Research Article
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Year 2018, Volume 48, Issue 3, 82 - 88, 01.12.2018

Abstract

References

  • Amidon G, Lennernȁs H, Shah VP, Crison JR (1995). A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12: 413-420. Antoine D, Pellequer Y, Tempesta C, Lorscheidt C, Kettel B, Tamaddon L, Jannin V, Demarne F, Lamprecht A, Béduneau A (2015). Biorelevant media resistant co-culture model mimicking permeability of human intestine. Int. J. Pharm. 481: 27 – 36. Berridge MV, Herst PM, Tan AS (2005). Tetrazolium dyes as tools in cell biology: new insights into their cellular reduction. Biotechnol Annu Rev 11: 127-152. Birch D, Diedrichsen RG, Christophersen PC, Mu H, Nielsen HM (2018). Evaluation of drug permeation under fed state conditions using mucus-covered Caco-2 cell epithelium. Eur J Pharm Sci 118: 144-153. Boni JE, Brickl RS, Dressman J, Pfefferle ML (2009). Instant FaSSIF and FeSSIF – biorelevance meets practicality. Diss Tech 16: 41-45. Dahl JE, Frangou-Polyzois MJ, Polyzois GL (2006). In vitro biocompatibility of denture relining materials. Gerodontology 23: 17-22. Dressman JB, Amidon GL, Reppas C, Shah VP (1998). Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms. Pharm Res 15: 11-22. Fagerberg JH, Tsinman O, Sun N, Tsinman K, Avdeef A, Bergström CAS (2010). Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media. Mol Pharm 7: 1419-1430. Fatouros DG, Walrand I, Bergenstahl B, Müllertz A (2009). Colloidal structures in media simulating intestinal fed state conditions with and without lipolysis products. Pharm Res 26: 361-374. Fuchs A, Leigh M, Kloefer B, Dressman JB (2015). Advances in the design of fasted state simulating intestinal fluids: FaSSIF-V3. Eur J Pharm Biopharm 94: 229-240. Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB (1998). Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res 15: 698-705. Ingels F, Deferme S, Destexhe E, Oth M, Mooter G, Augustijns p (2002). Simulated intestinal fluid as transport medium in the Caco-2 cell-culture model. Int J Pharm 232: 183-192. Ingels FM, Augustijns PF (2003). Biological, pharmaceutical and analytical consideration with respect to the transport media used in the absorption screening system Caco-2. J Pharm Sci 92: 1545-1558. Jantraid E, Janssen N, Reppas C, Dressman JB (2008). Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update. Pharm Res 25: 1663-1676. Kleberg K, Jacobsen F, Fatouros DG, Müllertz A (2010). Biorelevant media simulating fed state intestinal fluids: Colloid phase characterization and impact on solubilization capacity. J Pharm Sci 99: 3522-3532 Klein S (2010). The use of biorelevant dissolution media to forecast the in vivo performance of a drug. AAPS J 12: 397-406. Kostewicz ES, Brauns U, Becker R, Dressman JB (2002). Forecasting the oral absorption behavior of poorly soluble weak bases using solubility and dissoxlution studies in biorelevant media. Pharm Res 19: 345-349. Laitinen L, Takala E, Vuorela H, Vuorela P, Kaukonen AM, Marvola M (2007). Anthranoid laxatives influence the absorption of poorly permeable drugs in human intestinal cell culture model (Caco-2). Eur J Pharm Biopharm 66: 135-145. Li P, Zhao L (2003). Solubilization of flurbiprofen in pH-surfactant solutions. J Pharm Sci 92: 951-956. Marques M (2004). Dissolution media simulating fasted and fed states. Diss Tech 11: 16. Mathias N, Xu Y, Vig B, Kestur U, Saari A, Crison J, Desai D, Vanarase A, Hussain M (2015). Food effect in humans: predicting the risk through in vitro dissolution and in vivo pharmacokinetic models. AAPS J 17: 988-998. Nicolaides E, Galia E, Efthymiopoulus C, Dressman JB, Reppas C (1999). Forecasting the in vivo performance of four low solubility drugs from their in vitro dissolution data. Pharm Res 12: 1876-1882. Oh DM, Curl RL, Amidon GL (1993). Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model. Pharm Res 10: 264-270. Pargal A, Kelkar MG, Nayak PJ (1996). The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations. Biopharm Drug Disp 17: 511-519 Patel N, Forbes B, Eskola S, Murray J (2006). Use of Simulated Intestinal Fluids with Caco-2 Cells and Rat Ileum. Drug Dev Ind Pharm 32: 151-161. Tang L, Khan SU, Muhammad NA (2001). Evaluation and selection of bio-relevant dissolution media for a poorly water-soluble new chemical entity. Pharm Dev Technol 6: 531-540. Wiedman TS, Liang W, Kamel L (2002). Solubilization of drugs by physiological mixtures of bile salts. Pharm Res 19: 1203-1208. Xu H, Vela S, Shi Y, Marrroum P, Gao P (2017). In vitro characterization of ritonavir drug products and correlation to human in vivo performance. Mol Pharm 14: 3801-3814. Yazdanian M, Briggs K, Jankovsky C, Hawi A (2004). The high solubility definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm Res 21: 293-299. Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW (2017). Statistical investigation of simulated fed intestinal media composition on the equilibrum solubility of oral drugs. Eur J Pharm Sci 99: 95-104.

Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line

Year 2018, Volume 48, Issue 3, 82 - 88, 01.12.2018

Abstract

DOI: 10.26650/IstanbulJPharm.2018.180013


Biorelevant media are used to simulate the physiological conditions in terms of components, pH, osmolality and buffer capacity of the human stomach and intestine in both fasted and fed states  In this study, we aim to apply the biorelevant media to Caco-2 cell lines to investigate the cytotoxicity effects via the cell viability ratio and to compare the solubilizing effects of various dissolution media on a poorly soluble model drug. Flurbiprofen (Biopharmaceutics Classification System, BCS Class 2) was selected as a model drug.

In dissolution studies the pH effects were predominant at higher pH values, while bile salt effects were dominant at lower pH values. The preparation method, bile salts and the phospholipids did not show any additional effect on Caco-2 cell viability. In the cytotoxicity test, fed state media caused an additional 10-15% decrease in cell viability, compared to the fasted state. Similar results were obtained when using the blank of these media which did not include the bile salt or phospholipid. From this, it is evident that this decrease resulted from the pH values, not the components. In conclusion, the cytotoxicity assessment showed that all the biorelevant media were compatible with 70-90% of cell viability for at least 24 h, and this ratio might be increased by modifying the pH.

References

  • Amidon G, Lennernȁs H, Shah VP, Crison JR (1995). A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12: 413-420. Antoine D, Pellequer Y, Tempesta C, Lorscheidt C, Kettel B, Tamaddon L, Jannin V, Demarne F, Lamprecht A, Béduneau A (2015). Biorelevant media resistant co-culture model mimicking permeability of human intestine. Int. J. Pharm. 481: 27 – 36. Berridge MV, Herst PM, Tan AS (2005). Tetrazolium dyes as tools in cell biology: new insights into their cellular reduction. Biotechnol Annu Rev 11: 127-152. Birch D, Diedrichsen RG, Christophersen PC, Mu H, Nielsen HM (2018). Evaluation of drug permeation under fed state conditions using mucus-covered Caco-2 cell epithelium. Eur J Pharm Sci 118: 144-153. Boni JE, Brickl RS, Dressman J, Pfefferle ML (2009). Instant FaSSIF and FeSSIF – biorelevance meets practicality. Diss Tech 16: 41-45. Dahl JE, Frangou-Polyzois MJ, Polyzois GL (2006). In vitro biocompatibility of denture relining materials. Gerodontology 23: 17-22. Dressman JB, Amidon GL, Reppas C, Shah VP (1998). Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms. Pharm Res 15: 11-22. Fagerberg JH, Tsinman O, Sun N, Tsinman K, Avdeef A, Bergström CAS (2010). Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media. Mol Pharm 7: 1419-1430. Fatouros DG, Walrand I, Bergenstahl B, Müllertz A (2009). Colloidal structures in media simulating intestinal fed state conditions with and without lipolysis products. Pharm Res 26: 361-374. Fuchs A, Leigh M, Kloefer B, Dressman JB (2015). Advances in the design of fasted state simulating intestinal fluids: FaSSIF-V3. Eur J Pharm Biopharm 94: 229-240. Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB (1998). Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res 15: 698-705. Ingels F, Deferme S, Destexhe E, Oth M, Mooter G, Augustijns p (2002). Simulated intestinal fluid as transport medium in the Caco-2 cell-culture model. Int J Pharm 232: 183-192. Ingels FM, Augustijns PF (2003). Biological, pharmaceutical and analytical consideration with respect to the transport media used in the absorption screening system Caco-2. J Pharm Sci 92: 1545-1558. Jantraid E, Janssen N, Reppas C, Dressman JB (2008). Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update. Pharm Res 25: 1663-1676. Kleberg K, Jacobsen F, Fatouros DG, Müllertz A (2010). Biorelevant media simulating fed state intestinal fluids: Colloid phase characterization and impact on solubilization capacity. J Pharm Sci 99: 3522-3532 Klein S (2010). The use of biorelevant dissolution media to forecast the in vivo performance of a drug. AAPS J 12: 397-406. Kostewicz ES, Brauns U, Becker R, Dressman JB (2002). Forecasting the oral absorption behavior of poorly soluble weak bases using solubility and dissoxlution studies in biorelevant media. Pharm Res 19: 345-349. Laitinen L, Takala E, Vuorela H, Vuorela P, Kaukonen AM, Marvola M (2007). Anthranoid laxatives influence the absorption of poorly permeable drugs in human intestinal cell culture model (Caco-2). Eur J Pharm Biopharm 66: 135-145. Li P, Zhao L (2003). Solubilization of flurbiprofen in pH-surfactant solutions. J Pharm Sci 92: 951-956. Marques M (2004). Dissolution media simulating fasted and fed states. Diss Tech 11: 16. Mathias N, Xu Y, Vig B, Kestur U, Saari A, Crison J, Desai D, Vanarase A, Hussain M (2015). Food effect in humans: predicting the risk through in vitro dissolution and in vivo pharmacokinetic models. AAPS J 17: 988-998. Nicolaides E, Galia E, Efthymiopoulus C, Dressman JB, Reppas C (1999). Forecasting the in vivo performance of four low solubility drugs from their in vitro dissolution data. Pharm Res 12: 1876-1882. Oh DM, Curl RL, Amidon GL (1993). Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model. Pharm Res 10: 264-270. Pargal A, Kelkar MG, Nayak PJ (1996). The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations. Biopharm Drug Disp 17: 511-519 Patel N, Forbes B, Eskola S, Murray J (2006). Use of Simulated Intestinal Fluids with Caco-2 Cells and Rat Ileum. Drug Dev Ind Pharm 32: 151-161. Tang L, Khan SU, Muhammad NA (2001). Evaluation and selection of bio-relevant dissolution media for a poorly water-soluble new chemical entity. Pharm Dev Technol 6: 531-540. Wiedman TS, Liang W, Kamel L (2002). Solubilization of drugs by physiological mixtures of bile salts. Pharm Res 19: 1203-1208. Xu H, Vela S, Shi Y, Marrroum P, Gao P (2017). In vitro characterization of ritonavir drug products and correlation to human in vivo performance. Mol Pharm 14: 3801-3814. Yazdanian M, Briggs K, Jankovsky C, Hawi A (2004). The high solubility definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm Res 21: 293-299. Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW (2017). Statistical investigation of simulated fed intestinal media composition on the equilibrum solubility of oral drugs. Eur J Pharm Sci 99: 95-104.

Details

Primary Language English
Subjects Health Care Sciences and Services
Journal Section Original Article
Authors

Diren SARISALTIK YAŞIN This is me
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330 Ankara, Turkey; Department of Pharmaceutical Technology, Faculty of Pharmacy, Dicle University, 21280 Diyarbakır, Turkey


Şükran YILMAZ This is me
Foot and Mouth Disease Institute, 06044 Ankara, Turkey


Zeynep Şafak TEKSİN> (Primary Author)
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330 Ankara, Turkey

Publication Date December 1, 2018
Submission Date November 2, 2018
Acceptance Date
Published in Issue Year 2018, Volume 48, Issue 3

Cite

Bibtex @research article { iujp512476, journal = {İstanbul Journal of Pharmacy}, eissn = {2587-2087}, address = {İstanbul Üniversitesi Eczacılık Fakültesi Farmasötik Botanik AD}, publisher = {Istanbul University}, year = {2018}, volume = {48}, number = {3}, pages = {82 - 88}, title = {Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line}, key = {cite}, author = {Sarısaltık Yaşın, Diren and Yılmaz, Şükran and Teksin, Zeynep Şafak} }
APA Sarısaltık Yaşın, D. , Yılmaz, Ş. & Teksin, Z. Ş. (2018). Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line . İstanbul Journal of Pharmacy , 48 (3) , 82-88 . Retrieved from https://dergipark.org.tr/en/pub/iujp/issue/42527/512476
MLA Sarısaltık Yaşın, D. , Yılmaz, Ş. , Teksin, Z. Ş. "Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line" . İstanbul Journal of Pharmacy 48 (2018 ): 82-88 <https://dergipark.org.tr/en/pub/iujp/issue/42527/512476>
Chicago Sarısaltık Yaşın, D. , Yılmaz, Ş. , Teksin, Z. Ş. "Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line". İstanbul Journal of Pharmacy 48 (2018 ): 82-88
RIS TY - JOUR T1 - Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line AU - DirenSarısaltık Yaşın, ŞükranYılmaz, Zeynep ŞafakTeksin Y1 - 2018 PY - 2018 N1 - DO - T2 - İstanbul Journal of Pharmacy JF - Journal JO - JOR SP - 82 EP - 88 VL - 48 IS - 3 SN - -2587-2087 M3 - UR - Y2 - 2023 ER -
EndNote %0 İstanbul Journal of Pharmacy Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line %A Diren Sarısaltık Yaşın , Şükran Yılmaz , Zeynep Şafak Teksin %T Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line %D 2018 %J İstanbul Journal of Pharmacy %P -2587-2087 %V 48 %N 3 %R %U
ISNAD Sarısaltık Yaşın, Diren , Yılmaz, Şükran , Teksin, Zeynep Şafak . "Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line". İstanbul Journal of Pharmacy 48 / 3 (December 2018): 82-88 .
AMA Sarısaltık Yaşın D. , Yılmaz Ş. , Teksin Z. Ş. Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line. iujp. 2018; 48(3): 82-88.
Vancouver Sarısaltık Yaşın D. , Yılmaz Ş. , Teksin Z. Ş. Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line. İstanbul Journal of Pharmacy. 2018; 48(3): 82-88.
IEEE D. Sarısaltık Yaşın , Ş. Yılmaz and Z. Ş. Teksin , "Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line", İstanbul Journal of Pharmacy, vol. 48, no. 3, pp. 82-88, Dec. 2018