Development of Solid SEDDS: II. Application of Acconon C-44 and Gelucire 44/14 as Solidifying Agents for Self-emulsifying Drug Delivery Systems of Medium Chain Triglyceride

  • Abu T. M. Serajuddin Professor

Abstract

A self-emulsifying drug delivery system (SEDDS) is usually an isotropic liquid consisting of drug, lipid, surfactant and/or co surfactant that spontaneously form fine oil-in-water emulsion in contact with water. Since a solid dosage form is more preferable than a liquid, the present investigation was undertaken to determine whether liquid SEDDS containing medium-chain lipids (mono- or tri-glycerides) may be converted to solids by using lauroyl polyoxyl glycerides (Acconon C-44; ABITEC and Gelucire 44/14; Gattefosse) as solidifying agents such that the formulations may be filled into hard gelatin capsules. For the preparation of solid formulations, Acconon C-44 and Gelucire 44/14 were melted at 65?C, a liquid lipid or a liquid lipid-surfactant mixture with and without dissolved drug (Probucol) were added to them, and the hot liquid were filled into hard gelatin capsules. The melts were then allowed to solidify inside capsules. The results showed that a triglyceride of medium chain fatty acids (Captex 355; ABITEC), and not monoglycerides, could be solidified by this method. The powder X-ray diffraction, differential scanning calorimetric and microscopic analysis indicated that the lauroyl polyoxyl glycerides crystallized at room temperature, while the lipid or the lipid-surfactant mixtures present in the formulations remained interspersed in between solids as a separate liquid phase. The drug remained dissolved in the liquid phase and there was no crystallization of drug. Dispersion testing of the solid systems using 250 mL 0.01N HCl as dispersion medium and the USP dissolution apparatus II at 50 rpm and 37 ?C showed that, although Acconon C-44 and Gelucire 44/14 are themselves surface active in nature, a second surfactant (Cremophor EL; BASF) was needed as the co-surfactant to maximize drug release and dispersion from the system. Formulations containing 1:1 and 3:1 ratios of Captex 355 and Cremophor EL produced lipid particles in the range of 200 to 450 nm. Thus, the report presents a novel approach of preparing SEDDS that results into very fine emulsion with particle size ranging in <500nm.

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
2012-06-20
How to Cite
SERAJUDDIN, Abu T. M.. Development of Solid SEDDS: II. Application of Acconon C-44 and Gelucire 44/14 as Solidifying Agents for Self-emulsifying Drug Delivery Systems of Medium Chain Triglyceride. Journal of Excipients and Food Chemicals, [S.l.], v. 3, n. 2, p. 54-66, june 2012. ISSN 21502668. Available at: <https://ojs.abo.fi/ojs/index.php/jefc/article/view/141>. Date accessed: 19 oct. 2021.
Section
Original Research Articles

Keywords

Drug delivery; probucol; self-emulsifying system; lipid; surfactant; solidifying agent; Acconon C-44; Gelucire 44/14; dispersion test