Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

Poonam Negi; Surbhi Gautam; Aditi Sharma; Charul Rathore; Lalit Sharma; Navneet Upadhyay; Murtaza M Tambuwala; Dinesh Kumar Chellappan; Gaurav Gupta; Parteek Prasher; Kamal Dua; Shweta Agarwal; Uma Ranjan Lal

doi:10.4155/tde-2021-0062

Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

Poonam Negi, Surbhi Gautam, Aditi Sharma, Charul Rathore, Lalit Sharma, Navneet Upadhyay, Murtaza M Tambuwala, Dinesh Kumar Chellappan, Gaurav Gupta, Parteek Prasher, Kamal Dua, Shweta Agarwal, Uma Ranjan Lal

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Abstract

Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.

Original language	English
Pages (from-to)	81-93
Number of pages	13
Journal	Therapeutic Delivery
Volume	13
Issue number	2
Early online date	25 Jan 2022
DOIs	https://doi.org/10.4155/tde-2021-0062
Publication status	Published (in print/issue) - 28 Feb 2022

Bibliographical note

Publisher Copyright:
© 2022 The Authors.

Keywords

Pharmaceutical formulations
raft system
solid dispersion
tablets
Eudragit EPO
Antiulcer
Terminalia chebula
chebulinic acid

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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tde-2021-0062Final published version, 3.6 MBLicence: CC BY

Cite this

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title = "Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence",

abstract = "Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.",

keywords = "Pharmaceutical formulations, raft system, solid dispersion, tablets, Eudragit EPO, Antiulcer, Terminalia chebula, chebulinic acid",

author = "Poonam Negi and Surbhi Gautam and Aditi Sharma and Charul Rathore and Lalit Sharma and Navneet Upadhyay and Tambuwala, {Murtaza M} and Chellappan, {Dinesh Kumar} and Gaurav Gupta and Parteek Prasher and Kamal Dua and Shweta Agarwal and Lal, {Uma Ranjan}",

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doi = "10.4155/tde-2021-0062",

language = "English",

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T1 - Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

AU - Negi, Poonam

AU - Gautam, Surbhi

AU - Sharma, Aditi

AU - Rathore, Charul

AU - Sharma, Lalit

AU - Upadhyay, Navneet

AU - Tambuwala, Murtaza M

AU - Chellappan, Dinesh Kumar

AU - Gupta, Gaurav

AU - Prasher, Parteek

AU - Dua, Kamal

AU - Agarwal, Shweta

AU - Lal, Uma Ranjan

PY - 2022/2/28

Y1 - 2022/2/28

N2 - Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.

AB - Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.

KW - Pharmaceutical formulations

KW - raft system

KW - solid dispersion

KW - tablets

KW - Eudragit EPO

KW - Antiulcer

KW - Terminalia chebula

KW - chebulinic acid

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DO - 10.4155/tde-2021-0062

M3 - Article

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SN - 2041-5990

VL - 13

SP - 81

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JO - Therapeutic Delivery

JF - Therapeutic Delivery

IS - 2

ER -

Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

Abstract

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Keywords

UN SDGs

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