Solid dispersion technology as a formulation strategy for the fabrication of modified release dosage forms: A comprehensive review

Patel, Kaushika; Shah, Shreeraj; Patel, Jaymin

doi:10.1007/s40199-022-00440-0

Cited by 18 publications

(10 citation statements)

References 109 publications

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“…In order to increase its bioavailability, this low solubility must be improved which can be achieved through various methods. The application of solid dispersion is an increasingly popular way to formulate poor solubility drugs because of the advantageous properties of the final product [ 45 ]. In our study, we aimed to investigate binary dispersions of ketoprofen with three different molecular weight polymers, PEG 1000, 1500, and 2000 to highlight the effect of molecular weight on the manufactured solid dispersions and their dissolution characteristics.…”

Section: Discussionmentioning

confidence: 99%

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

et al. 2023

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Solid dispersions are typically binary systems with a hydrophilic matrix polymer and a lipophilic active substance. During formulation, the drug undergoes a crystalline to amorphous phase transition, which leads to a supersaturated solution providing enhanced bioavailability. The interaction of the active substance and the polymer is unique and influences the level of supersaturation. We aimed to investigate the relationship between low molecular weight polyethylene glycol derivates PEG 1000, 1500, and 2000 and ketoprofen regarding the effect of molecular weight. The physicochemical properties of solid dispersions prepared with hot melt homogenization and their respective physical mixtures were investigated with Fourier transform infrared spectroscopy, powder X-ray diffraction and scanning electron microscopy techniques. A phase solubility study was carried out in hydrochloric acid media which showed no difference between the three polymers, but the dissolution curves differed considerably. PEG 1000 had higher percentage of released drug than PEG 1500 and 2000, which had similar results. These results indicate that when multiple low molecular weight PEGs are suitable as matrix polymers of solid dispersions, the molecular weight has only limited impact on physicochemical characteristics and interactions and further investigation is needed to select the most applicable candidate.

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Section: Discussionmentioning

confidence: 99%

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

et al. 2023

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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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“…Spray drying can also be employed for taste masking of bitter drugs, modified release formulations, and manufacturing of inhalation formulations. It can also be used for manufacturing sterile formulations with an improved shelf life over liquid intravenous formulations [64][65][66] . A few case studies are discussed in which the spray drying approach was employed for developing ASDs of poorly water-soluble drug substances.…”

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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Solid dispersion technology as a formulation strategy for the fabrication of modified release dosage forms: A comprehensive review

Cited by 18 publications

References 109 publications

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

Contemporary Review on Solubility Enhancement Techniques

A Review of Various Manufacturing Approaches for Developing Amorphous Solid Dispersions

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