Characterization, stability and in vivo targeting of liposomal formulations containing cyclosporin

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

doi:10.1016/0378-5173(94)00243-x

Cited by 26 publications

(16 citation statements)

References 13 publications

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“…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

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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.

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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

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“…[2][3][4]45 Liposomes are also relatively non-toxic and biodegradable. 46 They therefore have a wide range of biomedical applications.…”

Section: Biomedical Applications Of Liposomesmentioning

confidence: 99%

“…The preferential distribution of liposomes into the RES can be modified by the incorporation in the liposome membrane of protein or carbohydrates possessing specific affinity toward a target tissue or organ. 45,53,54 A ligand selection is based on its recognition by, and specificity for, the target site. In cancer treatment, for example, one of the approaches is to target the drug to tumour cells via receptor specific ligands, which may be specific antibodies for antigens produced by the tumour cells.…”

Section: Drug Targetingmentioning

confidence: 99%

Current trends in the production and biomedical applications of liposomes: a review

Uhumwangho¹,

Okor²

2009

Journal of Medicine and Biomedical Research

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A review of literature was carried out to determine methods of production of liposomes, their stability, biodistribution and their uses as drug delivery systems. The conventional method of preparing liposomes is basically for the multilamellar vesicles (MLVs). However, other methods are used to reduce the size of these MLVs to small unilamellar vesicles (SUVs) so as to increase their plasma lifetime and consequently increase the possibility of achieving greater tissue localisation. Some of these methods of size reduction are sonication and high pressure extrusion. Each of these methods has its own advantages and disadvantages. Large unilamellar vesicles (LUVs), on the other hand, are prepared mainly by detergent removal method and reverse phase extrusion technique. There are also improved pharmacokinetic properties with liposomal drugs compared to free drugs, though some formulation factors affect the release kinetics of the liposomal drugs. The review also shows that liposomes have a lot of biomedical applications and uses. They have been used in drug targeting, oral delivery of vaccines, insulins, peptides and some compounds, which are usually degraded in the gastrointestinal tract. It has also found application in topical therapy especially in the eye and lungs. Other areas of application are in cancer chemotherapy and treatment of human immunovirus (HIV) infection. The control of the stability of liposomes is an essential prerequisite for effective use as drug carriers. Leakage of the liposome is attributable mainly to differences in lamellar structure. For instance, MLVs are less prone to leakage than ULVs. The use of a combination of saturated phospholipid and cholesterol in the formulation of the liposomes has also been found to enhance stability with lower tendency to leakage.

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“…Furthermore, cholesterol, a stabilizer of liposomes in the blood, reduces the incorporation levels of the drug. Thus, a compromise must be reached between stability and maximum drug incorporation [28,39]. Finally, as a result of the significant interlamellar exchange between the carrier and cellular membranes, which makes the controlled release of CsA impossible, the drug is rapidly redistributed while the liposomes are cleared from circulation [28] …”

Section: Lipid Membranes and Cyclosporine Amentioning

confidence: 99%

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

Czogalla¹

2009

Cellular and Molecular Biology Letters

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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.

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Characterization, stability and in vivo targeting of liposomal formulations containing cyclosporin

Cited by 26 publications

References 13 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

Current trends in the production and biomedical applications of liposomes: a review

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

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Characterization, stability and in vivo targeting of liposomal formulations containing cyclosporin

Cited by 26 publications

References 13 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

Current trends in the production and biomedical applications of liposomes: a review

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

Contact Info

Product

Resources

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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