Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes

Liposomes were prepared from DPPC (dipalmitoyl phosphatidyl choline) mixed with Chol (cholesterol) and CTA [cholest-5-en-3-ol(3β)(trimethylammonio) acetate] or DDAB (dioctadecyl dimethyl ammonium bromide) at various molar ratios by chloroform film method with sonication. The most physical stable (no...

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Main Authors: Manosroi A., Khositsuntiwong N., Komno C., Manosroi W., Werner R.G., Manosoi J.
Format: Article
Language:English
Published: 2014
Online Access:http://www.ncbi.nlm.nih.gov/pubmed/3502482
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spelling th-cmuir.6653943832-73512014-08-30T04:00:52Z Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes Manosroi A. Khositsuntiwong N. Komno C. Manosroi W. Werner R.G. Manosoi J. Liposomes were prepared from DPPC (dipalmitoyl phosphatidyl choline) mixed with Chol (cholesterol) and CTA [cholest-5-en-3-ol(3β)(trimethylammonio) acetate] or DDAB (dioctadecyl dimethyl ammonium bromide) at various molar ratios by chloroform film method with sonication. The most physical stable (no sedimentation with an average zeta potential value of 47.7±1.44 mV) liposomal formulation (DPPC/CTA/DDAB at 7:2:1 molar ratio) was selected to load with human insulin (0.45 mg/mL) by the freeze dried empty liposomes (FDELs) method with the entrapment efficiency of human insulin of 62.72% (determined by gel filtration). Liposomes were spherical shape with unilamellar structure and an average size of 2.26±0.87 μm determined by TEM. The percentages of insulin remaining in liposomes when stored at 4±2, 30±2 and 45±2 °C for 4 months were 26.21, 36.86 and 15.75% which were higher than human insulin solution of 6.13, 11.31 and 2.61 times, respectively. The percentages of entrapment of human insulin were 62.72 at initial and at 31.72, 64.10 and 8.10 when kept at 4±2, 30±2 and 45±2 °C, respectively, for 4 months. The synthesized cationic lipid, CTA, and the DPPC/Chol/CTA liposomes loaded with human insulin demonstrated no cytotoxicity on normal human skin fibroblast but some cytotoxic effects on mouth epidermal cancer cell line. This study has demonstrated the enhancement of chemical stability of human insulin with no cytotoxicity when loaded this protein in cationic DPPC/CTA/DDAB liposomes. The results indicated the potential application of this cationic liposomal formulation for topical therapeutic use. Copyright © 2011 American Scientific Publishers All rights reserved. 2014-08-30T04:00:52Z 2014-08-30T04:00:52Z 2011 Article 15507033 10.1166/jbn.2011.1282 http://www.ncbi.nlm.nih.gov/pubmed/3502482 http://www.scopus.com/inward/record.url?eid=2-s2.0-79960973034&partnerID=40&md5=6b8fff7a8308b5615e03861eff340c09 http://cmuir.cmu.ac.th/handle/6653943832/7351 English
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
language English
description Liposomes were prepared from DPPC (dipalmitoyl phosphatidyl choline) mixed with Chol (cholesterol) and CTA [cholest-5-en-3-ol(3β)(trimethylammonio) acetate] or DDAB (dioctadecyl dimethyl ammonium bromide) at various molar ratios by chloroform film method with sonication. The most physical stable (no sedimentation with an average zeta potential value of 47.7±1.44 mV) liposomal formulation (DPPC/CTA/DDAB at 7:2:1 molar ratio) was selected to load with human insulin (0.45 mg/mL) by the freeze dried empty liposomes (FDELs) method with the entrapment efficiency of human insulin of 62.72% (determined by gel filtration). Liposomes were spherical shape with unilamellar structure and an average size of 2.26±0.87 μm determined by TEM. The percentages of insulin remaining in liposomes when stored at 4±2, 30±2 and 45±2 °C for 4 months were 26.21, 36.86 and 15.75% which were higher than human insulin solution of 6.13, 11.31 and 2.61 times, respectively. The percentages of entrapment of human insulin were 62.72 at initial and at 31.72, 64.10 and 8.10 when kept at 4±2, 30±2 and 45±2 °C, respectively, for 4 months. The synthesized cationic lipid, CTA, and the DPPC/Chol/CTA liposomes loaded with human insulin demonstrated no cytotoxicity on normal human skin fibroblast but some cytotoxic effects on mouth epidermal cancer cell line. This study has demonstrated the enhancement of chemical stability of human insulin with no cytotoxicity when loaded this protein in cationic DPPC/CTA/DDAB liposomes. The results indicated the potential application of this cationic liposomal formulation for topical therapeutic use. Copyright © 2011 American Scientific Publishers All rights reserved.
format Article
author Manosroi A.
Khositsuntiwong N.
Komno C.
Manosroi W.
Werner R.G.
Manosoi J.
spellingShingle Manosroi A.
Khositsuntiwong N.
Komno C.
Manosroi W.
Werner R.G.
Manosoi J.
Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
author_facet Manosroi A.
Khositsuntiwong N.
Komno C.
Manosroi W.
Werner R.G.
Manosoi J.
author_sort Manosroi A.
title Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
title_short Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
title_full Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
title_fullStr Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
title_full_unstemmed Chemical stability and cytotoxicity of human insulin loaded in cationic DPPC/CTA/DDAB liposomes
title_sort chemical stability and cytotoxicity of human insulin loaded in cationic dppc/cta/ddab liposomes
publishDate 2014
url http://www.ncbi.nlm.nih.gov/pubmed/3502482
http://www.scopus.com/inward/record.url?eid=2-s2.0-79960973034&partnerID=40&md5=6b8fff7a8308b5615e03861eff340c09
http://cmuir.cmu.ac.th/handle/6653943832/7351
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