Transdermal Delivery of Carvedilol Containing Glycyrrhizin and Chitosan as Permeation Enhancers: Biochemical, Biophysical, Microscopic and Pharmacodynamic Evaluation

Sapra, Bharti; Jain, Subheet Kumar; Tiwary, Ashok K.

doi:10.1080/10717540802327047

Cited by 35 publications

(22 citation statements)

References 25 publications

(19 reference statements)

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“…The effect of GA and chitosan on the transdermal delivery of carvediol was also studied (Sapra et al, 2008). It has been found that the solubility of carvediol in solution containing 0.75% GA increases by a factor of 59 compared to the buffer solution.…”

Section: Self-association Of Ga and Its Use In Drug Deliverymentioning

confidence: 99%

“…It provides broad prospects of applying of glycyrrhizic acid as a multifunctional DDS. It was also established that GA enhance absorption effects of the variety of drugs (Kong et al, 2017;Sapra et al, 2008;Radwant and Aboul-Enein, 2002;Chen et al, 2009;Chakotiya et al, 2016). In view of the fact that the movement of small drug molecules through gastrointestinal epithelium is regulated by the distension and constriction of the tight junctions, observed effects could be connected with the ability of glycyrrhizin to enhance the penetration of molecules into the cells.…”

Section: Permeability Enhancement and Membrane-modifying Activitymentioning

confidence: 99%

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Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Selyutina

Polyakov

2019

International Journal of Pharmaceutics

156

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A B S T R A C TGlycyrrhizic acid is the main active component of Licorice root which has been known in traditional Chinese and Japanese medicine since ancient times. In these cultures glycyrrhizic acid (GA) is one of the most frequently used drugs. However, only in 21-st century a novel unusual property of the GA to enhance the activity of other drugs has been discovered. The review describes briefly the experimental evidences of wide spectrum of own biological activities of glycyrrhizic acid as well as discusses the possible mechanisms of the ability of GA to enhance the activity of other drugs. We have shown that due to its amphiphilic nature GA is able to form self-associates in aqueous and non-aqueous media, as well as water soluble complexes with a wide range of lipophilic drugs. The main purpose of our review is to focus reader's attention on physicochemical studies of the molecular mechanisms of GA activity as a drug delivery system (DDS). In our opinion, the most intriguing feature of glycyrrhizic acid which might be the key factor in its therapeutic activity is the ability of GA to incorporate into the lipid bilayer and to increase the membrane fluidity and permeability. The ability of biomolecules and their aggregates to change the properties of cell membranes is of great significance, from both fundamental and practical points of view. monstrated the ability of GA to interact with cell membrane and to https://doi.

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Section: Self-association Of Ga and Its Use In Drug Deliverymentioning

confidence: 99%

Section: Permeability Enhancement and Membrane-modifying Activitymentioning

confidence: 99%

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Selyutina

Polyakov

2019

International Journal of Pharmaceutics

156

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“…GA has been reported to have an influence on drug permeation in the skin (Sapra et al, 2008), and it has also been studied as a paclitaxel micelle carrier in our research group (Yang et al, 2015). In the present study, GA's solubilization property improved the solubility of POD and the formulation could reach a concentration of 5 mg/mL.…”

Section: Discussionmentioning

confidence: 53%

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

et al. 2016

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Context: As the first-line agent for genital warts, podophyllotoxin (POD) could induce extensively skin burning, itching, and erythema. Meanwhile, as a common anti-inflammatory agent, glycyrrhizic acid (GA), also has amphipathic and solubilizing properties, indicating that it might be a promising drug carrier.Objective: The objective of this study is to formulate and characterize the POD-loaded GA micelles preparation and to evaluate its drug release characteristics and anti-inflammatory properties. Materials and methods:The novel micelles preparation was prepared by ultrasonic dispersion method and characterized using different scanning calorimetries, dynamic light scattering, and transmission electron microscopies. Subsequently, its encapsulation efficiency (EE), drugloading content (LC), in vitro skin permeation, in vivo drug retention, and distribution of POD were detected. The anti-inflammatory effect of the preparation was reflected by HE staining and immunohistochemistry in the rat skin.Results: The POD-loaded GA micelles formed spherical shapes (approximately 10 nm) with an EE of 78.53 ± 2.17% and a LC of 7.293 ± 0.42%. Meaningfully, unlike the extensive distribution of the POD tincture throughout the skin tissue, POD released from the POD-loaded GA micelles mainly located in the epidermis and could maintain steady skin retention for 12 h. Moreover, the POD-loaded GA micelles induced less leukocyte infiltration and inflammatory factors (IL-6 and TNF-a) expression when compared with the POD tincture. Discussion and conclusion: Our results suggested that the POD-loaded GA micelles could achieve a higher POD distribution in the epidermal layer as well as a lighter skin inflammation. This new POD delivery system might be a potential and promising candidate for genital warts and deserved further researches.

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“…Permeation enhancement effect of chitosan has been reported by Sapra et al (2008) in the transdermal delivery of carvedilol.…”

Section: Chitosan and Its Derivativesmentioning

confidence: 99%

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

2013

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The highly organized structure of the stratum corneum provides an effective barrier to the drug delivery into or across the skin. To overcome this barrier function, penetration enhancers are always used in the transdermal and dermal drug delivery systems. However, the conventional chemical enhancers are often limited by their inability to delivery large and hydrophilic molecules, and few to date have been routinely incorporated into the transdermal formulations due to their incompatibility and local irritation issues. Therefore, there has been a search for the compounds that exhibit broad enhancing activity for more drugs without producing much irritation. More recently, the use of biomaterials has emerged as a novel method to increase the skin permeability. In this paper, we present an overview of the investigations on the feasibility and application of biomaterials as penetration enhancers for transdermal or dermal drug delivery systems.

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Transdermal Delivery of Carvedilol Containing Glycyrrhizin and Chitosan as Permeation Enhancers: Biochemical, Biophysical, Microscopic and Pharmacodynamic Evaluation

Cited by 35 publications

References 25 publications

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

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