Effect of partially methylated β cyclodextrin on percutaneous absorption of metopimazine

Bounoure, F.; Lahiani-Skiba, Malika; Barbot, Cécile; Sughir, Abdussalam; Mallet, Eric; Jezequel, Soizic; Didier, Ludovic; Arnaúd, Philippe; Sarakha, Mohamed

doi:10.1007/s10847-006-9195-x

Cited by 4 publications

(1 citation statement)

References 8 publications

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“…Acitretin RMbCD [21] Alkannin HPbCD [22] Avobenzone HPbCD [23] Beclometasone dipropionate gCD [24] 4-Biphenylylacetic acid bCD, DMbCD, HPbCD [25,26] Bupranolol HPbCD, MbCD [27] Capsaicin HPbCD [28] Celecoxib DMbCD [29] Curcumin HPbCD, HPgCD [30] Dexamethasone acetate bCD, HPbCD [31] 17b-Estradiol HPbCD [32] Hydrocortisone bCD, CMbCD, HPbCD, MLbCD, RMbCD [32][33][34][35][36][37][38][39] Ibuprofen HPbCD [40] Indometacin bCD, DEbCD, DMbCD [41,42] Ketoprofen HPbCD [43] Liarozole HPbCD [44] Lidocaine DMbCD, HPbCD, SBEbCD [45] Loteprednol etabonate DMbCD [46] Melatonin HPbCD [47] Metopimazine MbCD [48] Methyl paraben HPbCD [49] Miconazole aCD, HPbCD [50] Naproxen bCD [51] Piribedil RMbCD [52] Piroxicam HPbCD [53,54] Prednisolone bCD, gCD [55] Prostaglandin E1 aCD, bCD, CMEbCD, [56][57][58][59] Shikonin HPbCD [22] Sulfanilic acid bCD, DMbCD [41] Testosterone HPbCD [32] Tolnaftate bCD, bCD-polymer [60] Tretinoin bCD, H...…”

Section: Drugmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes

Loftsson

Brewster

2011

Journal of Pharmacy and Pharmacology

233

126

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Objectives Cyclodextrins are useful solubilizing excipients that have gained currency in the formulator's armamentarium based on their ability to temporarily camouflage undesirable physicochemical properties. In this context cyclodextrins can increase oral bioavailability, stabilize compounds to chemical and enzymatic degradation and can affect permeability through biological membranes under certain circumstances. This latter property is examined herein as a function of the published literature as well as work completed in our laboratories. Key findings Cyclodextrins can increase the uptake of drugs through biological barriers if the limiting barrier component is the unstirred water layer (UWL) that exists between the membrane and bulk water. This means that cyclodextrins are most useful when they interact with lipophiles in systems where such an UWL is present and contributes significantly to the barrier properties of the membrane. Furthermore, these principles are used to direct the optimal formulation of drugs in cyclodextrins. A second related critical success factor in the formulation of cyclodextrin-based drug product is an understanding of the kinetics and thermodynamics of complexation and the need to optimize the cyclodextrin amount and drug-to-cyclodextrin ratios. Drug formulations, especially those targeting compartments associated with limited dissolution (i.e. the eye, subcutaneous space, etc.), should be carefully designed such that the thermodynamic activity of the drug in the formulation is optimal meaning that there is sufficient cyclodextrin to solubilize the drug but not more than that. Increasing the cyclodextrin concentration decreases the formulation 'push' and may reduce the bioavailability of the system. Conclusions A mechanism-based understanding of cyclodextrin complexation is essential for the appropriate formulation of contemporary drug candidates.

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