Effect of Difference in Fatty Acid Chain Lengths of Medium-Chain Lipids on Lipid-Surfactant-Water Phase Diagrams and Drug Solubility

  • Hetal N Prajapati
  • Darshil P Patel
  • Nrupa G Patel
  • Damon D Dalrymple
  • Abu T. M. Serajuddin Professor

Abstract

Lipids of medium chain fatty acid are commonly used in the development of lipid-based self-emulsifying and self-microemulsifying drug delivery systems. However, there is no systematic approach of selecting one lipid over the other has been reported in the literature. In this study, propylene glycol (PG) monoester (PG monocaprylate; Capmul PG-8) and PG diester (PG dicaprylocaprate; Captex 200P) of C8-fatty acids were compared with PG monoester (PG monolaurate; Capmul PG-12) and PG diester (PG dilaurate; Capmul PG-2L) of C12-fatty acids for phase diagrams, and especially for their ability to form microemulsions, in presence of a common surfactant, Cremophor EL, and water. Solubility of two model drugs, danazol and probucol, in lipids and lipid-surfactant mixtures were also compared. The effect of chain length of medium-chain fatty acids (C8 vs. C12) on phase diagrams of lipids was minimal. Both shorter and longer chain lipids formed essentially similar microemulsions and emulsions in presence of Cremophor EL and water, although the C12-fatty acid esters formed larger gel regions in phase diagrams than those with C8-fatty acid esters. While the solubility of both danazol and probucol increased greatly in all lipids studied as compared to their aqueous solubility, the solubility enhancement in C12-fatty acid esters was found to be lower than those in C8-fatty acid esters . When monoesters were mixed with their respective diesters at 1:1 ratios, larger microemulsion regions with lower lipid particle sizes were observed as compared to those with individual lipids.

Author Biography

Abu T. M. Serajuddin, Professor
Abu Serajuddin, Ph.D., is a Professor of Industrial Pharmacy at St. Johns University, Queens, New York, USA. At St. Johns, he is building active research programs and centers of excellence in drug delivery sciences and pharmaceutical processing technologies. One focus of his research is identification and characterization of polymeric and lipidic carriers for developing bioavailable oral dosage forms of poorly water-soluble drugs. Prior to joining academia in September 2008, he worked in the pharmaceutical industry for three decades with increasing scientific and managerial responsibilities at Sanofi-Aventis (through mergers), Bristol-Myers Squibb and Novartis. In his latest positions in the industry, Dr. Serajuddin served as Executive Director and the US Head of Drug Product Development (1999-2003) and the Global Head of Science and Technology Development (2003-2008) for Novartis Pharmaceuticals Corp. In recognition of his extraordinary scientific achievements, he was named a Novartis Leading Scientist in 2005. He contributed extensively to basic pharmaceutics and drug delivery systems. He authored over 75 research papers and book chapters and made 80 invited presentations in major scientific conferences (US, France and China). He is a co-inventor in 14 patents, the majority of the patents being on drug delivery technology platforms. Among his professional recognitions, he attained Fellow status in American Association of Pharmaceutical Scientists (AAPS), American Pharmacists Association (APhA), International Union of Pure and Applied Chemistry (IUPAC), and American Association of Indian Pharmaceutical Scientists (AAiPS). He serves in the Editorial Advisory Board s of Journal of Pharmaceutical Sciences and Journal of Excipients and Food Chemicals. Among his many professional contributions, he chaired AAPS Pharmaceutics and Drug Delivery Section (2001) and AAPS Preformulation Focus Group (1994-1996). A graduate in pharmacy from Dhaka University, Bangladesh, Serajuddin received his Ph.D. in Industrial Pharmacy from St. John's University, New York, M.S. in Pharmaceutics from Columbia University, New York, and Advanced Training in Industrial Pharmacy from the University of Pisa, Italy.
Published
2011-09-13
How to Cite
PRAJAPATI, Hetal N et al. Effect of Difference in Fatty Acid Chain Lengths of Medium-Chain Lipids on Lipid-Surfactant-Water Phase Diagrams and Drug Solubility. Journal of Excipients and Food Chemicals, [S.l.], v. 2, n. 3, p. 73-88, sep. 2011. ISSN 21502668. Available at: <https://ojs.abo.fi/ojs/index.php/jefc/article/view/91>. Date accessed: 28 oct. 2021.
Section
Original Research Articles

Keywords

excipients