Fabrication and evaluation of a novel polymeric hydrogel of carboxymethyl chitosan-g-polyacrylic acid (CMC-g-PAA) for oral insulin delivery

RSC Advances ◽  
2016 ◽  
Vol 6 (58) ◽  
pp. 52858-52867 ◽  
Author(s):  
Jing Zhang ◽  
Xiaoyang Liang ◽  
Ying Zhang ◽  
Qing Shang
Keyword(s):  
Polyacrylic Acid ◽  
Potential Application ◽  
Oral Delivery ◽  
Insulin Delivery ◽  
Carboxymethyl Chitosan ◽  
Oral Insulin ◽  
Protein Drugs ◽  
Alkaline Environment ◽  
Polymeric Hydrogel

The CMC-g-PAA hydrogels could release INS in alkaline environment (i.e. intestinal), specifically. This method could prevent IND from destroying by pepsase. Therefore, the CMC-g-PAA hydrogel had a potential application on the oral delivery of protein drugs.

scholarly journals In vivo oral insulin delivery via covalent organic frameworks

2021 ◽  
Author(s):  
Farah Benyettou ◽  
Nawel Kaddour ◽  
Thirumurugan Prakasam ◽  
Gobinda Das ◽  
Sudhir Kumar Sharma ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Insulin Delivery ◽  
Oral Insulin ◽  
Covalent Organic Frameworks ◽  
Covalent Organic Framework ◽  
Organic Framework

We report the successful use of a gastro-resistant covalent organic framework for in vivo oral delivery of insulin.

scholarly journals Oral Insulin Delivery Using Poly (Styrene Co-Maleic Acid) Micelles in a Diabetic Mouse Model

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1026
Author(s):  
Fatemah Bahman ◽  
Sebastien Taurin ◽  
Diab Altayeb ◽  
Safa Taha ◽  
Moiz Bakhiet ◽  
...  
Keyword(s):  
Mouse Model ◽  
Maleic Acid ◽  
Oral Delivery ◽  
Animal Studies ◽  
Ex Vivo ◽  
Insulin Delivery ◽  
Diabetic Mouse ◽  
Oral Insulin

The oral delivery of insulin is a convenient and safe physiological route of administration for management of diabetes mellitus. In this study, we developed a poly-(styrene-co-maleic acid) (SMA) micellar system for oral insulin delivery to overcome the rapid degradation of insulin in the stomach, improve its absorption in the intestine, and provide a physiologically-relevant method of insulin to reach portal circulation. The insulin was encapsulated into SMA micelles in a pH-dependent process. The charge and size of the nanoparticles were determined by dynamic light scattering. The insulin loading of the nanoparticles was measured by HPLC. The transport of the SMA-insulin through biological membranes was assessed in vitro using Caco-2 cells, ex vivo rat intestinal section, and in vivo in a streptozotocin-induced diabetes mouse model. SMA-insulin micelles were negatively charged and had a mean diameter of 179.7 nm. SMA-insulin efficiently stimulated glucose uptake in HepG-2 hepatic cells and was transported across the Caco-2 epithelial cells in vitro by 46% and ex vivo across intestinal epithelium by 22%. The animal studies demonstrated that orally-administered SMA-insulin can produce a hypoglycemic effect up to 3 h after administration of one dose. Overall, our results indicate that SMA micelles are capable of the oral delivery of bioactive compounds like insulin and can be effective tools in the management of diabetes.

scholarly journals Oral insulin delivery for treatment of diabetes mellitus

2021 ◽  
pp. 66-70
Author(s):  
Durga Devi K
Keyword(s):  
Diabetes Mellitus ◽  
Oral Delivery ◽  
Proteolytic Enzymes ◽  
Insulin Delivery ◽  
Oral Route ◽  
Intestinal Lumen ◽  
Oral Insulin ◽  
Polymer Microsphere ◽  
Enzyme Degradation ◽  
Treatment Of Diabetes

Diabetes mellitus is characterized by a condition known as hyperglycemia which may be controlled through medication and insulin. Current insulin therapy for diabetes mellitus involves frequent dosing of subcutaneous injections, causing local discomfort, patient incompliance, hypoglycemia, and hyperinsulinemia, among others, one of the approaches to overcoming these issues is to administer insulin through oral route. An oral form of insulin has been the elusive goal for many investigators since the protein initial discovery by Banting and Best in 1922. Oral delivery of insulin is one of the promising and anticipated areas in the treatment of diabetes, primarily because it may significantly improve the quality of life of patients who receives insulin regularly. However, there are several challenges in developing an oral route for insulin delivery; include low bioavailability due to rapid enzyme degradation in the stomach, inactivation, and digestion by proteolytic enzymes in the intestinal lumen, poor permeability, and poor stability. Several companies have developed technology platforms that protect polypeptides and proteins from enzymatic hydrolysis, enable their transport across the epithelial lining, and promote their absorption from the GI tract. Most notably, the use of permeation enhancers, protease inhibitors, enteric coatings, and polymer microsphere formulation will be covered, including commentary on which methods hold more promise towards the successful development of oral insulin. This review, considers the current literature on the advances, methods, needs, and challenges in the development of oral insulin.

Carboxymethyl β-cyclodextrin grafted carboxymethyl chitosan hydrogel-based microparticles for oral insulin delivery

2020 ◽  
Vol 246 ◽  
pp. 116617 ◽  
Author(s):  
Yu Yang ◽  
Yang Liu ◽  
Shengqin Chen ◽  
Kit-Leong Cheong ◽  
Bo Teng
Keyword(s):  
Insulin Delivery ◽  
Carboxymethyl Chitosan ◽  
Oral Insulin ◽  
Chitosan Hydrogel

Preparation and characterization of layer-by-layer hypoglycemic nanoparticles with pH-sensitivity for oral insulin delivery

2018 ◽  
Vol 6 (45) ◽  
pp. 7451-7461 ◽  
Author(s):  
Li Zhang ◽  
Han Qin ◽  
Jian Li ◽  
Jia-Ni Qiu ◽  
Jing-Min Huang ◽  
...  
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Insulin Delivery ◽  
Ph Sensitive ◽  
Ph Sensitivity ◽  
Oral Insulin ◽  
Layer By Layer ◽  
Sensitive Material ◽  
Oral Delivery System

We developed an insulin oral delivery system with the combination of pH-sensitive material and structure to avoid intestinal degradation.

scholarly journals Preparation of snail cyst and PEG-4000 composite carriers via PEGylation for oral delivery of insulin: An in vitro and in vivo evaluation

2021 ◽  
Vol 18 (5) ◽  
pp. 919-926
Author(s):  
Mumuni A. Momoh ◽  
Ossai C. Emmanuel ◽  
Azubuike C. Onyeto ◽  
Youngson Darlington ◽  
Franklin C. Kenechukwu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Liquid Paraffin ◽  
Insulin Delivery ◽  
Diabetic Rats ◽  
Diffusion Method ◽  
Oral Insulin ◽  
Peg 4000

Purpose: To develop PEGylated mucin as a carrier system for oral insulin delivery. Methods: Varied ratios of snail cyst were molecularly modified with polyethylene glycol 4000 (PEG 4000). Briefly, In each case, 20 g quantities of snail cyst and PEG 4000 were separately dispersed in distilled water, stirred and allowed to stand for 24 h to produce a homogeneous dispersion and clear solution, respectively. The solution of PEG was added to the snail cyst dispersion, stirred and allowed 12 h for molecular interaction. The mixture was added to a 250-mL beaker containing 100 mL of light liquid paraffin. The microparticles were obtained after stirring and removing the paraffin using chilled acetone. The obtained PEGylated mucin matrices, which were subsequently loaded with insulin using a diffusion method, characterized for particles size, drug loading, encapsulation efficiency, in vitro drug release and evaluated for oral application in diabetic rats. Results: The polymer hybrids improved insulin encapsulation efficiency (max 82.3 %), gave. polydispersity indices that ranged from 0.11 ± 0.1 to 0.24 ± 0.2, zeta potential values between 28 ± 0.3 and 38 ± 1.1 mV. Insulin release was highest (68 % in 6 h) for batch C and was sustained for 10 h in simulated intestinal fluid. The optimized batch (C-5) showed higher hypoglycaemic activity (56.5 %) than control (0.5 %) in diabetic rats. Conclusion: The results suggest that PEGylated mucin can potentially be developed as a platform for oral insulin delivery

Physically crosslinked alginate/N,O-carboxymethyl chitosan hydrogels with calcium for oral delivery of protein drugs

Biomaterials ◽  
2005 ◽  
Vol 26 (14) ◽  
pp. 2105-2113 ◽  
Author(s):  
Yu-Hsin Lin ◽  
Hsiang-Fa Liang ◽  
Ching-Kuang Chung ◽  
Mei-Chin Chen ◽  
Hsing-Wen Sung
Keyword(s):  
Oral Delivery ◽  
Carboxymethyl Chitosan ◽  
Protein Drugs ◽  
Physically Crosslinked ◽  
Chitosan Hydrogels

Ionic gelated β-cyclodextrin-biotin-carboxymethyl chitosan nanoparticles prepared as carrier for oral delivery of protein drugs

2020 ◽  
Vol 40 (5) ◽  
pp. 440-447
Author(s):  
Kuanmin Chen ◽  
Suoju He ◽  
Hui Wang ◽  
Song Zhang ◽  
Lizhen Yu ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Carboxymethyl Chitosan ◽  
Simulated Gastric Fluid ◽  
Protein Drugs ◽  
Simulated Intestinal Fluid ◽  
Cytotoxicity Studies ◽  
Release Profiles

AbstractIn this paper, the β-cyclodextrin (β-CD) and biotin (Bi) were successfully grafted onto carboxymethyl chitosan (CMCS). And then the β-CD-Bi-CMCS nanoparticles (NPs) were prepared as oral nano-delivery carrier of protein drugs by ionic gelation method. The morphological feature of fabricated drug carrier was determined by dynamic light scattering and transmission electron microscopy. The result showed that the prepared NPs presented spherical structure with an average diameter of 138 nm. Bovine serum albumin (BSA) was selected as model protein drug that was entrapped in prepared drug carrier with satisfactory entrapment efficiency (79.18%) and loading content (3.96%). The drug release profiles of BSA/β-CD-Bi-CMCS NPs were studied at different pH environment for simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). It was found that the BSA/β-CD-Bi-CMCS NPs displayed a pH dependent drug release profiles. After 72 h, the cumulative release amount of BSA in SGF, SIF, and SCF was about 20.57, 74.46, and 91%, respectively. Furthermore, the enzymatic degradation and cytotoxicity studies showed the synthesized β-CD-Bi-CMCS NPs had high chemical stability and biocompatibility. This work indicated that the β-CD-Bi-CMCS NPs had the potentiality as promising nanocarriers for oral delivery of protein drugs.

Sign in / Sign up

Export Citation Format

Share Document