scholarly journals Micellar Nanocarriers from Dendritic Macromolecules Containing Fluorescent Coumarin Moieties

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2872
Author(s):  
Alberto Concellón ◽  
María San Anselmo ◽  
Silvia Hernández-Ainsa ◽  
Pilar Romero ◽  
Mercedes Marcos ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Materials Science ◽  
Nile Red ◽  
Drug Delivery Vehicles ◽  
Delivery Vehicles ◽  
Spherical Micelles ◽  
Assembly Behavior ◽  
Hexagonal Columnar

The design of efficient drug-delivery vehicles remains a big challenge in materials science. Herein, we describe a novel class of amphiphilic hybrid dendrimers that consist of a poly(amidoamine) (PAMAM) dendritic core functionalized with bisMPA dendrons bearing cholesterol and coumarin moieties. Their self-assembly behavior both in bulk and in water was investigated. All dendrimers exhibited smectic A or hexagonal columnar liquid crystal organizations, depending on the generation of the dendrimer. In water, these dendrimers self-assembled to form stable spherical micelles that could encapsulate Nile Red, a hydrophobic model compound. The cell viability in vitro of the micelles was studied in HeLa cell line, and proved to be non-toxic up to 72 h of incubation. Therefore, these spherical micelles allow the encapsulation of hydrophobic molecules, and at the same time provided fluorescent traceability due to the presence of coumarin units in their chemical structure, demonstrating the potential of these dendrimers as nanocarriers for drug-delivery applications.

Novel Phospholipid-Based Labrasol Nanomicelles Loaded Flavonoids for Oral Delivery with Enhanced Penetration and Anti-Brain Tumor Efficiency

2020 ◽  
Vol 17 (3) ◽  
pp. 229-245
Author(s):  
Gang Wang ◽  
Junjie Wang ◽  
Rui Guan
Keyword(s):  
Drug Delivery ◽  
Brain Tumor ◽  
Oral Delivery ◽  
Safe Delivery ◽  
Drug Delivery Vehicles ◽  
Therapeutic Benefits ◽  
Delivery Vehicles ◽  
The Brain

Background: Owing to the rich anticancer properties of flavonoids, there is a need for their incorporation into drug delivery vehicles like nanomicelles for safe delivery of the drug into the brain tumor microenvironment. Objective: This study, therefore, aimed to prepare the phospholipid-based Labrasol/Pluronic F68 modified nano micelles loaded with flavonoids (Nano-flavonoids) for the delivery of the drug to the target brain tumor. Methods: Myricetin, quercetin and fisetin were selected as the initial drugs to evaluate the biodistribution and acute toxicity of the drug delivery vehicles in rats with implanted C6 glioma tumors after oral administration, while the uptake, retention, release in human intestinal Caco-2 cells and the effect on the brain endothelial barrier were investigated in Human Brain Microvascular Endothelial Cells (HBMECs). Results: The results demonstrated that nano-flavonoids loaded with myricetin showed more evenly distributed targeting tissues and enhanced anti-tumor efficiency in vivo without significant cytotoxicity to Caco-2 cells and alteration in the Trans Epithelial Electric Resistance (TEER). There was no pathological evidence of renal, hepatic or other organs dysfunction after the administration of nanoflavonoids, which showed no significant influence on cytotoxicity to Caco-2 cells. Conclusion: In conclusion, Labrasol/F68-NMs loaded with MYR and quercetin could enhance antiglioma effect in vitro and in vivo, which may be better tools for medical therapy, while the pharmacokinetics and pharmacodynamics of nano-flavonoids may ensure optimal therapeutic benefits.

A modular approach towards drug delivery vehicles using oxanorbornane-based non-ionic amphiphiles

2016 ◽  
Vol 4 (48) ◽  
pp. 8025-8032 ◽  
Author(s):  
D. Sirisha Janni ◽  
U. Chandrasekhar Reddy ◽  
Soumya Saroj ◽  
K. M. Muraleedharan
Keyword(s):  
Drug Delivery ◽  
Amino Acid ◽  
Self Assembly ◽  
The Self ◽  
Head Group ◽  
Modular Approach ◽  
Drug Delivery Vehicles ◽  
Delivery Vehicles ◽  
Drug Delivery Applications ◽  
Supramolecular Aggregates

The self-assembly of non-ionic amphiphiles with hydroxylated oxanorbornane head-group was controlled using amino acid units as spacers between hydrophilic and lipophilic domains to get spherical supramolecular aggregates suitable for drug delivery applications.

Self-assembly of core-polyethylene glycol-lipid shell (CPLS) nanoparticles and their potential as drug delivery vehicles

Nanoscale ◽  
2016 ◽  
Vol 8 (31) ◽  
pp. 14821-14835 ◽  
Author(s):  
Zhiqiang Shen ◽  
David T. Loe ◽  
Joseph K. Awino ◽  
Martin Kröger ◽  
Jessica L. Rouge ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Polyethylene Glycol ◽  
Self Assembly ◽  
Drug Delivery Vehicles ◽  
Delivery Vehicles

Bioactive Molecules Delivered by Ceramic Nanoparticles Coated with a Film of Polyhydroxyl Oligomers

1995 ◽  
Vol 394 ◽  
Author(s):  
Nir Kossovsky
Keyword(s):  
Drug Delivery ◽  
Surface Adsorption ◽  
Bioactive Molecules ◽  
Aqueous Environment ◽  
Antigen Delivery ◽  
Drug Delivery Vehicles ◽  
Ceramic Nanoparticles ◽  
Delivery Vehicles ◽  
Carbon Ceramic

AbstractThe structural denaturation of polypeptides and other macromolecular pharmaceuticals upon surface adsorption from an aqueous environment is almost inevitable. Molecular denaturation, coupled with a net increase in entropy, accounts for the net negative ΔG and frequent irreversible nature of surface adsorption. The consequence of this interaction is that surface immobilized drugs lose their dynamic freedom and thus, all too often, their biological activity.This phenomenon has complicated the development of drug delivery vehicles. In this communication, a drug delivery system based on a novel surface modification process to help reverse the constraining activity of surfaces is described. Beginning with preformed carbon ceramic nanoparticles and self-assembled calcium-phosphate dihydrate particles (colloidal precipitation) to which glassy carbohydrates are then allowed to adsorb as a nanometer thick surface coating, a molecular carrier is formed. The carbohydrate coating functions as a dehydroprotectant and stabilizes subsequently non-covalently bound immobilized members of biochemically reactive surface members such as pharmaceuticals.Many of the physical properties of this enabling system have been characterized in vitro and in animal models. Antigen delivery, drug delivery, and enzyme stabilization experiments are described.

scholarly journals The influence of lipid digestion on the fate of orally administered drug delivery vehicles

2021 ◽  
Author(s):  
Ben J. Boyd ◽  
Andrew J. Clulow
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Liquid Crystalline ◽  
Drug Solubility ◽  
Lipid Digestion ◽  
Drug Delivery Vehicles ◽  
Packing Parameter ◽  
Lipid Chain ◽  
Polymorphic Forms ◽  
Delivery Vehicles

This review will focus on orally administered lipid-based drug delivery vehicles and specifically the influence of lipid digestion on the structure of the carrier lipids and their entrained drug cargoes. Digestion of the formulation lipids, which are typically apolar triglycerides, generates amphiphilic monoglycerides and fatty acids that can self-assemble into a diverse array of liquid crystalline structures. Tracking the dynamic changes in self-assembly of the lipid digestion products during digestion has recently been made possible using synchrotron-based small angle X-ray scattering. The influence of lipid chain length and degree of unsaturation on the resulting lipid structuring will be described in the context of the critical packing parameter theory. The chemical and structural transformation of the formulation lipids can also have a dramatic impact on the physical state of drugs co-administered with the formulation. It is often assumed that the best strategy for drug development is to maximise drug solubility in the undigested formulation lipids and to incorporate additives to maintain drug solubility during digestion. However, it is possible to improve drug absorption using lipid digestion in cases where the solubility of the dosed drug or one of its polymorphic forms is greater in the digested lipids. Three different fates for drugs administered with digestible lipid-based formulations will be discussed: (1) where the drug is more soluble in the undigested formulation lipids; (2) where the drug undergoes a polymorphic transformation during lipid digestion; and (3) where the drug is more soluble in the digested formulation lipids.

Peptide- and Aptamer-Functionalized Nanovectors for Targeted Delivery of Therapeutics

2009 ◽  
Vol 131 (7) ◽  
Author(s):  
Todd O. Pangburn ◽  
Matthew A. Petersen ◽  
Brett Waybrant ◽  
Maroof M. Adil ◽  
Efrosini Kokkoli
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
Peptide Ligands ◽  
Drug Delivery Vehicles ◽  
Delivery Vector ◽  
Current State ◽  
Dna Strands ◽  
Delivery Vehicles

Targeted delivery of therapeutics is an area of vigorous research, and peptide- and aptamer-functionalized nanovectors are a promising class of targeted delivery vehicles. Both peptide- and aptamer-targeting ligands can be readily designed to bind a target selectively with high affinity, and more importantly are molecules accessible by chemical synthesis and relatively compact compared with antibodies and full proteins. The multitude of peptide ligands that have been used for targeted delivery are covered in this review, with discussion of binding selectivity and targeting performance for these peptide sequences where possible. Aptamers are RNA or DNA strands evolutionarily engineered to specifically bind a chosen target. Although use of aptamers in targeted delivery is a relatively new avenue of research, the current state of the field is covered and promises of future advances in this area are highlighted. Liposomes, the classic drug delivery vector, and polymeric nanovectors functionalized with peptide or aptamer binding ligands will be discussed in this review, with the exclusion of other drug delivery vehicles. Targeted delivery of therapeutics, from DNA to classic small molecule drugs to protein therapeutics, by these targeted nanovectors is reviewed with coverage of both in vitro and in vivo deliveries. This is an exciting and dynamic area of research and this review seeks to discuss its broad scope.

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