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Article

Ileo-Colon Targeting of the Poorly Water-Soluble Drug Celecoxib Using a pH-Dependent Coating in Combination with Self-Emulsifying Drug Delivery or Solid Dispersion Systems

Groningen Research Institute of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands
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Author to whom correspondence should be addressed.
Academic Editor: Yunjin Jung
Pharmaceutics 2021, 13(5), 731; https://doi.org/10.3390/pharmaceutics13050731
Received: 29 April 2021 / Revised: 12 May 2021 / Accepted: 13 May 2021 / Published: 15 May 2021
(This article belongs to the Special Issue Colon-Targeted Drug Delivery)
Targeting celecoxib to the ileo-colonic region could be beneficial for the treatment and prevention of colon cancer. Ileo-colonic targeting can be achieved by using pH-dependent coating systems such as ColoPulse. Celecoxib has poor aqueous solubility, which may jeopardize optimal treatment. Therefore, we combined a pH-dependent coating with self-emulsifying drug delivery systems (SEDDS) or with solid dispersion systems (SD); two approaches that are often used to improve the dissolution behavior of lipophilic drugs. The dissolution behavior of various formulations of both systems was investigated. Optimized formulations with and without precipitation inhibitors were coated with the ColoPulse and the release of celecoxib was tested under non-sink conditions using an in vitro dissolution system, simulating the pH gradient of the gastrointestinal tract. The dissolution behavior of SDs with and without precipitation inhibitor (sodium dodecyl sulfate) and the SEDDS without precipitation inhibitor was negatively impacted by the coating. Control experiments indicated that components of the coating released in the dissolution medium acted as precipitation mediators. However, the SEDDS formulation with HPMC 4000 cps as a precipitation inhibitor showed excellent dissolution behavior. We hypothesize that HPMC accumulates at the oil/water interface of the emulsion thereby stabilizing the emulsion resulting in maintenance of the supersaturated state. View Full-Text
Keywords: ileo-colonic drug delivery; supersaturation; film coating; BCS class II drug; delayed release; ColoPulse ileo-colonic drug delivery; supersaturation; film coating; BCS class II drug; delayed release; ColoPulse
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MDPI and ACS Style

Broesder, A.; Berends, J.M.E.; Scheepers, S.M.; Nguyen, D.N.; Frijlink, H.W.; Hinrichs, W.L.J. Ileo-Colon Targeting of the Poorly Water-Soluble Drug Celecoxib Using a pH-Dependent Coating in Combination with Self-Emulsifying Drug Delivery or Solid Dispersion Systems. Pharmaceutics 2021, 13, 731. https://doi.org/10.3390/pharmaceutics13050731

AMA Style

Broesder A, Berends JME, Scheepers SM, Nguyen DN, Frijlink HW, Hinrichs WLJ. Ileo-Colon Targeting of the Poorly Water-Soluble Drug Celecoxib Using a pH-Dependent Coating in Combination with Self-Emulsifying Drug Delivery or Solid Dispersion Systems. Pharmaceutics. 2021; 13(5):731. https://doi.org/10.3390/pharmaceutics13050731

Chicago/Turabian Style

Broesder, Annemarie, Julia M.E. Berends, Sophie M. Scheepers, Duong N. Nguyen, Henderik W. Frijlink, and Wouter L.J. Hinrichs. 2021. "Ileo-Colon Targeting of the Poorly Water-Soluble Drug Celecoxib Using a pH-Dependent Coating in Combination with Self-Emulsifying Drug Delivery or Solid Dispersion Systems" Pharmaceutics 13, no. 5: 731. https://doi.org/10.3390/pharmaceutics13050731

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