Antidiabetic Activity from Gallic Acid Encapsulated Nanochitosan

Purbowatiningrum,; Ngadiwiyana, Ngadiwiyana; Ismiyarto, Ismiyarto; Fachriyah, Enny; Eviana, I; Eldiana, O; Amaliyah, Nur; Sektianingrum, A N

doi:10.1088/1757-899x/172/1/012042

Cited by 12 publications

(5 citation statements)

References 7 publications

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“…Various nanostructured systems have been proven to be prospective delivery strategies to improve the bioavailability and therapeutic efficacy of gallic acid [277,278]. Gallic-acid-encapsulated chitosan nanoparticles showed improvement in α-glucosidase inhibitory effect and would be a suitable antidiabetic nanoformulation [279]. Hydroxyapatite nanoparticles carrying insulin and gallic acid have been found to be an effective oral formulation to mitigate hyperglycaemia [280].…”

Section: Gallic Acidmentioning

confidence: 99%

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

Dewanjee

Chakraborty

Mukherjee

et al. 2020

IJMS

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Diabetes mellitus is a life-threatening metabolic syndrome. Over the past few decades, the incidence of diabetes has climbed exponentially. Several therapeutic approaches have been undertaken, but the occurrence and risk still remain unabated. Several plant-derived small molecules have been proposed to be effective against diabetes and associated vascular complications via acting on several therapeutic targets. In addition, the biocompatibility of these phytochemicals increasingly enhances the interest of exploiting them as therapeutic negotiators. However, poor pharmacokinetic and biopharmaceutical attributes of these phytochemicals largely restrict their clinical usefulness as therapeutic agents. Several pharmaceutical attempts have been undertaken to enhance their compliance and therapeutic efficacy. In this regard, the application of nanotechnology has been proven to be the best approach to improve the compliance and clinical efficacy by overturning the pharmacokinetic and biopharmaceutical obstacles associated with the plant-derived antidiabetic agents. This review gives a comprehensive and up-to-date overview of the nanoformulations of phytochemicals in the management of diabetes and associated complications. The effects of nanosizing on pharmacokinetic, biopharmaceutical and therapeutic profiles of plant-derived small molecules, such as curcumin, resveratrol, naringenin, quercetin, apigenin, baicalin, luteolin, rosmarinic acid, berberine, gymnemic acid, emodin, scutellarin, catechins, thymoquinone, ferulic acid, stevioside, and others have been discussed comprehensively in this review.

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Section: Gallic Acidmentioning

confidence: 99%

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

Dewanjee

Chakraborty

Mukherjee

et al. 2020

IJMS

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“…However, it is not stable at extreme temperatures and in presence of oxygen or light [22]. Furthermore, the pharmacological activities of GA are greatly discounted owing to its large particle size and poor solubility during the absorption process [23]. To improve the solubility and dissolution rate of GA, several CCFs have been used to screen GA-based cocrystals, including succinimide, caffeine, isoniazid, etc.…”

Section: Introductionmentioning

confidence: 99%

Characterizations and Assays of α-Glucosidase Inhibition Activity on Gallic Acid Cocrystals: Can the Cocrystals be Defined as a New Chemical Entity During Binding with the α-Glucosidase?

Xue

Jia

et al. 2020

Molecules

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Cocrystallization with co-former (CCF) has proved to be a powerful approach to improve the solubility and even bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). However, it is still uncertain whether a cocrystal would exert the pharmacological activity in the form of a new chemical entity, an API-CCF supramolecule. In the present study, gallic acid (GA)-glutaric acid and GA-succinimide cocrystals were screened. The solubility, dissolution rate and oral bioavailability of the two cocrystals were evaluated. As expected, AUCs of GA-glutaric acid and GA-succinimide cocrystals were 1.86-fold and 2.60-fold higher than that of single GA, respectively. Moreover, experimental evaluations on α-glucosidase inhibition activity in vitro and theoretical simulations were used to detect whether the two cocrystals would be recognized as a new chemical entity during binding with α-glucosidase, a target protein in hypoglycemic mechanisms. The enzyme activity evaluation results showed that both GA and glutaric acid displayed α-glucosidase inhibition activity, and GA-glutaric acid cocrystals showed strengthened α-glucosidase inhibition activity at a moderate concentration, which is attributed to synergism of the two components. Molecular docking displayed that the GA-glutaric acid complex deeply entered the active cavity of the α-glucosidase in the form of a supramolecule, which made the guest-enzyme binding configuration more stable. For the GA and succinimide system, succinimide showed no enzyme inhibition activity, however, the GA-succinimide complex presented slightly higher α-glucosidase inhibition activity than that of GA. Molecular docking simulation indicated that the guest molecules entering the active cavity of the α-glucosidase were free GA and succinimide, not the GA-succinimide supramolecule.

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“…Though the presence of gallic acid was not qualitatively run for TLC, it was quantitatively estimated in the drug TVKC. The gallic acid has been reported for anti-inflammatory, 20 cardioprotective effects in diabetes induced myocardial dysfunction, 21 antibacterial, 22 cytotoxic activity, 23 antioxidant 24 and anti-diabetic 24,25 activities. As the content of gallic acid as determined by HPTLC is 1.61% (w/w), TVKC will exhibit the similar activities of gallic acid.…”

Section: Discussionmentioning

confidence: 99%

Chemical Standardization of Thetran Vithai Kutinir Chooranam-An Antidiabetic Siddha Polyherbal Formulation

Elankani¹,

S²,

Shakila³

et al. 2019

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Antidiabetic Activity from Gallic Acid Encapsulated Nanochitosan

Cited by 12 publications

References 7 publications

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

Characterizations and Assays of α-Glucosidase Inhibition Activity on Gallic Acid Cocrystals: Can the Cocrystals be Defined as a New Chemical Entity During Binding with the α-Glucosidase?

Chemical Standardization of Thetran Vithai Kutinir Chooranam-An Antidiabetic Siddha Polyherbal Formulation

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