Folate-decorated, endostatin-loaded, nanoparticles for anti-proliferative chemotherapy in esophaegeal squamous cell carcinoma
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Published on: February 9, 2019
Samson A Adeyemi1, Yahya E Choonara1, Pradeep Kumar1
1Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Science, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.
Abstract:
This study aims to design and synthesize Endostatin (ENT)-loaded nanoparticles using Folic acid (FA) as a driver for targeted anti-proliferative chemotherapy in Esophageal Squamous Cell Carcinoma (ESCC). An ionic gelation method was employed to formulate FA-decorated, ENT-loaded nanoparticles, which were tested in vitro on KYSE-30 cells using unbiased stereological approaches. FA-ENT nanoparticles were internalized into ESCC cells with preferential binging to the nucleus and mitochondria for necrotic and apoptotic effects. Nanoparticles showed increased proliferation inhibition of 64.71% and reduced KYSE-30 cell migration of up to 74.12% when compared to the control. Positively charged spherical nanoparticles, with selective pH responsive ENT release, were further tested in vivo employing a tumor xenograft model. Tumor mass increased up to 5505.54 mm3 in the control group while a substantial reduction occurred in the treatment group (native ENT, ENT-nano and FA-ENT-nano) down to 128.23 mm3 (97.67%). Tumor volume was reduced from 1000.2 mm3 to 567.64 mm3 (43.25%) in the native ENT group, from 324.43 mm3 to 190.25 mm3 (41.36%) in ENT-nano group (non-targeted system), and from 1374.21 mm3 to 998.67 mm3 (27.33%) in FA-ENT-nano group (targeted system) following treatment. There were no significant differences in the body weight of mice treated with the nano-formulations as opposed to the control mice. FA-decorated nanoparticles for active transport of ENT into tumor cells with an enhanced in vitro and in vivo anti-proliferative efficacy in ESCC therapy were synthesized.
Insights
Folic acid-decorated nanoparticles carrying Endostatin show enhanced anti-cancer effects against Esophageal Squamous Cell Carcinoma. This targeted chemotherapy approach effectively inhibits tumor proliferation and migration in vitro and in vivo.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Esophageal Squamous Cell Carcinoma (ESCC) presents a significant therapeutic challenge.
- Targeted drug delivery systems offer potential for enhanced chemotherapy efficacy.
- Endostatin (ENT) is a potent anti-angiogenic and anti-proliferative agent.
Purpose of the Study:
- To design and synthesize Folic acid (FA)-decorated, Endostatin (ENT)-loaded nanoparticles for targeted ESCC chemotherapy.
- To evaluate the in vitro and in vivo anti-proliferative efficacy of these targeted nanoparticles.
Main Methods:
- Nanoparticles were formulated using an ionic gelation method with FA decoration.
- In vitro studies utilized KYSE-30 ESCC cells and unbiased stereological methods.
- In vivo studies involved a tumor xenograft model in mice.
Main Results:
- FA-ENT nanoparticles demonstrated significant internalization into ESCC cells, targeting the nucleus and mitochondria.
- In vitro studies showed increased proliferation inhibition (64.71%) and reduced cell migration (74.12%).
- In vivo studies revealed substantial tumor mass reduction (97.67%) with FA-ENT nanoparticles, with no adverse effects on body weight.
Conclusions:
- FA-decorated nanoparticles facilitate active transport of ENT into tumor cells.
- The developed nano-formulation exhibits enhanced in vitro and in vivo anti-proliferative efficacy for ESCC therapy.
- Targeted delivery via FA-functionalized nanoparticles represents a promising strategy for ESCC treatment.
