Biopharmaceutic Study and In Vivo Efficacy of Natural and Derivatives Flavanones Formulations

Abstract

Aim: The development and characterization of nanostructured flavanone formulations (FF) of 1 extracted from Eysenhardtia platycarpa and 1a, 1b, 1c and 1d derivatives by structural modification of 1 as anti-inflammatory candidates for topical treatment of local inflammation. Materials & methods: The FF were physicochemical characterized and the behavior release, skin permeation and, in vivo anti-inflammatory efficacy in the rat model were studied. Results: The FF revealed sustained drug release and showed slow drug penetration in human skin. The FF reduced inflammation in comparison with the standard formulation. Conclusion: The FF could be effective systems for the delivery and controlled release of flavanones on the skin, and the chemical modification of lead molecule 1 improved the efficacy.

Keywords::

• ex vivo permeation
• in vitro release
• in vivo anti-inflammation
• nanostructured formulations
• natural and derivatives flavanones

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at: www.tandfonline.com/doi/suppl/10.2217/nnm-2020-0368

Author contributions

Substantial contributions to the conception or design of the work; or the acquisition, analysis or interpretation of data for the work have been provided by P Bustos-Salgado, B Andrade-Carrera, A Calpena-Campmany, MJ Rodríguez-Lagunas, V Domínguez-Villegas and ML Garduño-Ramírez. Drafting the work or revising it critically for important intellectual content has been contributed by P Bustos-Salgado, B Andrade-Carrera, A Calpena-Campmany, MJ Rodríguez-Lagunas, A Boix-Montañes, V Domínguez-Villegas and ML Garduño-Ramírez. Final approval of the version to be published has been contributed by P Bustos-Salgado, B Andrade-Carrera, A Calpena-Campmany, MJ Rodríguez-Lagunas, A Boix-Montañes, V Domínguez-Villegas and ML Garduño-Ramírez. Agreement to be accountable for all aspects of the work in ensuring that questions related to the accuracy or integrity of any part of the work are appropriately investigated and resolved has been provided by P Bustos-Salgado, B Andrade-Carrera, A Calpena-Campmany, MJ Rodríguez-Lagunas, A Boix-Montañes, V Domínguez-Villegas and ML Garduño-Ramírez.

Financial & competing interests disclosure

This work was supported by a grant from CONACYT-México (grant number 709906). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

Acknowledgments

The authors thank L Gómez-Segura of the Bellvitge Hospital for her assistance in the management of the animals used in the experiments, as well as L Delgado and L Halbaut for their excellent technical support. Moreover, they express their acknowledgement to Gattefossé for supplying the formulation components and skin samples in this study, to Hospital Barcelona-SCIAS (Barcelona, Spain) and to H Paul for his review of the use of the English language.

Additional information

Funding

This work was supported by a grant from CONACYT-México (grant number 709906). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.