Related Experiment Video
Updated: Nov 26, 2025
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Gefitinib encapsulation based on nano-liposomes for enhancing the curative effect of lung cancer
Yanjie Hu1, Jisong Zhang1, Huihui Hu1
1Department of Pulmology and Critical Care Medicine, Regional medical center for National Institute of Respiratory Diseases, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine , Hangzhou, China.
Abstract:
Gefitinib (GEB) is one of the drugs used for patients with epidermal growth factor receptor (EGFR)-positive mutations in non-small cell lung cancer (NSCLC). However, application of GEB is limited by its low water solubility, stability, and utilization rate, especially the side effects while GEB is given by oral. In this study, nanoliposome was used as a carrier to prepare nanoliposome compound drug (GL) by embedding GEB in the nanoliposome perfectly combined with green nontoxic solvent and thin-film dispersion method. The nanoliposome structure was expected to improve the water solubility and biocompatibility of GEB, thus improving the effect of cancer treatment. The surface electronegative nanoliposomes can effectively avoid protein adsorption and prolong the circulation time in vivo. Meanwhile, the ratio of lecithin to cholesterol (LE/CH) was explored to maximize the encapsulation efficiency of nanoliposome. Subsequent test results showed that GL exhibited better stability, smaller particle size and higher encapsulation efficiency. In addition, in vitro drug release curve also further confirmed that GL had a promising drug sustained-release effect. In particular, a series of in vitro tests such as cell activity, apoptosis, colony formation, scratch, invasion, and cell cycle assays were performed. The results indicated that GL significantly enhanced the pro-apoptotic effect on A549 cells. Most cell cycles of A549 cells were blocked in the G0/G1 phase influenced by GL, thus inhibiting the proliferation of cancer cells. In vivo anti-tumor studies showed that compared with pure GEB, GL had a significant inhibiting effect on NSCLC. In conclusion, the GL which was synthesized by a simple method in this study significantly improved the treatment effect of cancer cells, which proved that the nanoliposome carrier had an excellent application prospect in the treatment of lung cancer.
Insights
Nanoliposome encapsulation of gefitinib (GEB) improved its solubility and anti-cancer efficacy for non-small cell lung cancer (NSCLC). This nanoliposome compound drug (GL) demonstrated enhanced stability, sustained release, and potent tumor inhibition in vitro and in vivo.
Area of Science:
- Nanomedicine
- Pharmaceutical Sciences
- Oncology
Background:
- Gefitinib (GEB) is a targeted therapy for EGFR-mutated non-small cell lung cancer (NSCLC).
- GEB's clinical application is hindered by poor water solubility, stability, and oral bioavailability, leading to side effects.
- Nanoliposomes offer a potential solution for improving drug delivery and therapeutic outcomes.
Purpose of the Study:
- To develop a nanoliposome-encapsulated gefitinib (GL) formulation to enhance GEB's solubility, stability, and anti-cancer activity.
- To investigate the physicochemical properties and in vitro/in vivo anti-tumor efficacy of the GL formulation.
- To evaluate the potential of nanoliposomes as a drug delivery system for NSCLC treatment.
Main Methods:
- Gefitinib was encapsulated into nanoliposomes using a thin-film dispersion method with optimized lecithin to cholesterol ratios.
- Physicochemical characterization included particle size, encapsulation efficiency, and stability assessments.
- In vitro studies involved drug release assays, and cytotoxicity, apoptosis, cell cycle, colony formation, scratch, and invasion assays on A549 cells.
- In vivo anti-tumor efficacy was evaluated in a murine model of NSCLC.
Main Results:
- The developed GL formulation exhibited improved stability, smaller particle size, and higher encapsulation efficiency compared to free GEB.
- GL demonstrated sustained drug release in vitro and significantly enhanced the pro-apoptotic effect on A549 cells.
- GL treatment led to G0/G1 cell cycle arrest in A549 cells, inhibiting proliferation and showing superior in vivo anti-tumor activity against NSCLC compared to GEB.
Conclusions:
- Nanoliposome encapsulation effectively improved the physicochemical properties and therapeutic efficacy of gefitinib for NSCLC.
- The GL formulation presents a promising strategy for overcoming GEB's limitations and enhancing lung cancer treatment.
- This study highlights the significant potential of nanoliposome drug delivery systems in advancing cancer therapy.
More Related Videos
08:35Therapeutic Gene Delivery and Transfection in Human Pancreatic Cancer Cells using Epidermal Growth Factor Receptor-targeted Gelatin Nanoparticles
Published on: January 4, 2012
08:03Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
Published on: December 1, 2016
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...