Pharmacokinetics of the new galenic formulation of cyclosporin A, Neoral, (Sandoz) was examined in 12 stable young patients after renal transplantation. Six of these patients were tested before and 4 weeks after switching from the standard formulation Sandimmun to Neoral. No significant changes were observed in trough levels, Lmax, Cmax, and AUC0-12 h, but the absorption rate constant (Ka) increased (P = 0.03). Glomerular filtration rate, as assessed by inulin clearance, increased by more than 10% in three patients and decreased in two, and was usually associated with a respective drop and rise in Cmax and AUC0-12 h of cyclosporin A. The large interindividual variability in the response to the conversion to the new formulation points to a need for close monitoring of cyclosporin A trough levels and renal function after switching from Sandimmun to Neoral in this age group in order to avoid nephrotoxicity.
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http://dx.doi.org/10.1007/BF00336825 | DOI Listing |
J Ocul Pharmacol Ther
January 2025
Ophtalmology Department, Rouen University Hospital, Rouen, France.
Cyclosporin A (CsA) is a drug used to prevent immune rejection in corneal transplantation. Most grafts performed today are endothelial grafts which are complicated with poor penetration of CsA into the endothelium due to its hydrophobicity. To improve CsA penetration into the corneal a new ocular formulation of CsA 2% with Miglyol was developed and is commercially available.
View Article and Find Full Text PDFOphthalmol Ther
February 2025
Santa Barbara Eye Care, Santa Barbara, CA, USA.
Perfluorohexyloctane ophthalmic solution (Miebo) and water-free cyclosporine ophthalmic solution 0.1% (Vevye) are recently approved treatments for dry eye disease (DED). Perfluorohexyloctane (PFHO) uses a novel approach to treat evaporative DED, whereas water-free cyclosporine (CsA 0.
View Article and Find Full Text PDFPharm Dev Technol
January 2025
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India.
Purpose: Supersaturated formulations have been widely explored for improving the oral bioavailability of drugs by using mesoporous silica (MS) to generate supersaturation molecular adsorption; however, this is followed by precipitation. Several precipitation inhibitors (PI) have been explored to prevent precipitation and maintain the drug in solution for a longer period. However, the combined approach of MS and PIs, the impact of MS and Silica, and the loading of high-molecular-weight neutral molecules such as Cyclosporine A (CsA) have not yet been explored.
View Article and Find Full Text PDFSmall
December 2024
Department of Pharmaceutics, School of Pharmacy, Air Force Medical University, Xi'an, 710032, China.
Mitochondrial dysfunction plays an important role in neuroinflammation and cognitive impairment in Alzheimer's disease (AD). Herein, this work designs a mitochondria-targeted micelle CsA-TK-SS-31 (CTS) to block the progression of AD by simultaneously alleviating mitochondrial dysfunction in microglia and neurons. The mitochondria-targeted peptide SS-31 drives cyclosporin A (CsA) to penetrate the blood-brain barrier (BBB) and delivers CsA to mitochondria of microglia and neurons in the brains of 5 × FAD mice.
View Article and Find Full Text PDFGraefes Arch Clin Exp Ophthalmol
November 2024
Novaliq GmbH, Heidelberg, Germany.
Purpose: This pooled analysis of two pivotal studies (ESSENCE-1 and ESSENCE-2) evaluated treatment effects of a water-free ciclosporin 0.1% solution in dry eye disease (DED) patients in the overall population and in subgroups according to sex, age, and baseline severity of disease.
Methods: In these randomized, multicenter, double-masked, vehicle-controlled studies patients received ciclosporin 0.
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