Enhanced microemulsion formation in lipid-based drug delivery systems by combining mono-esters of medium-chain fatty acids with di- or tri-esters
AbstractTo develop strategies for selecting appropriate lipids from mono-, di- and tri-esters of medium-chain fatty acids for the development of lipid-based drug delivery systems, ternary phase diagrams of propylene glycol (PG) monocaprylate (Capryol 90; HLB~7), PG dicaprylocaprate (Labrafac PG; HLB~2) and glycerol tricaprylocaprate (Labrafac Lipophile WL1349; HLB~2) were determined using a common surfactant, PEG-35 castor oil (Cremophor EL; HLB~13), and water. Particle size and viscosity in different regions of phase diagrams were measured, solubility of a model drug, danazol, in different lipid-surfactant mixtures was determined, and dispersion testing by diluting selected preconcentrates with 0.01NHCl was performed. Further, phase diagrams were constructed using binary mixtures of lipids (mono ester with diester, or monoester with triester) in place of single lipids. Phase diagrams of PG dicaprylocaprate and glycerol tricaprylocaprate were similar, while it was distinctly different for PG monocaprylate, indicating that the polarity of lipids rather than degree of esterification was the determining factor for structures of phase diagrams. The microemulsion regions in phase diagrams were rather limited for individual lipids. Additionally, di- and tri- esters showed pronounced gel regions in phase diagrams, which can influence drug release from preconcentrates. The mixing of PG monocaprylate (monoester) with PG dicaprylocaprate (diester) or glycerol tricaprylocaprate (triester) had dramatic effects on the performance of lipids as evident from greatly reduced gel phases, much bigger microemulsion regions, faster dispersion of preconcentrates in an aqueous medium, and lower particle size of microemulsions formed.
How to Cite
SERAJUDDIN, Abu T. M.. Enhanced microemulsion formation in lipid-based drug delivery systems by combining mono-esters of medium-chain fatty acids with di- or tri-esters. Journal of Excipients and Food Chemicals, [S.l.], v. 3, n. 2, p. 29-44, june 2012. ISSN 21502668. Available at: <https://ojs.abo.fi/ojs/index.php/jefc/article/view/138>. Date accessed: 28 oct. 2021.
Original Research Articles
Lipid-based drug delivery; medium chain lipid; propylene glycol ester; triglyceride; phase diagram; drug solubility; dispersion test
Authors who publish with this journal agree to the following terms: Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal. Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal. Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).