Match!

Optimization of pH-responsive carboxymethylated iota-carrageenan/chitosan nanoparticles for oral insulin delivery using response surface methodology

Published on Oct 1, 2017in Reactive & Functional Polymers3.074
· DOI :10.1016/j.reactfunctpolym.2017.08.014
Pratyusa Sahoo1
Estimated H-index: 1
(UM: University of Malaya),
Kok Hoong Leong10
Estimated H-index: 10
(UM: University of Malaya)
+ 3 AuthorsLip Yong Chung19
Estimated H-index: 19
(UM: University of Malaya)
Abstract
Abstract In designing an oral delivery method for insulin, we previously reported that pH-responsive carboxymethylated kappa -carrageenan-based microparticles protected insulin from acid degradation during transport through the gastrointestinal tract. However, the low surface-to-volume ratio of these microparticles and the presence of only one sulfate group in each kappa -carrageenan subunit for insulin stabilization may lead to a suboptimal delivery efficiency. To improve the delivery efficiency, we designed a nanoparticle from chitosan (CS) and carboxymethylated iota -carrageenan (CMCi) that possessed two sulfate groups per subunit based on response surface methodology together with multivariate spline interpolation (RSM MSI ). The resulting optimized nanoparticles had a zeta potential, mean particle size, loading capacity and entrapment efficiency of 52.5 ± 0.5 mV, 613 ± 41 nm, 10.7 ± 0.6%, and 86.9 ± 2.6%, respectively. The release of insulin from the optimized nanoparticles was low (4.91 ± 0.24%) in simulated gastric fluid (SGF) and high (86.64 ± 2.2%) in simulated intestinal fluid (SIF) during a 12-h release study, thereby showing a pH-responsive drug release property. The nanoparticles were stable at 4 °C and − 20 °C for at least 90 days and for up to 7 days at room temperature. The RSM MSI technique successfully expedited the design of the nanoparticles, which could serve as an improved oral insulin drug delivery system.
  • References (40)
  • Citations (4)
📖 Papers frequently viewed together
108 Citations
68 Citations
164 Citations
78% of Scinapse members use related papers. After signing in, all features are FREE.
References40
Newest
#1Muhammad RizwanH-Index: 4
#2Rosiyah YahyaH-Index: 20
Last. Cheyma Naceur AbouloulaH-Index: 1
view all 8 authors...
Improving the safety efficacy ratio of existing drugs is a current challenge to be addressed rather than the development of novel drugs which involve much expense and time. The efficacy of drugs is affected by a number of factors such as their low aqueous solubility, unequal absorption along the gastrointestinal (GI) tract, risk of degradation in the acidic milieu of the stomach, low permeation of the drugs in the upper GI tract, systematic side effects, etc. This review aims to enlighten reader...
60 CitationsSource
#1Jianyong Sheng (Fudan University)H-Index: 6
#2Huining He (Tianjin Medical University)H-Index: 18
Last. Victor C. Yang (Tianjin Medical University)H-Index: 43
view all 10 authors...
Abstract Although significant progress has been achieved, effective oral delivery of protein drugs such as insulin by nanoparticle-based carrier systems still faces certain formidable challenges. Considerable amount of protein drug is released from the nanoparticles (NPs) in the gastrointestinal (GI) tract. Because of their low permeability through the intestinal mucosa, the released protein would be soon degraded by the large amount of proteases in the GI tract. Herein, we report an oral insuli...
46 CitationsSource
Abstract In this paper, chitosan was reacted with monochloroacetic acid under alkaline conditions to prepare carboxymethyl chitosan. A 23 full-factorial central composite design was applied to evaluate the effect of molar ratio sodium hydroxide (NaOH)/Chitosan (Ch), time and molar ratio monochloroacetic acid (MCA)/Chitosan (Ch) on the reaction yield and on the characteristics of carboxymethyl chitosan such as average degree of substitution ( D S ¯ ) and solubility. An optimization strategy based...
36 CitationsSource
#1Frida J. Wende (SLU: Swedish University of Agricultural Sciences)H-Index: 2
#2Suresh Gohil (SLU: Swedish University of Agricultural Sciences)H-Index: 13
Last. Corine Sandström (SLU: Swedish University of Agricultural Sciences)H-Index: 17
view all 9 authors...
Abstract In hydrogels of cross-linked polysaccharides, the total amount of cross-linker and the degree of cross-linking influence the properties of the hydrogel. The substitution position of the cross-linker on the polysaccharide is another parameter that can influence hydrogel properties; hence methods for detailed structural analysis of the substitution pattern are required. NMR and LC–MS methods were developed to determine the positions and amounts of substitution of 1,4-butanediol diglycidyl...
11 CitationsSource
#1Xin JinH-Index: 1
#2Shi-bing ZhangH-Index: 1
Last. Zeng-yong JiaH-Index: 1
view all 5 authors...
Background: Salvianolic acid B (SalB) represents the most abundant and bio-active phenolic constituent among the water-soluble compounds of Salvia miltiorrhiza. But the therapeutic potential of SalB has been significantly restricted by its poor absorption. Methods: In this study, chitosans (CS) and CS nanoparticles (NPs) with different molecular weights (MWs), which have influence on the absorption of SalB, was also investigated. Results: As a preliminary study, water-soluble CS with various MWs...
7 CitationsSource
#1Milind Alai (NTU: National Taiwan University)H-Index: 4
#2Wen-Jen Lin (NTU: National Taiwan University)H-Index: 18
Last. Shailaja Suresh Pingale (AS: Academia Sinica)H-Index: 1
view all 3 authors...
Diabetes mellitus is an endocrine disease in which the pancreas does not produce sufficient insulin or the body cannot effectively use the insulin it produces. Insulin therapy has been the best choice for the clinical management of diabetes mellitus. The current insulin therapy is via subcutaneous injection, which often fails to mimic the glucose homeostasis that occurs in normal individuals. This provokes numerous attempts to develop a safe and effective noninvasive route for insulin delivery. ...
39 CitationsSource
#1Tadashi Norioka (Hoshi University)H-Index: 2
#2Yoshihiro Hayashi (Hoshi University)H-Index: 7
Last. Kozo Takayama (Hoshi University)H-Index: 47
view all 7 authors...
7 CitationsSource
Abstract Diabetes is a metabolic disease and is a major cause of mortality and morbidity in epidemic proportions. A type I diabetic patient is dependent on daily injections of insulin, for survival and also to maintain a normal life, which is uncomfortable, painful and also has deleterious effects. Extensive efforts are being made worldwide for developing noninvasive drug delivery systems, especially via oral route. Oral route is the most widely accepted means of administration. However it is no...
91 CitationsSource
#1Piyasi Mukhopadhyay (CU: University of Calcutta)H-Index: 11
#2Kishor Sarkar (CU: University of Calcutta)H-Index: 14
Last. Patit Paban Kundu (CU: University of Calcutta)H-Index: 29
view all 6 authors...
Abstract We have developed self-assembled chitosan/insulin nanoparticles for successful oral insulin delivery. The main purpose of our study is to prepare chitosan/insulin nanoparticles by self-assembly method, to characterize them and to evaluate their efficiency in vivo diabetic model. The size and morphology of the nanoparticles were analyzed by dynamic light scattering (DLS), atomic force microscopy (AFM) and scanning electron microscopy (SEM). The average particle size ranged from 200 to 55...
70 CitationsSource
#1Cody BulmerH-Index: 3
#2Argyrios MargaritisH-Index: 39
Last. Anargyros XenocostasH-Index: 21
view all 3 authors...
Novel chitosan-carrageenan nanoparticles were produced through the process of ionotropic gelation for the encapsulation and controlled release of recombinant human erythropoietin (rHu-EPO). The effects of chitosan concentration, chitosan to carrageenan mass ratio and solution pH on the nanoparticle diameter, polydispersity and surface charge were explored through both screening and response surface modeling (RSM) methods. The chitosan-carrageenan nanoparticles created had particle diameters betw...
22 CitationsSource
Cited By4
Newest
#1Xiangyan Chen (Ocean University of China)
#2Xia Zhao (Ocean University of China)H-Index: 14
Last. Guixiang Wang (Ocean University of China)
view all 3 authors...
Abstract Gold nanoparticles (AuNPs) have been attracted considerable attention in cancer therapy, drug delivery and other applications due to their unique physical, chemical, and optical properties. Marine carbohydrates are important biological macromolecules that widely exist in marine algae and animals, such as alginate, carrageenan, porphyran, fucoidan, ulvan, agarose, and chitosan. Their excellent properties, such as biocompatibility, biodegradability and no irritation, make them widely used...
Source
The oral drug administration was convenient and comfortable route for patients. Nevertheless, the oral uptake efficiency of many therapeutic agents was limited by physiological barriers of the gastrointestinal (GI) tract. This review summarized the challenges toward the oral delivery systems including instability and poor permeability in gastrointestinal environment. The transcellular and paracellular transport were main pathways of nanocarriers across intestinal epithelium. Chitosan is a nature...
Source
#1Nívia do Nascimento Marques (UFRN: Federal University of Rio Grande do Norte)H-Index: 4
view all 7 authors...
The synthesis of new polymeric materials from the monomers is an arduous task, which does not always achieve the desired success. A very promising alternative that grows each year is the chemical modification of existing polymers. In this case, the polymer is one of the reagents of well-known properties and, through conventional chemical reactions, new functional groups can be inserted into the polymer chain, leading to a wide diversity of properties and applications for the new materials obtain...
Source
#2Eleni VlassiH-Index: 4
Last. Aurel Radulescu (Forschungszentrum Jülich)H-Index: 23
view all 3 authors...
Abstract We use small angle neutron scattering (SANS) to characterize the internal morphology of nanoparticles (NPs) formed by the complexation between chondroitin sulfate (CS) and bovine serum albumin (BSA) and subsequent stabilization by thermal treatment. We demonstrate that SANS can quantify the internal rearrangements and protein morphology alterations upon thermal treatment and solution conditions variations. A three-level Guinier/power-law hierarchical model identifies BSA globules, inter...
Source
#1Pratyusa Sahoo (UM: University of Malaya)H-Index: 1
#2Kok Hoong Leong (UM: University of Malaya)H-Index: 10
Last. Lip Yong Chung (UM: University of Malaya)H-Index: 19
view all 6 authors...
Abstract We previously reported that insulin-entrapped chitosan complexed carboxymethylated iota-carrageenan (CS/CMCi) particles exhibit pH-responsive swelling behavior. However, the particles’ stability in the enzymatic gastrointestinal environment, their drug permeability mechanism, and related in vivo studies have not been discussed to date. In this study, we investigated the stability, muco-adhesiveness, transport mechanism and in vivo assessment of the particles. The particles retained thei...
Source
Abstract We combine electrostatic polysaccharide/protein complexation with subsequent thermal denaturation of proteins to produce chondroitin sulfate/bovine serum albumin nanoparticles that do not lose their integrity at neutral and basic pH. Light scattering at a wide angular range shows that nanoparticle size (radius of gyration and hydrodynamic radius) and molar mass may be tuned by the CS/BSA mass ratio while the irreversible protein-protein contacts upon temperature treatment endow the comp...
6 CitationsSource
#1Ahmed Gedawy (Curtin University)H-Index: 2
#2Jorge Martinez (Curtin University)H-Index: 5
Last. Crispin R. Dass (Curtin University)H-Index: 44
view all 4 authors...
14 CitationsSource