosis of cyclodextrin complexes can contribute to drug absorption processes.2015 Published by Elsevier B.V.

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Cyclodextrins in drug delivery

Cited by 692 publications

References 108 publications

Enhanced Solubility, Stability, and Transcorneal Permeability of Delta-8-Tetrahydrocannabinol in the Presence of Cyclodextrins

Enhanced Solubility, Stability, and Transcorneal Permeability of Delta-8-Tetrahydrocannabinol in the Presence of Cyclodextrins

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Endocytosis of fluorescent cyclodextrins by intestinal Caco-2 cells and its role in paclitaxel drug delivery

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