A novel oleanolic acid-loaded PLGA-TPGS nanoparticle for liver cancer treatment.

Abstract

OBJECTIVES:

Hepatocellular carcinoma is the third most common cause of cancer death. Oleanolic acid (OA) is a natural triterpenoid, has many important biological actions, including antitumor effect, but its poor solubility often leads to poor pharmacodynamics. The aim of our work is to make OA-loaded poly (lactide-co-glycolide)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (OPTN) to improve its efficacy to liver cancer and characterize it.

METHODS:

OPTN were prepared by ultrasonic emulsification-solvent evaporation technique using PLGA with or without the addition of TPGS (OPN). The coumarin-6-loaded nanoparticles were used as a fluorescence marker. The nanoparticles were characterized for surface morphology, surface charge, particle size, drug loading, encapsulation efficiency, in vitro drug-release, cellular uptake, cytotoxicity by human liver cancer cell line HepG2 cells, and therapeutic effect in vivo.

KEY FINDINGS:

The prepared nanoparticles were found to be spherical in shape. The in vitro drug-release profile of both nanoparticle formulations showed a biphasic release pattern. There was an increased level of uptake and cytotoxicity of OPTN in the HepG2 cells compared with that of OPN. The treatment of OPTN group was better than OPN and FS groups in vivo.

CONCLUSION:

The results showed advantages of OPTN in terms of sustainable release and efficacy in liver cancer chemotherapy compared with OPN. OPTN could be acted as a novel and new dosage form to be used in cancer treatment study.

• Authors: Xu Bao, Meng Gao, Hong Xu, Ke-Xin Liu, Cheng-Hong Zhang, Ni Jiang, Qiu-Chen Chu, Xin Guan, Yan Tian
• Journal: Drug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 41 Issue 7 Pg. 1193-203 ( 2015) ISSN: 1520-5762 [Electronic] England
• PMID: 25026246 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antineoplastic Agents
• Coumarins
• Delayed-Action Preparations
• Drug Carriers
• Thiazoles
• coumarin 6
• Vitamin E
• Polylactic Acid-Polyglycolic Acid Copolymer
• Polyglycolic Acid
• Lactic Acid
• Polyethylene Glycols
• Oleanolic Acid
• tocophersolan

Topics

• Antineoplastic Agents (administration & dosage, chemistry, pharmacology)
• Carcinoma, Hepatocellular (drug therapy, pathology)
• Coumarins (administration & dosage, chemistry)
• Delayed-Action Preparations
• Drug Carriers (chemistry)
• Drug Liberation
• Hep G2 Cells
• Humans
• Lactic Acid (chemistry)
• Liver Neoplasms (drug therapy, pathology)
• Nanoparticles
• Oleanolic Acid (administration & dosage, chemistry, pharmacology)
• Polyethylene Glycols (chemistry)
• Polyglycolic Acid (chemistry)
• Polylactic Acid-Polyglycolic Acid Copolymer
• Solubility
• Thiazoles (administration & dosage, chemistry)
• Vitamin E (analogs & derivatives, chemistry)