Characteristics and anticancer properties of Sunitinib malate-loaded poly-lactic-co-glycolic acid nanoparticles against human colon cancer HT-29 cells lines

Abdullah S Alshetaili,Sultan Alshehri,Faisal Imam,Bader B Alsulays,Md Khalid Anwer,Ahmed Alalaiwe,Saad M Alshahrani,Mohammad Javed Ansari

doi:10.4314/tjpr.v17i7.6

Abdullah S Alshetaili, Sultan Alshehri + Show 6 more

Open Access

https://doi.org/10.4314/tjpr.v17i7.6

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Abstract

Purpose : To develop poly-lactic-co-glycolic acid (PLGA) -based nanoparticles (NPs) for the delivery of sunitinib malate (STM) to colon cancer cells. Methods : Three different formulations (F1 – F3) were developed by nano-precipitation technique using various concentrations of PLGA. The NPs were evaluated for particle size, polydispersity index, zeta potential, drug entrapment, and drug loading, using differential scanning calorimetry (DSC), Fouriertransform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). Furthermore, in vitro drug release and anticancer studies were carried out on the formulations. Results : Among the three NPs, optimized NP (F3) of STM was chosen for in vitro anti-cancer study against H-29 human colon cancer cells lines based on its particle size (132.9 nm), PDI (0.115), zeta potential (-38.12 mV), entrapment efficiency (52.42 %), drug loading (5.24 %), and drug release (91.26 % in 48 h). A significant anti-cancer activity of the optimized NPs was observed, relative to free STM. Conclusion : These findings suggest that STM-loaded NPs possess significant anti-cancer activity against human colon cancer HT-29 cells lines. Keywords : Sunitinib malate, Poly-lactic-co-glycolic acid, Nanoparticles, Colon cancer

Highlights

Colorectal cancer (CRC) is the second main cause of malignancy-related death in the U.S and in developing nations [1,2]
Sunitinib malate (STM) is an orally-active compound approved by United States Food and Drug Administration (USFDA) as therapy for renal cell carcinoma and GIT stromal tumors
A successful attempt aimed at enhancing the solubility, dissolution, safety, and efficacy of the sunitinib malate through polymeric NP formations directly will improve the oral bioavailability of the drug, which, in turn, will reduce dosage and frequency

Summary

Introduction

Colorectal cancer (CRC) is the second main cause of malignancy-related death in the U.S and in developing nations [1,2]. Sunitinib malate (STM) is an orally-active compound approved by United States Food and Drug Administration (USFDA) as therapy for renal cell carcinoma and GIT stromal tumors. It. it would be beneficial to develop formulations that could deliver STM in a controlled manner for extended periods of time. It would be beneficial to develop formulations that could deliver STM in a controlled manner for extended periods of time This is difficult due to its poor watersolubility which limits its release, leading to instability. A successful attempt aimed at enhancing the solubility, dissolution, safety, and efficacy of the sunitinib malate through polymeric NP formations directly will improve the oral bioavailability of the drug, which, in turn, will reduce dosage and frequency. Poly-lactic-coglycolic acid (PLGA) is a biocompatible and biodegradable polymer frequently used in drug development due to its high solubility, encapsulation efficiency, controlled release, and low toxicity [12,13]

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