scholarly journals FORMULASI, EVALUASI, SERTA UJI SITOTOKSIK TERHADAP SEL KANKER MCF-7 DARI SISTEM NANOPARTIKEL POLIMERIK POLYVINYL PYRROLIDONE DENGAN ZAT AKTIF KURKUMIN (Formulation of Polymeric Nanoparticles System Polyvinyl Pyrrolidone Containing Curcumin as Active Ingredient, Its Evaluation and Cytotoxicity Test on MCF-7 Cancer Cells)

2013 ◽  
Vol 3 (3) ◽  
Author(s):  
Yenni Puspita Tanjung

AbstrakDalam beberapa tahun terakhir pengembangan sistem pembawa obat inovatif telah banyak dilakukan untuk mengatasi buruknya kelarutan suatu zat aktif. Salah satu contoh yang banyak mendapat perhatian adalah sistem pembawa obat berbasis nanopartikel. Pada penelitian ini dibuat suatu sistem nanopartikel dengan menggunakan pembawa polimer polyvinyl pyrrolidone (PVP). Polyvinyl pyrrolidone dapat digunakan sebagai solubilizer dan telah terbukti kemampuannya dalam meningkatkan disolusi dari obat yang memiliki kelarutan rendah. Zat aktif yang digunakan adalah kurkumin. Kurkumin penerapannya terbatas karena tidak larut dalam air, sedangkan potensinya sangat baik sebagai obat pada beberapa penyakit termasuk kanker. Formula dibuat dengan memvariasikan jumlah PVP dimana kurkumin banding PVP adalah (1:2), (1:6), dan (1:10). Prosedur pembuatan sistem nanopartikelnya adalah dengan melarutkan PVP ke dalam larutan PVA 0,1% sedangkan kurkumin dilarutkan dengan etanol. Selanjutnya dilakukan proses homogenisasi, sonikasi, dan pengadukan mekanik serta penguapan pelarut. Sistem nanopartikel ini dikarakterisasi ukuran partikelnya dengan alat PSA. Persentase enkapsulasi ditetapkan dengan HPLC. Formulasi yang menghasilkan sistem nanopartikel polimerik dengan ukuran partikel terkecil  yaitu 31,6 nm adalah formula X (Kurkumin 50 mg, PVP 500 mg, etanol 25 ml, dan larutan PVA 0,1% 75 ml) dengan proses homogenisasi kecepatan 17.000 rpm selama 12 menit 30 detik, sonikasi selama 30 menit, pengadukan mekanik selama 2 jam dan penguapan pelarut. Persen enkapsulasi kurkumin dari formula X adalah 98%. Pada penelitian ini dilakukan uji sitotoksik menggunakan sel kanker MCF-7 dimana hasilnya adalah kurkumin nanopartikel (IC50 1,7 ppm) memiliki efek sitotoksik yang lebih baik dibandingkan dengan kurkumin non nanopartikel (IC50 11,7 ppm). Untuk pengujian cellular uptake menghasilkan kurkumin nanopartikel memiliki kemampuan cellular uptake yang lebih baik dibandingkan dengan kurkumin non nanopartikel. Kata kunci : nanopartikel, kurkumin, ukuran partikel, sitotoksik.AbstractIn the last few years, an innovative development of drug carrier system has been done to overcome poor solubility of active ingredients. An interesting example of it is drug delivery system based nanoparticle. In this research a nanoparticle system was made by using a polymers polyvinyl pyrrolidone (PVP), which can be used as solubilizer and has proven its ability to improve dissolution of low solubility drugs. Curcumin is used as active ingredient. This compound is not dissolved in water, while its potential is very good as medicine in some diseases including cancer. The formula were prepared with various amount of PVP where curcumin comparation PVP were (1:2), (1:6), and (1:10). Nanoparticle system was created by dissolving PVP into PVA 0.1% solution, while curcumin was dissolved in ethanol. The procedure was continued with homogenizing, sonicating, mechanical stirring and solvent evaporating. Particle size the system were characterized by PSA. Encapsulation efficiency of curcumin was measured by HPLC. The best nanoparticle formula with (particle size 31.6 nm) was formula X (contained curcumin 50 mg, PVP 500 mg, ethanol 25 ml, and solution PVA 0.1 % 75 ml) which was made by homogenization speed 17,000 rpm for 12 minutes 30 seconds, sonication 30 minutes, stirring mechanics 2 hours, percent encapsulation of curcumin 98%. Both the cellular uptake ability and the cytotoxicity of this nanoparticle curcumin on MCF-7 cancer cells was better than non-nanoparticle system, with IC50 1.7 ppm and IC50 11.7 ppm, respectively.  Key words : nanoparticle, curcumin, Polyvinyl Pyrrolidone (PVP), cytotoxic.

Biomaterials ◽  
2010 ◽  
Vol 31 (13) ◽  
pp. 3657-3666 ◽  
Author(s):  
Chunbai He ◽  
Yiping Hu ◽  
Lichen Yin ◽  
Cui Tang ◽  
Chunhua Yin

Author(s):  
Elham Kamalkazemi ◽  
Fereydoon Abedi - Gaballu ◽  
Tala Farid Mohammad Hosseini ◽  
Ali Mohammadi ◽  
Behzad Mansoori ◽  
...  

: Lipid-based nanoparticles as drug delivery carriers have been mainly used for delivery of anti-cancer therapeutic agents. Lipid-based nanoparticles, due to their smaller particle size and similarity to cell membranes, are readily internalized into cancer cells. Interestingly, cancer cells also overexpress receptors for specific ligands including folic acid, hyaluronic acid, and transferrin on their surface. This allows the use of these ligands for surface modification of the lipid-based nanoparticle. These modifications then allow the specific recognition of these ligand-coated nanoparticles by their receptors on cancer cells allowing the targeted gradual intracellular accumulation of the functionalized nanoplatforms. These interactions could eventually enhance the internalization of desired drugs via increasing ligand-receptor mediated cellular uptake of the nanoplatforms. The cellular internalization of the nanoplatforms also varies and depends on their physicochemical properties including particle size, zeta potential, and shape. The cellular uptake is also influenced by the types of ligand internalization pathway utilized by cells such as phagocytosis, macropinocytosis, and multiple endocytosis pathways. In this review, we will classify and discuss lipid based nanoparticles engineered to express specific ligands, and are recognized by their receptors on cancer cell, and their cellular internalization pathways. Moreover, the intracellular fate of nanoparticles decorated with specific ligands and the best internalization pathways (caveolae mediated endocytosis) for safe cargo delivery will be discussed.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 3021 ◽  
Author(s):  
Lei Xu ◽  
Shengnan Xiao ◽  
Weihui Yuan ◽  
Jiongmo Cui ◽  
Guangyue Su ◽  
...  

To increase the antitumor activity of ginsenosides and acetylsalicylic acid, acid hydrolysis products of Panaxnotoginseng saponin were used as raw materials to be combined with salicylic acid to obtain ginsenoside salicylic acid derivatives. All derivatives were assessed for anti-cancer activity. A total of 20 target compounds were designed and synthesized. The cytotoxic activity on five cancer cell lines, including human colon cancer (HT-29), gastric cancer (BGC-823), cervical cancer (Hela), human breast cancer (MCF-7), human lung cancer cells (A549), and two normal cancer cell lines (human gastric epithelial cells (GES-1), and human ovarian epithelial cells (IOSE144)) was evaluated following treatment with the compounds. The results showed that all compounds inhibited the growth of cancer cells. Compounds 1a, 3a, 7a, 1b, 2b, 3b and 8b showed strong anticancer activity. For MCF-7 cells, compound 3b showed the strongest inhibitory activity, IC50 = 2.56 ± 0.09 μM. In the cytotoxicity test, all compounds showed low toxicity or no toxicity (IC50 > 100 μM). In addition, a cell cycle distribution assay and wound healing assay demonstrated that compound 3b specifically inhibited MCF-7 proliferation and migration ability. Our results indicate that compound 3b represents a promising compound for further cancer studies.


2019 ◽  
Vol 16 (1) ◽  
pp. 185-195
Author(s):  
Nihal S Elbialy

Curcumin as a natural medicinal agent has been proved to kill cancer cells effectively. However, its biomedical applications have been hindered owing to its poor bioavailability. Many nanoparticulate systems have been introduced to overcome this problem. Among this types polymeric-based nanoparticles which exhibit unique properties allowing their use as a efficient drug carrier. Developing a polymeric- blend nanoparticles will offer a promising nanocarrier with excellent biocompatibility, biodegradability and low immunogencity. In this study, curcumin nano-vehicle has been made up by combining dextren sulfate and chitosan (DSCSNPs). DSCSNPs have been characterized using different techniques. Transmission electron microscopy (TEM) which revealed the spherical, smooth surface of the nano-formulation. Dynamic light scattering (DLS) for measuring DSCSNPs hydrodynamic- diameter. Zeta potential measurements showed nanoparticles high stability. Fourier transform infrared spectroscopy (FTIR) confirmed  successful combination between the two polymers and curcumin loading on naoparticles surface. Curcumin release profile out of DSCSNPs showed high drug release in tumor acidic microenvironment. In vitro cytotoxicity measurements demonstrated that curcumin loaded polymeric nanoparticles (DSCSNPs-Cur) have high therapeutic efficacy against colon (HCT-116) and breast  (MCF-7) cancer cells compared with free curcumin.  DSCSNPs as a combined biopolymers is an excellent candidate for improving curcumin bioavailability  allowing its use as anticancer  agent.


Elkawnie ◽  
2020 ◽  
Vol 6 (1) ◽  
pp. 48 ◽  
Author(s):  
Vivi Mardina ◽  
Tisna Harmawan ◽  
Halimatussakdiah Halimatussakdiah ◽  
Syafruddin Ilyas ◽  
Masitta Tanjung

Abstract : Sphagneticola trilobata (L.) J.F. Pruski is one of the perennial herbs that is widely used by the national and international community to treat various diseases including cancer. The objective of this study was to assessment the anticancer activity of n-hexane extract of S. trilobata leaves for inhibiting the growth of MCF-7 breast cancer cells in vitro by MTT (microculture tetrazolium salt) method. The n-hexane extract of sernai leaves was obtained from the maceration process of samples that were collected from the Langsa city, Aceh. The cytotoxicity test was carried out by incubating MCF-7 cells which had been exposed to several series of sample levels, viz. 1000; 500; 100; 50; 25; 10; 5 and 1 µg/mL. LC50 values are calculated using probit analysis. The results revealed that the n-hexane extract of S. trilobata leaves was cytotoxic against breast cancer cells (MCF-7) with an LC50 value of  0.037 μg /mL.Abstrak : Sphagneticola trilobata (L.) J.F. Pruski merupakan salah satu tanaman herbal yang digunakan secara luas oleh masyarakat nasional dan internasional untuk mengobati berbagai penyakit termasuk kanker. Penelitian ini bertujuan untuk mengetahui aktivitas antikanker ekstrak n-heksana daun S. trilobata dalam menghambat pertumbuhan sel kanker payudara MCF-7 secara in vitro dengan metode MTT (microculture tetrazolium salt). Ekstrak n-heksana daun sernai diperoleh dari proses maserasi sampel yang dikoleksi dari kota Langsa, Aceh. Uji sitotoksisitas dilakukan dengan menginkubasi sel MCF-7 yang telah dipaparkan beberapa seri  kadar sampel yaitu 1000, 500, 100, 50, 25, 10, 5 dan 1 µg/mL. Nilai LC50 dihitung dengan menggunakan analisa probit. Hasil penelitian menunjukkan bahwa ekstrak n-heksana daun S. trilobata bersifat sitotoksik terhadap sel kanker payudara (MCF-7) dengan harga LC50 sebesar 0,037 µg/mL. 


2021 ◽  
Author(s):  
Saeedeh Ahmadi ◽  
Iman Akbarzadeh ◽  
Mohsen Chiani ◽  
Mahmoud Seraj ◽  
Hassan Noorbazargan ◽  
...  

Abstract This study aimed to improve the anticancer activity of letrozole through a niosomal formulation. Optimized niosomal formulation of letrozole was achieved by response surface methodology (RSM). The niosomes were well-characterized by several methods. The anticancer activity and its mechanism were studied in MCF-7 and MDA-MB-231 breast cancer cells. The release of the drug from the niosomes was according to the Kors Meyer-Peppa kinetic model. The niosomes were stable with high encapsulation efficiency. Significant higher anticancer activity and more induction of apoptosis were obtained for niosomal letrozole. Results indicated that niosomes could be a promising drug carrier for delivery of letrozole to breast cancer cells.


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