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Journals / Turkish Journal of Pharmaceutical Sciences / 2021 / Cilt: 18 - Sayı: 2

In Vitro Caco-2 Cell Permeability Studies of Ziprasidone Hydrochloride Monohydrate Nanocrystals

Ziprasidon Hidroklorür Monohidrat Nanokristallerinin Caco-2 Hücre İn Vitro Geçirgenlik Çalışmaları

Naile ÖZTÜRK
Alptuğ KARAKÜÇÜK
Nevin ÇELEBİ
Emine TAŞHAN
Pages
111–115
Publication Date
2022-11-06
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Conclusion: Nanocrystal technology helps to increase the permeability of drug particles by increasing the saturation solubility.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Objectives: The current study focused on the evaluation of the cytotoxic effect and permeability of ziprasidone hydrochloride monohydrate (ZHM) nanocrystals on Caco-2 cells.
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Key Findings & Data:In vitro cytotoxic effects of ZHM nanocrystals were investigated using the 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test.
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Conclusion & Impact:Conclusion: Nanocrystal technology helps to increase the permeability of drug particles by increasing the saturation solubility.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

Objectives: The current study focused on the evaluation of the cytotoxic effect and permeability of ziprasidone hydrochloride monohydrate (ZHM) nanocrystals on Caco-2 cells. Materials and Methods: ZHM nanocrystals were prepared by the microfluidization method in the presence of polyvinylpyrrolidone as a stabilizer. Particle size (PS), particle size distribution (PDI), and zeta potential (ZP) values were measured in characterization studies. In vitro cytotoxic effects of ZHM nanocrystals were investigated using the 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. Caco-2 transport studies were conducted with formulations of ZHM coarse powder and nanocrystals. Results: Nanocrystals were obtained with 400-600 nm PS, 0.1-0.4 PDI, and >20 mV ZP values. The cell viability remained 100% for all sample groups. The permeability value of ZHM nanocrystals through Caco-2 cells increased 2.3-fold in comparison with ZHM coarse powder. Cumulative drug transport also increased at the end of the sampling period. Conclusion: Nanocrystal technology helps to increase the permeability of drug particles by increasing the saturation solubility.

Özet

Amaç: Bu çalışma, ziprasidone hidroklorür monohidrat (ZHM) nanokristallerinin Caco-2 hücreleri üzerindeki sitotoksik etkisini ve geçirgenliğini değerlendirmeye odaklanmıştır. Gereç ve Yöntemler: ZHM nanokristalleri, stabilizan olan polivinilpirolidon varlığında mikrofluidizasyon yöntemi ile hazırlanmıştır. Partikül büyüklüğü (PB), partikül büyüklüğü dağılımı (PBD) ve zeta potansiyel (ZP) değerleri karakterizasyon çalışmalarıyla ölçülmüştür. ZHM nanokristallerinin in vitro sitotoksik etkisi 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide testi ile belirlenmiştir. Caco-2 hücreleri taşınma çalışmaları, ZHM kaba tozu ve nanokristal formülasyonları ile gerçekleştirilmiştir. Bulgular: ZHM nanokristalleri 400-600 nm PB, 0,1-0,4 PBD ve >20 mV ZP değerleri ile elde edilmiştir. Tüm çalışma gruplarında hücre canlılığı %100 kalmıştır. Caco-2 hücrelerinden geçiş çalışmalarında, ZHM nanokristalleri, permeabilite değerini ZHM kaba tozuna kıyasla 2,3 kat artırmıştır. Aynı zamanda kümülatif ilaç taşınımı örnek alma süresinin sonunda yükselmiştir. Sonuç: Nanokristal teknolojisi doygunluk çözünürlüğünü artırmasına bağlı olarak permeabiliteyi artırmada yarar sağlayabilir.

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Cite This Article

ÖZTÜRK, N., KARAKÜÇÜK, A., ÇELEBİ, N., TAŞHAN, E. (2022). In Vitro Caco-2 Cell Permeability Studies of Ziprasidone Hydrochloride Monohydrate Nanocrystals. Turkish Journal of Pharmaceutical Sciences, Cilt: 18 - Sayı: 2, 111–115. https://ajindex.com/articles/654558

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