The Value of Bead Coating in the Manufacturing of Amorphous Solid Dispersions: A Comparative Evaluation with Spray Drying

Boel, Eline; Reniers, Felien; Dehaen, Wim; Mooter, Guy Van den

doi:10.3390/pharmaceutics14030613

Cited by 5 publications

(3 citation statements)

References 43 publications

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“…Research has indicated various in vivo aspects of the lipid preparations are connected to increased bioavailability [90][91][92][93] .…”

Section: Self-emulsifying Drug Delivery Systems (Sedds)mentioning

confidence: 99%

Contemporary Review on Solubility Enhancement Techniques

NARMADA¹

2023

J. Drug Delivery Ther.

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The limited water solubility of pharmacoactive molecules hinders their ability to be used as pharmacological agents, yet the indispensability of a certain solubility parameter precludes any compromises. To overcome this challenge, various methods are employed in order to increase their bioavailability. Pharmaceutical molecules with lower solubility present an elevated risk of failure for drug development and innovation. Their solubility affects important processes such as pharmacokinetics, pharmacodynamics, distribution, protein binding, and absorption. As a result these parameters are greatly impacted by the dissolution rate of a particular molecule. Out of all pharmaceutical dosage forms, more than half are oral. For the drug molecule to reach its target site and be effective therapeutically, solubility and bioavailability must be taken into consideration. Unfortunately, during screening programs conducted by the pharmaceutical industry it became evident that nearly 40% of new chemical entities (NCEs) face various roadblocks when transitioning from formulation to development due to their poor solubility and bioavailability. The pharmaceutical industry is constantly confronted with the difficulty of improving drug bioavailability and solubility in formulations. This article covers a range of technological advancements to boost the solubility of insoluble drugs, such as complexation, emulsions and micelles production, microemulsion generation with cosolvents, polymeric micelle preparation methods, particle size decrease techniques, pharmaceutical salts application, prodrugs usage, solid-state alteration practices, soft gel technology implementation crystal engineering approaches and nanomorphology. Through this review, we will discuss a variety of more complex methods for improving solubility and bioavailability such as crystal engineering, micronization, solid dispersions, nano sizing, and use of cyclodextrins, solid lipid nanoparticles (SLNPs), colloidal drug delivery systems and drug conjugates. We'll also provide references to studies that have been conducted in connection with these topics. Keywords: Solubility, permeability, bioavailability, nano particles drug delivery systems, microemulsions, low water solubility

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“…Research has indicated various in vivo aspects of the lipid preparations are connected to increased bioavailability [90][91][92][93] .…”

Section: Self-emulsifying Drug Delivery Systems (Sedds)mentioning

confidence: 99%

Contemporary Review on Solubility Enhancement Techniques

NARMADA¹

2023

J. Drug Delivery Ther.

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show abstract

“…The screw configuration can be majorly divided into self-cleansing and non-selfcleansing. Within the self-cleansing type of screw configuration, the flight of one screw overlaps with the pitch of the other screw, thereby preventing the longer exposure of the materials to thermal energy [56,57]. In recent years, multiple extruders have been brought together and connected to a single die for the extrusion of multiple-layer films or for developing medical devices.…”

Section: Evolution Of Hmementioning

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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“…A schematic representation of the spray drying system is shown in Figure 2. The spray drying process remains expensive compared with HME since it requires high amounts of solvent for the feed material preparation [59][60][61][62][63] . It also requires a specialized collection unit for the recovery of solvents.…”

Section: Spray Dryingmentioning

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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The Value of Bead Coating in the Manufacturing of Amorphous Solid Dispersions: A Comparative Evaluation with Spray Drying

Cited by 5 publications

References 43 publications

Contemporary Review on Solubility Enhancement Techniques

Contemporary Review on Solubility Enhancement Techniques

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

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