Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery

2013 ◽  
Vol 30 (10) ◽  
pp. 2512-2522 ◽  
Author(s):  
Sneha A. Kulkarni ◽  
Si-Shen Feng
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Surface Modification ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles

Polymeric Nanoparticles for Brain Drug Delivery - A Review

2020 ◽  
Vol 21 (9) ◽  
pp. 649-660
Author(s):  
Subashini Raman ◽  
Syed Mahmood ◽  
Ayah R. Hilles ◽  
Md Noushad Javed ◽  
Motia Azmana ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Surface Modification ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Preparation Methods ◽  
Brain Drug Delivery ◽  
Polymeric Nanoparticle ◽  
Relationship Of ◽  
The Relationship ◽  
The Brain

Background: Blood-brain barrier (BBB) plays a most hindering role in drug delivery to the brain. Recent research comes out with the nanoparticles approach, is continuously working towards improving the delivery to the brain. Currently, polymeric nanoparticle is extensively involved in many therapies for spatial and temporal targeted areas delivery. Methods: We did a non-systematic review, and the literature was searched in Google, Science Direct and PubMed. An overview is provided for the formulation of polymeric nanoparticles using different methods, effect of surface modification on the nanoparticle properties with types of polymeric nanoparticles and preparation methods. An account of different nanomedicine employed with therapeutic agent to cross the BBB alone with biodistribution of the drugs. Results: We found that various types of polymeric nanoparticle systems are available and they prosper in delivering the therapeutic amount of the drug to the targeted area. The effect of physicochemical properties on nanoformulation includes change in their size, shape, elasticity, surface charge and hydrophobicity. Surface modification of polymers or nanocarriers is also vital in the formulation of nanoparticles to enhance targeting efficiency to the brain. Conclusion: More standardized methods for the preparation of nanoparticles and to assess the relationship of surface modification on drug delivery. While the preparation and its output like drug loading, particle size, and charge, permeation is always conflicted, so it requires more attention for the acceptance of nanoparticles for brain delivery.

scholarly journals Surface Modification of Polymeric Nanoparticles with M2pep Peptide for Drug Delivery to Tumor-Associated Macrophages

2019 ◽  
Vol 36 (4) ◽  
Author(s):  
Liang Pang ◽  
Yihua Pei ◽  
Gozde Uzunalli ◽  
Hyesun Hyun ◽  
L. Tiffany Lyle ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Surface Modification ◽  
Polymeric Nanoparticles ◽  
Tumor Associated Macrophages

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
Keyword(s):  
Particle Size ◽  
Surface Charge ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles

Anti-EGFR-mAb and 5-Fluorouracil conjugated Polymeric Nanoparticle for Colorectal Cancer

2020 ◽  
Vol 15 ◽  
Author(s):  
Sankha Bhattacharya
Keyword(s):  
Colorectal Cancer ◽  
Drug Delivery ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Reticuloendothelial System ◽  
Unhealthy Lifestyle ◽  
Anticancer Effects ◽  
Colorectal Cancer Cells ◽  
Specific Formulation

Background:: Due to the higher intake of junk food and unhealthy lifestyle, the percentage of U.S. adults aged 50 to 75 years who were up-to-date with colorectal cancer screening increased 1.4 percentage points, from 67.4% in 2016 to 68.8% in 2018. This represents an additional 3.5 million adults screened for colorectal cancer. This is a severe concern of this research, and an attempt was made to prepare a target-specific formulation that could circumvent chemotherapyrelated compilation and improvise higher cellular uptake. The fundamental agenda of this research was to prepare and develop Anti-EGFR mAb and 5-Fluorouracil (5-FU) fabricated polymeric nanoparticles for colorectal cancer. Objective: The main objective of this research was to prepare and evaluated more target specific formulation for the treatment of colorectal cancer. PLGA and PEG-based polymeric nanoparticles are capable of preventing opsonization via the reticuloendothelial system. Hence, prepared polymeric nanoparticles are capable of higher cellular uptake. Methods: The Poly(d,1-lactide-co-glycolide) (PLGA) & Polyethylene Glycol (PEG) were combined utilizing the ringopening polymerization method. The presence of PEG prevents opsonization and distinguished blood concentration along with enhanced targeting. The presence of PLGA benefits in the sustained release of polymeric formulations. The optimized formulation (5-FU-PLGA-PEG-NP) was lyophilized using 4% trehalose (cryoprotectants) & conjugated with Anti-EGFR mAb on its surface to produce Anti-EGFR-5-FU-PLGA-PEG-NP; the final formulation, which increases target specificity and drug delivery system of nanoparticles. Results: The spherical shaped optimized formulation; 5-FU-PLGA-PEG-NP-3 was found to have higher percentage drug entrapment efficacy (71.23%), higher percentage drug content (1.98 ± 0.34%) with minimum particles size (252.3nm) & anionic zeta potential ( -31.23mV). The IC50 value of Anti-EGFR-5-FU-PLGA-PEG-NP was 1.01 µg/mL after 48 hours incubation period in the HCT 116 cell line, indicating higher anticancer effects of the final formulation. Conclusions: From the outcomes of various experiments, it was concluded that Anti-EGFR-5-FU-PLGA-PEG-NP has biphasic drug release kinetics, higher cellular uptake & higher cytotoxicity. Therefore, Anti-EGFR-5-FU-PLGA-PEG-NP holds excellent potential for drug delivery to EGFR positive colorectal cancer cells.

Mechanisms of cellular uptake with hyaluronic acid—octadecylamine micelles as drug delivery nanocarriers

RSC Advances ◽  
2016 ◽  
Vol 6 (46) ◽  
pp. 39896-39902 ◽  
Author(s):  
Lipeng Qiu ◽  
Mengqin Zhu ◽  
Yan Huang ◽  
Kai Gong ◽  
Jinghua Chen
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Hyaluronic Acid ◽  
Anticancer Activity ◽  
Cellular Uptake ◽  
Drug Concentration

DOX/HM23, based on appropriate DS and proper particle size, presented enhanced anticancer activity and efficient internalization to achieve the highest intracellular drug concentration.

Cellular Uptake of PEGylated PLGA Nanoparticles in Hela Cells

2012 ◽  
Vol 528 ◽  
pp. 80-83
Author(s):  
Gang Li ◽  
Dong Hai Lin ◽  
Xin Xin Xie ◽  
Li Fang Qin ◽  
Jun Teng Wang
Keyword(s):  
Particle Size ◽  
Surface Modification ◽  
Controlled Release ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Cellular Uptake ◽  
Hela Cells ◽  
Drug Carriers ◽  
Plga Nanoparticles ◽  
Fluorescent Marker

PLGA nanoparticles (PLGA-NPs) are being extensively studied as drug carriers for their controlled release, biodegradability and biocompatibility. This study evaluated the cellular uptake of PEGylated PLGA-NPs in Hela cells. MePEG-PLGA (5%-15%) was used to prepare PEG modified PLGA nanoparticles (PEG-PLGA-NPs), and the fluorescent marker DiI was encapsulated in the nanoparticles for the visualized analysis. The nanoparticles were characterized for surface morphology, particle size, zeta potential, and for cellular uptake by Hela cells. Results showed that PLGA nanoparticles were lowly cytotoxic and could be uptaken by Hela cells freely. PEG-PLGA-NPs had faster cellular uptake than that of nude PLGA nanoparticles, especially 10%PEG-PLGA-NPs. It suggested that the surface modification of PLGA-NPs by PEG notably improved the cellular uptake.

scholarly journals Nanoformulations of α-Mangostin for Cancer Drug Delivery System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 1993
Author(s):  
Lisna Meylina ◽  
Muchtaridi Muchtaridi ◽  
I Made Joni ◽  
Ahmed Fouad Abdelwahab Mohammed ◽  
Nasrul Wathoni
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles ◽  
Cancer Drug ◽  
Garcinia Mangostana ◽  
Active Constituent ◽  
Anticancer Efficacy ◽  
Anticancer Properties ◽  
Cancer Drug Delivery

Natural compounds are emerging as effective agents for the treatment of malignant diseases. The active constituent of α-mangostin from the pericarp of Garcinia mangostana L. has earned significant interest as a plant base compound with anticancer properties. Despite α-mangostin’s superior properties as an anticancer agent, its applications are limited due to its poor solubility and physicochemical stability, rapid systemic clearance, and low cellular uptake. Our review aimed to summarize and discuss the nanoparticle formulations of α-mangostin for cancer drug delivery systems from published papers recorded in Scopus, PubMed, and Google Scholar. We investigated various types of α-mangostin nanoformulations to improve its anticancer efficacy by improving bioavailability, cellular uptake, and localization to specific areas These nanoformulations include nanofibers, lipid carrier nanostructures, solid lipid nanoparticles, polymeric nanoparticles, nanomicelles, liposomes, and gold nanoparticles. Notably, polymeric nanoparticles and nanomicelles can increase the accumulation of α-mangostin into tumors and inhibit tumor growth in vivo. In addition, polymeric nanoparticles with the addition of target ligands can increase the cellular uptake of α-mangostin. In conclusion, nanoformulations of α-mangostin are a promising tool to enhance the cellular uptake, accumulation in cancer cells, and the efficacy of α-mangostin as a candidate for anticancer drugs.

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
Keyword(s):  
Particle Size ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Active Ingredient ◽  
Polymeric Nanoparticles ◽  
Drug Carrier ◽  
Polyvinyl Pyrrolidone ◽  
Cytotoxicity Test ◽  
Nanoparticle System ◽  
Mcf 7

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.

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