Formulation and Characterisation of pH-Sensitive Eudragit L-100 Nanoparticles for Quercetin Delivery in Lung Carcinoma
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Abstract
Quercetin is a flavonoid found abundantly in many vegetables and fruits. Quercetin is known for its antioxidant, anti-inflammatory, and anti-proliferative properties. The present study aims to formulate quercetin nanoparticles (Qu-NPs) for targeting lung carcinoma cells. Qu-NPs were formulated using the pH-sensitive polymer Eudragit® L-100. The physicochemical properties of the Qu-NPs were characterized by dynamic light scattering (DLS), Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). In vitro drug release of Qu-NPs was assessed using the dialysis bag method. Cytotoxic activity of Qu-NPs against non-small cell lung cancer cell line (NCI-H460), and normal human lung fibroblasts cell line (CCD-19Lu) was assessed using the 3-[4,5-dimethylthiazol-2-yl]2,5-diphenyltetrazolium bromide (MTT) assay. DLS results indicated a mean particle size of 242.86 ± 20.61 nm, zeta potential of -18.2 ± 2.97 mV and polydispersion index of 0.266 ± 0.008 for Qu-NPs. FT-IR spectra confirmed the presence of hydrogen bonds between quercetin and the polymer, which is crucial for drug entrapment and release. XRD and SEM analysis demonstrated the amorphous nature of quercetin within the nanoparticles. In vitro drug release studies revealed a sustained drug release across different pH conditions including simulated gastric fluid (pH 1.2), and intestinal fluid (pH 6.8, and pH 7.4). Cytotoxicity assay revealed a potent cytotoxic effect of Qu-NPs against NCI-H460. This study underscores the potential of Eudragit® L-100 nanoparticles (NPs) as carriers for quercetin in cancer therapy. It also highlights the potential of Qu-NPs for improved drug efficacy through targeted and controlled release.
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World Health Organisation (WHO). Global cancer burden growing, amidst mounting need for services. Available from: https://www.who.int/news/item/01-02-2024-global-cancer-burden-growing--amidst-mounting-need-for-services
Lancet T. GLOBOCAN 2018: Counting the toll of cancer. Lancet. 2018; 392(10152):985.
Siegel RL, Miller KD, Jemal A. Cancer statistics, 2019. CA Cancer J Clin. 2019; 69(1):7-34.
World Health Organisation (WHO). Cancer: Key Facts. Available from: https://www.who.int/news-room/fact-sheets/detail/cancer
Zappa C and Mousa SA. Non-small cell lung cancer: current treatment and future advances. Transl Lung Cancer Res 2016; 5(3):288-300.
Wu Q, Yang Z, Nie Y, Shi Y, Fan D. Multi-drug resistance in cancer chemotherapeutics: mechanisms and lab approaches. Cancer Lett. 2014; 347(2):159-166.
Anwer MK, Al-Mansoor MA, Jamil S, Al-Shdefat R, Ansari MN, Shakeel F. Development and evaluation of PLGA polymer based nanoparticles of quercetin. Int J Biol Macromol. 2016; 92:213-219.
Cetin M, Aktas Y, Vural I, Capan Y, Dogan LA, Duman M, Dalkara T. Preparation and in vitro evaluation of bFGF-loaded chitosan nanoparticles. Drug Deliv. 2017; 14(8):525-529.
Adibkia K, Javadzadeh Y, Dastmalchi S, Mohammadi G, Niri FK, Alaei-Beirami M. Naproxen-eudragit® RS100 nanoparticles: preparation and physicochemical characterization. Colloids Surf B Biointerfaces. 2017; 83(1):155-159.
Russo M, Spagnuolo C, Tedesco I, Bilotto S, Russo GL. The flavonoid quercetin in disease prevention and therapy: facts and fancies. Biochem Pharmacol. 2012; 83(1):6-15.
Cai X, Fang Z, Dou J, Yu A, Zhai G. Bioavailability of quercetin: problems and promises. Curr Med Chem. 2016; 20(20):2572-2582.
Mokale VJ, Naik JB, Verma U, Yadava SK. Preparation and characterization of biodegradable glimepiride loaded PLA nanoparticles by o/w solvent evaporation method using high pressure homogenizer: a factorial design approach. SA J Pharm Pharmacol. 2014; 1(1):1.
Adibkia K, Javadzadeh Y, Dastmalchi S, Mohammadi G, Niri FK, Alaei-Beirami M. Naproxen-eudragit® RS100 nanoparticles: preparation and physicochemical characterization. Colloids Surf B Biointerfaces. 2017; 83(1):155-159.
Song X, Zhao Y, Hou S, Xu F, Zhao R, He J, Cai Z, Li Y, Chen Q. Dual agents loaded PLGA nanoparticles: systematic study of particle size and drug entrapment efficiency. Eur J Pharm Biopharm. 2018; 69(2):445-453.
Xu X, Fu Y, Hu H, Duan Y, Zhang Z. Quantitative determination of insulin entrapment efficiency in triblock copolymeric nanoparticles by high-performance liquid chromatography. J Pharm Biomed Anal. 2016; 41(1):266-273.
Tantishaiyakul V, Phadoongsombut N, Kamaung S, Wongwisansri S, Mathurod P. Fourier transform infrared spectrometric determination of paracetamol and ibuprofen in tablets. Pharmazie. 1999; 54(2):111-114.
Panwar P, Pandey B, Lakhera PC, Singh KP. Preparation, characterization, and in vitro release study of albendazole-encapsulated nanosize liposomes. Int J Nanomed. 2019; 5:101-108.
Jain A, Khare P, Agrawal RK, Jain SK. Metronidazole loaded pectin microspheres for colon targeting. J Pharm Sci. 2009; 98(11):4229-4236.
van Meerloo J, Kaspers GJL, Cloos J. Cell Sensitivity Assays: The MTT Assay. In: Cree, I. (eds) Cancer Cell Culture. Methods in Molecular Biology, Humana Press. 2011; Vol 731.
Maeda H, Sawa T, Konno T. Mechanism of tumor-targeted delivery of macromolecular drugs, including the EPR effect in solid tumor and clinical overview of the prototype polymeric drug SMANCS. J Control Release. 2021; 74(1-3):47-61.
Cho K, Wang XU, Nie S, Chen Z, Shin DM. Therapeutic nanoparticles for drug delivery in cancer. Clin Cancer Res. 2018; 14(5):1310-1316.
Wicki A, Witzigmann D, Balasubramanian V, Huwyler J. Nanomedicine in cancer therapy: challenges, opportunities, and clinical applications. J Control Release. 2015; 200:138-157.
Chourasiya A, Upadhaya A, Shukla RN. Isolation of quercetin from leaves of Azadirachta indica and anti-diabetic study of the crude extracts. J Pharm Biomed Sci. 2018; 25:179-181.
Abd El-Rahmanand SN, Suhailah S. Quercetin nanoparticles: preparation and characterization. Indian J Drugs. 2016; 2(3):96-103.
Mohammadi G, Mirzaeei S, Taghe S, Mohammadi P. Preparation and Evaluation of Eudragit® L100 Nanoparticles Loaded Impregnated with KT Tromethamine Loaded PVA -HEC Insertions for Ophthalmic Drug Delivery. Adv Pharm Bull. 2019; 9(4):593-600.
Govender T, Stolnik S, Garnett MC, Illum L, Davis SS. PLGA nanoparticles prepared by nanoprecipitation: drug loading and release studies of a water soluble drug. J Control Release. 1999; 57(2):171-185.
Verma A and Stellacci F. Effect of surface properties on nanoparticle–cell interactions. Small. 2010; 6(1):12-21.
Kakran M, Sahoo NG, Bao H, Pan Y, Li L. Functionalized graphene oxide as nanocarrier for loading and delivery of ellagic acid. Curr Med Chem. 2021; 18(29):4503-4512. doi:10.2174/092986711797287548.
Zhang T, Ma J, Li C, Lin K, Lou F, Jiang H, Gao Y, Yang Y, Ming C, Ruan B. Coreshell lipid polymer nanoparticles for combined chemo and gene therapy of childhood head and neck cancers. Oncol Rep. 2017; 37(3):1653-1661.
Trenkenschuh E and Friess W. Freeze-drying of nanoparticles: How to overcome colloidal instability by formulation and process optimization. Eur J Pharm Biopharm. 2021; 165:34.
Moustafine RI, Zaharov IM, Kemenova VA. Physicochemical characterization and drug release properties of Eudragit® E PO/Eudragit® L 100-55 interpolyelectrolyte complexes. Eur J Pharm Biopharm. 2006; 63(1):26-36.
Pecorini G, Ferraro E, Puppi D. Polymeric Systems for the Controlled Release of Flavonoids. Pharmaceutics. 2023;15(2):628.
Derakhshandeh K, Soheili M, Dadashzadeh S, Saghiri R. Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients. Int J Nanomedicine. 2010; 5:463-471.