TY - JOUR
T1 - Drug solubilisation in lipid nanoparticles containing high melting point triglycerides
AU - Wasutrasawat, Prawarisa
AU - Al-Obaidi, Hisham
AU - Gaisford, Simon
AU - Lawrence, M. Jayne
AU - Warisnoicharoen, Warangkana
PY - 2013/11
Y1 - 2013/11
N2 - The effect of lipid (either the triglyceride trilaurin or tripalmitin, melting points of 43 and 64 C, respectively) on the properties of lipid nanoparticles (LN) stabilised by the surfactant, polyoxyethylene-10-oleyl ether (C18:1E10) at a temperature of 22 C, has been determined. LN were prepared by heating lipid, surfactant and water to 70 C and cooling to ambient temperature with constant stirring. While lipid type influenced LN formation in that trilaurin-containing LN formed over the greatest range of compositions, phase inversion studies suggested that both lipids formed a core within the LN while light scattering studies indicated that the size of both types of LN varied with lipid concentration: in an approximately linear fashion for clear or opalescent LN and exponentially for cloudy LN. Additionally, both types of preformed LN exhibited an increase in solubilisation capacity of the hydrophobic drug, testosterone propionate compared to C18:1E 10 micelles, although the trilaurin-containing LN exhibited the greatest increase. Differential scanning calorimetry studies demonstrated that trilaurin formed a 'fluid-like' core and therefore liquefied-lipid nanoparticles, which allowed dissolution of testosterone propionate in the lipid core. In contrast, tripalmitin was present in a 'solid-like' state forming solid lipid nanoparticles which did not allow testosterone propionate dissolution in the core.
AB - The effect of lipid (either the triglyceride trilaurin or tripalmitin, melting points of 43 and 64 C, respectively) on the properties of lipid nanoparticles (LN) stabilised by the surfactant, polyoxyethylene-10-oleyl ether (C18:1E10) at a temperature of 22 C, has been determined. LN were prepared by heating lipid, surfactant and water to 70 C and cooling to ambient temperature with constant stirring. While lipid type influenced LN formation in that trilaurin-containing LN formed over the greatest range of compositions, phase inversion studies suggested that both lipids formed a core within the LN while light scattering studies indicated that the size of both types of LN varied with lipid concentration: in an approximately linear fashion for clear or opalescent LN and exponentially for cloudy LN. Additionally, both types of preformed LN exhibited an increase in solubilisation capacity of the hydrophobic drug, testosterone propionate compared to C18:1E 10 micelles, although the trilaurin-containing LN exhibited the greatest increase. Differential scanning calorimetry studies demonstrated that trilaurin formed a 'fluid-like' core and therefore liquefied-lipid nanoparticles, which allowed dissolution of testosterone propionate in the lipid core. In contrast, tripalmitin was present in a 'solid-like' state forming solid lipid nanoparticles which did not allow testosterone propionate dissolution in the core.
KW - C E
KW - Nanoparticles
KW - Polyoxyethylene-10-oleyl ether
KW - Solubilisation
KW - testosterone propionate
KW - Triglycerides
UR - http://www.scopus.com/inward/record.url?scp=84888332389&partnerID=8YFLogxK
U2 - 10.1016/j.ejpb.2013.04.020
DO - 10.1016/j.ejpb.2013.04.020
M3 - Article
C2 - 23688806
AN - SCOPUS:84888332389
SN - 0939-6411
VL - 85
SP - 365
EP - 371
JO - EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
JF - EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
IS - 3 PART A
ER -