Application of the combination of ball-milling and hot-melt extrusion in the development of an amorphous solid dispersion of a poorly water-soluble drug with high melting point

Wu, Fan; Zhu, Wenjing; Zhang, Xinyi; Xu, Yun; Di, Liuqing

doi:10.1039/c9ra00810a

Cited by 27 publications

(14 citation statements)

References 42 publications

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“…EE is the most used Eudragit in the goal to improve drug solubility by formulating ASDs, acting either as a polymeric matrix [ 50 , 51 , 63 , 66 ] or as a pH modifying agent [ 62 ]. This high demand is justified by the fact that EE has a good thermal stability and is a thermoplastic polymer, making it easier to process during HME due to its very low Tg.…”

Section: Hot Melt Extrusionmentioning

confidence: 99%

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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: Hot Melt Extrusionmentioning

confidence: 99%

“…The use of proper temperatures favours the production of extrudates and/or 3D printed forms, and the amorphization of the drug. Drugs with high melting point have greater difficulty in amorphization due to the greater energy required for this conversion [ 66 ].…”

Section: Quality Assessment Of Dosage Forms Produced By Hme and 3d Printingmentioning

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 this system, the API is dispersed in a matrix of the hydrophilic carrier in a solid state. Various methods, such as hot-melt extrusion [ 15 ], spray-drying [ 16 ], freeze-drying (FD) [ 17 ], precipitation [ 18 ], solvent evaporation [ 19 ], and ball milling [ 20 ], have been used to prepare SDs.…”

Section: Introductionmentioning

confidence: 99%

Enhancing the Solubility of Curcumin Using a Solid Dispersion System with Hydroxypropyl-β-Cyclodextrin Prepared by Grinding, Freeze-Drying, and Common Solvent Evaporation Methods

et al. 2020

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Cyclodextrins (CDs) and their derivatives significantly increase drug solubility by forming drug/CD complexes known as solid dispersions (SDs), which consist of an inclusion complex (IC), where the drug is entrapped within the CD cavity, and a non-IC. Here, the SDs of curcumin (CUR) and hydroxypropyl-β-cyclodextrin (HPβCD) were prepared using the grinding, freeze-drying (FD), and common solvent evaporation (CSE) methods and were physicochemically characterized using solubility, powder X-ray diffraction, Fourier transform infrared, differential scanning calorimetry, and dissolution studies. The second or higher order complex of CUR-HPβCD indicated the co-existence of ICs and non-ICs known as the SD system. When comparing the soluble drug amount with CUR crystals, the solubility of SDs was enhanced by up to 299-, 180-, and 489-fold, corresponding to the ground mixtures (GMs), freeze-drying mixtures (FDs), and common solvent evaporation mixtures (CSEs), respectively. The total transformation into the amorphous phase of CUR was observed in GMs and in CSE12, CSE14, and CSE18. The drug was well dispersed within HPβCD in GMs and CSEs, suggesting the formation of hydrogen bonds between CUR and HPβCD, whereas the dispersed behavior of FDs was similar to that of physical mixtures. In SDs, the melting temperature of CUR was in an increased order of CUR in 1:2 ICs, CUR in 1:1 ICs, and CUR crystals. The dissolution rate of CUR was positively improved as the amount of HPβCD in SDs increased. The SD system consisting of CUR and HPβCD significantly increased the drug solubility compared to ICs.

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“…The number of elements and offset angle of the mixing zones mainly depend on the melt viscosity of the processing material. The mixing zones can be customized as required depending on the amount of shear that needs to be imparted onto the processing material [39][40][41][42][43][44][45]. Apart from the conveying and mixing elements, the other elements include comb mixing, cutter element, and narrow-toothed mixing elements, which have not been investigated for developing ASDs.…”

Section: Hot Melt Extrusionmentioning

confidence: 99%

A review of hot melt extrusion paired fused deposition modeling three-dimensional printing for developing patient centric dosage forms

Dhoppalapudi¹,

Illa²

2022

GSC Biol. Pharm. Sci.

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In recent years, the demand for developing patient-centric dosage forms is increasing enormously with the increasing patient population. Much research is ongoing exploring various additive manufacturing techniques for developing pharmaceutical medications. Poor solubility of drug substances and underdeveloped manufacturing strategies are majorly affecting the pharmaceutical industry's revenue. Developing intravenous dosage forms for drug substances with poor solubility will affect the revenue of the pharmaceutical industries. Thus, improving solubility remains to be the major prerequisite for the developmental scientist. In addition to improving solubility, establishing a robust manufacturing process with commercial viability is also essential. In recent years hot melt extrusion (HME) has been most widely investigated for developing amorphous solid dispersions (ASDs) over other techniques such as spray drying and KinetisolÒ. The process of HME can be coupled with the fused deposition modeling (FDM) three-dimensional (3D) printing technique which is capable of fabricating on-demand patient-centric dosage forms. A continuous manufacturing line can be established by painting HME and FDM 3D printing processes. The quality of the product can be controlled and monitored by employing suitable process analytical technology (PAT) tools. Though the process of the HME-paired FDM 3D printing process has resulted in various advantages compared to the conventional manufacturing process, still many limitations, such as the limited number of polymers, reproducibility, and stability, need to be addressed.

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Application of the combination of ball-milling and hot-melt extrusion in the development of an amorphous solid dispersion of a poorly water-soluble drug with high melting point

Cited by 27 publications

References 42 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

Enhancing the Solubility of Curcumin Using a Solid Dispersion System with Hydroxypropyl-β-Cyclodextrin Prepared by Grinding, Freeze-Drying, and Common Solvent Evaporation Methods

A review of hot melt extrusion paired fused deposition modeling three-dimensional printing for developing patient centric dosage forms

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