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Startseite » News » A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare

A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare

17. February 2023
A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare

A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare

Eudragit, synthesized by radical polymerization, is used for enteric coating, precise temporal release, and targeting the entire gastrointestinal system. Evonik Healthcare Germany offers different grades of Eudragit. The ratio of methacrylic acid to its methacrylate-based monomers used in the polymerization reaction defines the final product’s characteristics and consequently its potential range of applications. Since 1953, these polymers have been made to use in a wide range of healthcare applications around the world. In this review, we reviewed the “known of knowns and known of unknowns” about Eudragit, from molecule to material design, its characterization, and its applications in healthcare.

1. Introduction

In the last decades, natural or synthetic polymers have made a significant difference in painting, cosmetics, bio-imaging, trade, and medicine. The contributions of polymer science and engineering to healthcare applications are showing promise. These polymers have many advantages in drug delivery applications, such as being biodegradable, biocompatible, simple to eliminate from the body, minimizing the number of doses needed, maintaining the drug concentration level in the optimal range, and making patients more likely to take their medicine because the polymer coat hides the organoleptic characteristics of the formulation. According to literature studies, each polymer has some unique properties that permit the fabrication of nanotechnology-based formulation with a controlled size distribution, solubility, flexibility, and permeation for the intended application.

 

These properties are crucial in the development of novel polymeric carriers for the preparation of nanocarrier coating test masking site-specific release time-dependent release accomplished using multiple types of polymers to alter the release pattern or modify the release kinetics in therapeutic drug delivery application. To deliver the drug at target sites, the drug was enclosed in a polymeric shell matrix. However, some polymers have a few limitations, such as being non-compatible with active ingredients, non-biodegradable, and toxic; to overcome these problems, there is a growing concern for the synthesis of polymer by modern polymerization method with catalysis. In recent years, Eudragit has proven to be one of the most attractive areas of research due to the importance of its advanced drug delivery system. Rohm & Hass GmbH, Darmstadt, first introduced Eudragit in 1953 as an acid-resistant, alkaline-soluble drug coating functional material. Eudragit is a brand name marketed primarily by Evonik Technologies Germany.
It is an extensive collection of anionic, cationic, or neutral copolymers derived from methacrylic acid and methacrylic or acrylic esters, as well as their derivatives. According to their physicochemical properties, such copolymers synthesized using diverse polymerization techniques such as reversible addition–fragmentation chain transfer (RAFT), atom transfer radical polymerization (ATRP), and group transfer exhibit varying degrees of pH-dependent or independent solubility in numerous studies. Different varieties of Eudragit polymer are utilized to selectively target the entire GIT, including the small intestine, colon, and large intestine. These copolymers are also investigated for protein and drug protection from the stomach’s acidic environment, etc. Eudragit are nonionic and synthetic polyionic copolymers, including different concentrations of methacrylic acid esters, alkyl methacrylates, 2-(dimethylamino)ethyl methacrylate. The various concentration of non-ionized and ionized groups in the structure of these copolymers generally controls. They are typically used as film-coating agents in oral tablets as well capsule formulations for protection and to give prolonged release dosage form. In both organic and aqueous wet granulation techniques, Eudragit polymers are used as binders [1].

 

The next paragraph discusses the nomenclature of several grades of Eudragit polymer. Eudragit E100, E12,5, and EPO are cationic copolymer made from methyl methacrylate, dimethylaminoethyl methacrylate, and butyl methacrylate in all three grades. Poly(butyl methacrylate-co-(2-dimethylamino) ethyl methacrylate-co-methyl methacrylate) is its chemical name. The alkali range is 180 mg KOH/g, the molecular weight is roughly 47,000 g/mol, and the solubility at gastric pH 5 is low viscosity. Both Eudragit S 12,5 and S 100 are anionic copolymers that are produced from methyl methacrylate and methacrylic acid. Glass transition temperature, acid value, and molecular weight is >150 °C, 190 mg KOH/g, 125,000 g/mol, and soluble in basic pH at 7.0. Soluble Eudragit FS 30D is an anionic copolymer of methacrylic acid, methyl acrylate, and methyl methacrylate. Glass transition temperature, acid value, and molecular weight is >150 °C, 190 mg KOH/g, 125,000 g/mol, and soluble in basic pH at 7.0. Soluble Eudragit FS 30D is an anionic copolymer of methacrylic acid, methyl acrylate, and methyl methacrylate. It is soluble in above pH 7 but insoluble in acid pH. Glass temperature, molecular weight, and acid value are 48 °C, 280,000 g/mol, and 70 mg KOH/g. Eudragit L12,5 and L 100 anionic derived methyl methacrylic acid and methacrylic acid have the same molecular weight, 125,000 g/mol, glass transition temperature of more than 150 °C acid value of 315 mg KOH/g, and soluble above pH 6. Eudragit RL100, RL 30 D, and RLPO are copolymers containing methyl methacrylate and ethyl acrylate with quaternary ammonium groups and less methacrylate acid. RL 30D grade has low viscosity and a milky-white appearance. Its glass transition temperatures are 40 °C and 55 °C, and its molecular weight is 32,000 g/mol. Eudragit RL 100 and RLPO share a 70 °C glass temperature, 32,000 g/mol molecular weight, and 28.1 mg KOH/g acid value [2].

 

Furthermore, the majority of Eudragit polymer grades are widely used for coating pharmaceutical formulations and the development of innovative drug delivery systems. In this review, we describe the Eudragit polymer, classification, chemical composition, characterization, and synthesis of Eudragit, as well as its applicability as a carrier system in multidisciplinary research on targeted drug administration. We also look at the use of functionalized Eudragit in many advanced drug delivery applications such as capsule and tablet coating, processing of microsphere nanoparticles nanofibers, and so on.

 

Table 1. Classification of polymethacrylate based on polymeric grades.

Eudragit GradeApplicationsChemical CompositionSolubility
Cationic (Aminoalkylmethacrylate copolymers)
Eudragit E 12.5
Eudragit E 100
Increased geriatric and pediatric patient compliance.
Increased bioavailability and dissolution profile.
Increased anti-inflammatory action.
High oral bioavailability
Poly(butyl methacrylate, (2-dimethyl aminoethyl) methacrylate, methyl methacrylate) 1:2:1
Poly(butyl methacrylate, (2-dimethyl aminoethyl) methacrylate, methyl methacrylate) 1:2:1
Both are soluble in gastric fluid to pH 5
Anionic (Methacrylic acid copolymers)
Eudragit L 100
Eudragit L 100-55
Eudragit L 12.5
Eudragit L 100-55
Eudragit L 12.5 P
Eudragit S 12.5
Eudragit S 12.5 P
Eudragit L 30 D-55
Eudragit S 100
Eudragit FS 30 D
pH-dependent and high release.
Increased oral absorption.
Increased taste masking.
Controlled release.
Colonic-specific drug delivery.
Targeting drug delivery.
Delay release profile.
High oral bioavailability
Poly(methacrylic acid, methyl methacrylate) 1:1
Poly(methacrylic acid, ethyl acrylate) 1:1
Poly(methacrylic acid, methyl methacrylate) 1:1
Poly(methacrylic acid, methyl methacrylate) 1:1
Poly(methacrylic acid, methyl methacrylate) 1:2
Poly(methacrylic acid, methyl methacrylate) 1:2
Poly(methacrylic acid, ethyl acrylate) 1:1
Poly(methacrylic acid, methyl methacrylate) 1:2
Methyl acrylate, methyl methacrylate, and methacrylic acid
Soluble in intestinal fluid around pH 6
Soluble in intestinal fluid around pH 5.5
Soluble in intestinal fluid around pH 6
Soluble in intestinal fluid around pH 6
Soluble in intestinal fluid around pH 7
Soluble in intestinal fluid around pH 7
Soluble in intestinal fluid from pH 5.5
Soluble in intestinal fluid around pH 7
Soluble above pH 6.8
Neutral (Methacrylic acid copolymers)
1. Eudragit RL PO
2. Eudragit RL 30 D
3. Eudragit RL 100 (Type A)
4. Eudragit RS PO
5. Eudragit RS 30 D
6. Eudragit RS 100 (Type B)
Increased release time and ocular bioavailability.
Increased shelf life for ophthalmic dosage form.
Sustainable drug release for more than 6 h.
Sustained release with significance for vaginal drug delivery.
Improved permeation and increased bioavailability as well as shelf life.
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.2
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.2
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.2
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.1
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.1
Poly(ethyl acrylate, methyl methacrylate, 2-trimethylammonioethyl methacrylate chloride” or “2-(methacryloyloxy)-N,N,N-trimethylethanaminium chloride) 1:2:0.1
Permeability is High
Permeability is High
Permeability is High
Permeability is Low
Permeability is Low
Permeability is Low
Neutral (Methacrylic acid copolymers)
1. Eudragit NM 30 D
2. Eudragit NE 30 D
3. Eudragit NE 40 D
Poly(ethyl acrylate, methyl methacrylate) with 0.7% (PEG stearyl ether) 2:1
Poly(ethyl acrylate, methyl methacrylate) with 1.5% (nonoxynol) 2:1
Poly(ethyl acrylate, methyl methacrylate) with 1.5% (nonoxynol) 2:1
Permeable, swellable
Permeable, swellable
Permeable, swellable

Download the full review as PDF here: A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare

or read it here

Nikam, A.; Sahoo, P.R.; Musale, S.; Pagar, R.R.; Paiva-Santos, A.C.; Giram, P.S. A Systematic Overview of Eudragit® Based Copolymer for Smart Healthcare. Pharmaceutics 2023, 15, 587.
https://doi.org/10.3390/pharmaceutics15020587

Tags: excipientsformulation

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