In vitro study of cyclosporin absorption: Vehicles and intestinal immaturity

Penaud, J; Decroix, M. O.; Arnaúd, Philippe; Magne, Denis; Gobert, J.G.; Chaumeil, Jean‐Claude

doi:10.1016/0378-5173(96)04585-1

Cited by 3 publications

(2 citation statements)

References 23 publications

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“…Studies with cyclosporine A in humans [53], rats [54] and mice [55] suggest that this peptide is primarily absorbed in the upper part of the small intestine. The variation among different subjects in oral bioavailability of cyclosporine A is related to the intestinal expression of P-glycoprotein (P-gp) and cytochrome P450 3A4 (CYP3A4).…”

Section: Oral Administrationmentioning

confidence: 98%

Chitosan Formulations as Carriers for Therapeutic Proteins

Andrade

Antunes²,

Nascimento³

et al. 2011

CDDT

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Protein drugs represent a significant part of the new pharmaceuticals coming on the market every year and are now widely spread in therapy to treat or relief symptomatology related to many metabolic and oncologic diseases. The delivery of therapeutic proteins is still a major drawback against their maximum pharmacodynamic due to their physicochemical properties, poor stability, permeability and biodistribution. Despite the fact that the parenteral route remains the primary route of protein administration, research continues on non-parenteral delivery routes. However, the high molecular weight of proteins, combined with their hydrophilic and charged nature, renders transport through membranes very difficult. In this regard, the biopolymer chitosan exhibits several favorable biological properties, such as biocompatibility, biodegradability, low-toxicity and mucoadhesiveness, which made it a promising candidate for the formulation of protein drugs. The success of a protein formulation depends not only on the stability of the delivery system but also on their ability to maintain the native structure and activity of the protein during preparation and the delivery, as well as during longterm storage of the formulation. Chitosan-based delivery systems have been proposed as valid approaches to provide such protective conditions. The development of novel protein delivery systems based on chitosan is a rising subject irrespective of the intended route of administration. In this review, the different approaches recently exploited to formulate and deliver therapeutic proteins are underlined.

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Section: Oral Administrationmentioning

confidence: 98%

Chitosan Formulations as Carriers for Therapeutic Proteins

Andrade

Antunes²,

Nascimento³

et al. 2011

CDDT

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“…These formulations demonstrated a large degree of variability in CsA bioavailability and pharmacokinetics (Mueller, 1994). After oral administration, the oily solutions are emulsified by bile salts forming mixed micelles in the gastrointestinal fluid; absorption depends on the emulsion droplet size and triglyceride digestion by pancreatic lipase (Penaud et al, 1996;Senel et al, 1997;Tarr & Yalkowsky, 1989). In accordance with this, meals rich in fat that lead to an increased bile flow can enhance bioavailability significantly.…”

Section: Introductionmentioning

confidence: 99%

Three Generations of Cyclosporine A Formulations: An In Vitro Comparison

Thomas

Koelwel

Machei

et al. 2005

Drug Development and Industrial Pharmacy

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When the microemulsion formulation of the critical dose drug cyclosporine A (CsA) (Sandimmun Optoral) was introduced in the mid-1990s, it became clear that this new formulation improves the oral bioavailability of CsA and has a positive influence on its pharmacokinetic variability. Previous studies with the original CsA formulation (Sandimmun) showed that the size of the emulsion droplets and concomitant food intake has an effect on the absorption of CsA from the small intestine when orally administered. It was suggested that these effects might have an influence on the drugs' pharmacokinetic parameters. In this study, we focused on the two above-mentioned aspects and compared the first and second generations of CsA products (Sandimmun, Sandimmun Optoral) to generic CsA formulations by analyzing the contents of cyclosporine A gel capsules with respect to their emulsion droplet and micelle sizes using photon correlation spectroscopy (PCS). We tried to discern any differences in droplet size between different generations of CsA formulations, primarily the second and third generation, through simple physical tests. Because a high fat content food may influence the absorption of CsA, we also determined the distribution of CsA between hydrophilic and lipophilic phases using high-performance liquid chromatography analysis. It became clear that when compared under simple physical conditions, established cyclosporine formulations and new generic products show significant differences in droplet size and distribution between an aqueous phase and a high fat content food. Whether these differences are of clinical relevance remains to be investigated.

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Drug Delivery Systems for Cyclosporine: Achievements and Complications

Klyashchitsky

Owen

1998

Journal of Drug Targeting

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The review deals with the preparation, properties, and analysis of different kinds of cyclosporine delivery systems, such as solid formulations, liposomes, emulsions and microemulsions and targeted cyclosporine formulations. The review points out a key role of delivery systems in increasing the therapeutic effectiveness of cyclosporine. Comparative studies of the prior marketed formulation, Sandimmune, with a new microemulsion formulation, Neoral, are discussed including some data on clinical development of Neoral.

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In vitro study of cyclosporin absorption: Vehicles and intestinal immaturity

Cited by 3 publications

References 23 publications

Chitosan Formulations as Carriers for Therapeutic Proteins

Chitosan Formulations as Carriers for Therapeutic Proteins

Three Generations of Cyclosporine A Formulations: An In Vitro Comparison

Drug Delivery Systems for Cyclosporine: Achievements and Complications

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