KaydedilenlerDerginizi ekleyin

Dergiler / İstanbul Journal of Pharmacy / 2020 / Cilt: 50 - Sayı: 3

Evaluation of Caco-2 cell permeability of ritonavir nanosuspensions

Alptuğ KARAKÜÇÜK
Naile ÖZTÜRK
Nevin ÇELEBİ
Sayfa
251–255
Yayın Tarihi
2020-12-30
DOI
—
🏛️Bu makalenin bibliyografik verileri ve tam metin bağlantısı DergiPark üzerinden sağlanmıştır.
DergiPark Kaydı ↗
✨

Yapay Zeka Hızlı Bakış & Çıkarımlar

AI Insight
⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

Conclusion: Particle size reduction of RTV into nanometer size and preparing nanosuspension system was found effective to obtain enhanced cell permeability.

📌 3 Maddede Bu Makale

🎯
Amaç & Hipotez:Background and Aims: Poor aqueous solubility limits drug absorption through intestinal mucosa.
📊
Temel Bulgular & Veri:The objective of this study was to investigate the cytotoxicity and in vitro cell permeability through human adenocarcinoma (Caco-2) cells of ritonavir (RTV) nanosuspensions.
💡
Sonuç & Katkı:Conclusion: Particle size reduction of RTV into nanometer size and preparing nanosuspension system was found effective to obtain enhanced cell permeability.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Ritonavir · nanosuspension · Caco-2

Abstract

Background and Aims: Poor aqueous solubility limits drug absorption through intestinal mucosa. Nanosuspensions with nanometer range particle size provides enhanced aqueous solubility and hence permeability. The objective of this study was to investigate the cytotoxicity and in vitro cell permeability through human adenocarcinoma (Caco-2) cells of ritonavir (RTV) nanosuspensions. Methods: The Microfluidization method was used to prepare nanosuspensions. Particle size (PS), polydispersity index (PI) and zeta potential (ZP) values were measured as characterization. MTT test was applied to evaluate the cytotoxic effect. Caco-2 cell lines were used for transport studies with RTV coarse powder, physical mixtures and nanosuspension. Results: Approximately 600 nm PS, 0.4 PDI and 22 mV ZP values were observed for nanosuspensions. The sample groups showed no cytotoxicity on the cell lines in any RTV concentration. However, significant cytotoxic effect was determined in groups with high amounts of sodium dodecyl sulfate. The transported RTV in nanosuspension formulation enhanced by 5.3- fold and 1.5-fold in comparison with RTV coarse powder and physical mixture, respectively. Rate of the transportation and also the amount of the transported RTV were improved with nanosuspension formulation. Conclusion: Particle size reduction of RTV into nanometer size and preparing nanosuspension system was found effective to obtain enhanced cell permeability.

🔖

Bu Makaleye Atıf Yap

KARAKÜÇÜK, A., ÖZTÜRK, N., ÇELEBİ, N. (2020). Evaluation of Caco-2 cell permeability of ritonavir nanosuspensions. İstanbul Journal of Pharmacy, Cilt: 50 - Sayı: 3, 251–255. https://ajindex.com/articles/83311

📄 Tam Metin PDF Okuyucu

📄

PDF görüntüleyici hazırlanıyor...

Kaynakça (1)

  1. Alsenz, J., Steffen, H., & Alex, R. (1998). Active apical secretory efflux of the HIV protease inhibitors saquinavir and ritonavir in Caco-2 cell monolayers. Pharmaceutical Research, 15(3), 423–428. https://doi.org/10.1023/A:1011924314899 • Chowdary, K. P. R., Annamma Devi, D. G., & Dhanalakshmi, K. (2012). A factorial study on enhancement of solubility and dissolution rate of ibuprofen by hydroxy propyl β cyclodextrin and solutol hs15. International Journal of Pharmaceutical Sciences Review and Research, 2(4), 1–7. • Holmstock, N., Annaert, P., & Augustijns, P. (2012). Boosting of HIV protease inhibitors by ritonavir in the intestine: The relative role of cytochrome P450 and P-glycoprotein inhibition based on Caco-2 monolayers versus in situ intestinal perfusion in mice. Drug Metabolism and Disposition, 40(8), 1473–1477. https://doi. org/10.1124/dmd.112.044677 • Janneh, O., Jones, E., Chandler, B., Owen, A., & Khoo, S. H. (2007). Inhibition of P-glycoprotein and multidrug resistance-associated proteins modulates the intracellular concentration of lopinavir in cultured CD4 T cells and primary human lymphocytes. Journal of Antimicrobial Chemotherapy, 60(5), 987–993. https://doi. org/10.1093/jac/dkm353 • Karakucuk, A., Celebi, N., & Teksin, Z. S. (2016). Preparation of ritonavir nanosuspensions by microfluidization using polymeric stabilizers: I. A Design of Experiment approach. European Journal of Pharmaceutical Sciences, 95, 111–121. https://doi.org/10.1016/j. ejps.2016.05.010 • Karakucuk, Alptug, Teksin, Z. S., Eroglu, H., & Celebi, N. (2019). Evaluation of improved oral bioavailability of ritonavir nanosuspension. European Journal of Pharmaceutical Sciences, 131(February), 153–158. https://doi.org/10.1016/j.ejps.2019.02.028 • Koga, K., Ohyashiki, T., Murakami, M., & Kawashima, S. (2000). Modification of ceftibuten transport by the addition of non-ionic surfactants. European Journal of Pharmaceutics and Biopharmaceutics, 49(1), 17–25. https://doi.org/10.1016/S0939-6411(99)00059-4 • Lenhardt, T., Vergnault, G., Grenier, P., Scherer, D., & Langguth, P. (2008). Evaluation of nanosuspensions for absorption enhancement of poorly soluble drugs: In vitro transport studies across intestinal epithelial monolayers. AAPS Journal, 10(3), 435–438. https://doi.org/10.1208/s12248-008-9050-7 • Matsumoto, T., Kaifuchi, N., Mizuhara, Y., Warabi, E., & Watanabe, J. (2018). Use of a Caco-2 permeability assay to evaluate the effects of several Kampo medicines on the drug tr