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Targeting liver cancer via ASGP receptor using 5-FU-loaded surface-modified PLGA nanoparticles.

AbstractCONTEXT:
Liver cancer is widespread liver malignancy in the world, for an estimated one million deaths annually.
OBJECTIVE:
In present work, lactobionic acid conjugated PLGA nanoparticles (LDNPs) bearing 5-Fluorouracil (5-FU) were developed for targeted delivery to hepatocellular carcinoma.
MATERIALS AND METHODS:
Lactobionic acid conjugated PLGA was used to prepare LDNPs using modified emulsion diffusion method.
RESULTS:
They were characterised for particle morphology, particle size (below 150 nm), zeta potential and polydispersity index (PDI ∼0.35), entrapment efficiency (∼60.23%), and cumulative percent drug release.
DISCUSSION:
LDNPs in ex-vivo cell line studies on human cancer cell line HepG2 exhibited significantly higher cytotoxicity compared to 5-FU and DNPs (unconjugated PLGA NPs) with growth inhibition 50% (GI50) of 66.7 µg/mL, 50.2 µg/mL and 35.5 µg/mL, respectively. In vivo studies exhibited higher drug concentration about 37.52 ± 0.68% in liver as compared to other organs and plasma.
CONCLUSION:
Thus, LDNPs showed high drug loading, specificity, biocompatibility and efficacy in treatment of liver cancer.
AuthorsRuchi Dangi, Pooja Hurkat, Ankit Jain, Satish Shilpi, Ashish Jain, Arvind Gulbake, Sanjay K Jain
JournalJournal of microencapsulation (J Microencapsul) Vol. 31 Issue 5 Pg. 479-87 ( 2014) ISSN: 1464-5246 [Electronic] England
PMID24697169 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antimetabolites, Antineoplastic
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Fluorouracil
Topics
  • Antimetabolites, Antineoplastic (administration & dosage, pharmacology)
  • Carcinoma, Hepatocellular (drug therapy)
  • Drug Delivery Systems
  • Fluorouracil (administration & dosage, pharmacology)
  • Hep G2 Cells
  • Humans
  • Lactic Acid (chemistry)
  • Liver Neoplasms (drug therapy)
  • Nanoparticles (chemistry)
  • Polyglycolic Acid (chemistry)
  • Polylactic Acid-Polyglycolic Acid Copolymer

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