+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Monoacyl phosphatidylcholine inhibits the formation of lipid multilamellar structures during in vitro lipolysis of self-emulsifying drug delivery systems



Monoacyl phosphatidylcholine inhibits the formation of lipid multilamellar structures during in vitro lipolysis of self-emulsifying drug delivery systems



European Journal of Pharmaceutical Sciences 108: 62-70



The colloidal structures formed during lipolysis of self-emulsifying drug delivery systems (SEDDS) might affect the solubilisation and possibly the absorption of drugs. The aim of the current study is to elucidate the structures formed during the in vitro lipolysis of four SEDDS containing medium-chain glycerides and caprylocaproyl polyoxyl-8 glycerides (Labrasol), with or without monoacyl phosphatidylcholine (MAPC). In situ synchrotron small-angle X-ray scattering (SAXS) was combined with ex situ cryogenic transmission electron microscopy (cryo-TEM) and dynamic light scattering (DLS) to elucidate the generated structures. The SAXS scattering curves obtained during the lipolysis of MAPC-free SEDDS containing 43-60% w/w Labrasol displayed a lamellar phase peak at q=2.13nm-1 that increased with Labrasol concentration, suggesting the presence of multilamellar structures (MLS) with a d-spacing of 2.95nm. However, SEDDS containing 20-30% w/w MAPC did not form MLS during the lipolysis. The cryo-TEM and DLS studies showed that MAPC-free SEDDS formed coarse emulsions while MAPC-containing SEDDS formed nanoemulsions during the dispersion in digestion medium. From the first minute and during the entire lipolysis process, SEDDS both with and without MAPC generated uni-, bi-, and oligo-lamellar vesicles. The lipolysis kinetics in the first minutes of the four SEDDS correlated with an increased intensity of the SAXS curves and the rapid transformation from lipid droplets to vesicles observed by cryo-TEM. In conclusion, the study elucidates the structures formed during in vitro lipolysis of SEDDS and the inhibitory effect of MAPC on the formation of MLS.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 058344798

Download citation: RISBibTeXText

PMID: 27890596

DOI: 10.1016/j.ejps.2016.11.022


Related references

In vitro and in vivo performance of monoacyl phospholipid-based self-emulsifying drug delivery systems. Journal of Controlled Release 255: 45-53, 2017

The lack of IVIVC for monoacyl phospholipid-based self-emulsifying drug delivery systems. Journal of Controlled Release 255: 279, 2017

The Effect of Media Composition, pH, and Formulation Excipients on the In Vitro Lipolysis of Self-Emulsifying Drug Delivery Systems (SEDDS). Journal of Dispersion Science and Technology 31(2): 226-232, 2010

Formulation and characterization of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine. International Journal of Pharmaceutics 502(1-2): 151-160, 2016

In vitro-in vivo correlations of self-emulsifying drug delivery systems combining the dynamic lipolysis model and neuro-fuzzy networks. European Journal of Pharmaceutics and Biopharmaceutics 69(3): 887-898, 2008

Molecular insights into the formation of drug-monoacyl phosphatidylcholine solid dispersions for oral delivery. European Journal of Pharmaceutical Sciences 108: 93, 2017

Lipid formulations for oral administration of drugs: Non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. European Journal of Pharmaceutical Sciences 11(Suppl 2): S93-S98, 2000

The In Vitro Lipolysis of Lipid-Based Drug Delivery Systems: A Newly Identified Relationship between Drug Release and Liquid Crystalline Phase. Biomed Research International 2016: 2364317, 2016

In vitro lipolysis and intestinal transport of β-arteether-loaded lipid-based drug delivery systems. Pharmaceutical Research 30(10): 2694-2705, 2013

Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro lipid digestion monitored by small-angle X-ray scattering. Pharmaceutical Research 24(10): 1844-1853, 2007

Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems. European Journal of Pharmaceutics and Biopharmaceutics 117: 300-307, 2017

Simulating the digestion of lipid-based drug delivery systems (LBDDS): overview of in vitro lipolysis models. Acta Chimica Slovenica 61(1): 1-10, 2014

In vitro lipolysis models as a tool for the characterization of oral lipid and surfactant based drug delivery systems. International Journal of Pharmaceutics 417(1-2): 245-255, 2011

In vitro lipolysis data does not adequately predict the in vivo performance of lipid-based drug delivery systems containing fenofibrate. Aaps Journal 16(3): 539-549, 2014

Basics of Compounding--Nonsterile: Compounding Self-emulsifying Drug Delivery Systems and Other Self-emulsifying Lipid Formulations, Part 2. International Journal of Pharmaceutical Compounding 22(4): 294-300, 2018