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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
Multilayer-Coated Liquid Crystalline Nanoparticles for Effective Sorafenib Delivery to Hepatocellular Carcinoma
Raj Kumar Thapa1, Ju Yeon Choi1, Bijay K Poudel1
1College of Pharmacy, Yeungnam University , 280 Daehak-Ro, Gyeongsan, Gyeongsanbuk-do 712-749, South Korea.
Abstract:
Hepatocellular carcinoma is one of the most common cancers in adults and develops due to activation of oncogenes and inactivation of tumor suppressor genes. Sorafenib (SF) is a U.S. Food and Drug Administration (FDA) approved drug for the treatment of hepatocellular carcinoma. However, its clinical use is limited by its poor aqueous solubility and undesirable side effects. Monoolein-based liquid crystalline nanoparticles (LCN) are self-assembled structures that have been determined as promising drug-delivery vehicles. Therefore, the main aim of this study was to prepare layer-by-layer (LbL) polymer-assembled SF-loaded LCNs (LbL-LCN/SF) for effective delivery of SF to hepatocellular carcinoma. Results revealed that LbL-LCN/SF presented optimum particle size (∼165 nm) and polydispersity index (PDI, ∼0.14) with appropriate polymer layer assembly confirmed by transmission electron microscopy (TEM) and atomic force microscopy (AFM). Furthermore, LbL-LCN/SF effectively controlled burst release and exhibited pH-sensitive release of SF, thereby increasing drug release in the acidic microenvironment of tumor cells. Compared to free SF and bare LCN, the hemolytic activity of LbL-LCN/SF was significantly reduced (p<0.01). Interestingly, LbL-LCN/SF was more cytotoxic to HepG2 cells than the free drug was. Additionally, high cellular uptake and greater apoptotic effects of LbL-LCN/SF in HepG2 cells indicates superior antitumor effects. Therefore, LbL-LCN/SF is a potentially effective formulation for hepatocellular carcinoma.
Insights
Researchers developed novel layer-by-layer polymer-assembled liquid crystalline nanoparticles loaded with sorafenib (LbL-LCN/SF) for improved hepatocellular carcinoma treatment. This formulation enhances drug delivery, reduces side effects, and shows superior antitumor activity against liver cancer cells.
Area of Science:
- Nanotechnology
- Drug Delivery Systems
- Oncology
Background:
- Hepatocellular carcinoma (HCC) is a prevalent cancer driven by genetic mutations.
- Sorafenib (SF) is an FDA-approved HCC drug with limitations in solubility and side effects.
- Monoolein-based liquid crystalline nanoparticles (LCN) show promise as drug carriers.
Purpose of the Study:
- To prepare and characterize layer-by-layer (LbL) polymer-assembled SF-loaded LCNs (LbL-LCN/SF) for HCC treatment.
- To evaluate the drug release profile and in vitro efficacy of the developed nanoparticles.
Main Methods:
- Preparation of LbL-LCN/SF using layer-by-layer assembly.
- Characterization of particle size, polydispersity index (PDI), and morphology using TEM and AFM.
- In vitro assessment of drug release, cytotoxicity, cellular uptake, and apoptosis in HepG2 cells.
Main Results:
- LbL-LCN/SF exhibited optimal particle size (~165 nm) and PDI (~0.14).
- pH-sensitive drug release was observed, with increased release in acidic tumor microenvironments.
- Reduced hemolytic activity and enhanced cytotoxicity against HepG2 cells compared to free SF.
Conclusions:
- LbL-LCN/SF demonstrates controlled and pH-sensitive release of sorafenib.
- The formulation exhibits improved safety profile and superior antitumor effects.
- LbL-LCN/SF represents a promising nanocarrier for effective hepatocellular carcinoma therapy.
