Progress and prospects of polysaccharide-based nanocarriers for oral delivery of proteins/peptides

Yuan, Haoyang; Chen, Guo; Liu, Lei; Zhao, Linxuan; Yin, Tian; He, Haibing; Gou, Jingxin; Pan, Bochen; Tang, Xing

doi:10.1016/j.carbpol.2023.120838

Cited by 31 publications

(4 citation statements)

References 178 publications

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“…The oral bioavailability of hydrophilic macromolecular drugs, such as peptides and proteins, is extremely low due to their low stability and poor membrane permeability in the gastrointestinal tract. Natural polysaccharides have been widely investigated as potential delivery systems to improve the oral bioavailability of peptides and proteins in the last decades, still remaining a subject of great interest [ 43 ]. The objective of this investigation was to formulate optimal delivery systems for oral insulin administration.…”

Section: Discussionmentioning

confidence: 99%

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

Bácskay,

Papp,

Pártos

et al. 2023

Pharmaceutics

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The development of oral insulin drug delivery systems is still an ongoing challenge for pharmaceutical technology researchers, as the formulation process has to overcome a number of obstacles due to the adverse characteristics of peptides. The aim of this study was to formulate different sodium-alginate microparticles as a possible method for oral insulin administration. In our previous studies, the method has been successfully optimized using a small model peptide. The incorporation of insulin into alginate carriers containing nonionic surfactants has not been described yet. In order to enhance the absorption of insulin through biological barriers, Labrasol ALF and Labrafil M 2125 CS were selected as permeation-enhancing excipients. They were applied at a concentration of 0.10% (v/v%), along with various combinations of the two, to increase oral bioavailability. Encapsulation efficiency showed sufficient drug incorporation, as it resulted in over 80% in each composition. In vitro dissolution and enzymatic stability test results proved that, as a pH-responsive polymer, alginate bead swelling and drug release occur at higher pH, thus protecting insulin against the harsh environment of the gastrointestinal tract. The remaining insulin content was 66% due to SIF degradation after 120 min. Permeability experiments revealed the impact of permeation enhancers and natural polymers on drug absorption, as they enhanced drug transport significantly through Caco-2 cells in the case of alginate microparticle formulations, as opposed to the control insulin solution. These results suggest that these formulations are able to improve the oral bioavailability of insulin.

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Section: Discussionmentioning

confidence: 99%

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

Bácskay,

Papp,

Pártos

et al. 2023

Pharmaceutics

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“…Their molecular structure enhances their binding efficiency and stability with proteins/peptides. This is due to their desirable characteristics, including low immunogenicity, high biocompatibility, and effective lymphatic absorption [ 120 ]. Bone morphogenetic protein 2 (BMP-2) is a soluble peptide that can activate cartilage formation.…”

Section: Research On Polysaccharide-aunps As Drug Delivery Carriersmentioning

confidence: 99%

Research Progress of Polysaccharide-Gold Nanocomplexes in Drug Delivery

Song,

Aipire,

Dilxat

et al. 2024

Pharmaceutics

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Clinical drug administration aims to deliver drugs efficiently and safely to target tissues, organs, and cells, with the objective of enabling their therapeutic effects. Currently, the main approach to enhance a drug’s effectiveness is ensuring its efficient delivery to the intended site. Due to the fact that there are still various drawbacks of traditional drug delivery methods, such as high toxicity and side effects, insufficient drug specificity, poor targeting, and poor pharmacokinetic performance, nanocarriers have emerged as a promising alternative. Nanocarriers possess significant advantages in drug delivery due to their size tunability and surface modifiability. Moreover, nano-drug delivery systems have demonstrated strong potential in terms of prolonging drug circulation time, improving bioavailability, increasing drug retention at the tumor site, decreasing drug resistance, as well as reducing the undesirable side effects of anticancer drugs. Numerous studies have focused on utilizing polysaccharides as nanodelivery carriers, developing delivery systems based on polysaccharides, or exploiting polysaccharides as tumor-targeting ligands to enhance the precision of nanoparticle delivery. These types of investigations have become commonplace in the academic literature. This review aims to elucidate the preparation methods and principles of polysaccharide gold nanocarriers. It also provides an overview of the factors that affect the loading of polysaccharide gold nanocarriers with different kinds of drugs. Additionally, it outlines the strategies employed by polysaccharide gold nanocarriers to improve the delivery efficiency of various drugs. The objective is to provide a reference for further development of research on polysaccharide gold nanodelivery systems.

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“…Such structural rigidity, contrary to linear peptides, improves the enzymatic stability in the GI tract and prevents them from digestion [102]. In addition, peptide cyclization may improve oral bioavailability by reducing polar atoms exposure and changing PPs conformations into bioactive ones [103,104].…”

Section: Peptide Cyclization and Substitutions Of Aasmentioning

confidence: 99%

The Current and Promising Oral Delivery Methods for Protein- and Peptide-Based Drugs

Nicze,

Borówka,

Dec

et al. 2024

IJMS

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Drugs based on peptides and proteins (PPs) have been widely used in medicine, beginning with insulin therapy in patients with diabetes mellitus over a century ago. Although the oral route of drug administration is the preferred one by the vast majority of patients and improves compliance, medications of this kind due to their specific chemical structure are typically delivered parenterally, which ensures optimal bioavailability. In order to overcome issues connected with oral absorption of PPs such as their instability depending on digestive enzymes and pH changes in the gastrointestinal (GI) system on the one hand, but also their limited permeability across physiological barriers (mucus and epithelium) on the other hand, scientists have been strenuously searching for novel delivery methods enabling peptide and protein drugs (PPDs) to be administered enterally. These include utilization of different nanoparticles, transport channels, substances enhancing permeation, chemical modifications, hydrogels, microneedles, microemulsion, proteolytic enzyme inhibitors, and cell-penetrating peptides, all of which are extensively discussed in this review. Furthermore, this article highlights oral PP therapeutics both previously used in therapy and currently available on the medical market.

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Progress and prospects of polysaccharide-based nanocarriers for oral delivery of proteins/peptides

Cited by 31 publications

References 178 publications

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

Research Progress of Polysaccharide-Gold Nanocomplexes in Drug Delivery

The Current and Promising Oral Delivery Methods for Protein- and Peptide-Based Drugs

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