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.

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.

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.

Physical stimuli-responsive liposomes and polymersomes as drug delivery vehicles based on phase transitions in the membrane

Nanoscale ◽  
2018 ◽  
Vol 10 (15) ◽  
pp. 6781-6800 ◽  
Author(s):  
Yangwei Deng ◽  
Jun Ling ◽  
Min-Hui Li
Keyword(s):  
Drug Delivery ◽  
Phase Transitions ◽  
Drug Release ◽  
Liquid Crystalline ◽  
Stimuli Responsive ◽  
Physical Stimulation ◽  
Drug Delivery Vehicles ◽  
Liquid Crystalline Phases ◽  
Physical Stimuli ◽  
Delivery Vehicles

Crystalline and liquid crystalline phases in the membrane lead to intriguing morphologies of vesicles for drug release upon physical stimulation.

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

Paclitaxel modified Fe3O4 loaded albumin nanoparticles as drug delivery vehicles by self-assembly

RSC Advances ◽  
2016 ◽  
Vol 6 (49) ◽  
pp. 43284-43292 ◽  
Author(s):  
Xiang-long Tang ◽  
Ben-lan Lin ◽  
Sheng Cui ◽  
Xin Zhang ◽  
Yang Zhong ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Self Assembly ◽  
Drug Delivery Vehicles ◽  
Albumin Nanoparticles ◽  
Assembly Method ◽  
Delivery Vehicles

Paclitaxel (PTX) modified superparamagnetic Fe3O4 nanoparticles (Fe3O4/PTX NPs) are obtained and then Fe3O4/PTX NPs are loaded into human serum albumin (HSA) to form novel Fe3O4/PTX/HSA NPs with pie structure by self-assembly method.

Dendrimers: General Aspects, Applications and Structural Exploitations as Prodrug/Drug-delivery Vehicles in Current Medicine

2018 ◽  
Vol 18 (5) ◽  
pp. 439-457 ◽  
Author(s):  
Merina Mariyam ◽  
Kajal Ghosal ◽  
Sabu Thomas ◽  
Nandakumar Kalarikkal ◽  
Mahima S. Latha
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Vehicles ◽  
Delivery Vehicles ◽  
General Aspects

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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