SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS USING MCTs

02 Jan 2018

Abstract

The primary objective of this study was to develop lipid-based self-microemulsifying drug delivery systems (SMEDDS) without using any organic cosolvents that would spontaneously form microemulsions upon dilution with water. Cosolvents were avoided to prevent possible precipitation of drug upon dilution and other stability issues. Different polysorbates, namely, Tween 20, Tween 40, Tween 60, and Tween 80, were used as surfactants, and Captex 355 EP/NF (glycerol tricaprylate/caprate) or its 1:1 mixture with Capmul MCM NF (glycerol monocaprylocaprate) were used as lipids. Captex 355-Tween-water ternary phase diagrams showed that oil-in-water microemulsions were formed only when the surfactant content was high (80–90%) and the lipid content low (10–20%). Thus, mixtures of Tweens with Captex 355 alone were not suitable to prepare SMEDDS with substantial lipid contents. However, when Captex 355 was replaced with the 1:1 mixture of Captex 355 and Capmul MCM, clear isotropic microemulsion regions in phase diagrams with sizes in the increasing order of Tween 20 < Tween 40 < Tween 60 < Tween 80 were obtained. Tween 80 had the most profound effect among all surfactants as microemulsions were formed with lipid to surfactant ratios as high as 7:3, which may be attributed to the presence of double bond in its side chain that increased the curvature of surfactant layer. Thus, lipid-surfactant mixtures containing 1:1 mixture of medium chain triglyceride (Captex 355) and monoglyceride (Capmul MCM) and as low as 30% Tween 80 were identified as organic cosolvent-free systems for the preparation of SMEDDS. Formulations with a model drug, probucol, dispersed spontaneously and rapidly upon dilution with water to form microemulsions without any drug precipitation.

Pages 215-223 | Received 30 May 2017, Accepted 18 Sep 2017, Published online: 23 Oct 2017
This study was supported, in part, by a research grant from ABITEC Corporation, Columbus 43215, OH, USA.

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About ABITEC Corporation

ABITEC Corporation is part of ABF Ingredients and is headquartered in Columbus, Ohio, US with two manufacturing sites in the Midwest. ABITEC specializes in the manufacturing and distribution of specialty lipid ingredients for use in the pharmaceutical, nutraceutical, and specialty chemical markets.

In addition, ABITEC offers contract and toll manufacturing services for customers looking to develop and manufacture new oleochemical molecules or blend/toll-manufacture an established product.

About ABF Ingredients

ABF Ingredients is a division of Associated British Foods that focuses on high value ingredients for both food and non-food areas and comprises a range of ingredient companies which include AB Enzymes, Ohly, PGP International, and SPI Pharma. The group has established strong market positions in cereal specialties, enzymes, esters, extruded ingredients, specialty lipids, specialty powders, specialty flours and yeast extracts worldwide.

For further information, please contact:

Amanda Coulter, Manager: Marketing Research and Communications

614-429-6453 | [email protected]