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Published on: February 19, 2016
Targeting Solid Lipid Nanoparticles with Anisamide for Docetaxel Delivery to Prostate Cancer: Preparation,
Milad Jalilian1, Katayoun Derakhshandeh1,2, Masoumeh Kurd3
1Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Abstract:
The purpose of the current study was to prepare and characterize the targeted solid lipid nanoparticles (SLNs) containing docetaxel (DTX) for prostate cancer treatment. The goal has been achieved by locating anisamide (Anis) ligand on the surface of SLNs, which can interact with the overexpressed sigma receptor on the prostate cancer cells. DTX loaded SLNs were prepared by high shear homogenization and ultra-sonication method and optimized by applying experimental design. The average particle size and the entrapment efficiency of the optimum DTX-SLN were 174 ± 9.1 nm and 83 ± 3.34%, respectively. The results of differential scanning calorimetry showed that DTX had been dispersed as amorphous in the nanocarriers. Scanning electron microscopy (SEM) images confirmed the nanoscale size and spherical shape of the nanoparticles. The cytotoxicity studies have demonstrated that IC50 of free drug, DTX-SLN and DTX-SLN-Anis was 0.25 ± 0.01, 0.23 ± 0.02, 0.12 ± 0.01 nM on PC3 cell line and 20.9 ± 3.89, 18.74 ± 7.43, and 14.68 ± 5.70 nM on HEK293 cell line, respectively. Targeted DTX-SLN-Anis was acted more effectively on prostate cancer cells in comparison to DTX-SLN and free drug. The results of this study have depicted that the anti-cancer drug loaded in targeted SLNs can be a promising way for cancer treatment. In addition, performing in-vivo studies will be complementary to these findings.
Insights
Targeted solid lipid nanoparticles (SLNs) loaded with docetaxel (DTX) and anisamide (Anis) show enhanced efficacy against prostate cancer cells. This targeted drug delivery system offers a promising approach for more effective cancer treatment.
Area of Science:
- Nanotechnology
- Pharmacology
- Oncology
Background:
- Prostate cancer treatment faces challenges with conventional drug delivery.
- Targeted drug delivery systems can improve therapeutic efficacy and reduce side effects.
- Solid lipid nanoparticles (SLNs) offer a promising platform for encapsulating anti-cancer drugs.
Purpose of the Study:
- To prepare and characterize docetaxel (DTX)-loaded solid lipid nanoparticles (SLNs) targeted with anisamide (Anis) for prostate cancer treatment.
- To evaluate the efficacy of targeted DTX-SLNs against prostate cancer cells.
- To investigate the potential of anisamide-functionalized SLNs for enhanced drug delivery.
Main Methods:
- Docetaxel (DTX) loaded SLNs were prepared using high shear homogenization and ultra-sonication.
- Anisamide (Anis) ligand was conjugated to the surface of SLNs for targeted delivery.
- Particle size, entrapment efficiency, drug dispersion, morphology, and cytotoxicity were evaluated.
- Experimental design was employed for optimization of the DTX-SLN formulation.
Main Results:
- Optimized DTX-SLNs exhibited an average particle size of 174 ± 9.1 nm and an entrapment efficiency of 83 ± 3.34%.
- Differential scanning calorimetry confirmed the amorphous dispersion of DTX within the nanocarriers.
- Scanning electron microscopy (SEM) images revealed spherical nanoparticles of nanoscale dimensions.
- Targeted DTX-SLN-Anis demonstrated significantly higher cytotoxicity against PC3 prostate cancer cells (IC50 = 0.12 ± 0.01 nM) compared to DTX-SLN and free DTX.
Conclusions:
- Targeted DTX-SLN-Anis exhibits superior efficacy against prostate cancer cells compared to non-targeted SLNs and free DTX.
- The developed targeted SLN formulation represents a promising strategy for enhancing prostate cancer therapy.
- Further in-vivo studies are recommended to complement these findings and assess clinical potential.

