Phosphate decorated lipid-based nanocarriers providing a prolonged mucosal residence time

Efiana, Nuri Ari; Fürst, Andrea; Saleh, Ahmad; Sahzadi, Iram; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ijpharm.2022.122096

Cited by 4 publications

(5 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Owing to the highly charged nature of polyphosphates at physiological pH they have been used to form polymeric NPs with oppositely charged polycations through ionic cross-linking resulting in particles with a small size and low polydispersity . Moreover, PP being regarded as safe auxiliary agents have been used in food industry as well and their mucus-permeating properties have already been reported. , …”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Peptide Antibiotic–Polyphosphate Nanoparticles: A Promising Strategy to Overcome the Enzymatic and Mucus Barrier of the Intestine

et al. 2023

Self Cite

View full text Add to dashboard Cite

The aim of this study was to develop peptide antibiotic–polyphosphate nanoparticles that are able to overcome the enzymatic and mucus barriers providing a targeted drug release directly on the intestinal epithelium. Polymyxin B–polyphosphate nanoparticles (PMB–PP NPs) were formed via ionic gelation between the cationic peptide and the anionic polyphosphate (PP). The resulting NPs were characterized by particle size, polydispersity index (PDI), zeta potential, and cytotoxicity on Caco-2 cells. The protective effect of these NPs for incorporated PMB was evaluated via enzymatic degradation studies with lipase. Moreover, mucus diffusion of NPs was investigated with porcine intestinal mucus. Isolated intestinal alkaline phosphatase (IAP) was employed to trigger the degradation of NPs and consequent drug release. PMB–PP NPs exhibited an average size of 197.13 ± 14.13 nm, a PDI of 0.36, a zeta potential of −11.1 ± 3.4 mV and a concentration and time-dependent toxicity. They provided entire protection toward enzymatic degradation and exhibited significantly (p < 0.05) higher mucus permeating properties than PMB. When incubated with isolated IAP for 4 h, monophosphate and PMB were constantly released from PMB–PP NPs and zeta potential raised up to −1.9 ± 0.61 mV. According to these findings, PMB–PP NPs are promising delivery systems to protect cationic peptide antibiotics against enzymatic degradation, to overcome the mucus barrier and to provide drug release directly at the epithelium.

show abstract

Section: Resultsmentioning

confidence: 99%

“… 16 Moreover, PP being regarded as safe auxiliary agents have been used in food industry as well 26 and their mucus-permeating properties have already been reported. 27 , 28 …”

Section: Resultsmentioning

confidence: 99%

Peptide Antibiotic–Polyphosphate Nanoparticles: A Promising Strategy to Overcome the Enzymatic and Mucus Barrier of the Intestine

et al. 2023

Self Cite

View full text Add to dashboard Cite

show abstract

“…When analyzing the zeta potential at least in the case of PLGA-NPs made from polyesters with free carboxylic end groups a high negative zeta potential would have been expected, but low values were obtained. This indicates high shielding of the surface charges by PVA, which was inevitably necessary for the stabilization and cryoprotection of the particle suspensions [ 45 , 46 ]. The lowering of the surface potential caused by the neutral polymer PVA coating the particle surface did not impede particle stability.…”

Section: Resultsmentioning

confidence: 99%

A Versatile Brij-Linker for One-Step Preparation of Targeted Nanoparticles

Anzengruber,

Nepustil,

Kurtaj

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

Background: Most frequently the functionalization of nanoparticles is hampered by time-consuming, sometimes harsh conjugation and purification procedures causing premature drug release and/or degradation. A strategy to circumvent multi-step protocols is to synthesize building blocks with different functionalities and to use mixtures thereof for nanoparticle preparation in one step. Methods: BrijS20 was converted into an amine derivative via a carbamate linkage. The Brij-amine readily reacts with pre-activated carboxyl-containing ligands such as folic acid. The structures of the building blocks were confirmed by different spectroscopic methods and their utility was assessed by one-step preparation and characterization of nanoparticles applying PLGA as a matrix polymer. Results: Nanoparticles were about 200 nm in diameter independent of the composition. Experiments with human folate expressing single cells and monolayer revealed that the nanoparticle building block Brij mediates a “stealth” effect and the Brij-amine-folate a “targeting” effect. As compared to plain nanoparticles, the stealth effect decreased the cell interaction by 13%, but the targeting effect increased the cell interaction by 45% in the monolayer. Moreover, the targeting ligand density and thus the cell association of the nanoparticles is easily fine-tuned by selection of the initial ratio of the building blocks. Conclusions: This strategy might be a first step towards the one-step preparation of nanoparticles with tailored functionalities. Relying on a non-ionic surfactant is a versatile approach as it might be extended to other hydrophobic matrix polymers and promising targeting ligands from the biotech pipeline.

show abstract

“…The mucosal residence time of phosphatedecorated NPs was prolonged up to 4.4-fold, compared to corresponding blank formulations. [118] Targeting respiratory mucosa can be of interest for the treatment of pulmonary diseases such as cancer and cystic fibrosis. A zwitterionic oligopeptide lipid, 1,5-dioctadecyl-l-glutamyl-2-histidyl-hexahydrobenzoic acid, was used for coating mesoporous silica NPs to achieve a pH-triggered charge reversal.…”

Section: Targeting Mucosal Membranesmentioning

confidence: 99%

“…The mucosal residence time of phosphate‐decorated NPs was prolonged up to 4.4‐fold, compared to corresponding blank formulations. [ 118 ]…”

Section: Applications For Charge‐reversible Nanoparticlesmentioning

confidence: 99%

Charge‐Reversible Nanoparticles: Advanced Delivery Systems for Therapy and Diagnosis

Veider,

Sanchez Armengol,

Bernkop‐Schnürch

2023

Small

View full text Add to dashboard Cite

The past two decades have witnessed a rapid progress in the development of surface charge‐reversible nanoparticles (NPs) for drug delivery and diagnosis. These NPs are able to elegantly address the polycation dilemma. Converting their surface charge from negative/neutral to positive at the target site, they can substantially improve delivery of drugs and diagnostic agents. By specific stimuli like a shift in pH and redox potential, enzymes, or exogenous stimuli such as light or heat, charge reversal of NP surface can be achieved at the target site. The activated positive surface charge enhances the adhesion of NPs to target cells and facilitates cellular uptake, endosomal escape, and mitochondrial targeting. Because of these properties, the efficacy of incorporated drugs as well as the sensitivity of diagnostic agents can be essentially enhanced. Furthermore, charge‐reversible NPs are shown to overcome the biofilm formed by pathogenic bacteria and to shuttle antibiotics directly to the cell membrane of these microorganisms. In this review, the up‐to‐date design of charge‐reversible NPs and their emerging applications in drug delivery and diagnosis are highlighted.

show abstract

Phosphate decorated lipid-based nanocarriers providing a prolonged mucosal residence time

Cited by 4 publications

References 32 publications

Peptide Antibiotic–Polyphosphate Nanoparticles: A Promising Strategy to Overcome the Enzymatic and Mucus Barrier of the Intestine

Peptide Antibiotic–Polyphosphate Nanoparticles: A Promising Strategy to Overcome the Enzymatic and Mucus Barrier of the Intestine

A Versatile Brij-Linker for One-Step Preparation of Targeted Nanoparticles

Charge‐Reversible Nanoparticles: Advanced Delivery Systems for Therapy and Diagnosis

Contact Info

Product

Resources

About