Synthesis of Eudragit® L100-coated chitosan-based nanoparticles for oral enoxaparin delivery

Patriota, Yuri Basílio Gomes; Arruda, Igor Eduardo Silva; Oliveira, Antônia Carla de Jesus; Oliveira, Thaísa Cardoso de; Silva, Eliadna de Lemos Vasconcelos; Chaves, Luíse L.; Ribeiro, Fábio de Oliveira Silva; Silva, Durcilene Alves da; Soares, Mônica Felts de La Roca; Soares-Sobrinho, José Lamartine

doi:10.1016/j.ijbiomac.2021.10.111

Cited by 18 publications

(4 citation statements)

References 38 publications

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“…The particles were less than 300 nm in size, exhibited a polydispersity index of about 0.12, a zeta potential of more than +25 mV, an entrapment efficiency greater than 95%, and negligible cumulative enoxaparin release (10%) when subjected to simulated gastric fluid conditions, thus demonstrating the success of the Eudragit ® L100-coating process. These results indicate that the enteric-coating method and drug delivery nanotechnology are viable options for enoxaparin oral administration [ 40 ]. Nanoparticles have gained prominence as a promising drug delivery technology in recent years.…”

Section: Nanotechnology In Delivery Systemsmentioning

confidence: 99%

Chitosan in Oral Drug Delivery Formulations: A Review

Sangnim,

Dheer,

Jangra

et al. 2023

Pharmaceutics

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Nanoformulations have become increasingly useful as drug delivery technologies in recent decades. As therapeutics, oral administration is the most common delivery method, although it is not always the most effective route because of challenges with swallowing, gastrointestinal discomfort, low solubility, and poor absorption. One of the most significant barriers that medications must overcome to exert a therapeutic effect is the impact of the first hepatic transit. Studies have shown that controlled-release systems using nanoparticles composed of biodegradable natural polymers significantly improve oral administration, which is why these materials have attracted significant attention. Chitosan possesses a wide variety of properties and functions in the pharmaceutical as well as healthcare industries. Drug encapsulation and transport within the body are two of its most important features. Moreover, chitosan can enhance drug efficacy by facilitating drug interaction with target cells. Based on its physicochemical properties, chitosan can potentially be synthesized into nanoparticles, and this review summarizes recent advances and applications of orally delivered chitosan nanoparticle interventions.

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Section: Nanotechnology In Delivery Systemsmentioning

confidence: 99%

Chitosan in Oral Drug Delivery Formulations: A Review

Sangnim,

Dheer,

Jangra

et al. 2023

Pharmaceutics

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“…Akhgari et al [22] also used ES100 and ERS100 polymers as carriers for preparing electrospun indomethacin-loaded nanofibers for specific drug delivery. Patriota et al [23] developed a new sort of spherical Eudragit-coated nanoparticle with the combined usage of Eudragit and chitosan (CS). These reports obviously suggested that Eudragit series polymers are popular for delivering a drug to the specific areas of the gut regardless of their formats of monolithic nanocomposites, core-shell nanofibers or particles.…”

Section: Introductionmentioning

confidence: 99%

Tri-Layer Core–Shell Fibers from Coaxial Electrospinning for a Modified Release of Metronidazole

Wang,

Liu,

Zhu

et al. 2023

Pharmaceutics

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Polymers are the backbone of drug delivery. Electrospinning has greatly enriched the strategies that have been explored for developing novel drug delivery systems using polymers during the past two decades. In this study, four different kinds of polymers, i.e., the water-soluble polymer poly (vinyl alcohol) (PVA), the insoluble polymer poly(ε-caprolactone) (PCL), the insoluble polymer Eudragit RL100 (ERL100) and the pH-sensitive polymer Eudragit S100 (ES100) were successfully converted into types of tri-layer tri-polymer core–shell fibers through bi-fluid coaxial electrospinning. During the coaxial process, the model drug metronidazole (MTD) was loaded into the shell working fluid, which was an emulsion. The micro-formation mechanism of the tri-layer core–shell fibers from the coaxial emulsion electrospinning was proposed. Scanning electron microscope and transmission electron microscope evaluations verified the linear morphology of the resultant fibers and their obvious tri-layer multiple-chamber structures. X-ray diffraction and Fourier transform infrared spectroscopy measurements demonstrated that the drug MTD presented in the fibers in an amorphous state and was compatible with the three polymeric matrices. In vitro dissolution tests verified that the three kinds of polymer could act in a synergistic manner for a prolonged sustained-release profile of MTD in the gut. The drug controlled-release mechanisms were suggested in detail. The protocols reported here pioneer a new route for creating a tri-layer core–shell structure from both aqueous and organic solvents, and a new strategy for developing advanced drug delivery systems with sophisticated drug controlled-release profiles.

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“…Eudragit and polylactic acid microspheres had low insulin entrapment e ciency and enzymatically degraded. Trimethyl-CT facilitated insulin absorption in synergism with Eudragit clay [17]. For insulin@ Eudragit microspheres, Mg-stearate lubricant optimize emulsion droplet size [17].…”

Section: Introductionmentioning

confidence: 99%

“…Trimethyl-CT facilitated insulin absorption in synergism with Eudragit clay [17]. For insulin@ Eudragit microspheres, Mg-stearate lubricant optimize emulsion droplet size [17].…”

Section: Introductionmentioning

confidence: 99%

New advanced approach for processing natural polymers chitin and guar gum for developing new bioactive biocompatible drug delivery systems for oral administration of insulin

Fetouh

A.Aleem

Mohammed

et al. 2022

Preprint

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Two nanocomposites samples of oral administrations insulin-drug delivery systems: insulin@chitin and insulin@chitin-grafted (g)-guar gum are prepared by using a modified sol-gel method. The novelty of this preparations is that, it is the first time to load insulin vials on such safe ecofriendly natural polymers using water as green solvent. The traces number of chemical agents used in these preparations are below the toxicity limits. Native chitin and chitin-g-guar gum crosslinked copolymer are used as inert bioactive carriers for insulin vials. Guar gum increased the numbers of functional groups of the copolymer. Spectrophotometric monitoring of insulin release at physiological temperature, 37 ± 0.5ºC and buffer solutions pH 1.2, 6.8, 7.4. These tested aqueous solutions simulating biological body fluids of stomach, intestine colon and blood stream. Insulin release from insulin@chitin only at pH 7.4 as monitored by spectrophotometry. No insulin released can be monitored at pH 1.2, and 6.8 due strong bonding of insulin to acetyl group of chitin. In contrast, insulin@chitin- g-guar gum showed sustained targeting insulin-release followed the order: pH 6.8 > pH 7.4 > pH 1.2. The release data obeyed pseudo second order kinetic model indicating that this coplymer is heterogeneous solid surface of energetically different active sites and each insulin molecule occupied two active sites. Slow rate of insulin release at pH 1.2 indicated its protection against stomach juice. The kinetic results and the physicochemical characteristics porosity, swelling ratio, peptide&amino acid sequence, zeta potential, particle size showed that: insulin loaded on chitin by chemisorbed monolayer and it is loaded on the copolymer by chemi-, and phyi-sorption forces. Both insulin@chitin and insulin@chitin-g-GG nanocomposites showed negative zeta potential indicating adequate stability against coagulation. However, insulin@chitin-g-GG nanocomposite showed more monodispersed particle size distribution (than insulin@chitin) enhancing insulin release.

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Synthesis of Eudragit® L100-coated chitosan-based nanoparticles for oral enoxaparin delivery

Cited by 18 publications

References 38 publications

Chitosan in Oral Drug Delivery Formulations: A Review

Chitosan in Oral Drug Delivery Formulations: A Review

Tri-Layer Core–Shell Fibers from Coaxial Electrospinning for a Modified Release of Metronidazole

New advanced approach for processing natural polymers chitin and guar gum for developing new bioactive biocompatible drug delivery systems for oral administration of insulin

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