- Effects of Particle Size and Surface Coating on Cellular Uptake of Polymeric Nanoparticles for Oral Delivery of Anticancer Drugs

2014 ◽  
pp. 756-775
2019 ◽  
Vol 39 (3) ◽  
pp. 271-278 ◽  
Author(s):  
Suruchi Suri ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Abdullah S. Alshetaili ◽  
Saad M. Alshahrani ◽  
...  

Abstract The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitro release profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.


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

2017 ◽  
Vol 6 (2) ◽  
pp. 9-15 ◽  
Author(s):  
Nandhakumar Loganathan ◽  
Mohan Sellappan

In this present study, dual loaded flavono nanoparticulate systems have been developed for oral delivery of Naringin and Hesperidin to enhance its antioxidant and antidiabetic activities. The fabrication of Dual Loaded Flavono Nanoparticles by suitable method was optimized by Plackett Burman method. Optimization of the formulation requires proper designing of the experiments. For this reason, only in our current study, the placket burman method has been projected for the formulation of nanoparticles biodegradable polymers encompass bioflavonoid isolates for the antidiabetic activity. Ten critical parameters influencing the formulation has been selected and designed in Plackett Burman method of experimentation for 12 runs to assess independent variables influencing the result outcome. The results revealed that the 9th run shows the optimum particle size of 126.1 nm with zeta potential of 29.9 mV. Remarkably significant nanoparticles were obtained by exploiting the Plackett Burman method as designing tool.Loganathan and Sellappan, International Current Pharmaceutical Journal, January 2017, 6(2): 9-15http://www.icpjonline.com/documents/Vol6Issue2/01.pdf


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.


2019 ◽  
Vol 9 (4-s) ◽  
pp. 322-331
Author(s):  
Prasad Shilpi ◽  
J.S Dangi

The objective of the present research was to develop folic acid conjugated polymeric nanoparticles (FCsPNP) and to investigate its therapeutic effectiveness in xenograft Colon tumor models after oral delivery. Chitosan coated PLGA nanoparticles (CsPNP) were prepared by polyelectrolyte complexation method and it was further conjugated with Folic acid. Optimized formulation was investigated for particle size, zeta potential, polydispersity index (PdI), % entrapment drug loading and in vitro release. The morphology was observed by SEM and TEM images. Tumor regression studies were conducted on Balb/c mice implanted with Colo-26 cells. FCsPNP were successfully prepared and optimized. In vitro parameters viz. Particle size, Zeta potential, PdI were found to be optimum. The in vitro % release is directly correlated with the nature of polymers and folate conjugation. In vivo tumor regression studies found the formulations to be less toxic than Irinotecan hydrochloride (IHCl). CsPNP and FCsPNP were successfully prepared and evaluated for antitumor efficacy after oral delivery. FCsPNP were more effective in the colon tumor treatment and found to be less toxic than IHCl thus making it a potential drug delivery candidate for future anticancer therapy. Keywords: Nanoparticles, Xenograft colon tumor, Chitosan, Irinotecan hydrochloride


2016 ◽  
Vol 17 (3) ◽  
pp. 248-255 ◽  
Author(s):  
Dominique Duchene ◽  
Roberta Cavalli ◽  
Ruxandra Gref

2011 ◽  
Vol 1 (1) ◽  
pp. 24-31
Author(s):  
G. Tosi ◽  
A. V. Vergoni ◽  
B. Ruozi ◽  
L. Bondioli ◽  
F. Forni ◽  
...  

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