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Hydrophobic ion pairing of a minocycline/Ca(2+)/AOT complex for preparation of drug-loaded PLGA nanoparticles with improved sustained release.

Holmkvist, Alexander LU ; Friberg, Annika LU ; Nilsson, Ulf J and Schouenborg, Jens LU (2016) In International Journal of Pharmaceutics 499(1-2). p.351-357
Abstract
Polymeric nanoparticles is an established and efficient means to achieve controlled release of drugs. Incorporation of minocycline, an antibiotic with anti-inflammatory and neuroprotective properties, into biodegradable nanoparticles may therefore provide an efficient means to combat foreign body reactions to implanted electrodes in the brain. However, minocycline is commonly associated with poor encapsulation efficiencies and/or fast release rates due to its high solubility in water. Moreover, minocycline is unstable under conditions of low and high pH, heat and exposure to light, which exacerbate the challenges of encapsulation. In this work drug loaded PLGA nanoparticles were prepared by a modified emulsification-solvent-diffusion... (More)
Polymeric nanoparticles is an established and efficient means to achieve controlled release of drugs. Incorporation of minocycline, an antibiotic with anti-inflammatory and neuroprotective properties, into biodegradable nanoparticles may therefore provide an efficient means to combat foreign body reactions to implanted electrodes in the brain. However, minocycline is commonly associated with poor encapsulation efficiencies and/or fast release rates due to its high solubility in water. Moreover, minocycline is unstable under conditions of low and high pH, heat and exposure to light, which exacerbate the challenges of encapsulation. In this work drug loaded PLGA nanoparticles were prepared by a modified emulsification-solvent-diffusion technique and characterized for size, drug encapsulation and in vitro drug release. A novel hydrophobic ion pair complex of minocycline, Ca(2+) ions and the anionic surfactant AOT was developed to protect minocycline from degradation and prolong its release. The optimized formulation resulted in particle sizes around 220nm with an entrapment efficiency of 43% and showed drug release over 30 days in artificial cerebrospinal fluid. The present results constitute a substantial increase in release time compared to what has hitherto been achieved for minocycline and indicate that such particles might provide useful for sustained drug delivery in the CNS. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
International Journal of Pharmaceutics
volume
499
issue
1-2
pages
351 - 357
publisher
Elsevier
external identifiers
  • pmid:26773599
  • scopus:84957824518
  • wos:000370048300035
ISSN
1873-3476
DOI
10.1016/j.ijpharm.2016.01.011
language
English
LU publication?
yes
id
ecad6711-8eab-4f79-81a1-42a5b62c10fd (old id 8577549)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/26773599?dopt=Abstract
date added to LUP
2016-02-03 17:17:17
date last changed
2017-11-05 04:43:18
@article{ecad6711-8eab-4f79-81a1-42a5b62c10fd,
  abstract     = {Polymeric nanoparticles is an established and efficient means to achieve controlled release of drugs. Incorporation of minocycline, an antibiotic with anti-inflammatory and neuroprotective properties, into biodegradable nanoparticles may therefore provide an efficient means to combat foreign body reactions to implanted electrodes in the brain. However, minocycline is commonly associated with poor encapsulation efficiencies and/or fast release rates due to its high solubility in water. Moreover, minocycline is unstable under conditions of low and high pH, heat and exposure to light, which exacerbate the challenges of encapsulation. In this work drug loaded PLGA nanoparticles were prepared by a modified emulsification-solvent-diffusion technique and characterized for size, drug encapsulation and in vitro drug release. A novel hydrophobic ion pair complex of minocycline, Ca(2+) ions and the anionic surfactant AOT was developed to protect minocycline from degradation and prolong its release. The optimized formulation resulted in particle sizes around 220nm with an entrapment efficiency of 43% and showed drug release over 30 days in artificial cerebrospinal fluid. The present results constitute a substantial increase in release time compared to what has hitherto been achieved for minocycline and indicate that such particles might provide useful for sustained drug delivery in the CNS.},
  author       = {Holmkvist, Alexander and Friberg, Annika and Nilsson, Ulf J and Schouenborg, Jens},
  issn         = {1873-3476},
  language     = {eng},
  number       = {1-2},
  pages        = {351--357},
  publisher    = {Elsevier},
  series       = {International Journal of Pharmaceutics},
  title        = {Hydrophobic ion pairing of a minocycline/Ca(2+)/AOT complex for preparation of drug-loaded PLGA nanoparticles with improved sustained release.},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2016.01.011},
  volume       = {499},
  year         = {2016},
}