Cyclodextrin as membrane protectant in spray-drying and freeze-drying of PEGylated liposomes

J.M. van den Hoven, Josbert Maarten Metselaar, Gerrit Storm, J.H. Beijnen, B. Nuijen

Research output: Contribution to journalArticleAcademicpeer-review

30 Citations (Scopus)

Abstract

Abstract In this study it was investigated whether hydroxypropyl-β-cyclodextrin (HPβCD) is able to stabilize the liposomal membranes during drying of long circulating polyethylene glycol (PEG) coated liposomes, as compared to the disaccharides trehalose and sucrose. PEGylated liposomes loaded with prednisolone disodium phosphate (PLP) were dried by spray-drying or freeze-drying. The dried powders were tested on their residual moisture content, glass transition temperature and amorphous character. Upon reconstitution the liposomal size, size distribution and drug retention were determined and the results were compared to the characteristics of the formulation solution before drying. In contrast to the disaccharides, HPβCD stabilizes the liposomal membranes of the PEGylated liposomes during the drying process of both spray drying and freeze-drying when present in a lipid:carbohydrate ratio of 1:6 (w/w). The resulting powder can be stored at room temperature. No changes in size and size distribution were seen upon reconstitution of the HPβCD containing formulations. Drying resulted in a minimal leaking of PLP from the liposomes. Its relatively high [Formula: see text] and T(g) of HPβCD, as compared to the disaccharides, make HPβCD an excellent membrane protectant for dry PEGylated liposomal formulations.
Original languageEnglish
Pages (from-to)209-216
Number of pages8
JournalInternational journal of pharmaceutics
Volume438
Issue number1-2
DOIs
Publication statusPublished - 2012

Fingerprint

Freeze Drying
Cyclodextrins
Liposomes
Disaccharides
Membranes
Powders
Trehalose
Transition Temperature
Glass
Sucrose
Carbohydrates
Lipids
Temperature
Pharmaceutical Preparations

Keywords

  • METIS-292663
  • IR-83079

Cite this

van den Hoven, J.M. ; Metselaar, Josbert Maarten ; Storm, Gerrit ; Beijnen, J.H. ; Nuijen, B. / Cyclodextrin as membrane protectant in spray-drying and freeze-drying of PEGylated liposomes. In: International journal of pharmaceutics. 2012 ; Vol. 438, No. 1-2. pp. 209-216.
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abstract = "Abstract In this study it was investigated whether hydroxypropyl-β-cyclodextrin (HPβCD) is able to stabilize the liposomal membranes during drying of long circulating polyethylene glycol (PEG) coated liposomes, as compared to the disaccharides trehalose and sucrose. PEGylated liposomes loaded with prednisolone disodium phosphate (PLP) were dried by spray-drying or freeze-drying. The dried powders were tested on their residual moisture content, glass transition temperature and amorphous character. Upon reconstitution the liposomal size, size distribution and drug retention were determined and the results were compared to the characteristics of the formulation solution before drying. In contrast to the disaccharides, HPβCD stabilizes the liposomal membranes of the PEGylated liposomes during the drying process of both spray drying and freeze-drying when present in a lipid:carbohydrate ratio of 1:6 (w/w). The resulting powder can be stored at room temperature. No changes in size and size distribution were seen upon reconstitution of the HPβCD containing formulations. Drying resulted in a minimal leaking of PLP from the liposomes. Its relatively high [Formula: see text] and T(g) of HPβCD, as compared to the disaccharides, make HPβCD an excellent membrane protectant for dry PEGylated liposomal formulations.",
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Cyclodextrin as membrane protectant in spray-drying and freeze-drying of PEGylated liposomes. / van den Hoven, J.M.; Metselaar, Josbert Maarten; Storm, Gerrit; Beijnen, J.H.; Nuijen, B.

In: International journal of pharmaceutics, Vol. 438, No. 1-2, 2012, p. 209-216.

Research output: Contribution to journalArticleAcademicpeer-review

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T1 - Cyclodextrin as membrane protectant in spray-drying and freeze-drying of PEGylated liposomes

AU - van den Hoven, J.M.

AU - Metselaar, Josbert Maarten

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AU - Nuijen, B.

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N2 - Abstract In this study it was investigated whether hydroxypropyl-β-cyclodextrin (HPβCD) is able to stabilize the liposomal membranes during drying of long circulating polyethylene glycol (PEG) coated liposomes, as compared to the disaccharides trehalose and sucrose. PEGylated liposomes loaded with prednisolone disodium phosphate (PLP) were dried by spray-drying or freeze-drying. The dried powders were tested on their residual moisture content, glass transition temperature and amorphous character. Upon reconstitution the liposomal size, size distribution and drug retention were determined and the results were compared to the characteristics of the formulation solution before drying. In contrast to the disaccharides, HPβCD stabilizes the liposomal membranes of the PEGylated liposomes during the drying process of both spray drying and freeze-drying when present in a lipid:carbohydrate ratio of 1:6 (w/w). The resulting powder can be stored at room temperature. No changes in size and size distribution were seen upon reconstitution of the HPβCD containing formulations. Drying resulted in a minimal leaking of PLP from the liposomes. Its relatively high [Formula: see text] and T(g) of HPβCD, as compared to the disaccharides, make HPβCD an excellent membrane protectant for dry PEGylated liposomal formulations.

AB - Abstract In this study it was investigated whether hydroxypropyl-β-cyclodextrin (HPβCD) is able to stabilize the liposomal membranes during drying of long circulating polyethylene glycol (PEG) coated liposomes, as compared to the disaccharides trehalose and sucrose. PEGylated liposomes loaded with prednisolone disodium phosphate (PLP) were dried by spray-drying or freeze-drying. The dried powders were tested on their residual moisture content, glass transition temperature and amorphous character. Upon reconstitution the liposomal size, size distribution and drug retention were determined and the results were compared to the characteristics of the formulation solution before drying. In contrast to the disaccharides, HPβCD stabilizes the liposomal membranes of the PEGylated liposomes during the drying process of both spray drying and freeze-drying when present in a lipid:carbohydrate ratio of 1:6 (w/w). The resulting powder can be stored at room temperature. No changes in size and size distribution were seen upon reconstitution of the HPβCD containing formulations. Drying resulted in a minimal leaking of PLP from the liposomes. Its relatively high [Formula: see text] and T(g) of HPβCD, as compared to the disaccharides, make HPβCD an excellent membrane protectant for dry PEGylated liposomal formulations.

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