NANOPARTICLE PREPARATION OF SIAM CITRUS PEEL EXTRACT (CITRUS NOBILIS L. VAR. MICROCARPA) USING SHORT-CHAIN CHITOSAN AND TRIPOLYPHOSPHATE AS CROSS LINKER AND CELLULAR UPTAKE STUDY ON MCF-7 CELL LINE BY IN VITRO

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI:10.22159/ijap.2024v16i1.49487

Wintari Taurina, Mohamad Andrie

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引用次数: 0

Abstract

Objective: High consumption of oranges causes a lot of orange peel waste. Orange peel contains the compound naringenin, which has a cytotoxic effect on various cancer cells. This research aims to develop a preparation of Siamese orange peel extract nanoparticles with short-chain chitosan and tripolyphosphate carriers as an oral drug delivery system and determine its cytotoxic activity against the Michigan Cancer Foundation-7 (MCF-7) cell line. Methods: This research uses the micro tetrazolium (MTT) method to see the cytotoxic activity extract of methanol obtained from maceration extraction. The extract was then formulated into nanoparticles using chitosan and tripolyphosphate. Characterization and evaluation of nanoparticles were carried out, including particle size, zeta potential, entrapment efficiency, and stability in the stomach using 0.1 N HCl and in the intestine using Artificial Intestinal Fluid (AIF) in vitro. This research was also conducted to assess the ability of nanoparticles to enter MCF-7 cells (cellular uptake). Results: Nanoparticles were successfully developed from Siamese orange peel extract. The results of the day 0 nanoparticle characterization were spherical, with average particle size 284.3 nm, zeta potential 0.713 mV, entrapment efficiency 96.73%, and stability in 0.1 N HCl at the 0th hours, respectively. 1st, 2nd, and 3rd. 99.16%, 98.70%, 98.47%, 98.31%, stability on AIF at hours 0, 1, 2, 3 and 4 respectively 99.52%, 99.30%, 99.40%, 98.99%, 99.29%. Characterization of nanoparticles on day 25 showed that the average particle size was 196.2 nm, zeta potential 0.476 mV, entrapment efficiency 96.92%, stability in 0.1 N HCl at 0, 1, 2 and 3 h respectively 99.51%, 98.67%, 98.51%, 98.27%, stability in AIF at 0th, 1st, 2nd, 3rd, and 4th hours 99.24 respectively %, 98.76%, 98.46%, 97.93%, 97.58%. Cytotoxic activity of extract Siamese citrus peel against MCF-7 cells with IC50 of 290.58 µg/ml. The result shows that cellular uptake of Siamese citrus peel nanoparticles can penetrate MCF-7 cells. Conclusion: Stable nanoparticles were successfully developed from Siamese orange peel extract, and their stability was maintained throughout a 30-day storage period. This extract displayed cytotoxic effects and showcased the ability for cellular uptake in MCF-7 cell cultures in vitro.

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使用短链壳聚糖和三聚磷酸钠作为交联剂制备暹罗柑果皮提取物（Citrus nobilis l. var. microcarpa）的纳米颗粒，并通过体外实验研究细胞对 mcf-7 细胞系的吸收情况

目的：大量食用橘子会造成大量橘皮废物。橘皮含有化合物柚皮苷，对多种癌细胞有细胞毒性作用。本研究旨在开发一种以短链壳聚糖和三聚磷酸钠为载体的暹罗橘皮提取物纳米粒子的制备方法，作为口服给药系统，并测定其对密歇根癌症基金会-7（MCF-7）细胞系的细胞毒活性：本研究采用微量四氮唑（MTT）法检测浸渍提取的甲醇提取物的细胞毒性活性。然后用壳聚糖和三聚磷酸钠将提取物配制成纳米颗粒。研究人员对纳米颗粒进行了表征和评估，包括粒度、ZETA电位、夹带效率以及在胃中使用 0.1 N HCl 和在肠道中使用人工肠液（AIF）的体外稳定性。这项研究还评估了纳米颗粒进入 MCF-7 细胞的能力（细胞摄取）：结果：从暹罗橙皮提取物中成功开发出了纳米颗粒。第 0 天的纳米颗粒表征结果为球形，平均粒径为 284.3 nm，zeta 电位为 0.713 mV，夹带效率为 96.73%，在 0.1 N HCl 中的稳定性分别为第 1、2 和 3 小时。第 1 次、第 2 次和第 3 次。99.16%、98.70%、98.47%、98.31%，第 0、1、2、3、4 小时在 AIF 上的稳定性分别为 99.52%、99.30%、99.40%、98.99%、99.29%。第 25 天的纳米颗粒表征显示，平均粒径为 196.2 nm，zeta 电位为 0.476 mV，夹带效率为 96.92%，在 0.1 N HCl 中 0、1、2 和 3 小时的稳定性分别为 99.51%、98.67%、98.51%、98.27%，在 AIF 中 0、1、2、3 和 4 小时的稳定性分别为 99.24%、98.76%、98.46%、97.93%、97.58%。暹罗柑提取物对 MCF-7 细胞的细胞毒活性 IC50 为 290.58 µg/ml。结果表明，暹罗柑橘皮纳米颗粒可穿透 MCF-7 细胞，并被细胞吸收：结论：从暹罗橘皮提取物中成功开发出稳定的纳米粒子，并在 30 天的储存期内保持稳定。该提取物具有细胞毒性作用，并能在体外培养的 MCF-7 细胞中被细胞吸收。

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来源期刊

International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

CiteScore

1.40

自引率

0.00%

发文量

219

期刊介绍： International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.