Self-Assembly of Zein-Based Microcarrier System for Colon-Targeted Oral Drug Delivery

Wang, Hongdi; Zhang, Xiaolin; Wang, Zhu; Jiang, Yanbin; Zhang, Zhibing

doi:10.1021/acs.iecr.8b02092

Cited by 29 publications

(10 citation statements)

References 53 publications

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“…Guo and Shi (2009) stated dry coated zein tablets that showed a preliminary swelling of around 80% and an erosion of 4% that continued persistently with time [52]. Zein has been reported to be nonerosive in aqueous media and tolerant to intestinal enzymes; nevertheless, the longer term may increase zein degradation [53,54]. Another reason for the lack of pepsin impact on the release of the drug may be the limited surface exposed to the dissolution media due to its buoyant nature.…”

Section: Discussionmentioning

confidence: 99%

Effect of Zein on Ciprofloxacin Floating Tablets

SINGH¹,

R²,

Mazumder³

et al. 2022

Int J App Pharm

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Objective: This work was aimed to formulate and evaluate the effect of zein on Ciprofloxacin HCl floating tablets. According to previous studies, it was set up to be useful against bacteria i.e. Helicobacter pylori which leads to peptic ulcers. Thus, it is quite necessary to enhance the Gastric Retention Time for similar medicines. Methods: 12 different floating tablets of Ciprofloxacin HCl were formulated with wet granulation method with a rise in the concentration of zein. Further, all different formulations prepared were evaluated for different parameters i.e. pre-compression considerations, along with post-compression factors like weight variation, content uniformity, thickness, visual assessment, hardness, friability, buoyancy studies i.e. total floating time as well as floating lag time, swelling index, dissolution and drug release kinetics. Results: The F6 formulation was considered to be among finest formulation with appropriate hardness. It was found that with the increasing concentration of zein, the hardness of tablets was also increased. It showed TFT of more than 7 h, FLT of 310 sec, a swelling index time of 99.5 % in 4 hr, while drug release kinetics was found to follow Higuchi Model. Conclusion: Overall it was also found that HPMCK-100M is more effective as compared to HPMC-K15M and Zein has a major role in increasing the hardness of tablets. In the future, the investigation will be continued with the following studies: An in vivo study and a long-term stability study.

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Section: Discussionmentioning

confidence: 99%

Effect of Zein on Ciprofloxacin Floating Tablets

SINGH¹,

R²,

Mazumder³

et al. 2022

Int J App Pharm

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“…Liu et al studied zein/pectin beads for colonic drug delivery, showing a delayed release of indomethacin in vitro in the presence of pectinate enzymes [25]. In another study, Wang et al investigated in situ polymerization of dopamine in indomethacin-encapsulating zein matrixes, which showed a sustained release of the drug under in vitro conditions [26]. More recently, Bisharat et al showed similar results for acetylated high amylose starch/zein film coatings for colonic delivery of paracetamol tablets [27].…”

Section: Introductionmentioning

confidence: 97%

Bioadhesive Tannic-Acid-Functionalized Zein Coating Achieves Engineered Colonic Delivery of IBD Therapeutics via Reservoir Microdevices

et al. 2022

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The biggest challenge in oral delivery of anti-inflammatory drugs such as 5-aminosalicylic acid (5-ASA) is to (i) prevent rapid absorption in the small intestine and (ii) achieve localized release at the site of inflammation in the lower gut, i.e., the colon. Here, we present an advanced biopolymeric coating comprising of tannic-acid-functionalized zein protein to provide a sustained, colon-targeted release profile for 5-ASA and enhance the mucoadhesion of the dosage form via a mussel-inspired mechanism. To enable localized delivery and provide high local concentration, 5-ASA is loaded into the microfabricated drug carriers (microcontainers) and sealed with the developed coating. The functionality and drug release profile of the coating are characterized and optimized in vitro, showing great tunability, scalability, and stability toward proteases. Further, ex vivo experiments demonstrate that the tannic acid functionalization can significantly enhance the mucoadhesion of the coating, which is followed up by in vivo investigations on the intestinal retention, and pharmacokinetic evaluation of the 5-ASA delivery system. Results indicate that the developed coating can provide prolonged colonic delivery of 5-ASA. Therefore, the here-developed biodegradable coating can be an eco-friendly substitute to the state-of-the-art commercial counterparts for targeted delivery of 5-ASA and other small molecule drugs.

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“…Besides its biocompatibility, biodegradability and low toxicity, zein can resist the degradation resulted from gastric acid and gastrointestinal enzymes. (Wang et al, 2018). In view of those advantages, zein-based NPs have been attempted to encapsulate drugs for colon delivery.…”

Section: Introductionmentioning

confidence: 99%

Colon-specific delivery of isoliquiritigenin by oral edible zein/caseate nanocomplex for ulcerative colitis treatment

Xiao

Cheng

et al. 2022

Front. Chem.

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Although a natural anti-inflammatory ingredient, isoliquiritigenin (ISL), plays an effective role in ulcerative colitis (UC) treatment, a series of drawbacks still limit its clinical application, including the poor solubility, instability in gastrointestinal tract, and rapid elimination rate of ISL. Zein-based NPs display the benefits on drug loading and delivery, whereas with the poor stability. In this study, an edible nano-system composed by zein/caseinate complex was fabricated for the colon-targeting delivery of ISL, to improve its colon retention and anti-UC effects. The optimized ISL loaded zein/caseinate NPs (ISL@NPs) were prepared by single-factor design by anti-solvent precipitation method, and then characterized. The improved cellular uptake of ISL@NPs on NCM460 and RAW 264.7 cells was evaluated in vitro. The colon tissue permeability and retention capacity in vivo, and the anti-UC efficacy of ISL@NPs in DSS-induce UC were implemented. As a result, ISL@NPs with the high drug loading efficiency of 9.39% ± 0.26%, the average particle diameter of 137.32 ± 2.54 nm, exhibited the pH-sensitive stability in the different simulated gastrointestinal buffer. Compared with free ISL, ISL@NPs showed significantly higher cellular uptake ability in NCM460 and RAW 264.7 cells. Based on in vivo imaging system, zein/caseinate NPs showed the prolonged colonic retention and the enhanced penetration into the colonic epithelium. Finally, the oral administration of ISL@NPs could effectively alleviate the UC-related symptoms, down-regulate the production of pro-inflammatory factors, and reduce the infiltration of macrophages and neutrophils in colon tissues. In this study, an oral colon-specific nano-system, composed with the natural compound and edible materials, was developed as the promising alternatives in the prevention and treatment of UC.

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Self-Assembly of Zein-Based Microcarrier System for Colon-Targeted Oral Drug Delivery

Cited by 29 publications

References 53 publications

Effect of Zein on Ciprofloxacin Floating Tablets

Effect of Zein on Ciprofloxacin Floating Tablets

Bioadhesive Tannic-Acid-Functionalized Zein Coating Achieves Engineered Colonic Delivery of IBD Therapeutics via Reservoir Microdevices

Colon-specific delivery of isoliquiritigenin by oral edible zein/caseate nanocomplex for ulcerative colitis treatment

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