Development and Evaluation of Azelaic Acid Based Ethosomes for Topical Delivery for the Treatment of Acne

Mistry, Anuja Mahesh; Ravikumar, Padmini

doi:10.5530/ijper.50.3.34

Cited by 26 publications

(15 citation statements)

References 1 publication

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“…Ethosomes were prepared by the simple modified "Hot" method [37]. Briefly, TGP (mmol) and PC (mg) were dispersed in phosphate buffer in a water bath adjusted at 50 °C with magnetic stirring at 700 rpm until a colloidal solution was obtained.…”

Section: Methodsmentioning

confidence: 99%

Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Cui

Zhang

et al. 2018

Molecules

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Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 ± 1.56%, PS of 137.9 ± 7.57 nm with PDI of 0.120 ± 0.005, ZP of −0.74 ± 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (Qn) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 ± 8.35 μg/cm2 and 548.11 ± 10.49 μg/cm2, respectively. Qn of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 ± 4.72 μg/cm2 and 307.17 ± 26.36 μg/cm2, respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system.

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Section: Methodsmentioning

confidence: 99%

Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Cui

Zhang

et al. 2018

Molecules

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“…Previously, a zero-order model was reported for the azelaic acid release through ethosomes. 10 In comparison between the MEs and ethosome, it seems that the solubility of azelaic acid in the ethosomes was not complete and that the solubility was a rate-controlling step. The solubility of the azelaic acid in MEs was complete and so diffusion was the rate-limiting step.…”

Section: Azelaic Acid Release Profilesmentioning

confidence: 99%

“…Carrier-based drug delivery systems can reduce these side effects by gradual drug release and by dispersing the drug through the different layers of skin that reduce the local concentration. 10 Therefore, preparation and optimization of ME for follicular delivery of azelaic acid for increasing the efficacy and decreasing the side effects was the main aim of this study.…”

mentioning

confidence: 99%

Development and Evaluation of Azelaic Acid-Loaded Microemulsion for Transfollicular Drug Delivery Through Guinea Pig Skin: A Mechanistic Study

et al. 2020

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Purpose: Azelaic acid is a natural keratolytic, comedolytic, and antibacterial drug that is used to treat acne. The topical application of azelaic acid is associated with problems such as irritation and low permeability. For dissolving, the problem is that microemulsion (ME) is used as a drug carrier. The aim of this study was to increase the azelaic acid affinity in the follicular pathway through ME. Methods: Azelaic acid-loaded MEs were prepared by the water titration method. The properties of the MEs included formulation stability, particle size, drug release profile, thermal behavior of MEs, the diffusion coefficient of the MEs and skin permeability in the non-hairy ear skin and hairy abdominal skin of guinea pig were studied in situ. Results: The MEs demonstrated a mean droplet size between 5 to 150 nm. In the higher ratios of surfactant/co-surfactant, a more extensive ME zone was found. All MEs increased the azelaic acid flux through both hairy and non-hairy skin compared with an aqueous solution of azelaic acid as a control. This effect of the ME was mainly dependent on the droplet diffusion coefficient and hydrodynamic radius. MEs with a higher diffusion coefficient demonstrated higher azelaic acid flux through hairy and non-hairy skin. Drug flux through both skins was affected by the surfactant/co-surfactant ratio in that the higher ratio increased the azelaic acid affinity into the follicular pathway. Conclusion: Finally, the ME with the highest droplet diffusion coefficient and the lowest surfactant/co-surfactant ratio was the best ME for azelaic acid delivery into the follicular pathway.

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“…Azelaic acid gel based ethosomes also known give a larger zone of inhibition than azelaic acid creams and gels in the market [6]. The low azelaic acid solubility of the water becomes an obstacle in the manufacture of topical formulations of azelaic acid.…”

Section: Introductionmentioning

confidence: 99%

Stability Testing of Azelaic Acid Cream Based Ethosome

Apriani

Nurleni

Nugrahani

et al. 2018

Asian J Pharm Clin Res

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Objective: Azelaic acid as an antibacterial to Propionibacterium acnes bacteria in recent years began to develop as an anti-acne using lipid bilayer vesicles to increase the penetration of azelaic acid to reach sebaceous tissue which is located in the dermis of skin where the growth of bacteria P. acnes. The development of azelaic acid in lipid bilayer vesicles is also due to the absorption of azelaic acid from cream preparations by only 4%. Azelaic acid gel based ethosomes also known give a larger zone of inhibition than azelaic acid creams and gels in the market.Methods: Preparation stability test of azelaic acid cream based ethosome was chemical and physical stability. The observed physics stability was organoleptic changes, homogeneity, pH, viscosity, cycling test, and mechanical test (centrifugal test). While chemical stability was performed to know the concentration of azelaic acid in cream to be periodically. Stability test was conducted for 12 weeks and observation every 2 weeks.Result: Physics stability test of that preparations was odorless, white, no change of phase, homogeneous, viscosity, and flow properties constant. While chemical stability test with the determination for 12 weeks to decreased content. However, these content is still included in the range of accuracy (90-110%). Conclusion:Azelaic acid of ethosome cream was physically and chemically stable.

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Development and Evaluation of Azelaic Acid Based Ethosomes for Topical Delivery for the Treatment of Acne

Cited by 26 publications

References 1 publication

Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Development and Evaluation of Azelaic Acid-Loaded Microemulsion for Transfollicular Drug Delivery Through Guinea Pig Skin: A Mechanistic Study

Stability Testing of Azelaic Acid Cream Based Ethosome

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