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 and safe polymer that possesses the capacity of opening intercellular tight junctions of epithelium and excellent mucoadhesive property. Chitosan-based nanocarriers have recently attracted considerable attentions, aiming to overcome GI limitations and enhance drug absorption. Recently developed chitosan-based nanocarriers administered via oral route were highlighted for protecting drugs against degradation, releasing drugs in small intestine, enhancing drug uptake, thus improving oral bioavailability. Finally, various biotherapeutics including hydrophobic and hydrophilic drugs applied in chitosan-based nanovectors were also reviewed.
Abstract To improve the quality of life of diabetic patients, oral delivery of insulin would be better than subcutaneous injection, and the encapsulation of insulin for its oral delivery is a promising alternative one. In this study, we prepared an oral insulin delivery system using thiolated chitosan nanoparticles (TCNPs) loaded with insulin (Ins) and tested under in vitro and in vivo systems. TCNPs prepared from CS and pentaerythritol tetrakis (3-mercaptopropionate) (PETMP) at 4:1 ratio showed...
#1Tiane Chen(GLMU: Guilin Medical University)H-Index: 2
Last. Jianfang Feng(JUTCM: Jiangxi University of Traditional Chinese Medicine)H-Index: 1
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Abstract Chitosan is widely used as a permeation enhancer for oral drug delivery, although its drawbacks include a limited enhancement of drug bioavailability and an inability to form micelles. In this study, we designed a novel chitosan derivative (GA-CS-TPGS copolymer) and constructed paclitaxel micelles (PTX-Micelles) designed to have multiple functions associated with the GA-CS-TPGS copolymer (enhanced bioadhesion, inhibited P-gp efflux and drug metabolism in liver) and the micelles (enhance...
Abstract The study investigated chitosan coated nanostructured lipid carriers (NLCs) for oral delivery of albendazole in treatment of trichinellosis. NLCs comprised precirol and oleic acid with Tween and Span 80. Dicetylphosphate was used as charging agent to allow chitosan coating. Trichinella spiralis infected mice were used and albendazole suspension, coated or uncoated NLCs were orally administered at different stages of infection. NLCs were spherical with size of 188 and 200 nm for coated a...
#1Xiao Du(CPU: China Pharmaceutical University)H-Index: 4
#2Shaoping Yin(CPU: China Pharmaceutical University)H-Index: 6
Last. Juan Li(CPU: China Pharmaceutical University)H-Index: 12
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Abstract A novel chitosan-based multifunctional nanoparticle (PY-CS-PLA) using cationic polylysine (PL) polymer and L-cysteine has been developed and investigated for the oral delivery of paclitaxel (PTX). As amphiphilic polymer, PY-CS-PLA presented good capability in self-assembling into spherical nanoparticle with mean size of 165 nm, and encapsulating PTX into the hydrophobic core. The encapsulated PTX was observed to be sustainedly released from the functionalized chitosan nanoparticle, and ...
Last. David Díaz(University of Regensburg)H-Index: 58
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Abstract In this study, insulin-loaded nanoparticles (NPs) were prepared via self-gelation method using chitosan and aqueous soluble snail mucin as natural polymers. Herein, mucins were ionically interacted with chitosan at different concentrations to obtained insulin-loaded NPs, labelled as A1 (1:1) (i.e., chitosan 2 % w/v + mucin 2 % w/v) and A2 (2:1) (chitosan 4 % w/v + mucin 2 % w/v), using poloxamer and poly vinyl alcohol as solid surfactant. Such formulation was selected to provide the nec...
#1Lai Pan Sze(CUHK: The Chinese University of Hong Kong)H-Index: 1
#2Ho Yin Li(CUHK: The Chinese University of Hong Kong)H-Index: 5
Last. Wai Yip Thomas Lee(CUHK: The Chinese University of Hong Kong)H-Index: 4
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Abstract Drug solubility and permeability are two major challenges affecting oral delivery, the most popular route of drug administration. Polymeric micelles is an emerging technology for overcoming the current oral drug delivery hurdles. Previous study primarily focused on developing new polymers or new micellar systems and a systematic investigation of the impact of the polymer block length on solubility and permeability enhancement; and their subsequent effect on oral bioavailability is lacki...
#1Xinying Yu(UQ: University of Queensland)H-Index: 2
#2Tinggang Wen(UQ: University of Queensland)H-Index: 1
Last. Li Li(UQ: University of Queensland)H-Index: 45
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Abstract Layered double hydroxide nanoparticles (LDHs) have shown the excellent capability and good adjuvant function as a nanocarrier for protein antigen delivery to enhance the immune response. Furthermore, LDHs have good biocompatibility and low cytotoxicity. However, their oral vaccine delivery efficiency is limited due to acidic/enzyme degradation in the stomach and low bioavailability in the small intestine. To overcome these challenges, alginate-chitosan coated LDHs nanocomposites (ALG-CH...
#2Fangqin Wang(Ocean University of China)H-Index: 3
Last. Ya Liu(Ocean University of China)H-Index: 21
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Abstract Colorectal cancer (CRC) is a prevalent and fatal cancer. Oral administration provided the potential for in situ treatment of the colorectal cancer. However, drugs couldn't be well-absorbed mainly due to its degradation in the gastric area and poor intestinal permeability. In this study, we synthesized deoxycholic acid and hydroxybutyl decorated chitosan nanoparticles (DAHBC NPs) as oral curcumin (CUR) delivery system for colorectal cancer treatment. DAHBC with lower critical solution te...
Abstract The bioadhesive drug delivery systems, chitosan modified nanoparticles, can efficiently adhere to mucosal surface of gastrointestinal tract and prolong residence time but a deeper understanding about its cellular uptake and transport is still lack. Hence, the present study was designed to compare the process of uptake and transport between chitosan modified and unmodified PLGA nanoparticles. Chitosan modified nanoparticles were formulated by classic and chemical methods. The morphology ...
Last. Liuqing Di(Nanjing University of Chinese Medicine)H-Index: 19
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Abstract This study compared the in vitro and in vivo effects of different aliphatic acid grafted N-trimethyl chitosan (TMC) surface-modified nanostructured lipid carriers (NLC) by oral delivery. Medium-chain fatty acids, decylic acids (DA), and long-chain fatty acids, palmitic acids (PA) were selected as contrasting objects. TMC, DA grafted TMC (DA-TMC), and PA grafted TMC (PA-TMC) were successively synthesized. Kaempferol loaded NLC (KNLC), KNLC coated with DA-TMC (DA-TMC-KNLC) and PA-TMC (PA-...
Abstract null null Here, we report a one-pot solvothermal method for the development of magnetically recoverable catalysts with Ru or Ag nanoparticles (NPs) capped by chitosan (CS), a derivative of natural chitin. The formation of iron oxide NPs was carried out in situ in the presence of CS and iron acetylacetonate in boiling triethyleneglycol (TEG) due to CS solubilization in warm TEG. Coordination with Ru or Ag species and the NP formation take place in the same reaction solution, eliminating ...
The postprandial glycemic regulation is essential for diabetic patients to reduce the risk of long-term microvascular and macrovascular complications. Herein, we designed a glucose-responsive oral insulin delivery system based on polyelectrolyte complexes (PECs) for controlling the increasing postprandial glucose concentrations. Briefly, alginate-g-3-aminophenylboronic acid (ALG-g-APBA) and chitosan-g-3-fluoro-4-carboxyphenylboronic acid (CS-g-FPBA) were wrapped on mesoporous silica (MSN) to for...
Abstract null null Infectious diseases continue to inflict a high global disease burden. The consensus is that vaccination is the most effective option against infectious diseases. Oral vaccines have unique advantages in the prevention of global pandemics due to their ease of use, high compliance, low cost, and the ability to induce both systemic and mucosal immune responses. However, challenges of adapting vaccines for oral administration remain significant. Foremost among these are enzymatic a...
#1Tivadar Feczkó(MTA: Hungarian Academy of Sciences)H-Index: 18
Abstract Nanoparticulate drug delivery systems provide a vast number of potential nanomedicines. Biocompatible synthetic and natural polymers are especially promising materials for nanoparticle (NP) preparation. Biodegradable polymeric NPs may improve the drug stability, availability and activity of insoluble active agents. Their size can be tunable and they might protect the drug from degradation. Due to their benefits, they can decrease dose frequency, thus, reduce side effects. They are espec...
Last. Wei Liu(Jiangxi Normal University)H-Index: 50
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Abstract A simple approach was developed to formulate polysaccharide-based high internal phase emulsions (HIPEs) using complexes of sugar beet pectin (SBP), tannic acid (TA), and chitosan (CS) to stabilize the system. The ability of pectin to stabilize the HIPEs was significantly improved after it formed complexes with TA, which were likely held together by hydrogen bonding. The stability of the HIPEs was further improved by adding CS, which was attributed to the formation of a 3D biopolymer net...
Abstract null null The widespread application of soluble enzymes in industrial processes is considered restrict due to instability of enzymes outside optimum operating conditions. For instance, enzyme immobilization can overcome this issue. In fact, chitosan–based nanofibers have outstanding properties, which can improve the efficiency in enzyme immobilization and the stability of enzymes over a wide range of operating conditions. These properties include biodegradability, antimicrobial activity...
Nanogels have high tunability and stability while being able to sense and respond to external stimuli by showing changes in the gel volume, water content, colloidal stability, mechanical strength, and other physical/chemical properties. In this article, advances in the preparation of nanogels will be reviewed. The application potential of nanogels in drug delivery will also be highlighted. It is the objective of this article to present a snapshot of the recent knowledge of nanogel preparation an...
The small intestine provides the major site for the absorption of numerous orally administered drugs. However, before reaching to the systemic circulation to exert beneficial pharmacological activities, the oral drug delivery is hindered by poor absorption/metabolic instability of the drugs in gastrointestinal (GI) tract and the presence of the mucus layer overlying intestinal epithelium. Therefore, a polymeric drug delivery system has emerged as a robust approach to enhance oral drug bioavailab...
Last. Mithun Sarker(DU: University of Dhaka)H-Index: 13
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A series of bifunctional nanohybrids containing different proportions of chitosan and titanium dioxide (TiO2) were prepared through precipitation technique and applied for removal of a model anionic azo dye, Remazol Orange 3R (RO), from aqueous solution. This study reveals the dual benefit of adsorption and photocatalytic degradation of RO by TiO2/Chitosan nanohybrids. Nanohybrid fabricated from 80% TiO2 (w/w) and 20% chitosan (w/w) termed as T0.80CS0.20 removed ∼98.8% RO within only 8 min at pH...
Last. Ya Liu(Ocean University of China)H-Index: 21
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Allergic rhinitis (AR), histamine-mediated upper airway inflammatory disorder, is characterized by sneezing, itching, airway hyperreactivity, etc. Though it is clinically well-managed by non-invasive inhaled antihistamines, for example, ketotifen (KT, histamine release inhibitor) and cetirizine (CTZ, histamine receptor antagonist), inherent defects of short mucosal in situ retention, frequent administration resulting in irritation to mucosa, and lack of target-specific sequential release of dual...