Formation of highly structured cubic micellar lipid nanoparticles of soy phosphatidylcholine and glycerol dioleate and their degradation by triacylglycerol lipase
(2014) In ACS Applied Materials and Interfaces 6(10). p.7063-7069- Abstract
- Lipid nanoparticles of reversed internal phase structures, such as cubic micellar (I2) structure show good drug loading ability of peptides and proteins as well as some small molecules. Due to their controllable small size and inner morphology, such nanoparticles are suitable for drug delivery using several different administration routes, including intravenous, intramuscular and subcutaneous injection. A very interesting system in this regard, is the two component soy phosphatidylcholine (SPC)/glycerol dioleate (GDO) system, which depending on the ratio of the lipid components form a range of reversed liquid crystalline phases. For a 50/50 (wt/wt) ratio in excess water, these lipids have been shown to form a reversed cubic micellar (I2)... (More)
- Lipid nanoparticles of reversed internal phase structures, such as cubic micellar (I2) structure show good drug loading ability of peptides and proteins as well as some small molecules. Due to their controllable small size and inner morphology, such nanoparticles are suitable for drug delivery using several different administration routes, including intravenous, intramuscular and subcutaneous injection. A very interesting system in this regard, is the two component soy phosphatidylcholine (SPC)/glycerol dioleate (GDO) system, which depending on the ratio of the lipid components form a range of reversed liquid crystalline phases. For a 50/50 (wt/wt) ratio in excess water, these lipids have been shown to form a reversed cubic micellar (I2) phase of the Fd3m structure. Here we demonstrate that this SPC/GDO phase, in the presence of small quantities (5-10 wt%) of Polysorbate 80 (P80), can be dispersed into nanoparticles, still with well-defined Fd3m structure. The resulting nanoparticle dispersion has a narrow size distribution and exhibit good long-term stability. In pharmaceutical applications, biodegradation pathways of the drug delivery vehicles and their components are important considerations. In the second part of the study we show how the structure of the particles evolves during exposure to a triacylglycerol lipase (TGL) under physiological-like temperature and pH. TGL catalyses the lipolytic degradation of acylglycerides, such as GDO, to monoglycerides, glycerol and free fatty acids. During the degradation, the interior phase of the particles is shown to undergo continuous phase transitions from the reversed I2 structure to structures of less negative curvature (2D hexagonal, bicontinuous cubic and sponge), ultimately resulting in the formation of multi-lamellar vesicles. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/4436066
- author
- Wadsäter, Maria LU ; Barauskas, Justas ; Nylander, Tommy LU and Tiberg, Fredrik LU
- organization
- publishing date
- 2014
- type
- Contribution to journal
- publication status
- published
- subject
- in
- ACS Applied Materials and Interfaces
- volume
- 6
- issue
- 10
- pages
- 7063 - 7069
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- pmid:24779728
- wos:000336639200012
- scopus:84901649928
- pmid:24779728
- ISSN
- 1944-8244
- DOI
- 10.1021/am501489e
- language
- English
- LU publication?
- yes
- id
- 50914abc-1fe7-4553-9299-c6480021ff27 (old id 4436066)
- date added to LUP
- 2016-04-01 10:47:34
- date last changed
- 2023-11-10 05:35:46
@article{50914abc-1fe7-4553-9299-c6480021ff27,
abstract = {{Lipid nanoparticles of reversed internal phase structures, such as cubic micellar (I2) structure show good drug loading ability of peptides and proteins as well as some small molecules. Due to their controllable small size and inner morphology, such nanoparticles are suitable for drug delivery using several different administration routes, including intravenous, intramuscular and subcutaneous injection. A very interesting system in this regard, is the two component soy phosphatidylcholine (SPC)/glycerol dioleate (GDO) system, which depending on the ratio of the lipid components form a range of reversed liquid crystalline phases. For a 50/50 (wt/wt) ratio in excess water, these lipids have been shown to form a reversed cubic micellar (I2) phase of the Fd3m structure. Here we demonstrate that this SPC/GDO phase, in the presence of small quantities (5-10 wt%) of Polysorbate 80 (P80), can be dispersed into nanoparticles, still with well-defined Fd3m structure. The resulting nanoparticle dispersion has a narrow size distribution and exhibit good long-term stability. In pharmaceutical applications, biodegradation pathways of the drug delivery vehicles and their components are important considerations. In the second part of the study we show how the structure of the particles evolves during exposure to a triacylglycerol lipase (TGL) under physiological-like temperature and pH. TGL catalyses the lipolytic degradation of acylglycerides, such as GDO, to monoglycerides, glycerol and free fatty acids. During the degradation, the interior phase of the particles is shown to undergo continuous phase transitions from the reversed I2 structure to structures of less negative curvature (2D hexagonal, bicontinuous cubic and sponge), ultimately resulting in the formation of multi-lamellar vesicles.}},
author = {{Wadsäter, Maria and Barauskas, Justas and Nylander, Tommy and Tiberg, Fredrik}},
issn = {{1944-8244}},
language = {{eng}},
number = {{10}},
pages = {{7063--7069}},
publisher = {{The American Chemical Society (ACS)}},
series = {{ACS Applied Materials and Interfaces}},
title = {{Formation of highly structured cubic micellar lipid nanoparticles of soy phosphatidylcholine and glycerol dioleate and their degradation by triacylglycerol lipase}},
url = {{http://dx.doi.org/10.1021/am501489e}},
doi = {{10.1021/am501489e}},
volume = {{6}},
year = {{2014}},
}