Related Experiment Video
Updated: Jul 1, 2025
Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Atorvastatin-loaded cubosome: a repurposed targeted delivery systems for enhanced targeting against breast cancer
Eman M El-Marakby1, Hend Fayez2, M A Motaleb2
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Abstract:
Cancer ranks as one of the most challenging illnesses to deal with because progressive phenotypic and genotypic alterations in cancer cells result in resistance and recurrence. Thus, the creation of novel medications or alternative therapy approaches is mandatory. Repurposing of old drugs is an attractive approach over the traditional drug discovery process in terms of shorter drug development duration, low-cost, highly efficient and minimum risk of failure. In this study Atorvastatin, a statin drug used to treat abnormal cholesterol levels and prevent cardiovascular disease in people at high risk, was introduced and encapsulated in cubic liquid crystals as anticancer candidate aiming at sustaining its release and achieving better cellular uptake in cancer cells. The cubic liquid crystals were successfully prepared and optimized with an entrapment effieciency of 73.57% ±1.35 and particle size around 200 nm. The selected formulae were effectively doped with radioactive iodine 131I to enable the noninvasive visualization and trafficking of the new formulae. The in vivo evaluation in solid tumor bearing mice was conducted for comparing131I-Atorvastatin solution,131I-Atorvastatin loaded cubosome and 131I-Atorvastatin chitosan coated cubosome. The in vivo biodistribution study revealed that tumor radioactivity uptake of 131I-Atorvastatin cubosome and chitosan coated cubosome exhibited high accumulation in tumor tissues (target organ) scoring ID%/g of 5.67 ± 0.2 and 5.03 ± 0.1, respectively 1h post injection compared to drug solution which recorded 3.09 ± 0.05% 1h post injection. Concerning the targeting efficiency, the target/non target ratio for 131I-Atorvastatin chitosan coated cubosome was higher than that of 131I-Atorvastatin solution and 131I ATV-loaded cubosome at all time intervals and recorded T/NT ratio of 2.908 2h post injection.
Insights
Drug repurposing offers a promising avenue for cancer therapy. This study successfully developed atorvastatin-loaded cubic liquid crystals, demonstrating enhanced tumor accumulation and targeting efficiency in preclinical models for improved cancer treatment.
Area of Science:
- Nanotechnology
- Drug Delivery
- Oncology
Background:
- Cancer recurrence and resistance necessitate novel therapeutic strategies.
- Drug repurposing presents a cost-effective and efficient alternative to traditional drug discovery.
- Atorvastatin, a statin, is explored for its potential anticancer properties.
Purpose of the Study:
- To develop and characterize atorvastatin-loaded cubic liquid crystals for sustained release and enhanced cellular uptake in cancer cells.
- To enable non-invasive visualization and tracking of the drug delivery system using radioactive iodine (¹³¹I).
- To evaluate the in vivo efficacy and targeting potential of the novel formulation in a preclinical cancer model.
Main Methods:
- Atorvastatin was encapsulated in cubic liquid crystals, optimized for entrapment efficiency and particle size.
- The optimized formulations were doped with ¹³¹I for in vivo imaging.
- Biodistribution studies in tumor-bearing mice compared ¹³¹I-Atorvastatin solution, cubosomes, and chitosan-coated cubosomes.
Main Results:
- Cubic liquid crystals with 73.57% ±1.35 entrapment efficiency and ~200 nm particle size were successfully prepared.
- In vivo studies showed significantly higher tumor radioactivity uptake for ¹³¹I-Atorvastatin cubosomes (5.67% ±0.2 ID%/g) and chitosan-coated cubosomes (5.03% ±0.1 ID%/g) at 1h post-injection compared to the drug solution (3.09% ±0.05 ID%/g).
- Chitosan-coated cubosomes demonstrated superior targeting efficiency, with a target/non-target ratio of 2.908 at 2h post-injection.
Conclusions:
- Atorvastatin-loaded cubic liquid crystals represent a viable drug delivery system for enhancing anticancer efficacy.
- The ¹³¹I-labeled formulations allow for effective non-invasive monitoring of drug biodistribution and tumor targeting.
- Chitosan coating further improves the targeting potential of atorvastatin cubosomes, offering a promising strategy for cancer therapy.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
01:15Drugs that Stabilize Microtubules