Improved oral bioavailability of cyclosporin A in male Wistar rats

González, Roberto Carlos Bravo; Huwyler, Jörg; Walter, Isabelle; Mountfield, Richard J.; Bittner, Beate

doi:10.1016/s0378-5173(02)00339-3

Cited by 37 publications

(8 citation statements)

References 22 publications

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“…Different types of macrogolglycerides have been used in the preparation of lipid-based drug delivery systems (8)(9)(10)(11)(12)(13)(14)(15). Formulations containing macrogolglycerides have been shown to increase the oral absorption of different compounds, e.g.…”

Section: Introductionmentioning

confidence: 99%

“…Formulations containing macrogolglycerides have been shown to increase the oral absorption of different compounds, e.g. formulations containing Labrasol® (11,14), Gelucire® 44/14 (10,12), and Labrafils (8,15). Labrafil® M2125CS used in the present study is composed of a mixture of mono-, di-, and triglycerides and mono-and di-fatty acid esters of polyethylene glycol 300 (PEG 300), but may also contain some free PEG 300 (16).…”

Section: Introductionmentioning

confidence: 99%

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Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

et al. 2008

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

et al. 2008

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“…The surface-active amphiphile Solutol ® HS15 (HS15), composed of the PEG-660 ester of 12-hydroxystearic acid, has the potential to increase the solubility of a number of poorly watersoluble compounds such as doxorubicin, 9-nitrocamptothecin, and curcumin. [10][11][12] HS15 has been approved as an excipient in a parenteral phytonadione formulation for human use in Canada, 13 which has been proven to promote solubilization of therapeutics in an aqueous environment, protect therapeutics from degradation without modifying the therapeutic activity, or prevent premature release; eventually, it enhances adhesion and permeation at the biological membranes. HS15 has also been proven to be of low toxicity for oral administration.…”

Section: Luo Et Almentioning

confidence: 99%

“…HS15 was proven effective in enhancing the intestinal permeability and oral absorption of lipophilic drugs. 13 Meanwhile, the nanometer-sized particles could improve the affinity and accessibility of nanomicelles to the intestinal membrane, thereby increasing its absorption in the intestine.…”

Section: Pharmacokinetics and Biodistribution Of Nim Nanomicellesmentioning

confidence: 99%

One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine

Luo¹,

Zhang²,

Gong³

et al. 2016

IJN

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Our study aimed to develop a self-assembled nanomicelle for oral administration of nimodipine (NIM) with poor water solubility. Using Solutol ® HS15, the NIM-loaded self-assembled nanomicelles displayed a near-spherical morphology with a narrow size distribution of 12.57±0.21 nm (polydispersity index =0.071±0.011). Compared with Nimotop ® (NIM tablets), the intestinal absorption of NIM from NIM nanomicelle in rats was improved by 3.13- and 2.25-fold in duodenum and jejunum at 1 hour after oral administration. The cellular transport of NIM nanomicelle in Caco-2 cell monolayers was significantly enhanced compared to that of Nimotop ® . Regarding the transport pathways, clathrin, lipid raft/caveolae, and macropinocytosis mediated the cell uptake of NIM nanomicelles, while P-glycoprotein and endoplasmic reticulum/Golgi complex (ER/Golgi) pathways were involved in exocytosis. Pharmacokinetic studies in our research laboratory have showed that the area under the plasma concentration–time curve (AUC 0–∞ ) of NIM nanomicelles was 3.72-fold that of Nimotop ® via oral administration in rats. Moreover, the NIM concentration in the brain from NIM nanomicelles was dramatically improved. Therefore, Solutol ® HS15-based self-assembled nanomicelles represent a promising delivery system to enhance the oral bioavailability of NIM.

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“…The surfactant has been approved in a parenteral Phytonadion formulation for human use on the Canadian market. Additionally, oral formulations containing Solutol have been shown to enhance the oral bioavailability of co-formulated compounds in rat experiments [5,6].…”

Section: Introductionmentioning

confidence: 99%

Impact of Oral Administration of the Surface-Active Excipient Solutol HS 15 on the Pharmacokinetics of Intravenously Administered Colchicine

Bittner¹,

González

Walter³

et al. 2005

LDDD

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Formulation ingredients may influence the pharmacokinetics of co-administered drugs. We investigated whether oral pre-dosing with the 'inactive' formulation ingredient Solutol affects the pharmacokinetic profile of intravenously administered colchicine in rats. Colchicine was administered intravenously to male Wistar rats as solution in isotonic sodium chloride (NaCl 0.9%, control group) at 1.5 mg/kg. A second group of rats received the intravenous dose of colchicine 20 minutes after oral pre-dosage with 4 mg/kg of a 90:10 (v/v) mixture of NaCl 0.9% and Solutol HS 15 (Solutol). At predetermined time points, plasma and urine were collected from the animals and analyzed for colchicine and its demethylated metabolites by LC/MS-MS. After oral pre-treatment with Solutol, colchicine plasma clearance (Cl) was decreased by a factor of two and its maximum plasma concentration (c max ) was almost twofold increased as compared to the control group. Moreover, the amount of parent colchicine excreted into urine within 24 hours after administration did increase twentyfold in the Solutol treated group. Renal excretion of colchicine metabolites was slightly increased. We conclude that absorption of Solutol and/or its degradation products into the systemic circulation seems to be a major contributor to the observed effects. Our results suggest that oral administration of formulation ingredients may alter the distribution kinetics of drugs, which are co-administered orally as well as intravenously.

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Improved oral bioavailability of cyclosporin A in male Wistar rats

Cited by 37 publications

References 22 publications

Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine

Impact of Oral Administration of the Surface-Active Excipient Solutol HS 15 on the Pharmacokinetics of Intravenously Administered Colchicine

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