Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

Tambe, Srushti; Jain, Divya; Meruva, Sai Kishore; Rongala, Gopinath; Juluri, Abhishek; Nihalani, Girish; Mamidi, Hemanth K.; Nukala, Pavan Kumar; Bolla, Pradeep Kumar

doi:10.3390/pharmaceutics14102203

Cited by 49 publications

(32 citation statements)

References 168 publications

(173 reference statements)

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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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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.

View full text Add to dashboard Cite

show abstract

“…The PAT tools continuously monitors, controls, and preserves the quality of the product. Though HME is most widely employed for manufacturing commercial products, a few limitations, such as high processing temperature, poor stability, poor compressibility of milled extrudates, and low drug loading, remained unaddressed [45][46][47][48][49] . A few case studies where HME has been recently investigated for developing ASDs are further discussed below.…”

Section: Hot Melt Extrusionmentioning

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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“…An ideal technique depends on various factors like physicochemical properties of the drug molecule, desired pharmacokinetic profile, intended dosage form and commercial viability (11,12). Out of all the solubility enhancement techniques, solid dispersions are widely explored with numerous commercially approved formulations (13,14). Their popularity can be attributed to the ease of manufacturing and commercialization (15).…”

Section: Introductionmentioning

confidence: 99%

Considerations in the formulation of amorphous solid dispersions by hot melt extrusion

Dhoppalapudi¹

2022

GSC Biol. Pharm. Sci.

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Hot melt extrusion is one of the most popular techniques for the manufacturing of amorphous solid dispersions (ASDs). Over few decades, it has transitioned from lab scale to commercial scale with various products in the market. The current review aims at summarizing various considerations in the formulation development of ASDs using HME. Various types of ASDs from Type I to Type IV are discussed along with the solid state of drug and polymeric carrier in each type. Also, various polymeric carriers used in ASDs are outlined along with information about their glass transition temperature, melting point, hygroscopicity and regulatory status. There are various mechanisms by which the polymeric carriers stabilize the amorphous form of drug in ASDs. These mechanisms are classified as crystallization inhibition, anti-plasticization, intermolecular interactions, and reduction of molecular mobility. These four mechanisms are discussed along with case studies. Finally, various considerations in the formulation of ASDs like, rationale selection of polymers, process design and optimization and stability testing with respect to formulation of ASDs using hot melt extrusion are discussed. In conclusion, the current state of formulating ASDs using HME are discussed and the need for restructuring the formulation approach is mentioned.

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Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

Cited by 49 publications

References 168 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

Considerations in the formulation of amorphous solid dispersions by hot melt extrusion

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