scholarly journals VP6-SUMO Self-Assembly as Nanocarriers for Gastrointestinal Delivery

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
V. Palmieri ◽  
F. Bugli ◽  
M. Papi ◽  
G. Ciasca ◽  
G. Maulucci ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Oral Delivery ◽  
Drug Stability ◽  
Intestinal Cells ◽  
Chimeric Construct ◽  
Poorly Soluble ◽  
Epithelial Barriers ◽  
Natural Target ◽  
Poor Absorption

High proteolytic degradation and poor absorption through epithelial barriers are major challenges to successful oral delivery of therapeutics. Nanoparticle platforms can enhance drug stability and extend the residence time in gastrointestinal (GI) tract. However, drug delivery systems are often inactivated in acidic environment of stomach or suffer poor absorption from intestinal cells due to the mucus layer. To overcome these issues we developed a drug delivery system constituted by a protein construct made by a Rotavirus capsid protein (VP6) and the small ubiquitin-like modifier SUMO. This chimeric construct allows specificity towards intestinal cells, the Rotavirus natural target, combined by an enhanced stability given by the eukaryotic protein transporter SUMO. Furthermore SUMO can act as a molecular switch that facilitates import/export of its ligand to the nucleus, the hypersensitive subcellular site target of many cell killing therapies. In this paper we show that SUMO-VP6 constructs self-assembly into stable nanocarriers. SUMO-VP6 nanocarriers display ideal features for drug delivery: a small size and high monodispersity, a high stability in different pH conditions and a high uptake in the nuclear and cytoplasmic compartment of intestinal cells. These features make SUMO-VP6 nanocarriers a promising novel system for oral delivery of poorly soluble drugs.

scholarly journals Polymeric Micelles: A Novel Approach towards Nano-Drug Delivery System

2021 ◽  
Vol 18 (4) ◽  
pp. 629-649
Author(s):  
Rutuja Hemant Vinchurkar ◽  
Ashwin Bhanudas Kuchekar
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Inner Core ◽  
Polymeric Micelles ◽  
Solvent Polarity ◽  
Physicochemical Characteristics ◽  
Polymeric Micelle ◽  
Absorption Mechanism ◽  
Novel Approach ◽  
Poorly Soluble

Nano delivery systems, polymeric micelles represent one of the most promising delivery platforms for therapeutic compounds. It has shown that a poorly soluble molecule which has high potency and remarkable toxicity can be encapsulated with the polymeric micelle. There are various poorly soluble drugs used in micellar preparations, mostly for their anti-cancer activity. Drugs in the inner core protect the drug from degradation and allow drug accumulation in the tumour site in the case of cancer treatment. Block copolymers are chosen based on the physicochemical characteristics of medicinal drugs. The amphiphilic block copolymer structure has both lipophilic and hydrophilic blocks, which enclose tiny hydrophobic molecules. It is a targeted drug delivery method because of its high effectiveness for drug retention in tissue, prevention of enzymes from degradation, and improvement of the cellular absorption mechanism. In an experimental environment, variations in temperature and solvent polarity stimulate copolymer micelle self-assembly. This is a thermodynamically guided procedure in which self-assembly happens by converting polymeric micelles. These aggregates go from a non-equilibrium to a thermodynamically equilibrium state, and they stay stable for a long time. The balance of thermodynamic and kinetic forces is critical in micelles self-assembly because the kinetic process predicts assembly behaviour and hierarchical structure. The purpose of this special issue is to provide an updated overview of micelles, a number of polymers and drugs commonly used in micellar preparation and their application.

scholarly journals Recent Progress on Nanostructures for Drug Delivery Applications

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Haijiao Lu ◽  
Jingkang Wang ◽  
Ting Wang ◽  
Jian Zhong ◽  
Ying Bao ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Nucleic Acids ◽  
Small Molecules ◽  
Self Assembly ◽  
Building Materials ◽  
Driving Forces ◽  
Rapid Development ◽  
Poorly Soluble Drugs ◽  
Normal Tissues ◽  
Poorly Soluble

With the rapid development of nanotechnology, the convergence of nanostructures and drug delivery has become a research hotspot in recent years. Due to their unique and superior properties, various nanostructures, especially those fabricated from self-assembly, are able to significantly increase the solubility of poorly soluble drugs, reduce cytotoxicity toward normal tissues, and improve therapeutic efficacy. Nanostructures have been successfully applied in the delivery of diverse drugs, such as small molecules, peptides, proteins, and nucleic acids. In this paper, the driving forces for the self-assembly of nanostructures are introduced. The strategies of drug delivery by nanostructures are briefly discussed. Furthermore, the emphasis is put on a variety of nanostructures fabricated from various building materials, mainly liposomes, polymers, ceramics, metal, peptides, nucleic acids, and even drugs themselves.

scholarly journals Self-Emulsifying Formulations: A Pharmaceutical Review

2020 ◽  
Vol 10 (3) ◽  
pp. 231-240
Author(s):  
Chukwuma Agubata
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Concept Design ◽  
Lipophilic Drugs ◽  
Oil In Water ◽  
Poorly Soluble ◽  
Mild Agitation

The oral route of drug delivery is commonly utilized for administration of medicines and is particularly preferred for the treatment of many chronic diseases which require continuous ingestion over a reasonably prolonged period of time. However the oral delivery of lipophilic drugs presents a major obstacle because of their low aqueous solubility. The aqueous solubility of a drug is a crucial determinant of its dissolution rate, absorption and bioavailability. Drugs with relatively high intrinsic lipophilicity can be dissolved in appropriate mixtures of oils/lipids, surfactants, cosolvents which can rapidly form oil-in-water (o/w) fine emulsions when dispersed in aqueous phase under mild agitation or mixing. These isotropic self-emulsifying formulations or self-emulsifying drug delivery systems are effective for delivery of poorly soluble, lipophilic drugs by dispersing the drugs within fine oil droplets in emulsions and this solubilization of drugs can then improve its absorption, bioavailability and therapeutic efficacy. The present paper reviews the concept, design, formulation, characterization and applications of self-emulsifying formulations. Keywords: Self-Emulsifying Formulations, lipophilicity, emulsions

Carbon Nanotubes, Quantum Dots and Dendrimers as Potential Nanodevices for Nanotechnology Drug Delivery Systems

2013 ◽  
Vol 6 (3) ◽  
pp. 2113-2124
Author(s):  
Prashant Malik ◽  
Neha Gulati ◽  
Raj Kaur Malik ◽  
Upendra Nagaich
Keyword(s):  
Carbon Nanotubes ◽  
Drug Delivery ◽  
Quantum Dots ◽  
Self Assembly ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Atomic Scale ◽  
Sustained Drug Delivery ◽  
Pharmaceutical Nanotechnology ◽  
Conventional Device

Nanotechnology deal with the particle size in nanometers. Nanotechnology is ranging from extensions of conventional device physics to completely new approaches based upon molecular self assembly, from developing new materials with dimensions on the nanoscale to direct control of matter on the atomic scale. In nanotechnology mainly three types of nanodevices are described: carbon nanotubes, quantum dots and dendrimers. It is a recent technique used as small size particles to treat many diseases like cancer, gene therapy and used as diagnostics. Nanotechnology used to formulate targeted, controlled and sustained drug delivery systems. Pharmaceutical nanotechnology embraces applications of nanoscience to pharmacy as nanomaterials and as devices like drug delivery, diagnostic, imaging and biosensor materials. Pharmaceutical nanotechnology has provided more fine tuned diagnosis and focused treatment of disease at a molecular level.    

Self-assembly of Amphiphilic Tripeptides into Nanoparticles for Drug Delivery

2013 ◽  
Vol 21 (2) ◽  
pp. 194-199
Author(s):  
Zhaoxu Tu ◽  
Xianghui Xu ◽  
Yeting Jian ◽  
Dan Zhong ◽  
Bin He ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly

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.

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