Formulation of gastroretentive sustained release floating in situ gelling drug delivery system of solubility enhanced curcumin-soy lecithin complex

Kathpalia, Harsha; Salunkhe, S. P.; Juvekar, Siddhesh

doi:10.1016/j.jddst.2019.101205

Cited by 10 publications

(6 citation statements)

References 18 publications

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“…In gastrointestinal applications, curcumin’s potential lies in enhancing bioavailability and cellular uptake [ 40 , 41 , 42 , 43 , 44 ]. Various formulations offer extended-release properties, gastric floatability, and sustained drug release, contributing to improved therapeutic outcomes.…”

Section: Discussionmentioning

confidence: 99%

“…Kathpalia et al formulated a gastroretentive floating in situ gelling system of solubility-enhanced curcumin specifically designed for gastric ulcers. This system exhibited extended release of curcumin for up to 12 h, indicating its potential as a reliable delivery platform for curcumin in treating gastric ulcers [ 42 ]. Similarly, Padhan et al developed a gastroretentive in situ gelling system of curcumin for gastric ulcers associated with Helicobacter pylori.…”

Section: Curcumin Delivery Systemsmentioning

confidence: 99%

“…Curcumin-loaded Pickering emulsions, emulsion gels, and oil-filled aerogels offer potential solutions for enhancing curcumin’s bioavailability and stability during digestion [ 40 , 41 ]. Gastroretentive floating in situ gelling systems have been formulated for gastric ulcer treatment, targeting Helicobacter-pylori-associated ulcers [ 42 , 43 ]. Moreover, ultra-high-pressure technology has been utilized to fabricate emulsion gels with unique physical characteristics and controlled release properties [ 44 ].…”

Section: Introductionmentioning

confidence: 99%

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Enhancing Therapeutic Efficacy of Curcumin: Advances in Delivery Systems and Clinical Applications

Omidian

Wilson

Chowdhury

2023

Gels

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Curcumin, a potent active compound found in turmeric and Curcuma xanthorrhiza oil, possesses a wide range of therapeutic properties, including antibacterial, anti-inflammatory, antioxidant, and wound healing activities. However, its clinical effectiveness is hindered by its low bioavailability and rapid elimination from the body. To overcome these limitations, researchers have explored innovative delivery systems for curcumin. Some promising approaches include solid lipid nanoparticles, nanomicelle gels, and transdermal formulations for topical drug delivery. In the field of dentistry, curcumin gels have shown effectiveness against oral disorders and periodontal diseases. Moreover, Pickering emulsions and floating in situ gelling systems have been developed to target gastrointestinal health. Furthermore, curcumin-based systems have demonstrated potential in wound healing and ocular medicine. In addition to its therapeutic applications, curcumin also finds use as a food dye, contraception aid, corrosion-resistant coating, and environmentally friendly stain. This paper primarily focuses on the development of gel compositions of curcumin to address the challenges associated with its clinical use.

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Section: Discussionmentioning

confidence: 99%

Section: Curcumin Delivery Systemsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Enhancing Therapeutic Efficacy of Curcumin: Advances in Delivery Systems and Clinical Applications

Omidian

Wilson

Chowdhury

2023

Gels

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“…For example, etoricoxib-famotidine was combined and was beneficial for the treatment of pain and preventing ulcers in long-term use [32]. Raft-forming formulations of several herbal medicines also supported the effectiveness of this system such as curcumin [33,34] chebulinic acid [35], Aloe vera [36], and quercetin [37]. Additionally, some of them, raft-forming of Centella asiatica extract [38] and curcumin [33], reached in vivo tests.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Delivery of Curcumin and Resveratrol via In Situ Gelling, Raft-Forming, Gastroretentive Formulations

Siripruekpong,

Praparatana,

Issarachot

et al. 2024

Pharmaceutics

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Curcumin and resveratrol are polyphenolic compounds that have been shown to exhibit synergistic therapeutic properties including anti-inflammatory, anticancer, and antiulcer activities, which may be exploited for the treatment of gastric diseases. However, both compounds have poor aqueous solubility and rapid metabolism, resulting in a low oral bioavailability. In situ gelling, liquid formulations were developed to produce a gastroretentive, raft-forming delivery vehicle to improve bioavailability. Solid dispersions containing a mixture of curcumin and resveratrol with Eudragit® EPO (Cur/Res-SD) were first prepared using solvent evaporation, to improve the solubility and dissolution of the compounds. Solid dispersions of a weight ratio of 1:10 curcumin/resveratrol to Eudragit® EPO were subsequently incorporated into in situ gelling, liquid formulations based on the gelling polymers, sodium alginate (low viscosity and medium viscosity), pectin, and gellan gum, respectively. Calcium carbonate and sodium bicarbonate were included to produce carbon dioxide bubbles in the gel matrix, on exposure to gastric fluid, and to achieve flotation. Moreover, the calcium ions acted as a crosslinking agent for the hydrogels. Optimized formulations floated rapidly (<60 s) in simulated gastric fluid (pH = 1.2) and remained buoyant, resulting in the gradual release of more than 80% of the curcumin and resveratrol content within 8 h. The optimized formulation based on medium-viscosity sodium alginate exhibited enhanced cytotoxic activity toward human gastric adenocarcinoma cell lines (AGS), compared with unformulated curcumin and resveratrol compounds, and increased anti-inflammatory activity against RAW 264.7 macrophage cells compared with the NSAID, indomethacin. These findings demonstrate that in situ gelling, liquid formulations, loaded with a combination of curcumin and resveratrol in the form of solid dispersions, show potential as gastroretentive delivery systems for local and systemic effects.

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“…In addition, lecithin may have another important role related to digestion of a thyme‐oil delivery system. In specific, phosphatidylcholine in lecithin creates a monolayer in the GIT and enhances the diffusion of lipophilic compounds through the gastrointestinal mucosa (Kathpalia, Salunkhe, & Juvekar, 2019).…”

Section: Introductionmentioning

confidence: 99%

Design of biopolymer carriers enriched with natural emulsifiers for improved controlled release of thyme essential oil

Volić

Obradović

Djordjević

et al. 2020

Journal of Food Science

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This work aims to characterize a novel system for thyme essential oil delivery based on the combination of natural emulsifiers (soy protein and soy lecithin) and alginate, produced using the extrusion technique. The formulations are optimized concerning alginate and soy protein concentrations (both 1 to 1.5 wt.%), and consequently lecithin amount, in order to achieve spherical beads in the range 2.0 to 2.3 mm and 1.2 to 1.4 mm, wet and dry, respectively. Fourier‐transform infrared analysis was performed, proving that there are interactions between all components. Lecithin–soy protein synergistic combination improved entrapment efficiency of total polyphenols (for nearly 12%) and decreased thymol release in a simulated gastric solution for nearly 35%, in comparison with beads without lecithin. The addition of lecithin enhances the thermal properties of the polysaccharide–protein systems at 50 °C after 3 hr of heating. The mechanical stability of the biopolymer carriers is improved with lecithin addition and the elastic modulus varied from 80.06 to 123.7 kPa, depending on the formulation. Alginate/soy protein/lecithin are effective carriers for the encapsulation, protection, and controlled release of thyme essential oil. Practical Application There is unfortunately growing human resistance to antibiotics. This work offers a novel system for effective protection and controlled release of thyme essential oil in the small intestine. The mechanical and thermal properties of the carrier were estimated as they indicate how the beads will be able to resist stress during their incorporation into food (i.e. cookies‐mixing, baking). The proposed approach offers ‘‘green advantage’’ as arises from all‐natural materials.

show abstract

Formulation of gastroretentive sustained release floating in situ gelling drug delivery system of solubility enhanced curcumin-soy lecithin complex

Cited by 10 publications

References 18 publications

Enhancing Therapeutic Efficacy of Curcumin: Advances in Delivery Systems and Clinical Applications

Enhancing Therapeutic Efficacy of Curcumin: Advances in Delivery Systems and Clinical Applications

Simultaneous Delivery of Curcumin and Resveratrol via In Situ Gelling, Raft-Forming, Gastroretentive Formulations

Design of biopolymer carriers enriched with natural emulsifiers for improved controlled release of thyme essential oil

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