A novel concept of overcoming the skin barrier using augmented liquid nanocrystals: Box-Behnken optimization, ex vivo and in vivo evaluation

Said, Mayada; Elsayed, Ibrahim; Aboelwafa, Ahmed A.; Elshafeey, Ahmed Hassen

doi:10.1016/j.colsurfb.2018.06.025

Cited by 16 publications

(19 citation statements)

References 40 publications

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“…Newly born male Wistar rats (weighing 70 ± 20 g) were euthanized and the dorsal hair was shaved. 4,5 The fullthickness skin was carefully removed and inspected for any abnormalities, bites, or scratches. The epidermal layers were separated from the underlying subcutaneous fats and stored at -20 °C until use within 3 days.…”

Section: Ex-vivo Drug Permeation Studiesmentioning

confidence: 99%

“…AGM-loaded samples of the optimum invasomes or the aqueous AGM dispersion (containing the equivalent of 5 mg of AMG) were added to the donor compartments while the receptor compartments were loaded with a 50:50 (v/v) mixture of ethanol and phosphate buffer saline (pH 7.4, 10 mL) to maintain sink conditions. 4,5 The stirring rate was set at 100 rpm, and the temperature was adjusted at 32 ± 0.5 °C. [13][14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32] Aliquots (1 mL) of the receptor compartments were collected and immediately replaced…”

Section: Ex-vivo Drug Permeation Studiesmentioning

confidence: 99%

“…4 AGM possesses an intermediate molecular weight (243.3 g/mol) and promising lipophilic properties (log P value, 2.83). In view of the aforementioned, few studies were conducted to enhance the transdermal delivery of AGM via the development of microemulsion gels, 4 liquid nanocrystals 5 and polymeric nanoparticles 6 to bypass the first pass metabolism and enhance drug bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…The withdrawn samples were analyzed using a previously validated HPLC method. 4,5 The drug permeation studies were conducted in triplicates and the results were presented as mean ± SD. The cumulative permeated drug amounts through the skin per unit area (μg/cm 2 ) were plotted against time (h).…”

mentioning

confidence: 99%

“…The AGM concentration in the withdrawn samples was analyzed, at 25 ± 1 °C, using a validated HPLC method at 230 nm with minor modifications. 4,5 HPLC system (Shimadzu, Kyoto, Japan) equipped with an LC-10 AD isocratic pump and a SPD-10 A UV/VIS detector connected to a C-R6A chromatopac integrator was utilized. A reversed phase C18 column (4.6 mm×250 mm, particle size 5 μm; Teknokroma, Barcelona, Spain) was used.…”

mentioning

confidence: 99%

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<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Tawfik¹,

Tadros²,

Mohamed³

et al. 2020

IJN

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Aim Agomelatine (AGM) is the first melatonergic antidepressant. It suffers from low oral bioavailability (<5%) due to extensive hepatic metabolism. The current work aimed to develop an alternative AGM-loaded invasomes to enhance transdermal drug bioavailability. Methodology AGM-loaded invasomes were developed using two drug: lipid ratios (1:10 or 1:7.5), four terpene types (limonene, cineole, fenchone or citral) and two terpene concentrations (0.75% or 1.5%, w/v). They were characterized for drug entrapment efficiency (EE%), particle size (PS), zeta potential (ZP) and drug released percentages after 0.5h (Q 0.5h ) and 8h (Q 8h ). The optimum invasomes (I1, I2 and I4) were evaluated for morphology, drug-crystallinity, and ex-vivo drug flux. The variables influencing sonophoresis of the best achieved invasomal gel system (I2) were optimized including, ultrasound frequency (low, LFU or high, HFU), mode (pulsed or continuous), application period (10 min or 15 min) and duty cycle (50% or 100%). AGM pharmacokinetics were evaluated in rabbits following transdermal application of I2-LFU-C4 system, relative to AGM oral dispersion. Results The superiority of I2 invasomes [comprising AGM and phosphatidylcholine (1:10) and limonene (1.5% w/v)] was statistically revealed with respect to EE% (78.6%), PS (313 nm), ZP (−64 mV), Q 0.5h (30.1%), Q 8h (92%), flux (10.79 µg/cm2/h) and enhancement ratio (4.83). The optimum sonophoresis conditions involved application of LFU in the continuous mode for 15 min at a 100% duty cycle (I2-LFU-C4 system). The latter system showed significantly higher C max , and relative bioavailability (≈ 7.25 folds) and a similar T max (0.5 h). Conclusion I2-LFU-C4 is a promising transdermal system for AGM.

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Section: Ex-vivo Drug Permeation Studiesmentioning

confidence: 99%

Section: Ex-vivo Drug Permeation Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Tawfik¹,

Tadros²,

Mohamed³

et al. 2020

IJN

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Nanocrystals: A Multifaceted Regimen for Dermatological Ailments

Giradkar,

Mhaske,

Shukla

2024

Part & Part Syst Charact

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Skin disorders are the most common apprehension worldwide among different regions of the world. Topical route of administration offers benefits over other routes such as avoidance of first‐pass metabolism, low dose, longer residence time, and absence of off‐target delivery. Skin serves as a mechanical barrier for therapeutic delivery with selectively permeable essential molecules. Considering the structural complexity of skin, delivery of therapeutics at targeted site requires sophisticated method such as nanotechnology‐assisted therapeutic delivery. The roadmap for combinatorial approach of nanotechnology and skin therapeutics has proven significant in clinical and marketed products. Currently, various pharmaceutical aids such as nanocrystal (NCs), nanoparticles, nanoemulsion, nano‐micelles, nano lipidic carriers, and hybrid nanocarriers are currently in market. Among all the other nanocarriers, nanocrystal offers precedence over other nanocarriers due to its facile method of preparation, reproducibility, low excipient concentration, and high therapeutic loading capacity. The recent literature data suggest the breakthrough evolution of NCs in topical therapeutic delivery. The outcome of these interventions envisages the applicability of NCs for delivering molecules with compromised physicochemical characteristics such as solubility, stability, toxicity, and bioavailability concerns.

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Enhanced Dermal Delivery of Flurbiprofen Nanosuspension Based Gel: Development and Ex Vivo Permeation, Pharmacokinetic Evaluations

et al. 2021

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A novel concept of overcoming the skin barrier using augmented liquid nanocrystals: Box-Behnken optimization, ex vivo and in vivo evaluation

Cited by 16 publications

References 40 publications

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Nanocrystals: A Multifaceted Regimen for Dermatological Ailments

Enhanced Dermal Delivery of Flurbiprofen Nanosuspension Based Gel: Development and Ex Vivo Permeation, Pharmacokinetic Evaluations

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