Abstract
Objective: Formulation of injectable In situ forming implant (ISI) systems of lornoxicam for dental and postoperative pain management to decrease dosing frequency and increase patient compliance.
Methods: Polymeric in situ implant solutions were prepared using different concentrations and inherent viscosities of Poly-DL-lactide (PDL) or DL-lactide/glycolide copolymer (PDLG) using 22X4 factorial experimental design. Nonpolymeric systems were prepared using different concentrations of lipids like cetyl alcohol and stearyl alcohol and also sucrose acetate isobutyrate (SAIB) using 32 factorial experimental design. In vitro release study, rheological measurement, syringeability assessment and effect of γ-sterilization were used for evaluation of the prepared formulae. In vivo pharmacokinetic study of lornoxicam from the most optimum formula was conducted in a rabbit model using HPLC analysis of blood samples.
Results: Polymeric systems showed high burst release followed by very slow release rate over 72 hours. Formula I 24 (containing SAIB 80% (w/w)) showed relatively low burst release followed by diffusion controlled release pattern, low viscosity, Newtonian flow behavior and good syringeability. γ- sterilization had no significant effect on the in vitro release and the physical nature of the most optimum formula. In vivo study concluded that intramuscularly injected In situ implant formula I 24 showed prolonged release pattern compared to the marketed product which was indicated by the increased Tmax and the extended mean residence time.
Conclusion: Lornoxicam ISI systems could be promising as convenient injectable sustained release delivery systems for dental and postoperative pain management.
Keywords: Lornoxicam, sucrose acetate isobutyrate, biodegradable, pharmacokinetics rabbit model, polymeric system, PDLG.
Current Drug Delivery
Title:Polymeric and Non Polymeric Injectable In-situ Forming Implant Systems for Sustained Delivery of Lornoxicam: In vitro and In vivo Evaluation
Volume: 15 Issue: 8
Author(s): Soad A. Yehia, Sally A.A. Halim and Mary Y. Aziz*
Affiliation:
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, 12411, Cairo,Egypt
Keywords: Lornoxicam, sucrose acetate isobutyrate, biodegradable, pharmacokinetics rabbit model, polymeric system, PDLG.
Abstract: Objective: Formulation of injectable In situ forming implant (ISI) systems of lornoxicam for dental and postoperative pain management to decrease dosing frequency and increase patient compliance.
Methods: Polymeric in situ implant solutions were prepared using different concentrations and inherent viscosities of Poly-DL-lactide (PDL) or DL-lactide/glycolide copolymer (PDLG) using 22X4 factorial experimental design. Nonpolymeric systems were prepared using different concentrations of lipids like cetyl alcohol and stearyl alcohol and also sucrose acetate isobutyrate (SAIB) using 32 factorial experimental design. In vitro release study, rheological measurement, syringeability assessment and effect of γ-sterilization were used for evaluation of the prepared formulae. In vivo pharmacokinetic study of lornoxicam from the most optimum formula was conducted in a rabbit model using HPLC analysis of blood samples.
Results: Polymeric systems showed high burst release followed by very slow release rate over 72 hours. Formula I 24 (containing SAIB 80% (w/w)) showed relatively low burst release followed by diffusion controlled release pattern, low viscosity, Newtonian flow behavior and good syringeability. γ- sterilization had no significant effect on the in vitro release and the physical nature of the most optimum formula. In vivo study concluded that intramuscularly injected In situ implant formula I 24 showed prolonged release pattern compared to the marketed product which was indicated by the increased Tmax and the extended mean residence time.
Conclusion: Lornoxicam ISI systems could be promising as convenient injectable sustained release delivery systems for dental and postoperative pain management.
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Cite this article as:
Yehia A. Soad , Halim A.A. Sally and Aziz Y. Mary *, Polymeric and Non Polymeric Injectable In-situ Forming Implant Systems for Sustained Delivery of Lornoxicam: In vitro and In vivo Evaluation, Current Drug Delivery 2018; 15 (8) . https://dx.doi.org/10.2174/1567201815666180320101125
DOI https://dx.doi.org/10.2174/1567201815666180320101125 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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