Pharmaceutical development of micro and nanocrystals of a poorly water-soluble drug: Dissolution rate enhancement of praziquantel

Silva, Andressa Daniele Artico; Sarcinelli, Michelle Alvares; Patricio, Beatriz Ferreira de Carvalho; Chaves, Marcelo Henrique da Cunha; Lima, Leandro Martins; Parreiras, Patrícia Martins; Pinto, Priscila de Faria; Prado, Livia Deris; Rocha, Helvécio Vinícius Antunes

doi:10.1016/j.jddst.2023.104260

Cited by 5 publications

(4 citation statements)

References 36 publications

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“…Several studies reported the possibility of amorphizing PZQ in the presence of a second compound through the formation of amorphous solid dispersions [ 17 , 29 , 30 , 31 , 32 , 33 , 34 , 36 , 37 , 50 , 51 , 56 , 57 , 98 , 99 ].…”

Section: Pzq Amorphous Formsmentioning

confidence: 99%

“…The literature provides little information about amorphous forms of PZQ. Several studies reported the possibility of amorphizing PZQ in the presence of a second compound through the formation of amorphous solid dispersions [17,[29][30][31][32][33][34]36,37,50,51,56,57,98,99].…”

Section: Pzq Amorphous Formsmentioning

confidence: 99%

“…Over 50 years of research on PZQ, several studies have been carried out to enhance its properties by preparing solid dispersions of the drug with povidone [ 17 , 29 , 30 , 31 ], sodium starch glycolate [ 32 ], mesoporous silica [ 33 ], calcium carbonate complexes [ 34 , 35 ], mannitol and Gelucire [ 36 ], and clay minerals [ 37 ], and by preparing PZQ-β-cyclodextrins systems [ 38 , 39 , 40 , 41 , 42 , 43 , 44 ], PZQ-liposomes systems [ 45 ], polymeric and solid lipid nanoparticles [ 46 , 47 , 48 , 49 ], coground systems [ 50 , 51 , 52 , 53 ], fast dispersible granules [ 54 ], melt granulation and ultrasonic spray congealing [ 55 ] and, more recently, micro and nanocrystals [ 56 , 57 ].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Praziquantel Fifty Years on: A Comprehensive Overview of Its Solid State

D’Abbrunzo,

Procida,

Perissutti

2023

Pharmaceutics

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This review discusses the entire progress made on the anthelmintic drug praziquantel, focusing on the solid state and, therefore, on anhydrous crystalline polymorphs, amorphous forms, and multicomponent systems (i.e., hydrates, solvates, and cocrystals). Despite having been extensively studied over the last 50 years, new polymorphs and the greater part of their cocrystals have only been identified in the past decade. Progress in crystal engineering science (e.g., the use of mechanochemistry as a solid form screening tool and more strategic structure-based methods), along with the development of analytical techniques, including Synchrotron X-ray analyses, spectroscopy, and microscopy, have furthered the identification of unknown crystal structures of the drug. Also, computational modeling has significantly contributed to the prediction and design of new cocrystals by considering structural conformations and interactions energy. Whilst the insights on praziquantel polymorphs discussed in the present review will give a significant contribution to controlling their formation during manufacturing and drug formulation, the detailed multicomponent forms will help in designing and implementing future praziquantel-based functional materials. The latter will hopefully overcome praziquantel’s numerous drawbacks and exploit its potential in the field of neglected tropical diseases.

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Section: Pzq Amorphous Formsmentioning

confidence: 99%

Section: Pzq Amorphous Formsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Praziquantel Fifty Years on: A Comprehensive Overview of Its Solid State

D’Abbrunzo,

Procida,

Perissutti

2023

Pharmaceutics

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“…In recent years, drug nanocrystals composed of drugs and stabilizers have been considered one of the most promising nanotechnologies, which can significantly improve the dissolution rate and solubility by reducing the particle size to the nanoscale. Nanocrystals have unique advantages, such as high drug content, high bioavailability, few adverse reactions, and strong adhesion ability to biofilms and tissues [28,29]. It is preferable to the development of BCS IV pharmaceutical formulations (e.g., Til) [30].…”

Section: Introductionmentioning

confidence: 99%

Enhanced Anti-Inflammatory Activity of Tilianin Based on the Novel Amorphous Nanocrystals

Sun,

Guo,

et al. 2024

Pharmaceuticals

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Tilianin (Til), a flavonoid glycoside, is well-known for its therapeutic promise in treating inflammatory disorders. Its poor water solubility and permeability limit its clinical applicability. In order to overcome these restrictions, an antisolvent precipitation and ultrasonication technique was used to prepare amorphous tilianin nanocrystals (Til NCs). We have adjusted the organic solvents, oil-to-water ratio, stabilizer composition, and ultrasonic power and time by combining single-factor and central composite design (CCD) methodologies. The features of Til NCs were characterized using powder X-ray diffraction (PXRD), scanning calorimetry (DSC), and transmission electron microscopy (TEM). Specifically, the optimized Til NCs were needle-like with a particle size ranging from 90 to 130 nm. PVA (0.3%, w/v) and TPGS (0.08%, w/v) stabilized them well. For at least two months, these Til NCs stayed amorphous and showed an impressive stability at 4 °C and 25 °C. Remarkably, Til NCs dissolved almost 20 times faster in simulated intestinal fluid (SIF) than they did in crude Til. In RAW264.7 cells, Til NCs also showed a better cellular absorption as well as safety and protective qualities. Til NCs were shown to drastically lower reactive oxygen species (ROS), TNF-α, IL-1β, and IL-6 in anti-inflammatory experiments, while increasing IL-10 levels and encouraging M1 macrophages to adopt the anti-inflammatory M2 phenotype. Our results highlight the potential of amorphous Til NCs as a viable approach to improve Til’s anti-inflammatory effectiveness, solubility, and dissolving rate.

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