Show simple item record

dc.contributor.authorGershkovich, Pavel
dc.contributor.authorBenito, Paloma
dc.date.accessioned2016-07-01T16:13:24Z
dc.date.available2016-07-01T16:13:24Z
dc.date.issued2016-07-01
dc.identifier.urihttps://rdmc.nottingham.ac.uk/handle/internal/51
dc.description.abstractTriglycerides (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.en_UK
dc.language.isoenen_UK
dc.publisherThe University of Nottinghamen_UK
dc.relation.urihttp://www.sciencedirect.com/science/article/pii/S0939641115002076en_UK
dc.subject.lcshOral medicationen_UK
dc.subject.lcshLipidsen_UK
dc.subject.lcshTriglycerides -- Pharmacokineticsen_UK
dc.subject.lcshDrug delivery systemsen_UK
dc.subject.lcshDrug carriers (Pharmacy)en_UK
dc.subject.lcshSolubilityen_UK
dc.subject.lcshBioavailabilityen_UK
dc.subject.lcshVolumetric analysisen_UK
dc.subject.lcshFatty acidsen_UK
dc.subject.lcshPharmacokineticsen_UK
dc.subject.lcshMonoglycerideen_UK
dc.titleChain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysisen_UK
dc.identifier.doihttp://doi.org/10.17639/nott.48
dc.subject.freeLipid based drug delivery systems; Poorly water-soluble drugs; Oral bioavailability; Back-titration; Fatty acid; Monoglycerideen_UK
dc.subject.jacsSubjects Allied to Medicine::Pharmacology, toxicology & pharmacy::Pharmacology, toxicology & pharmacy not elsewhere classifieden_UK
dc.subject.lcR Medicine::RM Therapeutics. Pharmacologyen_UK
dc.subject.lcR Medicine::RS Pharmacy and materia medicaen_UK
dc.subject.lcQS-QZ Preclinical sciences (NLM Classification)::QV Pharmacologyen_UK
dc.date.collection2014en_UK
uon.divisionUniversity of Nottingham, UK Campus::Faculty of Science::School of Pharmacyen_UK
uon.funder.controlledEngineering & Physical Sciences Research Councilen_UK
uon.datatypeExcel files with raw and processed data corresponding to the publication Benito-Gallo P., et al. Eur J Pharm Biopharm. (2015) 353-62en_UK
uon.grantEP/I01375X/1en_UK
uon.collectionmethodIn vitro lipolysis, DLSen_UK
uon.rightscontactUniversity of Nottinghamen_UK
uon.preservation.rarelyaccessedtrue
dc.relation.doi10.1016/j.ejpb.2015.04.027en_UK


Files in this item

Thumbnail
Thumbnail
Thumbnail
Thumbnail
Thumbnail
Thumbnail
Thumbnail

This item appears in the following Collection(s)

Show simple item record