Skip to main content
padlock icon - secure page this page is secure

Nanoparticulate Delivery Can Improve Peroral Bioavailability of Cyclosporine and Match Neoral Cmax Sparing the Kidney from Damage

Buy Article:

$106.67 + tax (Refund Policy)

Cyclosporine (CsA) as an immunosuppressant has demonstrated immense potential in the field of organ transplantation and autoimmune disorders, despite the nephrotoxicity. The present investigation is an attempt to develop biodegradable nanoparticles entrapping CsA that can match Cmax of Neoral®, the most potent formulation available to date. The Cmax and AUC0–72 of CsA administered as nanoparticles demonstrated an increase with increase in the dose administered, however the relative bioavailability decreased. The Cmax and AUC0–72 increased from 682 to 1073 ng/ml and 34854 to 55322 ng·h/ml, respectively whereas, the relative bioavailability decreased from 120 to 64%. On the other hand, the increase in initial CsA loading (10–30% w/w of polymer) recorded a proportional increase in Cmax and AUC0–72, from 494 to 1101 ng/ml and 17774 to 51763 ng·h/ml, respectively. The relative bioavailability also increased from 31 to 89%. The CsA nanoparticles at 30% CsA loading w/w of polymer and at 30 mg/Kg single dose demonstrated comparable Cmax of Neoral® at 15 mg/Kg, which upon chronic administration over a period of 30 days daily dosing showed low nephrotoxicity to that exhibited by Neoral®. The reduced toxicity of nanoparticulate CsA indicated by lower blood urea nitrogen, plasma creatinine and glomerular damage, was due to delay in Tmax as result of slow release of the CsA from the nanoparticles. The investigation unlocks the potential of polymeric nanoparticles in oral delivery of CsA.
No Reference information available - sign in for access.
No Citation information available - sign in for access.
No Supplementary Data.
No Article Media
No Metrics

Keywords: BIOAVAILABILITY; BIODEGRADABLE; NANOPARTICLES; NEPHROTOXICITY; ORAL DELIVERY

Document Type: Research Article

Publication date: April 1, 2011

More about this publication?
  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Terms & Conditions
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more