Design and In Vivo Anti-Inflammatory Effect of Ketoprofen Delayed Delivery Systems
Andrea Cerciello
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorCorresponding Author
Giulia Auriemma
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Telephone: +39-089969395; Fax: +39-089969602; E-mail: [email protected]Search for more papers by this authorSilvana Morello
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorAldo Pinto
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorPasquale Del Gaudio
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorPaola Russo
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorRita P. Aquino
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorAndrea Cerciello
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorCorresponding Author
Giulia Auriemma
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Telephone: +39-089969395; Fax: +39-089969602; E-mail: [email protected]Search for more papers by this authorSilvana Morello
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorAldo Pinto
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorPasquale Del Gaudio
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorPaola Russo
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorRita P. Aquino
Department of Pharmacy, University of Salerno, I-84084 Fisciano, (SA), Italy
Search for more papers by this authorAbstract
For the treatment of inflammatory-based diseases affected by circadian rhythms, the development of once-daily dosage forms is required to target early morning symptoms. In this study, Zn–alginate beads containing ketoprofen (K) were developed by a tandem technique prilling/ionotropic gelation. The effect of main critical variables on particles micromeritics, inner structure as well as on drug loading and in vitro drug release was studied. The in vivo anti-inflammatory efficacy was evaluated using a modified protocol of carrageenan-induced edema in rat paw administering beads to rats by oral gavage at 0, 3, or 5 h before edema induction. Good drug loading and desired particle size and morphology were obtained for the optimized formulation F20. In vitro dissolution studies showed that F20 had a gastroresistant behavior and delayed release of the drug in simulated intestinal fluid. The in vitro delayed release pattern was clearly reflected in the prolonged anti-inflammatory effect in vivo of F20, compared to pure ketoprofen; F20, administered 3 h before edema induction, showed a significant anti-inflammatory activity, reducing maximum paw volume in response to carrageenan injection, whereas no response was observed for ketoprofen. The designed beads appear a promising platform suitable for a delayed release of anti-inflammatory drugs. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:3451–3458, 2015
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