Stable amorphous solid dispersion of flubendazole with high loading via electrospinning

Becelaere, Jana; Broeck, Elias Van Den; Schoolaert, Ella; Vanhoorne, Valérie; Guyse, Joachim F. R. Van; Vergaelen, Maarten; Borgmans, Sander; Creemers, Karolien; Speybroeck, Véronique Van; Vervaet, Chris; Hoogenboom, Richard; Clerck, Karen De

doi:10.1016/j.jconrel.2022.09.028

Cited by 24 publications

(17 citation statements)

References 76 publications

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“…With decreasing infill density, the tablet will possess network-like openings where the dissolution media can penetrate rapidly into the tablet matrix resulting in faster release profiles. However, with decreasing infill density, the amount of dose the tablet can accommodate will decrease [90,91]. Thus the additive manufacturing technique is suitable for fabricating low-infill tablets with smaller therapeutic doses.…”

Section: Dose and Design Flexibilitymentioning

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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Section: Dose and Design Flexibilitymentioning

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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“…Jana Becelaere et al, (2022) 92 developed high drug-loaded ASDs of flubendazole (55 % drug loading) by electrospinning approach. The solutions of the drug and polymer (2-phenyl-2oxazoline) are prepared in formic acid.…”

Section: Electrospinningmentioning

confidence: 99%

A Review of Various Manufacturing Approaches for Developing Amorphous Solid Dispersions

Konda

Dhoppalapudi

2022

J. Drug Delivery Ther.

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In recent years amorphous solid dispersions (ASD) has gained a tremendous response for improving the solubility of poorly water-soluble drug substances. Despite the stability challenges, various ASD commercial products have been successfully launched into the market over the last two decades. Among various manufacturing approaches, hot melt extrusion (HME) and spray drying techniques have attracted industries attributing to their simple manufacturing processes. In addition, KinetisolÒ, a solvent-free approach, is also being most widely investigated for developing ASDs since the thermal exposure time of the formulations is significantly less compared with the hot melt extrusion process. KinetisolÒ can be employed for developing ASDs of thermolabile drug substances. Another solvent-based technique, electrospinning, is also employed for developing nanofibers-based ASD. However, much research is warranted for the electrospinning process before implementing it in commercial manufacturing. Various critical factors such as drug-polymer solubility, the solubility of the drug in the polymer, drug-polymer interactions, type of manufacturing process, and storage conditions need to be considered for developing a stable and robust ASD formulation. This review mainly focuses on the most advanced manufacturing technologies of ASDs, namely HME, spray drying, KinetisolÒ, and electrospinning, along with a note on the various critical factors that affect the stability of ASD formulations. Keywords: amorphous solid dispersions; hot melt extrusion; spray drying; KinetisolÒ; electrospinning

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“…With increasing offset angle, the amount of mechanical shear imparted on the processing material increases, and the conveying property decreases. Distributive mixing ensures the uniform distribution of active substances within the polymeric carrier, and dispersive mixing breaks the crystals of the drug into the smaller molecular level [48][49][50][51][52][53][54]. To convert the crystalline form of the drug into an amorphous form, energy greater than the lattice energy needs to be incorporated.…”

Section: Hot Melt Extrusionmentioning

confidence: 99%

Hot melt extrusion: A single-step continuous manufacturing process for developing amorphous solid dispersions of poorly soluble drug substances

Dhoppalapudi¹,

Parupathi²

2022

GSC Adv. Res. Rev.

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In today’s world with increasing patient population, the demand for pharmaceutical medications is increasing enormously. However, poor solubility of drug substances and underdeveloped manufacturing process are affecting the revenue of the pharmaceutical industries. Improving the solubility and establishing a robust manufacturing process is the primary prerequisite of the developmental scientists. Among various approaches amorphous solid dispersion has gained a tremendous response for improving the solubility of the drug substances. In addition, the process of hot melt extrusion has attracted the investigators from regulatory agencies and industries. The process of hot melt extrusion involves application of thermal and mechanical energy on to the processing material. The process requires no solvent and is referred as “green technique.” Various factors need to be taken into consideration for developing amorph amorphous solid dispersions. The miscibility of drug and polymer, solubility of drug in polymer, drug-polymer interactions, glass transition temperature, storage conditions majorly influence the stability of the amorphous solid dispersions systems. Though hot melt extrusion is most widely employed for developing amorphous solid dispersions still a lot of research is warranted for developing strategies to formulate high drug loading medications with improved stability. This review article mainly focuses on the instrumentation, and process for developing amorphous solid dispersions by hot melt extrusion with a small note on the various advantages and limitations.

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Stable amorphous solid dispersion of flubendazole with high loading via electrospinning

Cited by 24 publications

References 76 publications

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

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

A Review of Various Manufacturing Approaches for Developing Amorphous Solid Dispersions

Hot melt extrusion: A single-step continuous manufacturing process for developing amorphous solid dispersions of poorly soluble drug substances

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