Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Wang, Lu; Zhao, Pengfei; Luo, Ting; Yang, Dandan; Jiang, Qianqian; Chen, Jinliang; Lou, Honggang; Ruan, Zourong; Jiang, Bo

doi:10.1111/cts.13633

Cited by 2 publications

(2 citation statements)

References 17 publications

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“…Given the pivotal role of BE studies in drug development, judicious application of physiological models for forecasting BE outcomes (i.e., virtual BE or VBE) can offer invaluable insights for advancing formulation by enhancing our mechanistic understanding of factors influencing drug absorption. This approach also facilitates streamlined product development, 2 enables efficient design of BE studies, 3 and supports the potential for utilization in biowaivers. 4 Several recent reports have highlighted successful applications of VBE trials in the evaluation of BE across various formulations.…”

Section: Introductionmentioning

confidence: 79%

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Physiologically based absorption modeling to predict the bioequivalence of two apixaban formulations

Luo,

Wang,

Ruan

et al. 2024

Clinical Translational Sci

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The equivalence of absorption rates and extents between generic drugs and their reference formulations is crucial for ensuring therapeutic comparability. Bioequivalence (BE) studies are widely utilized and play a pivotal role in substantiating the approval and promotional efforts for generic drugs. Virtual BE simulation is a valuable tool for mitigating risks and guiding clinical BE studies, thereby minimizing redundant in vivo BE assessments. Herein, we successfully developed a physiologically based absorption model for virtual BE simulations, which precisely predicts the BE of the apixaban test and reference formulations. The modeling results confirm that the test and reference formulations were bioequivalent under both fasted and fed conditions, consistent with clinical studies. This highlights the efficacy of physiologically based absorption modeling as a powerful tool for formulation screening and can be adopted as a methodological and risk assessment strategy to detect potential clinical BE risks.

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Section: Introductionmentioning

confidence: 79%

“… 4 Several recent reports have highlighted successful applications of VBE trials in the evaluation of BE across various formulations. 3 , 5 Early identification and assessment of potential BE risks are vital for refining clinical pharmacology strategies and guiding study design.…”

Section: Introductionmentioning

confidence: 99%

Physiologically based absorption modeling to predict the bioequivalence of two apixaban formulations

Luo,

Wang,

Ruan

et al. 2024

Clinical Translational Sci

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Cilostazol niosomes-loaded transdermal gels: An in vitro and in vivo anti-aggregant and skin permeation activity investigations towards preparing an efficient nanoscale formulation

Mahmoud,

Abdelhafez,

Mahmoud

et al. 2024

Nanotechnology Reviews

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Cilostazol, an anti-platelet aggregation medicine, is also known to have vasodilation properties and is commonly used for treating muscle soreness and cramps by increasing the muscle oxygen supply. The medication has limited oral bioavailability, is prone to pre-systemic metabolism, and is poorly soluble in aqueous media. A transdermal administration was planned to increase the drug’s solubility and therapeutic efficacy. The current work intended to develop cilostazol niosome-loaded transdermal gel, which was prepared, and with the use of Fourier transform infrared and differential scanning calorimetry analyses, drug-excipient interactions were observed. The medication was formulated utilizing Carbopol-934, Pluronic-F-127, and HPMC gel bases for the transdermally delivered niosomal gels. The produced niosomes had a maximum percentage of drug entrapment at 96.4%, with a particle size of 102 ± 11.30 nm and polydispersity index of 0.29 ± 0.069. The highest percentage of the medication that was entrapped was 96.4%, and the Carbopol-934 gel basis released the major part of the drug under in vitro conditions. A maximum transdermal flux was recorded at 3850.92 μg after 4 h, indicating a 10% increase in cilostazol permeation through rat skin. The flux rate for the niosomal preparation containing the drug ranged from 14.85 to 28.02 μg/cm2 h−1. In comparison to the pure cilostazol-loaded gels, the pharmacokinetics investigation showed that the niosomal gel formulations had considerably greater C max, T max, and AUC0. The niosomes loaded with cilostazol exhibited greater solubility, higher bioavailability, and improved effectiveness. Better therapeutic results may be achieved with systemic and site-directed delivery of cilostazol using the designed transdermal niosomal gel with appropriate molecular tagging modification/(s).

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Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Cited by 2 publications

References 17 publications

Physiologically based absorption modeling to predict the bioequivalence of two apixaban formulations

Physiologically based absorption modeling to predict the bioequivalence of two apixaban formulations

Cilostazol niosomes-loaded transdermal gels: An in vitro and in vivo anti-aggregant and skin permeation activity investigations towards preparing an efficient nanoscale formulation

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