The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes
Purpose: The major limitation in the widespread use of liposome drug delivery system is its instability. Lyophilization is a promising approach to ensure the long-term stability of liposomes. The aim of this study was to prepare sirolimus-loaded liposomes, study their stability and investigate the e...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Tabriz University of Medical Sciences
2013-02-01
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| Series: | Advanced Pharmaceutical Bulletin |
| Subjects: | |
| Online Access: | http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-3-25.pdf |
| _version_ | 1818552737699201024 |
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| author | Parvin Zakeri-Milani Hadi Valizadeh Saeed Ghanbarzadeh |
| author_facet | Parvin Zakeri-Milani Hadi Valizadeh Saeed Ghanbarzadeh |
| author_sort | Parvin Zakeri-Milani |
| collection | DOAJ |
| description | Purpose: The major limitation in the widespread use of liposome drug delivery system is its instability. Lyophilization is a promising approach to ensure the long-term stability of liposomes. The aim of this study was to prepare sirolimus-loaded liposomes, study their stability and investigate the effect of lyophilization either in the presence or in the absence of lyoprotectant on liposome properties. Methods: Two types of multi-lamellar liposomes, conventional and fusogenic, containing sirolimus were prepared by modified thin film hydration method with different ratio of dipalmitoylphosphatidylcholine (DPPC), cholesterol and dioleoylphosphoethanolamine (DOPE), and were lyophilized with or without dextrose as lyoprotectant. Chemical stability investigation was performed at 4°C and 25°C until 6 months using a validated HPLC method. Physical stability was studied with determination of particle size (PS) and encapsulation efficiency (EE %) of formulations through 6 months. Results: Chemical stability test at 4°C and 25°C until 6 months showed that drug content of liposomes decreased 8.4% and 20.2% respectively. Initial mean EE % and PS were 72.8 % and 582 nm respectively. After 6 months mean EE % for suspended form, lyophilized without lyoprotectant and lyophilized with lyoprotectant were 54.8 %, 62.3% and 67.1 % at 4°C and 48.2%, 60.4 % and 66.8 % at 25°C respectively. Corresponding data for mean PS were 8229 nm, 2397 nm and 688nm at 4°C and 9362 nm, 1944 nm and 737 nm at 25°C respectively. Conclusion: It is concluded that lyophilization with and without dextrose could increase shelf life of liposome and dextrose has lyoprotectant effect that stabilized liposomes in the lyophilization process. |
| first_indexed | 2024-12-12T09:17:05Z |
| format | Article |
| id | doaj.art-3c3a78091b8a4cc2a506784781a58061 |
| institution | Directory Open Access Journal |
| issn | 2228-5881 2251-7308 |
| language | English |
| last_indexed | 2024-12-12T09:17:05Z |
| publishDate | 2013-02-01 |
| publisher | Tabriz University of Medical Sciences |
| record_format | Article |
| series | Advanced Pharmaceutical Bulletin |
| spelling | doaj.art-3c3a78091b8a4cc2a506784781a580612022-12-22T00:29:20ZengTabriz University of Medical SciencesAdvanced Pharmaceutical Bulletin2228-58812251-73082013-02-0131252910.5681/apb.2013.005The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus LiposomesParvin Zakeri-MilaniHadi ValizadehSaeed GhanbarzadehPurpose: The major limitation in the widespread use of liposome drug delivery system is its instability. Lyophilization is a promising approach to ensure the long-term stability of liposomes. The aim of this study was to prepare sirolimus-loaded liposomes, study their stability and investigate the effect of lyophilization either in the presence or in the absence of lyoprotectant on liposome properties. Methods: Two types of multi-lamellar liposomes, conventional and fusogenic, containing sirolimus were prepared by modified thin film hydration method with different ratio of dipalmitoylphosphatidylcholine (DPPC), cholesterol and dioleoylphosphoethanolamine (DOPE), and were lyophilized with or without dextrose as lyoprotectant. Chemical stability investigation was performed at 4°C and 25°C until 6 months using a validated HPLC method. Physical stability was studied with determination of particle size (PS) and encapsulation efficiency (EE %) of formulations through 6 months. Results: Chemical stability test at 4°C and 25°C until 6 months showed that drug content of liposomes decreased 8.4% and 20.2% respectively. Initial mean EE % and PS were 72.8 % and 582 nm respectively. After 6 months mean EE % for suspended form, lyophilized without lyoprotectant and lyophilized with lyoprotectant were 54.8 %, 62.3% and 67.1 % at 4°C and 48.2%, 60.4 % and 66.8 % at 25°C respectively. Corresponding data for mean PS were 8229 nm, 2397 nm and 688nm at 4°C and 9362 nm, 1944 nm and 737 nm at 25°C respectively. Conclusion: It is concluded that lyophilization with and without dextrose could increase shelf life of liposome and dextrose has lyoprotectant effect that stabilized liposomes in the lyophilization process.http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-3-25.pdfLiposomeSirolimusLyophilizationStability |
| spellingShingle | Parvin Zakeri-Milani Hadi Valizadeh Saeed Ghanbarzadeh The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes Advanced Pharmaceutical Bulletin Liposome Sirolimus Lyophilization Stability |
| title | The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes |
| title_full | The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes |
| title_fullStr | The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes |
| title_full_unstemmed | The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes |
| title_short | The Effects of Lyophilization on the Physico-Chemical Stability of Sirolimus Liposomes |
| title_sort | effects of lyophilization on the physico chemical stability of sirolimus liposomes |
| topic | Liposome Sirolimus Lyophilization Stability |
| url | http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-3-25.pdf |
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