Successful Delivery of Zidovudine-Loaded Docosanol Nanostructured Lipid Carriers (Docosanol NLCs) into Rat Brain

  • Tapash Chakraborty
  • Malay K. DasEmail author
  • Lopamudra Dutta
  • Biswajit Mukherjee
  • Sanjoy Das
  • Anupam Sarma


The major challenges to the clinical application of zidovudine are its moderate aqueous solubility, relative short half-life, and incapability to go across BBB after systemic administration makes the brain one of the dominant HIV reservoirs. We investigated the development of zidovudine-loaded NLCs based on docosanol and oleic acid which were further surface modified with PEG4000 and HAS. The drug content and entrapment efficiencies were assessed by UV analysis. The mean diameter of the SyLN was found to be at 54.7 ± 1.4 nm with a zeta potential of −21.6 ± 0.2 mV and relatively low polydispersity. The NLCs showed excellent stability in the refrigerated condition, in blood serum and were safe for IV administration. In vitro release studies showed a sustained release profile of zidovudine in aCSF. In vivo plasma and brain pharmacokinetics investigation in a rat model showed that SyLN and SyLN-Peg NLCs rapidly reached the brain and yielded higher MRT, Cmax, and AUC. The rat brain pharmacokinetic data confirm the brain localization and accumulation of the developed NLCs delivering AZT in a sustained manner for a prolonged period of time, which is further confirmed by CLSM images of brain cryosections labeled with SyLN-C6 NLCs. Our results suggest that the developed docosanol NLCs could be a promising drug delivery system for long-term brain delivery of zidovudine in the treatment of Neuro-AIDS.


Docosanol NLCs Zidovudine Blood–brain barrier Brain targeted NLCs Sustained release NLCs Neuro-AIDS 



The authors gratefully acknowledge the experimental/analytical support of Guwahati Biotech Park, Technology Complex, IIT Guwahati and The Sophisticated Analytical Instrument Facility (SAIF), NEHU Shillong, and College of Veterinary Science, Guwahati. This work was financially supported by the Department of Biotechnology, Ministry of Science & Technology, Government of India under Grant No. BT/504/NE/TBP/2013.


All figures and tables are original and self-made.


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Copyright information

© Springer Nature Switzerland AG 2019

Authors and Affiliations

  • Tapash Chakraborty
    • 1
  • Malay K. Das
    • 1
    Email author
  • Lopamudra Dutta
    • 2
  • Biswajit Mukherjee
    • 2
  • Sanjoy Das
    • 1
  • Anupam Sarma
    • 1
  1. 1.Drug Delivery Research Laboratory, Department of Pharmaceutical SciencesDibrugarh UniversityDibrugarhIndia
  2. 2.Department of Pharmaceutical TechnologyDibrugarh UniversityDibrugarhIndia

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