A new nanosuspension prepared with wet milling method for oral delivery of highly variable drug Cyclosporine A: development, optimization and in vivo evaluation

Pinar, Sıla Gülbağ; Canpınar, Hande; Tan, Çağman; Çelebi, Nevin

doi:10.1016/j.ejps.2022.106123

Cited by 24 publications

(14 citation statements)

References 64 publications

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“…x j,inf = C j BL −0.25 D 0.12 b YM 0.24 API (8) With the additional flexibility provided by Equations ( 7) and ( 8), Model C (Equation ( 6)) is a convenient model that can be parameterized with as few as one experiment for a specific drug product and formulation. It can then predict the particle size and milling time required to reach a target particle size for any process condition across milling scales (from lab to pilot or commercial scales).…”

Section: Model C: Semi-mechanistic Milling Model Fitted To Milled Par...mentioning

confidence: 99%

“…Model B, as shown in Equation (5) with N 3 = 1.4 and N 4 = 0.3 and N 5 = N 1 , was fitted to the reciprocal particle size quantiles to find the ω and BL exponents, N 1 and N 2 . Milling was not carried out for long enough to find an x j,inf fit for the x 90 population; so, this was estimated as 0.219 µm using Equation (8) for the DV2000 dataset. The resulting model parameter fits and model goodness-of-fit (R 2 values) as calculated by JMP version 17 using analytic Gauss Newton nonlinear solver for the prediction of 1/x 10 , 1/x 50 , and 1/x 90 for the DV2000 dataset are shown in Figure 3.…”

Section: Case Studies Inmentioning

confidence: 99%

“…A deeper examination of apparent grinding limits and Equation (8) shows that x j,inf values for GF varied in a relatively narrow range as the process parameters were changed (see Table 5), and the exponents in Equation ( 8) were rather small, signifying no impact of U tip (or w) and a weak impact of BL and D b . This is unsurprising because the grinding limit is mainly determined by material properties, not by the process parameters, provided the milling time is sufficiently long.…”

Section: Mill-scale Efficiency Factor (E)mentioning

confidence: 99%

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Development of a Semi-Mechanistic Modeling Framework for Wet Bead Milling of Pharmaceutical Nanosuspensions

Clancy,

Guner,

Chattoraj

et al. 2024

Pharmaceutics

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This study aimed to develop a practical semi-mechanistic modeling framework to predict particle size evolution during wet bead milling of pharmaceutical nanosuspensions over a wide range of process conditions and milling scales. The model incorporates process parameters, formulation parameters, and equipment-specific parameters such as rotor speed, bead type, bead size, bead loading, active pharmaceutical ingredient (API) mass, temperature, API loading, maximum bead volume, blade diameter, distance between blade and wall, and an efficiency parameter. The characteristic particle size quantiles, i.e., x10, x50, and x90, were transformed to obtain a linear relationship with time, while the general functional form of the apparent breakage rate constant of this relationship was derived based on three models with different complexity levels. Model A, the most complex and general model, was derived directly from microhydrodynamics. Model B is a simpler model based on a power-law function of process parameters. Model C is the simplest model, which is the pre-calibrated version of Model B based on data collected from different mills across scales, formulations, and drug products. Being simple and computationally convenient, Model C is expected to reduce the amount of experimentation needed to develop and optimize the wet bead milling process and streamline scale-up and/or scale-out.

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Section: Model C: Semi-mechanistic Milling Model Fitted To Milled Par...mentioning

confidence: 99%

Section: Case Studies Inmentioning

confidence: 99%

Section: Mill-scale Efficiency Factor (E)mentioning

confidence: 99%

See 1 more Smart Citation

Development of a Semi-Mechanistic Modeling Framework for Wet Bead Milling of Pharmaceutical Nanosuspensions

Clancy,

Guner,

Chattoraj

et al. 2024

Pharmaceutics

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“…Optimasi dilakukan dengan menvariasikan konsentrasi bahan penstabil menjadi 1; 1,5; dan 2 %. Untuk mengetahui distribusi ukuran partikel dan potensial zeta dari formula optimum dilakukan pengukuran menggunaan alat particle size analyzer [18].…”

Section: Optimasi Formula Nanosuspensi Ekstrak Kulit Batang Kayu Mani...unclassified

Formulasi Nanosuspensi Ekstrak Etanol Kulit Batang Kayu Manis dengan Metode Bottom-Up

Priani

2023

Maj. Farmasetika

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Kayu manis memiliki berbagai aktivitas farmakologi salah satunya adalah aktivitas sitotoksik. Beberapa penelitian menunjukkan nanosuspensi dapat menjadi salah satu cara untuk meningkatkan aktivitas sitotoksik bahan aktif. Nanosuspensi adalah sistem dispersi koloidal mengandung partikel obat dengan ukuran <1µm yang distabilkan oleh molekul surfaktan dan atau polimer. Penelitian ini bertujuan untuk melakukan optimasi formula nanosuspensi ekstrak etanol kulit batang kayu manis menggunakan metode bottom up dengan variasi jenis surfaktan/polimer sebagai bahan penstabil. Kulit batang kayu manis diekstraksi menggunakan etanol 96% dengan metode maserasi. Ekstrak dikembangkan menjadi sediaan nanosuspensi dengan teknik antisolvent precipitation menggunakan variasi bahan penstabil yakni tween 80, natrium lauril sulfat, polivinil alkohol (PVA), dan polivinil pirolidon (PVP). Berdasarkan hasil optimasi formula, diketahui bahwa sediaan nanosuspensi mengandung ekstrak kulit batang kayu manis 0,5% menggunakan bahan penstabil PVA 2% memiliki karakteristik fisik paling sesuai, yang ditandai dengan penampilan yang jernih, tanpa endapan, nilai persen transmitan 79,57±0,13 %, ukuran partikel 589±17 nm serta nilai PDI 0,50 ± 0,01. Nanosuspensi kayu manis menggunakan PVA 2% sebagai penstabil memiliki karakteristik yang paling optimum.

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“…The HPH method was used to prepare the Chinese herbal compound Yinxia-1 nano-suspension for the treatment of psoriasis, and the therapeutic effects were compared with the API of YinXie No.1 (21). The results showed that the average particle size of YinXie No.…”

Section: Effects Of Chinese Herbal Compound Nanosuspension On Stat3 A...mentioning

confidence: 99%

Regulation of Janus Kinase-signal Transducers and Activators of Transcription Pathways in Psoriatic Mice by Chinese Herbal Compound and Efficacy of Chinese Traditional Medicine under Nano-suspension Technology

Wang¹,

Liu²,

Cao³

et al. 2022

Cell Mol Biol (Noisy-le-grand)

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The mechanism of the treatment of psoriasis-like mice with the Chinese herbal compound YinXie No.1 prepared by nano-suspension technology was investigated based on Janus kinase-signal transducers and activators of transcription (JAKs/STATs) pathway. The high-pressure homogenization technology was used in the preparation of the YinXie No.1 nano-suspensions. Then, 50 Kunming mice were equally classified into the negative control group (NC), the psoriasis model group (PsM) prepared with 5% imiquimod cream on the back, the Tripterygium glycosides-gavage group (TrG), the YinXie No.1gavage group (YX1), and the YinXie No.1 nano-suspension group (Nano-YX1). The pathological changes and the differential expressions of STAT3 and STAT5 were compared in each group after the treatment. The results showed that the particle size of nano-suspension powder was smaller and had strong stability compared with the active pharmaceutical ingredient (API). Compared with the NC group, psoriasis-like lesions were observed in the PsM group. Compared with the PsM group, the conditions of the erythema on skin lesions, the mRNA expression of STAT3 and STAT5, and protein expression of p-STAT3 and p-STAT5 in the TrG group, YX1 group, and Nano-YX1 group were notably decreased (P<0.05). Compared with the TrG group and YX1 group, the improvement effect of various indexes in the Nano-YX1 group was closer to that in the NC group, but there were differences between the NC group (P<0.05). Chinese herbal compound was helpful to regulate and control the JAKs/STATs pathway to improve the symptoms of psoriasis mice, and the preparation of Chinese herbal compound decoction by nano-suspension technology could improve the therapeutic effect.

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A new nanosuspension prepared with wet milling method for oral delivery of highly variable drug Cyclosporine A: development, optimization and in vivo evaluation

Cited by 24 publications

References 64 publications

Development of a Semi-Mechanistic Modeling Framework for Wet Bead Milling of Pharmaceutical Nanosuspensions

Development of a Semi-Mechanistic Modeling Framework for Wet Bead Milling of Pharmaceutical Nanosuspensions

Formulasi Nanosuspensi Ekstrak Etanol Kulit Batang Kayu Manis dengan Metode Bottom-Up

Regulation of Janus Kinase-signal Transducers and Activators of Transcription Pathways in Psoriatic Mice by Chinese Herbal Compound and Efficacy of Chinese Traditional Medicine under Nano-suspension Technology

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