Effects of particle size and surface charge on cellular uptake and biodistribution of polymeric nanoparticles

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


2015 ◽  
Vol 28 (3) ◽  
pp. 420-427 ◽  
Author(s):  
Ho-Kyung Ha ◽  
Jin Wook Kim ◽  
Mee-Ryung Lee ◽  
Woojin Jun ◽  
Won-Jae Lee

2014 ◽  
Vol 57 ◽  
pp. 187-201 ◽  
Author(s):  
Ruijing Liang ◽  
Liyun Dong ◽  
Renhua Deng ◽  
Jing Wang ◽  
Ke Wang ◽  
...  

Nano LIFE ◽  
2013 ◽  
Vol 03 (04) ◽  
pp. 1343003 ◽  
Author(s):  
BRANDON MATTIX ◽  
THOMAS MOORE ◽  
OLGA UVAROV ◽  
SAMUEL POLLARD ◽  
LAUREN O'DONNELL ◽  
...  

Current chemotherapy treatments are limited by poor drug solubility, rapid drug clearance and systemic side effects. Additionally, drug penetration into solid tumors is limited by physical diffusion barriers [e.g., extracellular matrix (ECM)]. Nanoparticle (NP) blood circulation half-life, biodistribution and ability to cross extracellular and cellular barriers will be dictated by NP composition, size, shape and surface functionality. Here, we investigated the effect of surface charge of poly(lactide)-poly(ethylene glycol) NPs on mediating cellular interaction. Polymeric NPs of equal sizes were used that had two different surface functionalities: negatively charged carboxyl ( COOH ) and neutral charged methoxy ( OCH 3). Cellular uptake studies showed significantly higher uptake in human brain cancer cells compared to noncancerous human brain cells, and negatively charged COOH NPs were uptaken more than neutral OCH 3 NPs in 2D culture. NPs were also able to load and control the release of paclitaxel (PTX) over 19 days. Toxicity studies in U-87 glioblastoma cells showed that PTX-loaded NPs were effective drug delivery vehicles. Effect of surface charge on NP interaction with the ECM was investigated using collagen in a 3D cellular uptake model, as collagen content varies with the type of cancer and the stage of the disease compared to normal tissues. Results demonstrated that NPs can effectively diffuse across an ECM barrier and into cells, but NP mobility is dictated by surface charge. In vivo biodistribution of OCH 3 NPs in intracranial tumor xenografts showed that NPs more easily accumulated in tumors with less collagen. These results indicate that a robust understanding of NP interaction with various tumor environments can lead to more effective patient-tailored therapies.


2016 ◽  
Vol 7 (32) ◽  
pp. 5123-5131 ◽  
Author(s):  
O. L. J. Virtanen ◽  
M. Brugnoni ◽  
M. Kather ◽  
A. Pich ◽  
W. Richtering

Many applications of poly(N-isopropylacrylamide) microgels necessitate robust control over particle size.


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