scholarly journals Colonic Delivery of Celastrol-Loaded Layer-by-Layer Liposomes with Pectin/Trimethylated Chitosan Coating to Enhance Its Anti-Ulcerative Colitis Effects

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2005
Author(s):  
Jing Xian ◽  
Xuemei Zhong ◽  
Huan Gu ◽  
Xiao Wang ◽  
Jiaxin Li ◽  
...  
Keyword(s):  
Therapeutic Strategy ◽  
Inflammatory Factors ◽  
Layer By Layer ◽  
Colonic Delivery ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Chitosan Coating ◽  
Targeting Delivery ◽  
Prolonged Retention ◽  
Layer Coating

Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and accelerated colitis repair in DSS-treated mice by regulating the levels of pro-inflammatory factors related to the TLR4/MyD88/NF-κB signaling pathway. Collectively, this study demonstrates that the pectin/trimethylated chitosan coating may allow for Cel/PT-LbL Lipo to function as a more beneficial therapeutic strategy for UC treatment.

scholarly journals Studies on the Drug Loading and Release Profiles of Degradable Chitosan-Based Multilayer Films for Anticancer Treatment

Cancers ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 593 ◽  
Author(s):  
Hyeongdeok Sun ◽  
Daheui Choi ◽  
Jiwoong Heo ◽  
Se Yong Jung ◽  
Jinkee Hong
Keyword(s):  
Drug Release ◽  
Multilayer Film ◽  
Drug Loading ◽  
Building Blocks ◽  
Multilayer Films ◽  
Release Profile ◽  
Layer By Layer ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Release Profiles

This study demonstrates the possibility of developing a rapidly degradable chitosan-based multilayer film for controlled drug release. The chitosan (CHI)-based multilayer nanofilms were prepared with three different types of anions, hyaluronic acid (HA), alginic acid (ALG) and tannic acid (TA). Taking advantage of the Layer-by-Layer (LBL) assembly, each multilayer film has different morphology, porosity and thickness depending on their ionic density, molecular structure and the polymer functionality of the building blocks. We loaded drug models such as doxorubicin hydrochloride (DOX), fluorescein isothiocyanate (FITC) and ovalbumin (Ova) into multilayer films and analyzed the drug loading and release profiles in phosphate-buffered saline (PBS) buffer with the same osmolarity and temperature as the human body. Despite the rapid degradation of the multilayer film in a high pH and salt solution, the drug release profile can be controlled by increasing the functional group density, which results in interaction with the drug. In particular, the abundant carboxylate groups in the CHI/HA film increased the loading amount of DOX and decreased rapid drug release. The TA interaction with DOX via electrostatic interaction, hydrogen bonding and hydrophobic interaction showed a sustained drug release profile. These results serve as principles for fabricating a tailored multilayer film for drug delivery application.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Water Solubility ◽  
Tween 80 ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Bacterial Conjunctivitis ◽  
Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

Collagen-based layer-by-layer coating on electrospun polymer scaffolds

Biomaterials ◽  
2012 ◽  
Vol 33 (36) ◽  
pp. 9198-9204 ◽  
Author(s):  
Yen B. Truong ◽  
Veronica Glattauer ◽  
Kelsey L. Briggs ◽  
Stefan Zappe ◽  
John A.M. Ramshaw
Keyword(s):  
Layer By Layer ◽  
Polymer Scaffolds ◽  
Layer Coating

scholarly journals Receptor-mediated mitophagy regulates EPO production and protects against renal anemia

eLife ◽  
2021 ◽  
Vol 10 ◽  
Author(s):  
Guangfeng Geng ◽  
Jinhua Liu ◽  
Changlu Xu ◽  
Yandong yan Pei ◽  
Linbo Chen ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Quality Control ◽  
Therapeutic Strategy ◽  
Inflammatory Responses ◽  
Critical Role ◽  
Renal Anemia ◽  
Inflammatory Factors ◽  
Oxygen Species ◽  
Mitochondrial Quality Control ◽  
Hematopoietic Disorders

Erythropoietin (EPO) drives erythropoiesis and is secreted mainly by the kidney upon hypoxic or anemic stress. The paucity of EPO production in renal EPO-producing cells (REPs) causes renal anemia, one of the most common complications of chronic nephropathies. Although mitochondrial dysfunction is commonly observed in several renal and hematopoietic disorders, the mechanism by which mitochondrial quality control impacts renal anemia remains elusive. In this study, we showed that FUNDC1, a mitophagy receptor, plays a critical role in EPO-driven erythropoiesis induced by stresses. Mechanistically, EPO production is impaired in REPs in Fundc1-/- mice upon stresses, and the impairment is caused by the accumulation of damaged mitochondria, which consequently leads to the elevation of the reactive oxygen species (ROS) level and triggers inflammatory responses by up-regulating proinflammatory cytokines. These inflammatory factors promote the myofibroblastic transformation of REPs, resulting in the reduction of EPO production. We therefore provide a link between aberrant mitophagy and deficient EPO generation in renal anemia. Our results also suggest that the mitochondrial quality control safeguards REPs under stresses, which may serve as a potential therapeutic strategy for the treatment of renal anemia.

scholarly journals Improving the Vertical Thermal Conductivity of Carbon Fiber-Reinforced Epoxy Composites by Forming Layer-by-Layer Contact of Inorganic Crystals

Materials ◽  
2019 ◽  
Vol 12 (19) ◽  
pp. 3092 ◽  
Author(s):  
Eunbi Lee ◽  
Chi Hyeong Cho ◽  
Sae Hoon Hwang ◽  
Min-Geun Kim ◽  
Jeong Woo Han ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Thermal Conductivity ◽  
Carbon Fiber ◽  
Layer By Layer ◽  
Fiber Reinforced ◽  
Cfrp Composites ◽  
Inorganic Crystals ◽  
Layer Contact ◽  
Carbon Fiber Reinforced ◽  
Layer Coating

A carbon fiber-reinforced polymer (CFRP) is a light and rigid composite applicable in various fields, such as in aviation and automobile industry. However, due to its low thermal conductivity, it does not dissipate heat sufficiently and thus accumulates heat stress. Here, we reported a facile and effective strategy to improve the through-thickness thermal conductivity of CFRP composites by using a layer-by-layer coating of inorganic crystals. They could provide efficient heat transfer pathways through layer-by-layer contact within the resulting composite material. The high thermally conductive CFRP composites were prepared by employing three types of inorganic crystal fillers composed of aluminum, magnesium, and copper on prepreg through the layer-by-layer coating process. The vertical thermal conductivity of pure CFRP was increased by up to 87% on using magnesium filler at a very low content of 0.01 wt %. It was also confirmed that the higher the thermal conductivity enhancement was, the better were the mechanical properties. Thus, we could demonstrate that the layer-by-layer inclusion of inorganic crystals can lead to improved through-thickness thermal conductivity and mechanical properties of composites, which might find applications in varied industrial fields.

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