Hydrophobic ion pairing of a minocycline/Ca(2+)/AOT complex for preparation of drug-loaded PLGA nanoparticles with improved sustained release.
(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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/8577549
- author
- D. Holmkvist, Alexander LU ; Friberg, Annika LU ; Nilsson, Ulf LU and Schouenborg, Jens LU
- organization
- publishing date
- 2016
- 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
- pmid:26773599
- 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)
- date added to LUP
- 2016-04-04 08:33:19
- date last changed
- 2022-04-15 20:24:39
@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 = {{D. Holmkvist, Alexander and Friberg, Annika and Nilsson, Ulf 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}}, doi = {{10.1016/j.ijpharm.2016.01.011}}, volume = {{499}}, year = {{2016}}, }