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Systematically Optimized Ketoprofen-Loaded Novel Proniosomal Formulation for Periodontitis: In Vitro Characterization and In Vivo Pharmacodynamic Evaluation

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ABSTRACT

Various preclinical/clinical studies support the effectiveness of ketoprofen in periodontitis; however, the literature reveals that novel delivery systems have been less explored for the drug in periodontitis. The current investigation aims to explore the potential of a pro-vesicular approach-based proniosomal drug delivery of ketoprofen for its effectiveness and validation in experimental periodontal disease (EPD). Formulations were developed using I-optimal mixture design. Developed formulations were characterized for entrapment efficiency, vesicle size, and in vitro drug release. Selected proniosomal gels were evaluated for mucoadhesiveness, ex vivo drug permeation, and retention studies. Optimized proniosomal gel was evaluated for surface morphology, rheological behavior, texture studies, and pharmacodynamic activity in EPD. The results showed that ketoprofen-loaded proniosomal formulations formed a mucoadhesive hydrogel comprising spherical and flexible vesicles. Viscosity and texture studies showed good adhesion and smoothness, which are desired for enhanced permeation. The disease condition was improved with preserved bone resorption process, that too with intact cementum vis-à-vis marketed gel formulation, when evaluated in the EPD model. The results lead to the conclusion that proniosomes can act as a promising carrier and can be effectively used for improved ketoprofen delivery in periodontal pockets.

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Acknowledgements

The authors are thankful to M/s BEC Chemicals (Mumbai, India), VAV Life Sciences (Mumbai, India), and M/s Lubrizol (Mumbai, India) for generously providing the gift samples of ketoprofen, soya lecithin, and Carbopol® 974P, respectively. The authors are also grateful to M/s Jubilant Life Sciences Ltd. (Noida, India) for providing the research facilities for a part of the research work.

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Correspondence to Sanju Nanda or O. P. Katare.

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Yadav, N.K., Nanda, S., Sharma, G. et al. Systematically Optimized Ketoprofen-Loaded Novel Proniosomal Formulation for Periodontitis: In Vitro Characterization and In Vivo Pharmacodynamic Evaluation. AAPS PharmSciTech 18, 1863–1880 (2017). https://doi.org/10.1208/s12249-016-0665-1

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