Optimization of ethosomes for topical thymoquinone delivery for the treatment of skin acne

Kausar, Hina; Mujeeb, Mohd; Ahad, Abdul; Moolakkadath, Thasleem; Aqil, Mohd.; Ahmad, Adil; Akhter, Md. Habban

doi:10.1016/j.jddst.2018.11.016

Cited by 71 publications

(47 citation statements)

References 30 publications

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“…Box–Behnken Design Expert (Design-Expert VR Software Version 10, State-Ease Inc., Minneapolis, MN, USA) software was used for optimization of PLM-loaded GMs and CLs [ 13 , 31 , 32 ]. Based on the design expert software, 17 total runs were generated with 3-level and 3-factor experimental model for optimization of the GMs formulation.…”

Section: Methodsmentioning

confidence: 99%

“…The gel base was prepared as the method described in our earlier work [ 13 ]. 1.0% w / w carbopol 934 was continuously stirred for 2 h using magnetic bead in 10 mL of distilled water separately for both PLM-loaded GMs and CLs.…”

Section: Methodsmentioning

confidence: 99%

“…Ethosomes, when administered, fuse with the cutaneous layer of skin due to the interaction of ethanol with skin lipid. The permeation of drug is enhanced into the epidermal layer of skin owing to elastic deformation process [ 13 ]. However, the alcoholic interaction with lipid molecules of skin leads to decreased transition temperature in stratum corneum.…”

Section: Introductionmentioning

confidence: 99%

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Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

et al. 2021

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Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

et al. 2021

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“…Nevertheless, the topical application of ethosomes is suffers from a low contact time with the skin due to the liquid status. [26][27][28][29][30] The main objective of the present study is primarily to optimize the ethosomes by varying independent variables, such as the cinnamaldehyde, phospholipon 90G, ethanol and propylene glycol concentrations, for the topical delivery of HSYA, icariin, epimedin B and DA. Furthermore, the optimized formulation was incorporated into gel matrices to provide ease of application and increase the retention time on skin as a drug reservoir.…”

Section: Introductionmentioning

confidence: 99%

<p>Topical Delivery of Four Neuroprotective Ingredients by Ethosome-Gel: Synergistic Combination for Treatment of Oxaliplatin-Induced Peripheral Neuropathy</p>

Lin¹,

Lin²,

Sun³

et al. 2020

IJN

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Background: Peripheral neuropathy is a common and painful side effect that occurs in patients with cancer induced by Oxaliplatin (OXL). The neurotoxicity correlates with the damage of dorsal root ganglion (DRG) neurons and Schwann cells (SCs). Hydroxysafflor yellow A (HSYA), icariin, epimedin B and 3, 4-dihydroxybenzoic acid (DA) are the main neuroprotective ingredients identified in Wen-Luo-Tong (WLT), a traditional Chinese medicinal topical compound. The purpose of this study was to prepare and evaluate the efficacy of an ethosomes gel formulation loaded with a combination of HSYA, icariin, epimedin B and DA. However, the low LogP value, poor solubility and macromolecule are several challenges for topical delivery of these drugs. Methods: Ethosomes were prepared by the single-step injection technique. Particle size, entrapment efficiency and in vitro drug deposition studies were determined to select the optimum ethosomes. The optimized ethosomes were further incorporated into carbopol to obtain a gel. The rheological properties, morphology, in vitro drug release, in vitro gel application and skin distribution of the ethosomes gels were studied. A rat model of oxaliplatin-induced neuropathy was established to assess the therapeutic efficacy of the ethosomes gel. Results: Seventy percent (v/v) ethanol, cinnamaldehyde and Phospholipon 90G were employed to develop ethosomes a carrier system. This system had a high entrapment efficiency, carried large amounts of HSYA, epimedin B, DA and icarrin, and penetrated deep into the epidermis and dermis. The optimized ethosomes had the maximum deposition of icariin, HSYA, epimedin B and relative higher amount of DA in epidermis (2.00±0.13 µg/cm 2 , 5.72 ±0.75 µg/cm 2 , 1.97±0.27 µg/cm 2 and 9.25±1.21 µg/cm 2 , respectively). 0.5% carbopol 980 was selected to develop the ethosomes gel with desirable viscoelasticity and spreadability, which was suitable for topical application. The mechanical allodynia and hyperalgesia induced by OXL in rats were significantly reduced after the new ethosomes gel was applied to rats compared to model group. Conclusion: Based on our findings, the ethosomes gel delivery system provided a new formulation for the topical delivery of HSYA, icariin, epimedin B and DA to counteract OXL-induced peripheral neuropathy.

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“…12 Thymoquinone is the chief compound of the aqueous extract of NS, constituting about 72.94% of the weight of its oil. 13 This herb has been reported to have frequent pharmacological properties such as attenuation of glucose, lipid, and hypertension, protection of kidney, and hepatic tissues, and antimicrobial effects owing to its antioxidant, anti-inflammatory effects. 14 Daba et al described the antioxidant effects of NS against liver toxicity induced by cisplatin.…”

Section: Introductionmentioning

confidence: 99%

Administration of Thymoquinone Offer a Protective Effect through the Apoptogenic and Antioxidant Pathway in Acute Liver Failure induced by Taxol

Salahshoor

Roshankhah

Jalili

et al. 2020

J. Contemp. Med. Sci.

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Objectives Due to the increasing use of chemotherapy drug and herbs in medicine, this study was designed to assess the effects of Thymoquinone and Taxol on apoptogenic, oxidative and histomorphometric changes in liver. Methods Sixty-four male rats were assigned to 8 groups including control groups (normal group and Taxol (20 mg/kg group), Thymoquinone groups (4.5, 9, 18 mg/kg) and Taxol + Thymoquinone (TT) treated groups. All experimental groups were treated intraperitoneally daily for two weeks. The relative expression level of apoptotic genes and hepatocyte apoptotic index were analyses. Also, Nitrite oxide (NO), lipid peroxidation (LP), total antioxidant capacity (TAC), hepatic enzymes and histomorphometric parameters were evaluated. Results In the Taxol control group (TCG) all parameters investigated in this study significantly increase except TAC level, which was decreased in compared to the normal control group (NCG) (P < 0.01). Additionally, all evaluated parameters were reduced in Thymoquinone and TT groups, except TAC level (which was increased) as compared to the TCG (P < 0.01). Conclusion Our results discovered that Thymoquinone successfully moderate liver injury induced by Taxol through the activation of antioxidant pathways, reduce the apoptogenic and the regeneration of histopathological alterations.

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Optimization of ethosomes for topical thymoquinone delivery for the treatment of skin acne

Cited by 71 publications

References 30 publications

Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

<p>Topical Delivery of Four Neuroprotective Ingredients by Ethosome-Gel: Synergistic Combination for Treatment of Oxaliplatin-Induced Peripheral Neuropathy</p>

Administration of Thymoquinone Offer a Protective Effect through the Apoptogenic and Antioxidant Pathway in Acute Liver Failure induced by Taxol

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