Construction and evaluation of liraglutide delivery system based on milk exosomes: a new idea for oral peptide delivery

2021 ◽  
Vol 22 ◽  
Author(s):  
Yanan Shi ◽  
Shiqi Guo ◽  
Yanzi Liang ◽  
Lanze Liu ◽  
Aiping Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Freeze Thaw ◽  
Loading Methods ◽  
Incubation Method ◽  
Oral Drug Delivery Systems ◽  
Extrusion Method

Background: Increasing the bioavailability of peptide or protein drugs has always been an essential topic in pharmacy. Milk exosomes as a carrier for oral drug delivery systems have begun to attract attention in recent years. The application of oral milk exosomes carriers to peptide drugs such as liraglutide is worth trying. Objective: Milk-derived exosomes are used in this study to encapsulate the GLP-1 receptor agonist liraglutide. It also explored the feasibility of using this drug delivery system for oral biomolecules delivery in the future. Methods: The size and morphology of milk exosomes were characterized. The gastrointestinal stability of milk exosomes was evaluated in a dialysis bag. The cellular uptake of milk exosomes in an intestinal cell was observed. Six drug loading methods have been evaluated and compared preliminarily, and they are the incubation method, sonication method, extrusion method, freeze-thaw cycles method, saponin-assisted method, and electroporation method. Results: As demonstrated in this study, milk exosomes showed significant stability in the gastrointestinal environment and excellent affinity with intestinal cells, indicating their unique benefits used for oral drug delivery. Effective drug loading method for exosomes is challenging. Among the six drug loading methods used in this study, the liraglutide-Exo prepared by the extrusion method obtained the most significant drug load, which was 2.45 times the direct incubation method. The liraglutide-Exo obtained by the freeze-thaw cycles method has the slightest morphological change. Conclusion: The study showed milk exosome-based oral drug delivery systems are promising.

scholarly journals Supersaturated Silica-Lipid Hybrid Oral Drug Delivery Systems: Balancing Drug Loading and In Vivo Performance

2018 ◽  
Vol 370 (3) ◽  
pp. 742-750 ◽  
Author(s):  
Hayley B. Schultz ◽  
Miia Kovalainen ◽  
Karl F. Peressin ◽  
Nicky Thomas ◽  
Clive A. Prestidge
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Delivery Systems ◽  
Oral Drug ◽  
Oral Drug Delivery Systems

Applications of Ion Exchange Resin in Oral Drug Delivery Systems

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Kathpalia Harsha ◽  
Das Sukanya
Keyword(s):  
Drug Delivery ◽  
Ion Exchange ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Physical Stability ◽  
Delivery Systems ◽  
Oral Drug ◽  
Ion Exchange Resins ◽  
Exchange Resins ◽  
Oral Drug Delivery Systems

Ion Exchange Resins (IER) are insoluble polymers having styrene divinylbenzene copolymer backbone that contain acidic or basic functional groups and have the ability to exchange counter ions with the surrounding aqueous solutions. From the past many years they have been widely used for purification and softening of water and in chromatographic columns, however recently their use in pharmaceutical industry has gained considerable importance. Due to the physical stability and inert nature of the resins, they can be used as a versatile vehicle to design several modified release dosage forms The ionizable drug is complexed with the resin owing to the property of ion exchange. This resin complex dissociatesin vivo to release the drug. Based on the dissociation strength of the drug from the drug resin complex, various release patterns can be achieved. Many formulation glitches can be circumvented using ion exchange resins such as bitter taste and deliquescence. These resins also aid in enhancing disintegrationand stability of formulation. This review focuses on different types of ion exchange resins, their preparation methods, chemistry, properties, incompatibilities and their application in various oral drug delivery systems as well as highlighting their use as therapeutic agents.

DETERMINATION OF THE OPTIMAL CONCENTRATIONS OF PECTIN AND CALCIUM CHLORIDE FOR THE SYNTHESIS OF CHITOSAN-PECTIN MICROPARTICLES

2021 ◽  
Author(s):  
Alla Krasnoshtanova ◽  
Anastasiya Bezyeva
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Calcium Chloride ◽  
Active Substance ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Oral Route ◽  
Delivery Systems ◽  
Oral Drug ◽  
Oral Drug Delivery Systems

"The oral route of drug inclusion is the most convenient for the patient. In addition to ease of use, this method of drug inclusion has such advantages as non-invasiveness of inclusion, absence of complications during injection; comparative safety for the organism due to the passage of the active substance and auxiliary compounds through the gastrointestinal tract; the possibility of introducing larger doses of the drug at one time. However, despite the obvious advantages, the oral route of inclusion has a number of significant disadvantages that significantly limit its use for a number of drugs. Among them are: relatively slow therapeutic action of the drug with this route of inclusion; the aggressive effect of a number of drugs (for example, antibiotics) on the gastrointestinal tract; low bioavailability of a number of substances (especially high molecular weight hydrophilic compounds), caused by poor permeability of the intestinal epithelium for hydrophilic and large molecules, as well as enzymatic and chemical degradation of the active substance in the gastrointestinal tract. There are various approaches used in the development of oral drug delivery systems. In particular, for the targeted delivery of drugs, it is proposed to use nano- and microcapsules with mucoadhesive properties. Among the polymers used for the synthesis of these microparticles, it is preferable to use pH-dependent, gelable biopolymers that change their structure depending on the acidity of the environment. Microcapsules obtained from compounds with the above properties are capable of protecting the active substance (or from the active substance) in the stomach environment and ensuring its release in the intestine. These properties are possessed by such polysaccharides as alginate, pectin, carrageenan, xylan, etc. The listed biopolymers are non-toxic, biocompatible, and biodegradable, which makes microparticles containing these polysaccharides promising as oral drug delivery systems. To impart mucoadhesive properties to nanoparticles, complexes of the listed polymers with chitosan are used. In this research, pectin, a polysaccharide formed mainly by residues of galacturonic acid, was used as a structural polymer. The concentrations of substances in the initial solutions were selected that were optimal for the synthesis of microcapsules. The main parameters for evaluating the resulting microparticles were the size of the capsules (less than 1 μm for oral inclusion), the zeta-potential, showing the tendency of the microparticles to stick together, and the completeness of the binding of the microparticles to chitosan. It was found that the optimal solutions for the synthesis of microparticles are: 15.7 ml of a solution of pectin 0.093% by weight, 3.3 ml of a solution of chitosan 0.07% by weight and 1.0 ml of a solution of CaCl2 20 mM. The diameter of the microparticles obtained by this method was 700-800 nm, and the value of their zetta-potential, equal to - (34 ± 3) mV, does not cross the particle adhesion threshold. It was also found that the synthesis of microparticles at these concentrations of calcium chloride provides the most complete binding of chitosan to their surface, which increases the mucoadhesive properties of microparticles."

Nanoparticles with surface features of dendritic oligopeptides as potential oral drug delivery systems

2020 ◽  
Vol 8 (13) ◽  
pp. 2636-2649
Author(s):  
Yuli Bai ◽  
Rui Zhou ◽  
Lei Wu ◽  
Yaxian Zheng ◽  
Xi Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Specific Surface ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Protein Drugs ◽  
Surface Features ◽  
Oral Drug Delivery Systems

Endowing the NPs with specific surface features of dendritic oligopeptides holds great potential for the oral delivery of peptide/protein drugs.

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