In-vitro and in-vivo cytotoxicity and efficacy evaluation of novel glycyl-glycine and alanyl-alanine conjugates of chitosan and trimethyl chitosan nano-particles as carriers for oral insulin delivery

Omid, Nersi Jafary; Javan, Nika Bahari; Dehpour, Ahmad Reza; Partoazar, Alireza; Tehrani, Morteza Rafiee; Dorkoosh, Farid Abedin

doi:10.1016/j.ijpharm.2017.11.020

Cited by 35 publications

(13 citation statements)

References 46 publications

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“…It is advantageous in term of enhancing the paracellular transport through binding directly to negatively-charged mucus and increasing the retention time of cargo on the mucosal surface prior to opening the tight junctions of epithelial cells [ 105 ]. Many researches have synthesised TMC due to its solubility in a wide range of pH (1–9), thus regardless varying pH value along GIT, the positive charge is maintained and so the advantageous properties of the polymer [ 106 , 107 ].…”

Section: Chitosan Modificationmentioning

confidence: 99%

“…The prepared GG- and AA-conjugated TMC nanoparticles exhibited 2.5–3.3-fold higher permeability of insulin in Caco-2 cell line compared to unmodified TMC nanoparticles. In animal model, oral administration of GG and AA conjugate nanoparticles of TMC demonstrated reasonable increase in serum insulin level (almost 50%, 45%), with relative bioavailability of 17.19% and 15.46%, respectively compared with TMC nanoparticles (14.15%) [ 106 ].…”

Section: Chitosan Modificationmentioning

confidence: 99%

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Recent Progress of Chitosan and Chitosan Derivatives-Based Nanoparticles: Pharmaceutical Perspectives of Oral Insulin Delivery

2020

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Diabetes mellitus is a chronic endocrine disease, affecting more than 400 million people around the world. Patients with poorly controlled blood glucose levels are liable to suffer from life-threatening complications, such as cardiovascular, neuropathy, retinopathy and even premature death. Today, subcutaneous parenteral is still the most common route for insulin therapy. Oral insulin administration is favourable and convenient to the patients. In contrast to injection route, oral insulin delivery mimics the physiological pathway of endogenous insulin secretion. However, oral insulin has poor bioavailability (less than 2%) due to the harsh physiological environment through the gastrointestinal tract (GIT). Over the last few decades, many attempts have been made to achieve an effective oral insulin formulation with high bioavailability using insulin encapsulation into nanoparticles as advanced technology. Various natural polymers have been employed to fabricate nanoparticles as a delivery vehicle for insulin oral administration. Chitosan, a natural polymer, is extensively studied due to the attractive properties, such as biodegradability, biocompatibility, bioactivity, nontoxicity and polycationic nature. Numerous studies were conducted to evaluate chitosan and chitosan derivatives-based nanoparticles capabilities for oral insulin delivery. This review highlights strategies that have been applied in the recent five years to fabricate chitosan/chitosan derivatives-based nanoparticles for oral insulin delivery. A summary of the barriers hurdle insulin absorption rendering its low bioavailability such as physical, chemical and enzymatic barriers are highlighted with an emphasis on the most common methods of chitosan nanoparticles preparation. Nanocarriers are able to improve the absorption of insulin through GIT, deliver insulin to the blood circulation and lower blood glucose levels. In spite of some drawbacks encountered in this technology, chitosan and chitosan derivatives-based nanoparticles are greatly promising entities for oral insulin delivery.

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Section: Chitosan Modificationmentioning

confidence: 99%

Section: Chitosan Modificationmentioning

confidence: 99%

Recent Progress of Chitosan and Chitosan Derivatives-Based Nanoparticles: Pharmaceutical Perspectives of Oral Insulin Delivery

2020

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“…Chitin is a natural biopolymer extracted from the exoskeleton of crustaceans (shrimp, crabs, lobsters, etc. ) and from the cell walls of fungi or yeast (Illum, 1998;Mukhopadhyay et al, 2013;Vasiliev, 2015;Bugnicourt and Ladavière, 2016;Jafary Omid et al, 2018;Primex, 2019).…”

Section: Chitosan: Potential and Versatilitymentioning

confidence: 99%

“…This polymer is one of the most widely used for biomedical applications. Actually, chitosan has been under investigation for drug and vaccine delivery (Borges et al, 2008;Esmaeili et al, 2010;Jafary Omid et al, 2018;Bento et al, 2019), gene delivery (Thanou et al, 2002), surgical sutures (Muzzarelli et al, 1993;Altinel et al, 2018), rebuilding of bone (Lee et al, 2009), corneal contact lenses (Silva et al, 2016), dental implants (Yokoyama et al, 2002), wound healing (Mizuno et al, 2003), antimicrobial applications (Dai et al, 2009), and tissue engineering (Madihally and Matthew, 1999;Kanimozhi et al, 2016). Moreover, chitosan has been used as a dietary supplement in preparations for treatment of obesity and hypercholesterolemia (Bokura and Kobayashi, 2003;Zhang et al, 2008) and also in medical devices for the treatment and control of bleeding (Millner et al, 2009).…”

Section: Chitosan: Potential and Versatilitymentioning

confidence: 99%

How the Lack of Chitosan Characterization Precludes Implementation of the Safe-by-Design Concept

Marques

Som

Schmutz

et al. 2020

Front. Bioeng. Biotechnol.

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Efficacy and safety of nanomedicines based on polymeric (bio)materials will benefit from a rational implementation of a Safe-by-Design (SbD) approach throughout their development. In order to achieve this goal, however, a standardization of preparation and characterization methods and their accurate reporting is needed. Focusing on the example of chitosan, a biopolymer derived from chitin and frequently used in drug and vaccine delivery vector preparation, this review discusses the challenges still to be met and overcome prior to a successful implementation of the SbD approach to the preparation of chitosan-based protein drug delivery systems.

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“…Transports various natural di/tri-peptides and comprehensive peptide-mimetics. High capacity, low affinity82., 83.CSK peptide transportersIn goblet cellsCSK peptide specifically recognize goblet cells84AT-1002 peptideOpen TJsA hexamer peptide derived from ZOT open the TJs transiently and reversibly85Monocarboxylate transporterIn the intestineCellular uptake of SCFAs efficiently, among which butyrate is in majority, a key mediator of physiological function in the intestine86CD44 receptorIn the intestineA highly heterogeneous single-stranded transmembrane glycoprotein widely expressed on the membrane87ASBT, apical sodium-dependent bile acid transporter; CSK, CSKSSDYQC; ZOT, zonula occludins toxin; TJs, tight junctions; UEA-1, ulex europaeus agglutinin-1; SCFAs, short chain fatty acids.…”

Section: Introductionmentioning

confidence: 99%

Multifunctional oral delivery systems for enhanced bioavailability of therapeutic peptides/proteins

Han

Gao

Chen

et al. 2019

Acta Pharmaceutica Sinica B

113

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In last few years, therapeutic peptides/proteins are rapidly growing in drug market considering their higher efficiency and lower toxicity than chemical drugs. However, the administration of therapeutic peptides/proteins is mainly limited in parenteral approach. Oral therapy which was hampered by harsh gastrointestinal environment and poorly penetrating epithelial barriers often results in low bioavailability (less than 1%–2%). Therefore, delivery systems that are rationally designed to overcome these challenges in gastrointestinal tract and ameliorate the oral bioavailability of therapeutic peptides/proteins are seriously promising. In this review, we summarized various multifunctional delivery systems, including lipid-based particles, polysaccharide-based particles, inorganic particles, and synthetic multifunctional particles that achieved effective oral delivery of therapeutic peptides/proteins.

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In-vitro and in-vivo cytotoxicity and efficacy evaluation of novel glycyl-glycine and alanyl-alanine conjugates of chitosan and trimethyl chitosan nano-particles as carriers for oral insulin delivery

Cited by 35 publications

References 46 publications

Recent Progress of Chitosan and Chitosan Derivatives-Based Nanoparticles: Pharmaceutical Perspectives of Oral Insulin Delivery

Recent Progress of Chitosan and Chitosan Derivatives-Based Nanoparticles: Pharmaceutical Perspectives of Oral Insulin Delivery

How the Lack of Chitosan Characterization Precludes Implementation of the Safe-by-Design Concept

Multifunctional oral delivery systems for enhanced bioavailability of therapeutic peptides/proteins

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