The effect of surface charge on oral absorption of polymeric nanoparticles

2018 ◽  
Vol 6 (3) ◽  
pp. 642-650 ◽  
Author(s):  
Xiao-Jiao Du ◽  
Ji-Long Wang ◽  
Shoaib Iqbal ◽  
Hong-Jun Li ◽  
Zhi-Ting Cao ◽  
...  
Keyword(s):  
Small Intestine ◽  
Surface Charge ◽  
Oral Bioavailability ◽  
Oral Absorption ◽  
Polymeric Nanoparticles ◽  
Charged Nanoparticles ◽  
Positively Charged ◽  
Effect Of Surface

Positively charged nanoparticles showed a favorable distribution in the small intestine, and significantly improved oral bioavailability.

scholarly journals Bacteria-Targeted Clindamycin Loaded Polymeric Nanoparticles: Effect of Surface Charge on Nanoparticle Adhesion to MRSA, Antibacterial Activity, and Wound Healing

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 236 ◽  
Author(s):  
Nurhasni Hasan ◽  
Jiafu Cao ◽  
Juho Lee ◽  
Shwe Phyu Hlaing ◽  
Murtada A. Oshi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Surface Charge ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Sustained Drug Release ◽  
Bactericidal Efficacy ◽  
Infected Wounds ◽  
Pei Nanoparticles ◽  
Positively Charged ◽  
Effect Of Surface

Adhesion of nanoparticles (NPs) to the bacterial cell wall by modifying their physicochemical properties can improve the antibacterial activity of antibiotic. In this study, we prepared positively charged clindamycin-loaded poly (lactic-co-glycolic acid)-polyethylenimine (PLGA-PEI) nanoparticles (Cly/PPNPs) and negatively charged clindamycin-loaded PLGA NPs (Cly/PNPs) and investigated the effect of NP adhesion to bacteria on the treatment of methicillin-resistant Staphylococcus aureus (MRSA)-infected wounds. The Cly/PPNPs and Cly/PNPs were characterized according to particle size, polydispersity index, surface charge, and drug loading. Both Cly/PPNPs and Cly/PNPs exhibited sustained drug release over 2 days. The Cly/PPNPs bind to the MRSA surface, thereby enhancing bactericidal efficacy against MRSA compared with the Cly/PNPs. Furthermore, compared with other groups, Cly/PPNPs significantly accelerated the healing and re-epithelialization of wounds in a mouse model of a MRSA-infected wounds. We also found that both NPs are harmless to healthy fibroblast cells. Therefore, our results suggest that the Cly/PPNPs developed in this study improve the efficacy of clindamycin for the treatment of MRSA-infected wounds.

scholarly journals Effect of Surface Charge and Hydrophobicity Modulation on the Antibacterial and Antibiofilm Potential of Magnetic Iron Nanoparticles

2017 ◽  
Vol 2017 ◽  
pp. 1-15 ◽  
Author(s):  
Rania Ibrahim Shebl ◽  
Faten Farouk ◽  
Hassan Mohamed El-Said Azzazy
Keyword(s):  
Surface Charge ◽  
Biofilm Formation ◽  
E Coli ◽  
Inhibitory Potential ◽  
Average Size ◽  
Positively Charged ◽  
Significant Concentration ◽  
Effect Of Surface ◽  
Antibacterial Potential ◽  
Trimethoxy Silane

Unmodified magnetic nanoparticles (MNPs) lack antibacterial potential. We investigated MNPs surface modifications that can impart antibacterial activity. Six MNPs species were prepared and characterized. Their antibacterial and antibiofilm potentials, surface affinity, and cytotoxicity were evaluated. Prepared MNPs were functionalized with citric acid, amine group, amino-propyl trimethoxy silane (APTMS), arginine, or oleic acid (OA) to give hydrophilic and hydrophobic MNPs with surface charge ranging from −30 to +30 mV. Prepared MNPs were spherical in shape with an average size of 6–15 nm. Hydrophobic (OA-MNPs) and positively charged MNPs (APTMS-MNPs) had significant concentration dependent antibacterial effect. OA-MNPs showed higher inhibitory potential againstS. aureusandE. coli(80%) than APTMS-MNPs (70%). Both particles exhibited surface affinity toS. aureusandE. coli.Different concentrations of OA-MNPs decreasedS. aureusandE. colibiofilm formation by 50–90%, while APTMS-MNPs reduced it by 30–90%, respectively. Up to 90% of preformed biofilms ofS. aureusandE. coliwere destroyed by OA-MNPs and APTMS-MNPs. In conclusion, surface positivity and hydrophobicity enhance antibacterial and antibiofilm properties of MNPs.

scholarly journals Influence of Surface Charge on the Functional Properties of Silica Nanoparticles and Cellular Toxicity

2020 ◽  
Vol 9 (3) ◽  
pp. 1225-1238
Keyword(s):  
Surface Charge ◽  
Silica Nanoparticles ◽  
Sio2 Nanoparticles ◽  
Carboxyl Groups ◽  
Raw 264.7 ◽  
Sem Images ◽  
Raw 264.7 Macrophages ◽  
Charged Nanoparticles ◽  
The Difference ◽  
Positively Charged

The effect of silica nanoparticles with a different surface charge on the cell viability of Caco-2 and RAW 264.7 cell lines was studied. Silica nanoparticles with narrow size distribution were prepared by Stobers method. These silica nanoparticles surface charge was varied from highly positive to highly negative, were single functionalized by APTES and multi functionalized by cysteine for amine and carboxyl groups. All other properties of the nanoparticles were kept constant. The unfunctionalized nanoparticles were used as control. Fourier Transform Infrared spectroscopy (FTIR) confirmed the presence of amine and carboxyl groups present on the surface of silica nanoparticles. The zeta potential measurements confirmed the successful modification of surface charge of silica nanoparticles in water. SEM images showed that the negatively charged, positively charged, and unfunctionalized nanoparticles with similar size and shape. MTT assay results indicated that the toxicity of SiO2 was cell type-dependent. CaCo-2 cells were highly resistant to nanoparticle treatment whereas RAW 264.7 (macrophages) predominantly charge dependent. The difference in toxicity could be attributed to the difference in the physiological function of each cell line. Among the three kinds of nanoparticles (negative, positive, and untreated), positively charged nanoparticles showed higher toxicity, which might be due to the attractive interaction between the negatively charged cell membrane and positively charged SiO2 nanoparticles.

Surface Charge and the Association of Liposomes with Colon Carcinoma Cells

2001 ◽  
Vol 56 (9-10) ◽  
pp. 872-877 ◽  
Author(s):  
Dagmara Baczynska ◽  
Katarzyna Widerak ◽  
Maciej Ugorski ◽  
Marek Langner
Keyword(s):  
Surface Charge ◽  
Lipid Bilayer ◽  
Electrostatic Interactions ◽  
Cationic Lipid ◽  
Human Colon ◽  
Carcinoma Cells ◽  
Colon Carcinoma Cells ◽  
Lipid Surface ◽  
Positively Charged ◽  
Effect Of Surface

Abstract Interaction between the plasma membrane and aggregate lipid surface determines how efficiently the encapsulated drug will be delivered into the cell. Electrostatic interactions are one of the main forces affecting liposome and aggregate association with the charged cell surface. In this study, the effect of surface charge on the association of liposomes with human colon CX-1.1 cancer cells was studied. When phosphatidylserine was incorporated into a lipid bilayer, the amount of liposomes associated with cells tended to increase along with the amount of negatively charged lipid present in the liposomal lipid bilayer. When the cationic lipid dioleoyl-1,2-diacyl-3-trimethylammonium-propane (DOTAP) was included into the liposome formula, their uptake by the cells was also increased. Maximum binding occurred when the amount of positively charged lipids in liposomes was about 10 mol% of lipids.

scholarly journals Charge reversal nano-systems for tumor therapy

2022 ◽  
Vol 20 (1) ◽  
Author(s):  
Peng Zhang ◽  
Daoyuan Chen ◽  
Lin Li ◽  
Kaoxiang Sun
Keyword(s):  
Surface Charge ◽  
Cellular Uptake ◽  
Blood Circulation ◽  
Tumor Therapy ◽  
Polymeric Materials ◽  
Antitumor Effects ◽  
Charge Reversal ◽  
Physiological Conditions ◽  
Positively Charged ◽  
Effect Of Surface

AbstractSurface charge of biological and medical nanocarriers has been demonstrated to play an important role in cellular uptake. Owing to the unique physicochemical properties, charge-reversal delivery strategy has rapidly developed as a promising approach for drug delivery application, especially for cancer treatment. Charge-reversal nanocarriers are neutral/negatively charged at physiological conditions while could be triggered to positively charged by specific stimuli (i.e., pH, redox, ROS, enzyme, light or temperature) to achieve the prolonged blood circulation and enhanced tumor cellular uptake, thus to potentiate the antitumor effects of delivered therapeutic agents. In this review, we comprehensively summarized the recent advances of charge-reversal nanocarriers, including: (i) the effect of surface charge on cellular uptake; (ii) charge-conversion mechanisms responding to several specific stimuli; (iii) relation between the chemical structure and charge reversal activity; and (iv) polymeric materials that are commonly applied in the charge-reversal delivery systems. Graphical Abstract

Development and Oral Bioavailability of Self-Emulsifying Formulation of Ketoconazole

2013 ◽  
Vol 5 (4) ◽  
pp. 1858-1865
Author(s):  
Arundhati Bhattacharyya ◽  
M Bajpai
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Aqueous Suspension ◽  
Droplet Diameter ◽  
Tween 80 ◽  
Concurrent Administration ◽  
System Maintenance ◽  
Pure Drug ◽  
Ph Dependent

Ketoconazole is an imidazole antifungal drug belonging to the class II of Biopharmaceutic Classification System. Maintenance of gastric acidity is essential for adequate dissolution and absorption of ketoconazole. Concurrent administration of antacid and antiulcer preparations decreases the oral absorption of ketoconazole often causing therapeutic failure.  The aim of this study was to evaluate whether a self-emulsifying formulation of ketoconazole would be able to overcome the pH dependent dissolution and oral bioavailability. Self-emulsifying drug delivery system (SEDDS) was prepared after selecting the oil, surfactant and co-surfactant by solubility analysis. Optimum ratio of the components was finalized on the basis of drug content, self-emulsification and mean droplet diameter. The effect of pH on dissolution was studied in comparison to the pure drug. Oral bioavailability was determined in comparison to aqueous suspension in rats and the effect of co-administration of ranitidine hydrochloride solution and a commercially available liquid antacid preparation was studied. The optimized formulation containing 20% Capryol 90 and 40% each of Carbitol and Tween 80, exhibited 100% drug release regardless of the pH whereas the pure drug exhibited a highly pH dependent dissolution. The AUC0-24 resulted with oral administration of the SEDDS formulation was about 34%, 43% and 60% higher compared to the aqueous suspension when administered alone, administered with ranitidine and administered with antacid respectively. The results of the present study demonstrate that self-emulsifying formulations can be utilized for oral delivery of weakly basic drugs like ketoconazole which exhibit pH dependent dissolution.

Effect of Polyphosphate on Removal of Endocrine-Disrupting Chemicals of Nonylphenol and Bisphenol-A by Activated Carbons

2005 ◽  
Vol 40 (4) ◽  
pp. 484-490 ◽  
Author(s):  
Keun J. Choi ◽  
Sang G. Kim ◽  
Chang W. Kim ◽  
Seung H. Kim
Keyword(s):  
Activated Carbon ◽  
Bisphenol A ◽  
Surface Charge ◽  
Activated Carbons ◽  
Endocrine Disrupting Chemicals ◽  
Dipole Interaction ◽  
High Affinity ◽  
Calcium Polyphosphate ◽  
Endocrine Disrupting ◽  
Positively Charged

Abstract This study examined the effect of polyphosphate on removal of endocrine-disrupting chemicals (EDCs) such as nonylphenol and bisphenol-A by activated carbons. It was found that polyphosphate aided in the removal of nonylphenol and bisphenol- A. Polyphosphate reacted with nonylphenol, likely through dipole-dipole interaction, which then improved the nonylphenol removal. Calcium interfered with this reaction by causing competition. It was found that polyphosphate could accumulate on carbon while treating a river. The accumulated polyphosphate then aided nonylphenol removal. The extent of accumulation was dependent on the type of carbon. The accumulation occurred more extensively with the wood-based used carbon than with the coal-based used carbon due to the surface charge of the carbon. The negatively charged wood-based carbon attracted the positively charged calcium-polyphosphate complex more strongly than the uncharged coal-based carbon. The polyphosphate-coated activated carbon was also effective in nonylphenol removal. The effect was different depending on the type of carbon. Polyphosphate readily attached onto the wood-based carbon due to its high affinity for polyphosphate. The attached polyphosphate then improved the nonylphenol removal. However, the coating failed to attach polyphosphate onto the coal-based carbon. The nonylphenol removal performance of the coal-based carbon remained unchanged after the polyphosphate coating.

scholarly journals Surface charge modulation of rifampicin-loaded PLA nanoparticles to improve antibiotic delivery in Staphylococcus aureus biofilms

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
David Da Costa ◽  
Chloé Exbrayat-Héritier ◽  
Basile Rambaud ◽  
Simon Megy ◽  
Raphaël Terreux ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Surface Charge ◽  
Treatment Efficacy ◽  
Particle Migration ◽  
Bacterial Biofilm ◽  
Poly Lactic Acid ◽  
Retention Capacity ◽  
The Impact ◽  
Positively Charged ◽  
Antibiotic Delivery

Abstract Background After the golden age of antibiotic discovery, bacterial infections still represent a major challenge for public health worldwide. The biofilm mode of growth is mostly responsible for chronic infections that current therapeutics fail to cure and it is well-established that novel strategies must be investigated. Particulate drug delivery systems are considered as a promising strategy to face issues related to antibiotic treatments in a biofilm context. Particularly, poly-lactic acid (PLA) nanoparticles present a great interest due to their ability to migrate into biofilms thanks to their submicronic size. However, questions still remain unresolved about their mode of action in biofilms depending on their surface properties. In the current study, we have investigated the impact of their surface charge, firstly on their behavior within a bacterial biofilm, and secondly on the antibiotic delivery and the treatment efficacy. Results Rifampicin-loaded PLA nanoparticles were synthetized by nanoprecipitation and characterized. A high and superficial loading of rifampicin, confirmed by an in silico simulation, enabled to deliver effective antibiotic doses with a two-phase release, appropriate for biofilm-associated treatments. These nanoparticles were functionalized with poly-l-lysine, a cationic peptide, by surface coating inducing charge reversal without altering the other physicochemical properties of these particles. Positively charged nanoparticles were able to interact stronger than negative ones with Staphylococcus aureus, under planktonic and biofilm modes of growth, leading to a slowed particle migration in the biofilm thickness and to an improved retention of these cationic particles in biofilms. While rifampicin was totally ineffective in biofilms after washing, the increased retention capacity of poly-l-lysine-coated rifampicin-loaded PLA nanoparticles has been associated with a better antibiotic efficacy than uncoated negatively charged ones. Conclusions Correlating the carrier retention capacity in biofilms with the treatment efficacy, positively charged rifampicin-loaded PLA nanoparticles are therefore proposed as an adapted and promising approach to improve antibiotic delivery in S. aureus biofilms.

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