Oral administration of liposomes containing cyclosporine: a pharmacokinetic study

Al‐Meshal, M. A.; Khidr, S. H.; Bayomi, Mohsen A.; Al‐Angary, A. A.

doi:10.1016/s0378-5173(98)00066-0

Cited by 46 publications

(33 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…29 The EE of CsA in proliposomes is mainly dependent on the amount of cholesterol present. 30,31 Similar results with a high EE percentage of CsA in proliposomes have been reported in previous studies. 2,7,20,32 Dsc analysis of proliposomes DSC studies were performed to evaluate the physical state of the drug in the formulation and to analyze the thermal properties of the drug.…”

Section: Yield and Ee Of Proliposomessupporting

confidence: 77%

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

Karn¹,

Jin²,

Lee³

et al. 2014

IJN

View full text Add to dashboard Cite

Objectives The objectives of this study were to prepare cyclosporin A (CsA)-containing proliposomes using the supercritical antisolvent (SAS) process and the conventional thin film method for the comparative study of proliposomal formulations and to evaluate the physicochemical properties of these proliposomes. Methods CsA-containing proliposomes were prepared by the SAS process and the conventional film method, composed of natural and synthetic phospholipids. We investigated particle size, polydispersity index, and zeta potential of CsA-containing proliposomes. In addition, both production yield and entrapment efficiency of CsA in different proliposomes were analyzed. Physicochemical properties of CsA-containing proliposomes were also evaluated, using differential scanning calorimetry and X-ray diffraction. The morphology and size of CsA-containing proliposomes were confirmed, using scanning electron microscopy. We checked the in vitro release of CsA from CsA-containing proliposomes prepared by different preparation methods, comparing them with Restasis ® as a positive control and the stability of SAS-mediated proliposomes was also studied. Results CsA-containing proliposomes formed by the SAS process had a relatively smaller particle size, with a narrow size distribution and spherical particles compared with those of conventionally prepared proliposomes. The yield and entrapment efficiency of CsA in all proliposomes varied from 85% to 92% and from 86% to 89%, respectively. Differential scanning calorimetry and X-ray diffraction studies revealed that the anhydrous lactose powder used in this formulation retained its crystalline form and that CsA was present in an amorphous form. Proliposome powders were rapidly converted to liposomes on contact with water. The in vitro release study of proliposomal formulations demonstrated a similar pattern to Restasis ® . The SAS-mediated CsA-containing proliposomes were stable on storage, with no significant changes in particle size, polydispersity index, and entrapment efficiency. Conclusion These results show promising features of CsA-containing proliposomal formulations, using the SAS process for the large-scale industrial application.

show abstract

Section: Yield and Ee Of Proliposomessupporting

confidence: 77%

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

Karn¹,

Jin²,

Lee³

et al. 2014

IJN

View full text Add to dashboard Cite

show abstract

“…8 Over the past two decades, a number of studies [9][10][11][12][13][14][15] have examined the potential application of liposomes as carriers for CsA. However, these studies are restricted to only smallscale manufacture of liposomal CsA.…”

Section: Introductionmentioning

confidence: 99%

Characterization and stability studies of a novel liposomal cyclosporin A prepared using the supercritical fluid method: comparison with the modified conventional Bangham method

Karn

Cho

Park

et al. 2013

IJN

View full text Add to dashboard Cite

Abstract:A novel method to prepare cyclosporin A encapsulated liposomes was introduced using supercritical fluid of carbon dioxide (SCF-CO 2 ) as an antisolvent. To investigate the strength of the newly developed SCF-CO 2 method compared with the modified conventional Bangham method, particle size, zeta potential, and polydispersity index (PDI) of both liposomal formulations were characterized and compared. In addition, entrapment efficiency (EE) and drug loading (DL) characteristics were analyzed by reversed-phase high-performance liquid chromatography. Significantly larger particle size and PDI were revealed from the conventional method, while EE (%) and DL (%) did not exhibit any significant differences. The SCF-CO 2 liposomes were found to be relatively smaller, multilamellar, and spherical with a smoother surface as determined by transmission electron microscopy. SCF-CO 2 liposomes showed no significant differences in their particle size and PDI after more than 3 months, whereas conventional liposomes exhibited significant changes in their particle size. The initial yield (%), EE (%), and DL (%) of SCF-CO 2 liposomes and conventional liposomes were 90.98 ± 2.94, 92.20 ± 1.36, 20.99 ± 0.84 and 90.72 ± 2.83, 90.24 ± 1.37, 20.47 ± 0.94, respectively, which changed after 14 weeks to 86.65 ± 0.30, 87.63 ± 0.72, 18.98 ± 0.22 and 75.04 ± 8.80, 84.59 ± 5.13, 15.94 ± 2.80, respectively. Therefore, the newly developed SCF-CO 2 method could be a better alternative compared with the conventional method and may provide a promising approach for large-scale production of liposomes.

show abstract

“…Liposomal CsA was reported to be preferably absorbed by Peyer's patches following oral administration [53]. It was shown that such formulations may exhibit both bioequivalence with microemulsions [54,55] and diminished inter-individual variations in bioavailability [56]. The problem of the poor shelf-life stability of liposomal CsA formulations can be overcome via the preparation of a dry proliposome powder [55].…”

Section: Systems For the Oral Delivery Of Cyclosporine Amentioning

confidence: 99%

Oral cyclosporine A - the current picture of its liposomal and other delivery systems

Czogalla¹

2009

Cellular and Molecular Biology Letters

View full text Add to dashboard Cite

Abstract:The discovery of cyclosporine A was a milestone in organ transplantation and the treatment of autoimmune diseases. However, developing an efficient oral delivery system for this drug is complicated by its poor biopharmaceutical characteristics (low solubility and permeability) and the need to carefully monitor its levels in the blood. Current research is exploring various approaches, including those based on emulsions, microspheres, nanoparticles, and liposomes. Although progress has been made, none of the formulations is flawless. This review is a brief description of the main pharmaceutical systems and devices that have been described for the oral delivery of cyclosporine A in the context of the physicochemical properties of the drug and the character of its interactions with lipid membranes.

show abstract

Oral administration of liposomes containing cyclosporine: a pharmacokinetic study

Cited by 46 publications

References 18 publications

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

Characterization and stability studies of a novel liposomal cyclosporin A prepared using the supercritical fluid method: comparison with the modified conventional Bangham method

Oral cyclosporine A - the current picture of its liposomal and other delivery systems

Contact Info

Product

Resources

About

Oral administration of liposomes containing cyclosporine: a pharmacokinetic study

Cited by 46 publications

References 18 publications

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of&nbsp;the supercritical antisolvent process with the conventional film method

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of&nbsp;the supercritical antisolvent process with the conventional film method

Characterization and stability studies of a novel liposomal cyclosporin A prepared using the supercritical fluid method: comparison with the modified conventional Bangham method

Oral cyclosporine A - the current picture of its liposomal and other delivery systems

Contact Info

Product

Resources

About

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method