Naringenin-Loaded Chitosan Nanoparticles Formulation, and Its in Vitro Evaluation Against T47d Breast Cancer Cell Line

, S. TAMIZHARASI, T. SIVAKUMAR Nandha College of Pharmacy and Research Institute, Erode 630052, Tamilnadu, IndiaEmail: sumoraji@gmail.comObjective: The objective of this study was to formulate and evaluate the poorly soluble drug, naringenin (NAR) into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspenion of naringenin (NARNS) was prepared using high-pressure homogenization method using Soya lecithin, Polaxamer-407, Polaxamer-188, Hydroxypropyl methyl cellulose (HPMC) and Tween-80. Ten formulations were prepared to show the effect of stabilizer and its ratio. D-α-Tocopheryl polyethene glycol succinate 1000 (TPGS) was added as a co-stabilizer. All these formulations were evaluated for their particle size, PDI, zeta potential, FT-IR study, drug content, saturation solubility studies, entrapment efficiency, in vitro permeability and in vitro drug release. The formulation was further evaluated for scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Powder X-ray diffraction (P-XRD) and hemocompatibility assessment.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation was found 1:1.5:1 (drug: stabilizer: co-stabilizer ratio). Dramatic effect of the particle size reduction was found by the addition of the co-stabilizer (TPGS) in formulation N2 that has P. S 80.52±0.13 nm. The solubility and dissolution of NAR in the form of NARNS were significantly higher than those of pure NAR. SEM report shows that naringenin nanosuspension revealed a smooth texture. P-XRD crystallography diffraction and DSC studies indicated that the crystalline state of NAR was converted into amorphous nature. The safety evaluation showed that NARNS provided a lower rate of erythrocyte hemolysis.Keywords: Naringenin, High-Pressure Homogenization, Nanosuspenion, Solubility, Bioavailability Conclusion:In this study, (NARNS) was successfully carried out by high-pressure homogenization technique and characterized. The physiochemical characterization shown that crystalline naringenin was converted to a polymorphic form (DSC and P-XRD Study) which evidenced by enhanced dissolution rate in comparisons of the formulation with (NAR) pure drug. The NARNS has shown 7.5±0.4 fold increased relative bioavailability when compared to the NAR. The increased drug dissolution rate may have a significant impact in absorption which in turn the improved oral bioavailability of naringenin. Thus, this delivery system may prefer to improve the dissolution of poorly soluble drugs like NAR and thus enhanced oral bioavailability. The safety evaluation showed that nanoformulation (NF2) shows a lower rate of erythrocyte hemolysis. These findings suggest that the selected formulation may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.

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“…The samples were scanned over a frequency range 4000-400 cm -1 Formulation of naingnin nanosuspension [19].…”

Section: Preparation Of Calibration Curvesmentioning

confidence: 99%

Formulation and Evaluation of Polymeric Nanosuspension of Naringenin

Sumathi¹,

Sengodan²,

Sivakumar³

2017

Int J App Pharm

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“…In particular, the advancement of oncological therapy has drawn attention to the use of nanoparticles made of biodegradable polymer materials like chitosan (CS). D-glucosamine and N-acetyl-D-glucosamine, which were joined by a (1,4) glycosidic link, each make up two subunits of CS [52,58]. Because it provides a strong and reactive positive charge, the amine group on the glucosamine unit of the CS is a crucial component.…”

Section: Sdh Target For Anticancer Therapymentioning

confidence: 99%

The Regulation Impact of Naringenin-loaded Chitosan Nanoparticles on Succinate Dehydrogenase Activity in Cancer Cells

Ragab,

Khamis,

El Gamal

et al. 2023

J Cell Immunol

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Oxidative phosphorylation dysregulation (OXPHOS) has been demonstrated to be essential for the development of cancer. Therefore, it may be argued that chaperone and deacetylase activities modulate OXPHOS activity. For instance, a complicated network of interactions connects a cell’s bioenergetic features and neoplastic potential through the imbalance of sirtuin 3 (SIRT3) and succinate dehydrogenase (SDH) enzymatic activity in mitochondria. The studies outlined in this review indicate that targeting SDH regulators is a promising novel therapeutic strategy for this extremely resistant disease. Additionally, a viable therapeutic strategy may involve triggering the cell death mechanism in cancer cells by blocking mitochondrial metabolism with a natural substance. A naturally occurring flavonoid called naringenin (NAR) has been extensively investigated for its pharmacological properties, which include anti-tumor actions. However, due to its low bioavailability in this situation, nanoencapsulation is designed to improve NAR anticancer efficacy. NAR can be encapsulated by chitosan nanoparticles-TPP conjugates, thereby improving NAR cellular absorption and cytotoxicity against cancer cells. Consequently, we proposed naringenin nanoparticles as a novel therapeutic target for SDH regulators in cancer.

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“…T47D breast cancer cell line was used for the research and was found that the encapsulated naringenin showed an increased cell toxic effect. Also, it resulted in the increased cellular uptake and caused induction in the programmed cell death [78].…”

Section: Naringeninmentioning

confidence: 99%

Nanoparticle Formulation of Bioflavonoids for Enhanced Anti-Cancer Activity

et al. 2020

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Among the natural sources, plant origin drugs constitute around 25% which includes various secondary metabolites such as bioflavonoids, alkaloids, terpenes, saponins, glucosides, and lignans. The bioflavonoids belonging to the polyphenol group shows many beneficial effects like hepatoprotective, antioxidant, antibacterial, anticancer, anti-inflammatory and antiviral. The main objective of this article is to collectively present the research data published worldwide about the anticancer activity of bioflavonoids by loading them in novel formulations. Thus, the present review explored the novel formulations of the bioflavonoids with improved pharmacokinetic properties along with the enhanced anticancer activity. The major drawback with bioflavonoids is its poor solubility and bioavailability, which restricts the usage of bioflavonoids in the treatment of cancer in the market worldwide. Novel drug delivery system seems to possess many benefits like site-specific drug delivery along with minimal side effects and improves pharmaceutical and therapeutic properties of drugs compared to a conventional dosage form of bioflavonoids. The scope for improvement of anticancer activity of bioflavonoids by incorporating in novel pharmaceutical formulations like nanoparticles is very high, and it has to be considered as a potential area of research.

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Naringenin-Loaded Chitosan Nanoparticles Formulation, and Its in Vitro Evaluation Against T47d Breast Cancer Cell Line

Cited by 13 publications

References 22 publications

Formulation and Evaluation of Polymeric Nanosuspension of Naringenin

Formulation and Evaluation of Polymeric Nanosuspension of Naringenin

The Regulation Impact of Naringenin-loaded Chitosan Nanoparticles on Succinate Dehydrogenase Activity in Cancer Cells

Nanoparticle Formulation of Bioflavonoids for Enhanced Anti-Cancer Activity

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