The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake

Wei-Kuo Chang1, Yu-Ju Tai2, Chiao-Hsi Chiang3, Chieh-Shen Hu2, Po-Da Hong2, Ming-Kung Yeh3,4 1Division of Gastroenterology, Department of Internal Medicine, Tri-Service General Hospital, National Defense Medical Center, Taiwan, ROC; 2Graduate Institute of Engineering, National Taiwan University of S...

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Autores principales:	Chang WK, Tai YJ, Chiang CH, Hu CS, Hong PD, Yeh MK
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/3ac202b631ef4ea78fba827279747ed2
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spelling	oai:doaj.org-article:3ac202b631ef4ea78fba827279747ed22021-12-02T08:07:45ZThe comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake1176-91141178-2013https://doaj.org/article/3ac202b631ef4ea78fba827279747ed22011-10-01T00:00:00Zhttp://www.dovepress.com/the-comparison-of-protein-entrapped-liposomes-and-lipoparticles-prepar-a8525https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Wei-Kuo Chang1, Yu-Ju Tai2, Chiao-Hsi Chiang3, Chieh-Shen Hu2, Po-Da Hong2, Ming-Kung Yeh3,4 1Division of Gastroenterology, Department of Internal Medicine, Tri-Service General Hospital, National Defense Medical Center, Taiwan, ROC; 2Graduate Institute of Engineering, National Taiwan University of Science and Technology, Taipei, Taiwan, ROC; 3School of Pharmacy, National Defense Medical Center, Taipei, Taiwan, ROC; 4Institute of Preventive Medicine, National Defense Medical Center, Sanhsia, Taipei, Taiwan, ROC Abstract: Fluorescein isothiocyanate-conjugated bovine serum albumin (FITC-BSA)-loaded polyethylene glycol (PEG)-modified liposomes and lipoparticles with high protein entrapment were developed. The lipid formula of the liposomes contained PEGylated lipids and unsaturated fatty acids for enhancing membrane fluidity and effective delivery into cells. The preparation techniques, lipid content, and PEG-modified lipoparticle ratios were evaluated. The PEG-modified lipoparticles prepared by ethanol injection extrusion (100 nm pore size) achieve a population of blank liposomes with a mean size of 125 &plusmn; 2.3 nm and a zeta potential of &mdash;12.4 &plusmn; 1.5 mV. The average particle size of the PEG-modified lipoparticles was 133.7 &plusmn; 8.6 nm with a zeta potential of +13.3 mV. Lipoparticle conformation was determined using transmission electron microscopy and field-emission scanning electron microscopy. The FITC-BSA encapsulation efficiency was dramatically increased from 19.0% for liposomes to 59.7% for lipoparticles. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) results confirmed the preparation process, and an 8-hour leaching test did not harm the protein structure. Once prepared, the physical and chemical stability of the PEG-modified lipoparticle formulations was satisfactory over 90 days. In vitro retention tests indicated that the 50% retention time for the protein-containing lipoparticles was 7.9 hours, substantially longer than the liposomes at 3.3 hours. A Caco-2 cell model was used for evaluating the cytotoxicity and cell uptake efficiency of the PEG-modified lipoparticles. At a lipid content below 0.25 mM, neither the liposomes nor the lipoparticles caused significant cellular cytotoxicity (P &lt; 0.01) and FITC-BSA was significantly taken up into cells within 60 minutes (P &lt; 0.01). Keywords: liposomes, lipoparticles, formulation, protein, stabilityChang WKTai YJChiang CHHu CSHong PDYeh MKDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 2403-2417 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Chang WK Tai YJ Chiang CH Hu CS Hong PD Yeh MK The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
description	Wei-Kuo Chang1, Yu-Ju Tai2, Chiao-Hsi Chiang3, Chieh-Shen Hu2, Po-Da Hong2, Ming-Kung Yeh3,4 1Division of Gastroenterology, Department of Internal Medicine, Tri-Service General Hospital, National Defense Medical Center, Taiwan, ROC; 2Graduate Institute of Engineering, National Taiwan University of Science and Technology, Taipei, Taiwan, ROC; 3School of Pharmacy, National Defense Medical Center, Taipei, Taiwan, ROC; 4Institute of Preventive Medicine, National Defense Medical Center, Sanhsia, Taipei, Taiwan, ROC Abstract: Fluorescein isothiocyanate-conjugated bovine serum albumin (FITC-BSA)-loaded polyethylene glycol (PEG)-modified liposomes and lipoparticles with high protein entrapment were developed. The lipid formula of the liposomes contained PEGylated lipids and unsaturated fatty acids for enhancing membrane fluidity and effective delivery into cells. The preparation techniques, lipid content, and PEG-modified lipoparticle ratios were evaluated. The PEG-modified lipoparticles prepared by ethanol injection extrusion (100 nm pore size) achieve a population of blank liposomes with a mean size of 125 &plusmn; 2.3 nm and a zeta potential of &mdash;12.4 &plusmn; 1.5 mV. The average particle size of the PEG-modified lipoparticles was 133.7 &plusmn; 8.6 nm with a zeta potential of +13.3 mV. Lipoparticle conformation was determined using transmission electron microscopy and field-emission scanning electron microscopy. The FITC-BSA encapsulation efficiency was dramatically increased from 19.0% for liposomes to 59.7% for lipoparticles. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) results confirmed the preparation process, and an 8-hour leaching test did not harm the protein structure. Once prepared, the physical and chemical stability of the PEG-modified lipoparticle formulations was satisfactory over 90 days. In vitro retention tests indicated that the 50% retention time for the protein-containing lipoparticles was 7.9 hours, substantially longer than the liposomes at 3.3 hours. A Caco-2 cell model was used for evaluating the cytotoxicity and cell uptake efficiency of the PEG-modified lipoparticles. At a lipid content below 0.25 mM, neither the liposomes nor the lipoparticles caused significant cellular cytotoxicity (P &lt; 0.01) and FITC-BSA was significantly taken up into cells within 60 minutes (P &lt; 0.01). Keywords: liposomes, lipoparticles, formulation, protein, stability
format	article
author	Chang WK Tai YJ Chiang CH Hu CS Hong PD Yeh MK
author_facet	Chang WK Tai YJ Chiang CH Hu CS Hong PD Yeh MK
author_sort	Chang WK
title	The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
title_short	The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
title_full	The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
title_fullStr	The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
title_full_unstemmed	The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
title_sort	comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/3ac202b631ef4ea78fba827279747ed2
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The comparison of protein-entrapped liposomes and lipoparticles: preparation, characterization, and efficacy of cellular uptake

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