Ascorbic acid derivative-loaded modified aspasomes: formulation,
            <i>in vitro, ex vivo</i>
            and clinical evaluation for melasma treatment

Aboul-Einien, Mona Hassan; Kandil, Soha M; Abdou, Ebtsam M; Diab, Heba; Zaki, Marwa

doi:10.1080/08982104.2019.1585448

Cited by 40 publications

(24 citation statements)

References 45 publications

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“…This effect was due to the presence of 6-AAP in the lipid bilayer which maintained its intrinsic property of skin whitening agent after self-assembling into the aspasomes. [9] This property, combined to the capability…”

Section: Chemmedchemmentioning

confidence: 99%

“…Moreover, its intrinsic antioxidant properties allow the synthesis of nanocarriers which results therapeutic per se and may potentiate the efficacy of payloads. [9] These features make aspasomes proper nanocarriers for drug delivery in several inflammatory diseases that are strongly correlated to an increased production of reactive oxygen species (ROS). [7,10] Based on this evidence, the aim of this work was the synthesis of aspasomes to co-delivery anti-inflammatory (naproxen) and antioxidant (idebenone) drugs for the topical treatment of cutaneous inflammation.…”

Section: Introductionmentioning

confidence: 99%

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Multidrug Idebenone/Naproxen Co‐loaded Aspasomes for Significant in vivo Anti‐inflammatory Activity

et al. 2022

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The use of proper nanocarriers for dermal and transdermal delivery of anti-inflammatory drugs recently gained several attentions in the scientific community because they pass intact and accumulate payloads in the deepest layers of skin tissue. Ascorbyl palmitate-based vesicles (aspasomes) can be considered a promising nanocarrier for dermal and transdermal delivery due to their skin whitening properties and suitable delivery of payloads through the skin. The aim of this study was the synthesis of multidrug Idebenone/naproxen co-loaded aspasomes for the development of an effective anti-inflamma-tory nanomedicine. Aspasomes had suitable physicochemical properties and were safe in vivo if topically applied on human healthy volunteers. Idebenone/naproxen co-loaded aspasomes demonstrated an increased therapeutic efficacy of payloads compared to the commercially available Naprosyn® gel, with a rapid decrease of chemical-induced erythema on human volunteers. These promising results strongly suggested a potential application of Idebenone/naproxen multidrug aspasomes for the development of an effective skin anti-inflammatory therapy.

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Section: Chemmedchemmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Multidrug Idebenone/Naproxen Co‐loaded Aspasomes for Significant in vivo Anti‐inflammatory Activity

et al. 2022

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“…In addition to THD ascorbate, a recent research study utilized magnesium ascorbyl phosphate (MAP), a derivative of ascorbic acid, within an aspasome vesicular system for delivery and found that 35% of melasma patients had an excellent response, proving superior to 15% trichloroacetic acid chemical peeling without the side effects, 24 suggesting that ascorbic acid, delivered appropriately, may be more efficacious and tolerable than chemical peeling.…”

Section: Discussionmentioning

confidence: 99%

Effective lightening of facial melasma during the summer with a dual regimen: A prospective, open‐label, evaluator‐blinded study

Kelm

Zahr²,

Kononov³

et al. 2020

J of Cosmetic Dermatology

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Background Melasma is a chronic pigmentary condition that can have significant negative effects on quality of life. Vitamin C can be effective in the treatment melasma, but its delivery often proves to be challenging due to instability of the drug and subsequent cutaneous irritation at higher concentrations. Aim In this prospective, open‐label, evaluator‐blinded study, we aimed to assess the efficacy and tolerability of twice‐daily application of a novel, highly potent, non‐irritating 30% tetrahexyldecyl (THD) ascorbate serum in combination with 100% mineral‐based sunscreen in the treatment of melasma during the summer months. Patients/Methods Ten female subjects of ages ranging from 18 to 60 years underwent twice‐daily application of 30% THD ascorbate serum in combination with an anti‐aging 100% mineral tinted broad‐spectrum protection SPF 45 sunscreen moisturizer for 12 weeks during the summer months (July to September). Two blinded evaluators scored baseline and post‐treatment photographs using the Griffiths’ 10‐point scale and global aesthetic improvement scale. Results All subjects showed an improvement in hyperpigmentation with an average improvement of 33.7%. Seventy percent of subjects showed an improvement in skin tone evenness (redness), and among those subjects, the average improvement was 33.3%. The median global aesthetic improvement score was 2.0 (very much improved). Conclusion Our study demonstrated efficacy and safety in treating the pigmentary as well as vascular components of melasma with a novel 30% THD ascorbate serum and a purely mineral‐based tinted moisturizing sunscreen.

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“…Higher EH amounts resulted in higher EE% at constant PC: CA ratio and TMC concentration. It was explained previously that increasing the drug concentration in the hydration medium could impart more driving force for the drug to be encapsulated into the vesicles resulting in higher EE% [39,40]. Unlike other factors, increasing TMC concentration resulted in lower EE%, which may be related to increased viscosity of the hydration medium resulting in hindering encapsulation of more drugs [41].…”

Section: Effect Of Different Factors On Dependent Variablesmentioning

confidence: 99%

Assessment of Nasal-Brain-Targeting Efficiency of New Developed Mucoadhesive Emulsomes Encapsulating an Anti-Migraine Drug for Effective Treatment of One of the Major Psychiatric Disorders Symptoms

et al. 2022

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Migraine is one of the major symptoms of many psychiatric and mental disorders like depression and anxiety. Eletriptan Hydrobromide (EH) is a well-tolerated drug in migraine treatment, but suffers from low oral bioavailability and low brain targeting after oral delivery. New nasal mucoadhesive EH-emulsomes development could be a new means to direct the drug from the nose-to-brain to achieve rapid onset of action and high drug concentration in the brain for acute migraine treatment. Eletriptan mucoadhesive emulsomes formulations were prepared using thin-film hydration method and 23 full factorial design was adopted to study different formulation factors’ effect on the emulsomes characters. The emulsomes were characterized for entrapment efficiency (EE%), zeta potential (ZP), particle size (PS), morphology, and ex-vivo permeation through the nasal mucosa. The selected formula was evaluated in mice for its in-vivo bio-distribution in comparison with EH intranasal and intravenous solutions. Drug targeting efficacy (DTE%) and nose-to-brain direct transport percentage (DTP%) were calculated. The optimization formulation showed a nanoparticle size of 177.01 nm, EE 79.44%, and ZP = 32.12 ± 3.28 mV. In addition, in-vitro permeability studies revealed enhanced drug permeability with suitable mean residence time up to 120 ± 13 min. EH-emulsomes were stable under different storage conditions for three months. In vivo examination and pharmacokinetic drug targeting parameters revealed EH transport to the CNS after EH nanoparticle nasal administration. Histopathology study showed no ciliotoxic effect on the nasal mucosa. From the results, it can be confirmed that the emulsomes formulation of EH proved safe direct nose-to-brain transport of EH after nasal administration of EH emulsomes.

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Ascorbic acid derivative-loaded modified aspasomes: formulation, in vitro, ex vivo and clinical evaluation for melasma treatment

Cited by 40 publications

References 45 publications

Multidrug Idebenone/Naproxen Co‐loaded Aspasomes for Significant in vivo Anti‐inflammatory Activity

Multidrug Idebenone/Naproxen Co‐loaded Aspasomes for Significant in vivo Anti‐inflammatory Activity

Effective lightening of facial melasma during the summer with a dual regimen: A prospective, open‐label, evaluator‐blinded study

Assessment of Nasal-Brain-Targeting Efficiency of New Developed Mucoadhesive Emulsomes Encapsulating an Anti-Migraine Drug for Effective Treatment of One of the Major Psychiatric Disorders Symptoms

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