TY - JOUR
T1 - Exploring the utility of co-amorphous materials to concurrently improve the solubility and permeability of Fexofenadine
AU - Uppala, Sravya
AU - Vullendula, Sai Krishna Anand
AU - Yarlagadda, Dani Lakshman
AU - Dengale, Swapnil Jayant
N1 - Funding Information:
The authors would like to acknowledge the kind help rendered by Ms. Sayalee Mane and Mr. Ajay Sabbavarapu from the Department of Pharmaceutical Analysis, NIPER-G, during the revision of the manuscript.
Publisher Copyright:
© 2022 Elsevier B.V.
PY - 2022/6
Y1 - 2022/6
N2 - In this study, the co-amorphous materials of BCS class-IV drug Fexofenadine were prepared by employing Naringin as a co-former. Naringin was employed as a coformer anticipating the concurrent improvement in the solubility and permeability by virtue of its good glass-forming ability and p-gp inhibition potential, respectively. The solid-state characterization of prepared co-amorphous materials by powder-XRD, DSC, and FTIR revealed amorphous state and π-π interactions between Fexofenadine and Naringin. The interactions were confirmed by Molecular Dynamic studies employing Schrodinger material science Suite®. The co-amorphous materials demonstrated improved solubility and dissolution for both Fexofenadine and Naringin. The deliquescent nature of Naringin led to the significant moisture uptake by coamorphous materials. However, the dissolution advantage of Fexofenadine and Naringin sustained in the stability samples due to accelerated π-π interactions in the presence of water. The permeability of co-amorphous samples was estimated using everted gut sac method which was found improved by 5-fold and 3.5-fold for Fexofenadine and Naringin, respectively. The improvement in the permeability was attributed to the interplay between solubility improvement and dose-dependent P-gp inhibition by Naringin.
AB - In this study, the co-amorphous materials of BCS class-IV drug Fexofenadine were prepared by employing Naringin as a co-former. Naringin was employed as a coformer anticipating the concurrent improvement in the solubility and permeability by virtue of its good glass-forming ability and p-gp inhibition potential, respectively. The solid-state characterization of prepared co-amorphous materials by powder-XRD, DSC, and FTIR revealed amorphous state and π-π interactions between Fexofenadine and Naringin. The interactions were confirmed by Molecular Dynamic studies employing Schrodinger material science Suite®. The co-amorphous materials demonstrated improved solubility and dissolution for both Fexofenadine and Naringin. The deliquescent nature of Naringin led to the significant moisture uptake by coamorphous materials. However, the dissolution advantage of Fexofenadine and Naringin sustained in the stability samples due to accelerated π-π interactions in the presence of water. The permeability of co-amorphous samples was estimated using everted gut sac method which was found improved by 5-fold and 3.5-fold for Fexofenadine and Naringin, respectively. The improvement in the permeability was attributed to the interplay between solubility improvement and dose-dependent P-gp inhibition by Naringin.
UR - http://www.scopus.com/inward/record.url?scp=85130332032&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85130332032&partnerID=8YFLogxK
U2 - 10.1016/j.jddst.2022.103431
DO - 10.1016/j.jddst.2022.103431
M3 - Article
AN - SCOPUS:85130332032
SN - 1773-2247
VL - 72
JO - Journal of Drug Delivery Science and Technology
JF - Journal of Drug Delivery Science and Technology
M1 - 103431
ER -