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Updated: Apr 27, 2026
PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
Published on: December 27, 2013
A novel oleanolic acid-loaded PLGA-TPGS nanoparticle for liver cancer treatment
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.
Insights
Novel nanoparticles loaded with oleanolic acid (OA) show improved efficacy for liver cancer treatment. These OA-loaded poly(lactide-co-glycolide)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles offer better drug release and cytotoxicity.
Area of Science:
- Nanotechnology
- Pharmacology
- Oncology
Background:
- Hepatocellular carcinoma (HCC) is a leading cause of cancer mortality.
- Oleanolic acid (OA) exhibits antitumor properties but suffers from poor solubility and pharmacodynamics.
- Developing effective drug delivery systems is crucial for improving OA's therapeutic potential in liver cancer.
Purpose of the Study:
- To develop OA-loaded poly(lactide-co-glycolide)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (OPTN).
- To enhance the efficacy of OA in treating liver cancer.
- To characterize the physicochemical properties and therapeutic effects of OPTN.
Main Methods:
- OPTN were prepared using ultrasonic emulsification-solvent evaporation.
- Nanoparticles were characterized for morphology, charge, size, drug loading, and encapsulation efficiency.
- In vitro drug release, cellular uptake, cytotoxicity in HepG2 cells, and in vivo therapeutic effects were evaluated.
Main Results:
- Prepared nanoparticles were spherical with a biphasic in vitro drug release pattern.
- OPTN demonstrated significantly increased cellular uptake and cytotoxicity in HepG2 cells compared to OPN (OA without TPGS).
- In vivo studies showed superior therapeutic effects of OPTN compared to OPN and free OA (FS).
Conclusions:
- OPTN exhibit advantages in sustained release and improved efficacy for liver cancer chemotherapy.
- OPTN represent a promising novel dosage form for cancer treatment.
- The use of PLGA-TPGS nanoparticles enhances OA's therapeutic potential against liver cancer.
