Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

Qian, Kaijie; Stella, Lorenzo; Jones, David S.; Andrews, Gavin; Du, Huachuan

doi:10.3390/pharmaceutics13060889

Cited by 18 publications

(9 citation statements)

References 166 publications

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“…Formulation A, which contains Soluplus ® and Vitamin E TPGs, converted the crystalline curcumin into an amorphous form, as shown by the XRD results. It was reported that the conversion of crystalline drugs into an amorphous form can contribute to increasing the drug solubility [ 84 , 85 , 86 ]. In a similar study, a solid formulation made from Soluplus ® /Vitamin E TPGs was reported to show the conversion of insoluble valsartan from a crystalline to an amorphous state, which increased the aqueous solubility of the drug and ultimately led to a significant increase in oral bioavailability [ 12 ].…”

Section: Discussionmentioning

confidence: 99%

Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

et al. 2022

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Several therapeutically active molecules are poorly water-soluble, thereby creating a challenge for pharmaceutical scientists to develop an active solution for their oral drug delivery. This study aimed to investigate the potential for novel polymer-surfactant-based formulations (designated A and B) to improve the solubility and permeability of curcumin. A solubility study and characterization studies (FTIR, DSC and XRD) were conducted for the various formulations. The cytotoxicity of formulations and commercial comparators was tested via MTT and LDH assays, and their permeability by in vitro drug transport and cellular drug uptake was established using the Caco-2 cell model. The apparent permeability coefficients (Papp) are considered a good indicator of drug permeation. However, it can be argued that the magnitude of Papp, when used to reflect the permeability of the cells to the drug, can be influenced by the initial drug concentration (C0) in the donor chamber. Therefore, Papp (suspension) and Papp (solution) were calculated based on the different values of C0. It was clear that Papp (solution) can more accurately reflect drug permeation than Papp (suspension). Formulation A, containing Soluplus® and vitamin E TPGs, significantly increased the permeation and cellular uptake of curcumin compared to other samples, which is believed to be related to the increased aqueous solubility of the drug in this formulation.

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Section: Discussionmentioning

confidence: 99%

Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

et al. 2022

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“…Based on a database from FDA, more than 20 ASD drugs were approved; among them, more than 50% have doses higher than 100 mg [ 18 , 27 ]. Between 2015 and 2020, approximately 14 new ASDs were approved [ 71 ]. In a process of formulating a stable, a robust ASD product of higher strength, would require a higher amount and number of excipients.…”

Section: Advances In Asd Formulation Approachesmentioning

confidence: 99%

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

et al. 2022

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Amorphous solid dispersions (ASDs) are among the most popular and widely studied solubility enhancement techniques. Since their inception in the early 1960s, the formulation development of ASDs has undergone tremendous progress. For instance, the method of preparing ASDs evolved from solvent-based approaches to solvent-free methods such as hot melt extrusion and Kinetisol®. The formulation approaches have advanced from employing a single polymeric carrier to multiple carriers with plasticizers to improve the stability and performance of ASDs. Major excipient manufacturers recognized the potential of ASDs and began introducing specialty excipients ideal for formulating ASDs. In addition to traditional techniques such as differential scanning calorimeter (DSC) and X-ray crystallography, recent innovations such as nano-tomography, transmission electron microscopy (TEM), atomic force microscopy (AFM), and X-ray microscopy support a better understanding of the microstructure of ASDs. The purpose of this review is to highlight the recent advancements in the field of ASDs with respect to formulation approaches, methods of preparation, and advanced characterization techniques

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“…Crystal engineering alters the intermolecular interactions responsible for holding the molecules together, affects the packing of the molecules and impacts the physical properties of solids (e.g., compressibility, solubility and dissolution rate) [ 9 , 10 , 11 ]. In this respect, the disarrangement of the crystalline structure of drugs by the production of their amorphous counterparts is regarded as one of the most promising strategies to enhance drug solubility and bioavailability [ 12 , 13 , 14 ]. In fact, amorphous materials, unlike their corresponding crystalline materials, possess high free energy, i.e., low enthalpy and high entropy [ 15 ], which positively affects properties such as solubility in water and dissolution rate [ 12 , 16 ].…”

Section: Introductionmentioning

confidence: 99%

Amorphous and Co-Amorphous Olanzapine Stability in Formulations Intended for Wet Granulation and Pelletization

Costa

Daniels

Fernandes

et al. 2022

IJMS

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The preparation of amorphous and co-amorphous systems (CAMs) effectively addresses the solubility and bioavailability issues of poorly water-soluble chemical entities. However, stress conditions imposed during common pharmaceutical processing (e.g., tableting) may cause the recrystallization of the systems, warranting close stability monitoring throughout production. This work aimed at assessing the water and heat stability of amorphous olanzapine (OLZ) and OLZ-CAMs when subject to wet granulation and pelletization. Starting materials and products were characterized using calorimetry, diffractometry and spectroscopy, and their performance behavior was evaluated by dissolution testing. The results indicated that amorphous OLZ was reconverted back to a crystalline state after exposure to water and heat; conversely, OLZ-CAMs stabilized with saccharin (SAC), a sulfonic acid, did not show any significant loss of the amorphous content, confirming the higher stability of OLZ in the CAM. Besides resistance under the processing conditions of the dosage forms considered, OLZ-CAMs presented a higher solubility and dissolution rate than the respective crystalline counterpart. Furthermore, in situ co-amorphization of OLZ and SAC during granule production with high fractions of water unveils the possibility of reducing production steps and associated costs.

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Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

Cited by 18 publications

References 166 publications

Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

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

Amorphous and Co-Amorphous Olanzapine Stability in Formulations Intended for Wet Granulation and Pelletization

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