Nanoliposomal minocycline for ocular drug delivery

James M. Kaiser, Hisanori Imai, Jeremy K. Haakenson, Robert M. Brucklacher, Todd E. Fox, Sriram S. Shanmugavelandy, Kellee A. Unrath, Michelle M. Pedersen, Pingqi Dai, Willard M. Freeman, Sarah K. Bronson, Thomas W. Gardner, Mark Kester

Research output: Contribution to journalArticle

34 Scopus citations

Abstract

Nanoliposomal technology is a promising drug delivery system that could be employed to improve the pharmacokinetic properties of clearance and distribution in ocular drug delivery to the retina. We developed a nanoscale version of an anionic, cholesterol-fusing liposome that can encapsulate therapeutic levels of minocycline capable of drug delivery. We demonstrate that size extrusion followed by size-exclusion chromatography can form a stable 80-nm liposome that encapsulates minocycline at a concentration of 450 ± 30 μM, which is 2% to 3% of loading material. More importantly, these nontoxic nanoliposomes can then deliver 40% of encapsulated minocycline to the retina after a subconjunctival injection in the STZ model of diabetes. Efficacy of therapeutic drug delivery was assessed via transcriptomic and proteomic biomarker panels. For both the free minocycline and encapsulated minocycline treatments, proinflammatory markers of diabetes were downregulated at both the messenger RNA and protein levels, validating the utility of biomarker panels for the assessment of ocular drug delivery vehicles. From the Clinical Editor: Authors developed a nano-liposome that can encapsulate minocycline for optimized intraocular drug delivery. These nontoxic nanoliposomes delivered 40% of encapsulated minocycline to the retina after a subconjunctival injection in a diabetes model.

Original languageEnglish (US)
Pages (from-to)130-140
Number of pages11
JournalNanomedicine: Nanotechnology, Biology, and Medicine
Volume9
Issue number1
DOIs
StatePublished - Jan 2013

All Science Journal Classification (ASJC) codes

  • Bioengineering
  • Medicine (miscellaneous)
  • Molecular Medicine
  • Biomedical Engineering
  • Materials Science(all)
  • Pharmaceutical Science

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  • Cite this

    Kaiser, J. M., Imai, H., Haakenson, J. K., Brucklacher, R. M., Fox, T. E., Shanmugavelandy, S. S., Unrath, K. A., Pedersen, M. M., Dai, P., Freeman, W. M., Bronson, S. K., Gardner, T. W., & Kester, M. (2013). Nanoliposomal minocycline for ocular drug delivery. Nanomedicine: Nanotechnology, Biology, and Medicine, 9(1), 130-140. https://doi.org/10.1016/j.nano.2012.03.004