Proliposome powders prepared using a slurry method for the generation of beclometasone dipropionate liposomes

Khan, I., Yousaf, S., Subramanian, S. , Korale, O., Alhnan, M. A., Ahmed, W., Taylor, K. M. G. and Elhissi, A. (2015) Proliposome powders prepared using a slurry method for the generation of beclometasone dipropionate liposomes. International Journal of Pharmaceutics, 496 (2). pp. 342-350. ISSN 0378-5173

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Item Type:Article
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A novel "slurry method" was described for the preparation of proliposome powders using soya phosphatidylcholine (SPC) with cholesterol (1:1) and for incorporation of beclometasone dipropionate (BDP) at 2 mole of the total lipid phase. Proliposomes made with a range of lipid to sucrose carrier ratios were studied in terms of surface morphology using scanning electron microscopy (SEM) and thermal properties using differential scanning calorimetry (DSC). Following hydration of proliposomes, the resultant vesicles were compared to liposomes made using the traditional proliposome method, in terms of vesicle size and drug entrapment efficiency. SEM showed that sucrose was uniformly coated with lipid regardless of lipid to carrier ratio. Liposomes generated using the slurry proliposome method tended to have smaller median size than those generated with the conventional proliposome method, being in the range of 4.72-5.20 μm and 5.89-7.72 μm respectively. Following centrifugation of liposomes using deuterium oxide (D2O) as dispersion medium, vesicles entrapping BDP were separated as a floating creamy layer, whilst the free drug was sedimented as crystals. Drug entrapment was dependent on formulation composition and preparation method. When 1:15 w/w lipid to carrier was used, liposomes generated using the slurry method had an entrapment efficiency of 47.05 compared to 18.67 for those generated using the conventional proliposome method. By contrast, liposomes made by the thin-film hydration method had an entrapment efficiency of 25.66. DSC studies using 50 mole BDP demonstrated that the drug was amorphous in the proliposome formulation and tended to crystallize on hydration, resulting in low drug entrapment. In conclusion, a novel approach to the preparation of proliposomes using a slurry method has been introduced, offering higher entrapment for BDP than liposomes made using the conventional proliposome method and those prepared by thin-film hydration technique. © 2015 Elsevier B.V. All rights reserved.

Keywords:beclometasone dipropionate, deuterium oxide, lipid, liposome, proliposome, sucrose, unclassified drug, beclometasone, powder, prodrug, analytic method, Article, crystal, differential scanning calorimetry, dispersion, morphology, priority journal, scanning electron microscopy, slurry method, surface property, thermal analysis, high performance liquid chromatography, medicinal chemistry, procedures, synthesis, Beclomethasone, Chemistry, Pharmaceutical, Chromatography, High Pressure Liquid, Liposomes, Microscopy, Electron, Scanning, Powders, Prodrugs, NotOAChecked
Subjects:F Physical Sciences > F200 Materials Science
J Technologies > J510 Materials Technology
Divisions:College of Science > School of Mathematics and Physics
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ID Code:27112
Deposited On:20 Jun 2017 16:56

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