Characterization of amorphous solid dispersions: An update

Ma, Xiangyu; Williams, Robert O.

doi:10.1016/j.jddst.2019.01.017

Cited by 104 publications

(81 citation statements)

References 99 publications

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“…The distribution of the drug in the polymeric matrix and any traces of crystallinity in the extruded filaments were observed using PLM analysis [ 42 ]. From Figure 4 , the bulk drug exhibits birefringence in both lights ( Figure 4 A) and dark conditions ( Figure 4 B) due to its crystalline nature and property to refract light.…”

Section: Resultsmentioning

confidence: 99%

Novel On-Demand 3-Dimensional (3-D) Printed Tablets Using Fill Density as an Effective Release-Controlling Tool

et al. 2020

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This research demonstrates the use of fill density as an effective tool for controlling the drug release without changing the formulation composition. The merger of hot-melt extrusion (HME) with fused deposition modeling (FDM)-based 3-dimensional (3-D) printing processes over the last decade has directed pharmaceutical research towards the possibility of printing personalized medication. One key aspect of printing patient-specific dosage forms is controlling the release dynamics based on the patient’s needs. The purpose of this research was to understand the impact of fill density and interrelate it with the release of a poorly water-soluble, weakly acidic, active pharmaceutical ingredient (API) from a hydroxypropyl methylcellulose acetate succinate (HPMC-AS) matrix, both mathematically and experimentally. Amorphous solid dispersions (ASDs) of ibuprofen with three grades of AquaSolveTM HPMC-AS (HG, MG, and LG) were developed using an HME process and evaluated using solid-state characterization techniques. Differential scanning calorimetry (DSC), powder X-ray diffraction (pXRD), and polarized light microscopy (PLM) confirmed the amorphous state of the drug in both polymeric filaments and 3D printed tablets. The suitability of the manufactured filaments for FDM processes was investigated using texture analysis (TA) which showed robust mechanical properties of the developed filament compositions. Using FDM, tablets with different fill densities (20–80%) and identical dimensions were printed for each polymer. In vitro pH shift dissolution studies revealed that the fill density has a significant impact (F(11, 24) = 15,271.147, p < 0.0001) and a strong negative correlation (r > −0.99; p < 0.0001) with the release performance, where 20% infill demonstrated the fastest and most complete release, whereas 80% infill depicted a more controlled release. The results obtained from this research can be used to develop a robust formulation strategy to control the drug release from 3D printed dosage forms as a function of fill density.

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Section: Resultsmentioning

confidence: 99%

Novel On-Demand 3-Dimensional (3-D) Printed Tablets Using Fill Density as an Effective Release-Controlling Tool

et al. 2020

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“…Variations in the thermodynamic state of a material lead to variations in its physical properties (e.g., viscosity) that impact processability. Therefore, the identification of the transitions of phase can anticipate the performance of the materials when extruded or printed [ 135 ]. In this respect, the specific heat capacity, thermal conductivity, density, or the existence of glass transition temperature(s) (Tg) or a melting point (Tm) of the polymers must be well-known.…”

Section: Characterization Of Filaments and 3d Dosage Forms Producementioning

confidence: 99%

Polymer Selection for Hot-Melt Extrusion Coupled to Fused Deposition Modelling in Pharmaceutics

et al. 2020

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Three-dimensional (3D) printing offers the greatest potential to revolutionize the future of pharmaceutical manufacturing by overcoming challenges of conventional pharmaceutical operations and focusing design and production of dosage forms on the patient’s needs. Of the many technologies available, fusion deposition modelling (FDM) is considered of the lowest cost and higher reproducibility and accessibility, offering clear advantages in drug delivery. FDM requires in-house production of filaments of drug-containing thermoplastic polymers by hot-melt extrusion (HME), and the prospect of connecting the two technologies has been under investigation. The ability to integrate HME and FDM and predict and tailor the filaments’ properties will extend the range of printable polymers/formulations. Hence, this work revises the properties of the most common pharmaceutical-grade polymers used and their effect on extrudability, printability, and printing outcome, providing suitable processing windows for different raw materials. As a result, formulation selection will be more straightforward (considering the characteristics of drug and desired dosage form or release profile) and the processes setup will be more expedite (avoiding or mitigating typical processing issues), thus guaranteeing the success of both HME and FDM. Relevant techniques used to characterize filaments and 3D-printed dosage forms as an essential component for the evaluation of the quality output are also presented.

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“…First, the level of drug crystallinity in SDs can be evaluated via techniques such as powder X-ray diffraction and different scanning calorimetry [57]. Second, the molecular interactions can be characterized by infrared spectroscopy, Raman spectroscopy, nuclear magnetic resonance spectroscopy, X-ray photoelectron spectroscopy, molecular modeling, quantum chemical calculation, and water vapor sorption [58,59]. Third, scanning electron microscopy, atomic force microscopy, and transmission electron microscopy are usually utilized to observe the morphologies of SDs and nano-sized particles [26,58].…”

Section: Fundamental Properties and Physicochemical Characterization mentioning

confidence: 99%

“…Third, scanning electron microscopy, atomic force microscopy, and transmission electron microscopy are usually utilized to observe the morphologies of SDs and nano-sized particles [ 26 , 58 ]. The details of those methods can be found in prominent reviews [ 57 , 58 , 59 ].…”

Section: Fundamental Properties and Physicochemical Characterizatimentioning

confidence: 99%

Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Tran

2020

Polymers

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In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

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Characterization of amorphous solid dispersions: An update

Cited by 104 publications

References 99 publications

Novel On-Demand 3-Dimensional (3-D) Printed Tablets Using Fill Density as an Effective Release-Controlling Tool

Novel On-Demand 3-Dimensional (3-D) Printed Tablets Using Fill Density as an Effective Release-Controlling Tool

Polymer Selection for Hot-Melt Extrusion Coupled to Fused Deposition Modelling in Pharmaceutics

Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

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