Lipid Effects on Expulsion Rate of Amphotericin B from Solid Lipid Nanoparticles

• Published in: AAPS PharmSciTech Vol. 15; no. 2; pp. 287 - 295
• Main Authors: Tan, See Wei, Billa, Nashiru
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01.04.2014
• Subjects: Amphotericin B - chemistry; Antifungal Agents - chemistry; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Lipids - chemistry; Microscopy, Electron, Scanning; Microscopy, Electron, Scanning Transmission; Nanoparticles; Pharmacology/Toxicology; Pharmacy; Research Article; Spectrum Analysis - methods; Theobroma; lipid nanoparticles; amphotericin B; beeswax; expulsion; theobroma oil
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-013-0056-9

We aimed to investigate the effects that natural lipids, theobroma oil (TO) and beeswax (BW), might have on the physical properties of formulated nanoparticles and also the degree of expulsion of encapsulated amphotericin B (AmB) from the nanoparticles during storage. Lecithin and sodium cholate were used as emulsifiers whilst oleic acid (OA) was used to study the influence of the state of orderliness/disorderliness within the matrices of the nanoparticles on the degree of AmB expulsion during storage. BW was found to effect larger z-average diameter compared with TO. Lecithin was found to augment the stability of the nanoparticles imparted by BW and TO during storage. An encapsulation efficiency (%EE) of 59% was recorded when TO was the sole lipid as against 42% from BW. In combination however, the %EE dropped to 39%. When used as sole lipid, TO or BW formed nanoparticles with comparatively higher enthalpies, 21.1 and 23.3 J/g respectively, which subsequently caused significantly higher degree of AmB expulsion, 81 and 83% respectively, whilst only 11.8% was expelled from a binary TO/BW mixture. A tertiary TO/BW/OA mixture registered the lowest enthalpy at 8.07 J/g and expelled 12.6% of AmB but encapsulated only 22% of AmB. In conclusion, nanoparticles made from equal concentrations of TO and BW produced the most desirable properties and worthy of further investigations.