Enhanced biopharmaceutical performance of brick dust molecule nilotinib via stabilized amorphous nanosuspension using a facile acid–base neutralization approach

Chougule, Mahendra; Sirvi, Arvind; Saini, Vanshul; Kashyap, Mahesh Chand; Sangamwar, Abhay T.

doi:10.1007/s13346-023-01334-7

Cited by 10 publications

(2 citation statements)

References 49 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Consequently, several approaches have been devised to obtain the amorphous solid of nilotinib free base. These methods include the formation of an amorphous solid dispersion by spray drying with polymeric excipients [ 22 ], the fabrication of amorphous nanosuspension by an acid-base neutralization approach [ 23 ], the encapsulation into yeast glucan particles to prepare the amorphous solids [ 24 ], and the formulation of supersaturating formulations [ 20 ]. However, there is a scarcity of research on methods to enhance the physical stability of amorphous solids of nilotinib free base.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the Influence of Anti-Solvent Precipitation Parameters on the Physical Stability of Amorphous Solids

Li,

Gong,

Zhang

et al. 2024

Molecules

View full text Add to dashboard Cite

Amorphous solids exhibit enhanced solubility and dissolution rates relative to their crystalline counterparts. However, attaining optimal bioavailability presents a challenge, primarily due to the need to maintain the physical stability of amorphous solids. Moreover, the precise manner in which precipitation parameters, including the feeding rate of the anti-solvent, agitation speed, and aging time, influence the physical stability of amorphous solids remains incompletely understood. Consequently, this study aimed to investigate these three parameters during the precipitation process of the anticancer drug, nilotinib free base. The physical stability of the resultant samples was evaluated by employing characterization techniques including powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), focused beam reflectance measurement (FBRM), and data analysis methods such as pair distribution function (PDF), reduced crystallization temperature (Rc), and principal component analysis (PCA). This study’s findings indicated that amorphous solids exhibited the greatest physical stability under particular conditions, namely a feeding rate of 5 mL/min, an agitation speed of 500 rpm, and an aging time of 10 min. Furthermore, the physical stability of the amorphous solids was primarily influenced by particle size and distribution, molecular interactions, microstructure, surface area, and interfacial energy. Notably, the parameters involved in the anti-solvent precipitation process, including the feeding rate of the anti-solvent, agitation speed, and aging time, exerted a significant impact on these factors. Consequently, they directly affected the physical stability of amorphous solids. Hence, this study comprehensively elucidated the mechanistic influence of these operational parameters on the physical stability of amorphous solids during the anti-solvent precipitation process.

show abstract

Section: Introductionmentioning

confidence: 99%

Investigation of the Influence of Anti-Solvent Precipitation Parameters on the Physical Stability of Amorphous Solids

Li,

Gong,

Zhang

et al. 2024

Molecules

View full text Add to dashboard Cite

show abstract

“…[11][12][13] Nanosuspensions, often referred to as particles resembling fine dust, aid in the dissolution of a scheme and enhance absorption, promoting increased effectiveness. 14 Moreover, it demonstrated the photostability, stability at room temperature in addition to humidity, and compatibility using the excipient and solvent. 15 However, for chemicals with a higher log p-value, higher melting point, as well as higher dosages that are insoluble in water but soluble in oil; nanosuspension is favored.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Optimization, and Evaluation of Gliclazide loaded Nanosuspension for Dissolution Rate Enhancement

Bhatt

2023

IJPQA

View full text Add to dashboard Cite

Diabetes mellitus is a prolonged metabolic condition categorized through elevated blood glucose levels. To treat this condition, oral antihyperglycemic medications like gliclazide, a second-generation sulfonylurea insulin secretagogue, are commonly used. Gliclazide comes into the biopharmaceutical classification system (BCS) class-II types, known for its lower solubility. To enhance its solubility, gliclazide was integrated into nanosuspensions. This study focused on formulating these gliclazide nanosuspensions using Kollicoat IR and Soluplus through the anti-solvent-precipitation method, through optimization achieved using the Box Behnken Design. Key parameters assessed included particle size (224 ± 1.23 nm) and entrapment efficiency (95.65 ± 0.12%). The drug release studies conducted on pH 7.4 indicated that over 95% of the drug was released within 30 minutes for the nanosuspension, whereas the pure drug solution released less than 70% in the same time frame, indicating immediate release with the nanosuspension. The morphology was examined using scanning electron microscopy (SEM), while fourier transform infrared (FTIR), X-Ray diffractometers (XRD), and differential scanning calorimeter (DSC) analyses confirmed the presence of the drug within the nanosuspension. In summary, the incorporation of gliclazide into nanosuspensions proved successful, resulting in enhanced release characteristics and ameliorated solubility.

show abstract

Synergistic effect of polymers in stabilizing amorphous pretomanid through high drug loaded amorphous solid dispersion

Juneja,

Mehtre,

Saini

et al. 2024

Drug Deliv. and Transl. Res.

View full text Add to dashboard Cite

Enhanced biopharmaceutical performance of brick dust molecule nilotinib via stabilized amorphous nanosuspension using a facile acid–base neutralization approach

Cited by 10 publications

References 49 publications

Investigation of the Influence of Anti-Solvent Precipitation Parameters on the Physical Stability of Amorphous Solids

Investigation of the Influence of Anti-Solvent Precipitation Parameters on the Physical Stability of Amorphous Solids

Formulation, Optimization, and Evaluation of Gliclazide loaded Nanosuspension for Dissolution Rate Enhancement

Synergistic effect of polymers in stabilizing amorphous pretomanid through high drug loaded amorphous solid dispersion

Contact Info

Product

Resources

About