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Oil-Based Delivery Control Release System Targeted to the Later Part of the Gastrointestinal Tract—A Mechanistic Study

Zhang, Lingping LU ; Wahlgren, Marie LU orcid and Bergenståhl, Björn LU (2022) In Pharmaceutics 14(5).
Abstract

Oil-based drug delivery systems have been studied in different aspects. The present study proposes a new application for an oil-based delivery system, focusing on controlled release until the drug reaches the later part of the small intestine. Bulk surfactants and interfacial surfactants were added into the oil formulation to provide a better mechanistic understating of the lipolysis. Validation of the modified in vitro method shows the overall conversion from medium-chain triglyceride oil (MCT oil) to free fatty acids (FFA) of 100 ± 4% in five replicates. This fully converted level and high reproducibility are fundamental for the following investigations where any retarding effect can be distinguished from the experimental errors. The... (More)

Oil-based drug delivery systems have been studied in different aspects. The present study proposes a new application for an oil-based delivery system, focusing on controlled release until the drug reaches the later part of the small intestine. Bulk surfactants and interfacial surfactants were added into the oil formulation to provide a better mechanistic understating of the lipolysis. Validation of the modified in vitro method shows the overall conversion from medium-chain triglyceride oil (MCT oil) to free fatty acids (FFA) of 100 ± 4% in five replicates. This fully converted level and high reproducibility are fundamental for the following investigations where any retarding effect can be distinguished from the experimental errors. The results show that viscosity and thermodynamic activity have limited retardation. Furthermore, the former may change the kinetics of lipolysis, while the latter changes the equilibrium level. The gel-forming retarder (ethylcellulose) displayed a strong effect. Whereas the lipolysis was significantly retarded (>50%) when the retarders altered the interfacial composition (poloxamer 407), degradable interfacial surfactants did not have the same effect. However, surface-active, lipolysis-resistant retarders with a high CMC did not show a retarding effect.

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Please use this url to cite or link to this publication:
author
; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
in vitro method, later part of the small gastrointestinal tract, oil-based delivery system
in
Pharmaceutics
volume
14
issue
5
article number
896
publisher
MDPI AG
external identifiers
  • scopus:85129364890
  • pmid:35631482
ISSN
1999-4923
DOI
10.3390/pharmaceutics14050896
language
English
LU publication?
yes
id
907ed874-3044-4bdb-9d9a-2e72bdd02cf3
date added to LUP
2022-07-06 15:20:00
date last changed
2024-04-18 04:55:11
@article{907ed874-3044-4bdb-9d9a-2e72bdd02cf3,
  abstract     = {{<p>Oil-based drug delivery systems have been studied in different aspects. The present study proposes a new application for an oil-based delivery system, focusing on controlled release until the drug reaches the later part of the small intestine. Bulk surfactants and interfacial surfactants were added into the oil formulation to provide a better mechanistic understating of the lipolysis. Validation of the modified in vitro method shows the overall conversion from medium-chain triglyceride oil (MCT oil) to free fatty acids (FFA) of 100 ± 4% in five replicates. This fully converted level and high reproducibility are fundamental for the following investigations where any retarding effect can be distinguished from the experimental errors. The results show that viscosity and thermodynamic activity have limited retardation. Furthermore, the former may change the kinetics of lipolysis, while the latter changes the equilibrium level. The gel-forming retarder (ethylcellulose) displayed a strong effect. Whereas the lipolysis was significantly retarded (&gt;50%) when the retarders altered the interfacial composition (poloxamer 407), degradable interfacial surfactants did not have the same effect. However, surface-active, lipolysis-resistant retarders with a high CMC did not show a retarding effect.</p>}},
  author       = {{Zhang, Lingping and Wahlgren, Marie and Bergenståhl, Björn}},
  issn         = {{1999-4923}},
  keywords     = {{in vitro method; later part of the small gastrointestinal tract; oil-based delivery system}},
  language     = {{eng}},
  number       = {{5}},
  publisher    = {{MDPI AG}},
  series       = {{Pharmaceutics}},
  title        = {{Oil-Based Delivery Control Release System Targeted to the Later Part of the Gastrointestinal Tract—A Mechanistic Study}},
  url          = {{http://dx.doi.org/10.3390/pharmaceutics14050896}},
  doi          = {{10.3390/pharmaceutics14050896}},
  volume       = {{14}},
  year         = {{2022}},
}