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Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis

Publication Date
July 1, 2016
Creators
Description
Triglycerides (TG) are one of the most common excipients used in oral lipid-based formulations. The chain length of the TG plays an important role in the oral bioavailability of the co-administered drug. Fatty acid (FA) chain-length specificity of porcine pancreatic lipase was studied by means of an in vitro lipolysis model under bio-relevant conditions at pH 6.80. In order to determine the total extent of lipolysis, back-titration experiments at pH 11.50 were performed. Results suggest that there is a specific chain length range (C2–C8) for which pancreatic lipase shows higher activity. This specificity could result from a combination of physicochemical properties of TGs, 2-monoglycerides (2-MGs) and FAs, namely the droplet size of the TGs, the solubility of 2-MGs within mixed micelles, and the relative stability of the FAs as leaving groups in the hydrolysis reaction. During experimentation, it was evident that an optimisation of lipolysis conditions was needed for tighter control over pH levels so as to better mimic in vivo conditions. 1 M NaOH, 3.5 mL/min maximum dosing rate, and 3 μL/min minimum dosing rate were the optimised set of conditions that allowed better pH control, as well as the differentiation of the lipolysis of different lipid loads. Collection dates: 2014
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DOI
Associate publ. DOI
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Subjects (LCSH)

Oral medication

Lipids

Triglycerides -- Phar...

Drug delivery systems...

Drug carriers (Pharma...

Solubility

Bioavailability

Volumetric analysis

Fatty acids

Pharmacokinetics

Monoglyceride

Subjects

Lipid based drug deli...

Subjects (JACS)

Subjects Allied to Me...

Subjects (LC)

R Medicine::RM Therap...

R Medicine::RS Pharma...

QS-QZ Preclinical sci...

Divisions
University of Nottingham, UK Campus::Faculty of Science::School of Pharmacy
Data type
Excel files with raw and processed data corresponding to the publication Benito-Gallo P., et al. Eur J Pharm Biopharm. (2015) 353-62
Funders
Grant Number
EP/I01375X/1
Data collection method
In vitro lipolysis, DLS
Resource languages
English
Publisher
The University of Nottingham
Date Issued
July 1, 2016
File(s)
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Name

Droplet size and total surface of the equimolar triglyceride emulsions.xlsx

Description
Experimental data: droplet size and total surface area of the equimolar triglyceride emulsions following the dispersion in the lipolysis buffer
Size

14.74 KB

Format

Microsoft Excel XML

Checksum (MD5)

73f1cb69419f70ed2e3d1a0d01e21b68

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Name

In vitro lipolysis of equimolar amounts of different triglycerides + Back titration studies.xlsx

Description
Experimental data: In vitro lipolysis of equimolar amounts of different triglycerides + Back-titration studies
Size

1.97 MB

Format

Microsoft Excel XML

Checksum (MD5)

77a601696b969b3d0d0a9ea0fb0904b0