Hot-melt extrusion: Highlighting recent advances in pharmaceutical applications

Tambe, Srushti; Jain, Divya; Agarwal, Yashvi; Amin, Purnima D.

doi:10.1016/j.jddst.2021.102452

Cited by 44 publications

(25 citation statements)

References 282 publications

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“…The temperature used in HME is usually above the glass transition (T g ) and melting (Tm) temperature of the chosen polymer. This process favours the mixing of drug and polymer at a molecular level, and its use is justified by a number of advantages, such as being a solvent-free technique, with few steps until the final product, and being easily automated, which is desired by the industry [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

et al. 2021

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Eudragit® polymers are polymethacrylates highly used in pharmaceutics for the development of modified drug delivery systems. They are widely known due to their versatility with regards to chemical composition, solubility, and swelling properties. Moreover, Eudragit polymers are thermoplastic, and their use has been boosted in some production processes, such as hot melt extrusion (HME) and fused deposition modelling 3D printing, among other 3D printing techniques. Therefore, this review covers the studies using Eudragit polymers in the development of drug delivery systems produced by HME and 3D printing techniques over the last 10 years. Eudragit E has been the most used among them, mostly to formulate immediate release systems or as a taste-masker agent. On the other hand, Eudragit RS and Eudragit L100-55 have mainly been used to produce controlled and delayed release systems, respectively. The use of Eudragit polymers in these processes has frequently been devoted to producing solid dispersions and/or to prepare filaments to be 3D printed in different dosage forms. In this review, we highlight the countless possibilities offered by Eudragit polymers in HME and 3D printing, whether alone or in blends, discussing their prominence in the development of innovative modified drug release systems.

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Section: Introductionmentioning

confidence: 99%

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

et al. 2021

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“…In pharmaceutical industries, HME is widely used to successfully apply various formulation approaches like cocrystals, ASD, melt granulations, co-extruded formulation, micronized system, 3D printing, and coamorphous systems, polymeric film, etc. [ 63 ]. Broadly, this equipment consists of a barrel and an extruder.…”

Section: Methods Of Preparing Transdermal Coamorphous Systemmentioning

confidence: 99%

“…Such flexibility helps the formulator optimizing the residence time of certain materials in a particular zone controlling the heat exposure of drug and other excipients. Different features and applications of HME have been reviewed recently by various other researchers [ 63 , 64 ]. HME’s application has largely propagated to formulate ASD and to enhance oral bioavailability of poorly water-soluble drugs, mainly BCS class II [ 65 , 66 ].…”

Section: Methods Of Preparing Transdermal Coamorphous Systemmentioning

confidence: 99%

Amorphization of Drugs for Transdermal Delivery-a Recent Update

et al. 2022

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Amorphous solid dispersion is a popular formulation approach for orally administered poorly water-soluble drugs, especially for BCS class II. But oral delivery could not be an automatic choice for some drugs with high first-pass metabolism susceptibility. In such cases, transdermal delivery is considered an alternative if the drug is potent and the dose is less than 10 mg. Amorphization of drugs causes supersaturation and enhances the thermodynamic activity of the drugs. Hence, drug transport through the skin could be improved. The stabilization of amorphous system is a persistent challenge that restricts its application. A polymeric system, where amorphous drug is dispersed in a polymeric carrier, helps its stability. However, high excipient load often becomes problematic for the polymeric amorphous system. Coamorphous formulation is another approach, where one drug is mixed with another drug or low molecular weight compound, which stabilizes each other, restricts crystallization, and maintains a single-phase homogenous amorphous system. Prevention of recrystallization along with enhanced skin permeation has been observed by the transdermal coamorphous system. But scalable manufacturing methods, extensive stability study and in-depth in vivo evaluation are lacking. This review has critically studied the mechanistic aspects of amorphization and transdermal permeation by analyzing recent researches in this field to propose a future direction.

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“…This technology also shows other notable advantages such as solvent-free, economical, industrially feasible, high yield, highly reproducible, automation potentiality, and online real-time monitoring. 104 The hot-melt extrusion process involves the feeding of materials through a hopper into the extruder, melting/ conveying/mixing of the blends with a heated barrel and rotating screws, extrusion and cooling of molten materials. The process parameters including the feed rate, screw design, screw speed, barrel temperature, melt pressure, and motor load have impacts on the yield and quality of final formulations.…”

Section: Puerarin Lurasidone Hydrochloride (Lh)mentioning

confidence: 99%

Insights into Cocrystallization and Coamorphization Engineering Techniques in the Delivery of Traditional Chinese Medicine: Formation Mechanism, Solid-State Characterization, and Improved Pharmaceutical Properties

Song

Han

et al. 2022

Crystal Growth & Design

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Many active ingredients from traditional Chinese medicine (TCM) exhibit poor pharmaceutical properties (e.g., low aqueous solubility, slow dissolution, low bioavailability, poor stability, and high hygroscopicity, etc.), which are closely associated with various formulation performance issues. Cocrystals or coamorphous systems, incorporating drug and guest molecules into a homogeneous single crystalline or amorphous phase, have been shown to offer potential advantages in enhancing pharmaceutical properties of TCM. This review outlines the definition, classification, preparation methods, characterization techniques, and pharmaceutical properties (such as solubility, dissolution, stability, mechanical properties, permeability, and in vivo performance) of cocrystals and coamorphous systems. More insights into the formation mechanisms of cocrystals and coamorphous systems, the identification of single-phase homogeneous coamorphous systems, and the characterization of their intermolecular interactions between components are covered. Latest research studies on the delivery of TCM via cocrystallization and coamorphization technologies are also summarized. The mechanisms of enhancement in druggability-related properties through cocrystals and coamorphous systems are further discussed. In particular, several common kinetic solubility behaviors of cocrystal and coamorphous systems, including "spring and parachute" and "spring and hover" models, are deeply understood, which will contribute to the maintenance of high supersaturation and in vivo bioavailability.

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Hot-melt extrusion: Highlighting recent advances in pharmaceutical applications

Cited by 44 publications

References 282 publications

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

Amorphization of Drugs for Transdermal Delivery-a Recent Update

Insights into Cocrystallization and Coamorphization Engineering Techniques in the Delivery of Traditional Chinese Medicine: Formation Mechanism, Solid-State Characterization, and Improved Pharmaceutical Properties

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