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Do surface active parenteral formulations cause inflammation?

Söderberg, Lars LU ; Engblom, Johan; Lanbeck, Peter LU and Wahlgren, Marie LU (2015) In International Journal of Pharmaceutics 484(1-2). p.246-251
Abstract
Local irritation and inflammation at the site of administration is a common side effect following administration of parenteral formulations. Biological effects of surface (interfacial) activity in solutions are less well investigated than effects caused by other physico-chemical parameters such as pH and osmolality. The interfacial activity in different systems, including human plasma, typical amphiphilic substances with fundamental biological relevance such as free fatty acids, anaesthetic depot formulations and six different antibiotics was measured. The relative interfacial pressure, and/or concentration of active substance, required to obtain 50% of the maximal attainable effect in terms of interfacial pressure were calculated. The aim... (More)
Local irritation and inflammation at the site of administration is a common side effect following administration of parenteral formulations. Biological effects of surface (interfacial) activity in solutions are less well investigated than effects caused by other physico-chemical parameters such as pH and osmolality. The interfacial activity in different systems, including human plasma, typical amphiphilic substances with fundamental biological relevance such as free fatty acids, anaesthetic depot formulations and six different antibiotics was measured. The relative interfacial pressure, and/or concentration of active substance, required to obtain 50% of the maximal attainable effect in terms of interfacial pressure were calculated. The aim was to test the hypothesis that these parameters would allow comparison to biological effects reported in in-vivo studies on the investigated substances. The highest interfacial activity was found in a triglyceride/plasma system. Among the antibiotic tested, the highest interfacial activities were found in erythromycin and dicloxacillin, which is in accordance with previous clinical findings of a high tendency of infusion phlebitis and cell toxicity. Independently of investigated system, biological effects were minimal below a 15% relative increase of interfacial activity. Above 35-45% the effects were severe. Interfacial activity in parenteral formulations may well cause damages to tissues followed by inflammation. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Fatty acid, Anesthetic, Antibiotic, Parenteral formulation, Surface activity, Inflammation
in
International Journal of Pharmaceutics
volume
484
issue
1-2
pages
246 - 251
publisher
Elsevier
external identifiers
  • pmid:25708007
  • wos:000351317400028
  • scopus:84924068791
ISSN
1873-3476
DOI
10.1016/j.ijpharm.2015.02.045
language
English
LU publication?
yes
id
074bdb33-2a9b-4718-b990-0e73421334ef (old id 5142974)
date added to LUP
2016-02-15 11:43:29
date last changed
2017-04-30 03:17:15
@article{074bdb33-2a9b-4718-b990-0e73421334ef,
  abstract     = {Local irritation and inflammation at the site of administration is a common side effect following administration of parenteral formulations. Biological effects of surface (interfacial) activity in solutions are less well investigated than effects caused by other physico-chemical parameters such as pH and osmolality. The interfacial activity in different systems, including human plasma, typical amphiphilic substances with fundamental biological relevance such as free fatty acids, anaesthetic depot formulations and six different antibiotics was measured. The relative interfacial pressure, and/or concentration of active substance, required to obtain 50% of the maximal attainable effect in terms of interfacial pressure were calculated. The aim was to test the hypothesis that these parameters would allow comparison to biological effects reported in in-vivo studies on the investigated substances. The highest interfacial activity was found in a triglyceride/plasma system. Among the antibiotic tested, the highest interfacial activities were found in erythromycin and dicloxacillin, which is in accordance with previous clinical findings of a high tendency of infusion phlebitis and cell toxicity. Independently of investigated system, biological effects were minimal below a 15% relative increase of interfacial activity. Above 35-45% the effects were severe. Interfacial activity in parenteral formulations may well cause damages to tissues followed by inflammation.},
  author       = {Söderberg, Lars and Engblom, Johan and Lanbeck, Peter and Wahlgren, Marie},
  issn         = {1873-3476},
  keyword      = {Fatty acid,Anesthetic,Antibiotic,Parenteral formulation,Surface activity,Inflammation},
  language     = {eng},
  number       = {1-2},
  pages        = {246--251},
  publisher    = {Elsevier},
  series       = {International Journal of Pharmaceutics},
  title        = {Do surface active parenteral formulations cause inflammation?},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2015.02.045},
  volume       = {484},
  year         = {2015},
}