TY - JOUR
T1 - Efficacy of resveratrol encapsulated microsponges delivered by pectin based matrix tablets in rats with acetic acid-induced ulcerative colitis
AU - Gandhi, Himanshu
AU - Rathore, Charul
AU - Dua, Kamal
AU - Vihal, Samar
AU - Tambuwala, Murtaza M.
AU - Negi, Poonam
PY - 2020/3/3
Y1 - 2020/3/3
N2 - Objectives: The objective of the present work to encapsulate the resveratrol (RES) inside the chitosan-based microsponges, employing the systematic optimization by 3
3 Box–Behnken design for the colonic targeting. Significance: Enhanced therapeutic efficacy of RES-loaded microsponges and matrix tablets, vis-a-vis pureRES for ulcerative colitis. Methods: RES-loaded microsponges were prepared employing the systematic optimization by 3
3 Box–Behnken design for the colonic targeting. The best-optimizedRES-loaded microsponge was compressed in the form of a tablet, employing pectin as a matrix-forming material. The encapsulation of RES inside microsponge was confirmed by XRD, DSC and FT-IR. Further, both RES-loaded microsponges and matrix tablets were evaluated for in vitro release kinetics and further evaluated for in vivo ulcerative colitis animal model. Results: Optimization experiments was obtained as the high value of r
2 (particle size = 0.9999; %EE = 0.9652; %CDR = 0.9469) inferred excellent goodness of fit. SEM revealed nearly spherical and porous nature of RES-loaded microsponges. The in vitro release kinetic showed zero-order release for RES-loaded microsponges and Korsmeyer–Peppas model for matrix tablets. The pharmacodynamic studies, in ulcerative colitis rat model, indicated better therapeutic efficacy of drug-loaded microsponges and matrix tablets, vis-a-vis pure RES. Thus, the present study advocates the potential of RES based microsponges delivered by pectin based matrix tablet, in the treatment of various colonic disorders. Conclusion: The present study proved that RES-loaded microsponges and matrix tablets based on chitosan and pectin can be the ideal delivery system for colonic delivery of RES.
AB - Objectives: The objective of the present work to encapsulate the resveratrol (RES) inside the chitosan-based microsponges, employing the systematic optimization by 3
3 Box–Behnken design for the colonic targeting. Significance: Enhanced therapeutic efficacy of RES-loaded microsponges and matrix tablets, vis-a-vis pureRES for ulcerative colitis. Methods: RES-loaded microsponges were prepared employing the systematic optimization by 3
3 Box–Behnken design for the colonic targeting. The best-optimizedRES-loaded microsponge was compressed in the form of a tablet, employing pectin as a matrix-forming material. The encapsulation of RES inside microsponge was confirmed by XRD, DSC and FT-IR. Further, both RES-loaded microsponges and matrix tablets were evaluated for in vitro release kinetics and further evaluated for in vivo ulcerative colitis animal model. Results: Optimization experiments was obtained as the high value of r
2 (particle size = 0.9999; %EE = 0.9652; %CDR = 0.9469) inferred excellent goodness of fit. SEM revealed nearly spherical and porous nature of RES-loaded microsponges. The in vitro release kinetic showed zero-order release for RES-loaded microsponges and Korsmeyer–Peppas model for matrix tablets. The pharmacodynamic studies, in ulcerative colitis rat model, indicated better therapeutic efficacy of drug-loaded microsponges and matrix tablets, vis-a-vis pure RES. Thus, the present study advocates the potential of RES based microsponges delivered by pectin based matrix tablet, in the treatment of various colonic disorders. Conclusion: The present study proved that RES-loaded microsponges and matrix tablets based on chitosan and pectin can be the ideal delivery system for colonic delivery of RES.
KW - Box–Behnken design
KW - Chitosan
KW - pectin
KW - quasi emulsion solvent diffusion method
KW - release kinetics
KW - ulcerative colitis
UR - http://www.scopus.com/inward/record.url?scp=85079387357&partnerID=8YFLogxK
UR - https://www.tandfonline.com/doi/full/10.1080/03639045.2020.1724127
U2 - 10.1080/03639045.2020.1724127
DO - 10.1080/03639045.2020.1724127
M3 - Article
C2 - 32041433
SN - 0363-9045
VL - 46
SP - 365
EP - 375
JO - Drug Development and Industrial Pharmacy
JF - Drug Development and Industrial Pharmacy
IS - 3
ER -