Topical Nano and Microemulsions for Skin Delivery

Nastiti, Christofori Maria Ratna Rini; Ponto, Thellie; Abd, Eman; Grice, Jeffrey E.; Benson, Heather A. E.; Roberts, Michael S.

doi:10.3390/pharmaceutics9040037

Cited by 285 publications

(200 citation statements)

References 98 publications

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“…The formulation of vismodegib into a stable colloidal vehicle may be of crucial importance in order to achieve increased skin penetration and a controlled drug release. Micro‐emulsions are fairly simple systems that allow the solubility of hydrophobic molecules, such as vismodegib, increasing their bioavailability and thus holding promise for topical drug delivery as they may facilitate increased drug uptake through the skin . The present in vitro study aims to demonstrate the potential of combining the use of AFL‐assisted delivery and a novel micro‐emulsion drug formulation for enhancing the topical delivery of vismodegib.…”

Section: Introductionmentioning

confidence: 99%

Topical delivery of vismodegib using ablative fractional laser and micro‐emulsion formulation in vitro

et al. 2018

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Section: Introductionmentioning

confidence: 99%

Topical delivery of vismodegib using ablative fractional laser and micro‐emulsion formulation in vitro

et al. 2018

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“…Among the 24 formulations additionally selected, three kinds of formulations (F2, F10 and F18) were eventually selected, although they had relatively small amounts of surfactants and co-surfactant. Previous studies have reported that IPM as oil has been widely used for topical medications as well as cosmetic applications [40,41]. In this study, IPM experimentally demonstrated the highest CoQ10 solubility, approximately 4 fold higher than OA and Labrafil M1944, and is widely used in preparing microemulsions [42,43].…”

Section: Discussionmentioning

confidence: 66%

Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration

et al. 2020

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The aim of this study was to develop a coenzyme Q10 (CoQ10) microemulsion system with improved solubility, penetration, and wound healing efficacy. Based on the pseudo-ternary diagram, microemulsions containing isopropyl myristate (IPM), Cremophor EL ® , and Transcutol ® HP were selected and confirmed to be nanosized (<20 nm) and thermodynamically stable based on the dilution and thermodynamic stability tests. The CoQ10-loaded microemulsion with a surfactant/co-surfactant (S/CoS) ratio of 2:1 (w/w %) demonstrated a higher permeation efficacy compared to microemulsions with S/CoS ratio of 3:1 or 4:1 (w/w %). Additionally, the CoQ10-loaded microemulsion with an S/CoS ratio of 2:1 demonstrated a relatively rapid wound healing effect in keratinocytes and fibroblasts. Overall, these data suggest that a microemulsion based on IPM, Cremophor EL ® , and Transcutol ® HP could be an effective vehicle for the topical administration of CoQ10 and could be utilized for the application of other therapeutic agents that have difficulty in penetrating the skin.Pharmaceutics 2020, 12, 332 2 of 15 minimal side effects (e.g., systemic toxicity) compared to oral drug delivery [10]. However, due to the skin barrier, the penetration of therapeutics across the stratum corneum remains challenging. Especially, general therapeutic agents demonstrate a considerably low penetration efficacy unlike moderately lipophilic substances (molecular weight < 500 Da and log P of 1 to 4) [11]. Hence, these therapeutic agents require skin penetration enhancement strategies such as physical permeation enhancement (e.g., iontophoresis and microneedle) [12], chemical permeation enhancement (e.g., chemical enhancer and ionic liquid) [13], and nanocarrier-based permeation enhancement (e.g., microemulsion and transfersomes) [14,15].Microemulsions are thermodynamically stable vehicles that contain oil and water stabilized by amphiphiles such as surfactants and co-surfactants [16]. Such microemulsions are transparent, isotropic colloidal systems with a droplet size less than 100 nm and have been widely studied since microemulsions were defined [17,18]. As previously reported, compared with conventional emulsions, these systems demonstrate enhanced transdermal permeation owing to their smaller size and disruption of the stratum corneum [19,20]. In addition, these systems are conventionally advantageous due to the fact of their pharmaceutical stability, easy fabrication, and scale-up [21]. Therefore, microemulsions are preferred in dermatological cosmetic applications over the past decades.Coenzyme Q10 (CoQ10, Mw = 863.3 g/mol) is a quinone with side chains of 10 isoprenoids [22]. CoQ10 generally plays an important role as an electron carrier in the oxidative phosphorylation process of the mitochondria while acting as an antioxidant outside the mitochondria [23]. Recently, CoQ10 has gained attention for its therapeutic application for several disorders including cardiovascular diseases, diabetes mellitus, and even cancer [24]. For example, previous literature has ...

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“…21 Microemulsions can be used as nano-structured delivery vehicles for poorly water-soluble drugs that have better water solubility, higher bioavailability, and greater drug skin permeation than conventional formulations. 22 In our study, an O/W microemulsion was observed in a phase diagram at a region of 18-22% AITC (or oil), 47-52% surfactant/cosurfactants (Tween 80:Tween 20:Span 80 = 33:2:1), and 28-32% water. The AITC-encapsulated O/W microemulsions were then subsequently used for preparation of nanoparticles by using a complex coacervation technique involving the formation of a complex coacervate on the surface of microemulsions through electrostatic interaction between positively charged alkali-treated gelatin (ATG) and a negative sulfate group of -carrageenan.…”

Section: Characterization and Stability Of Nanoparticlesmentioning

confidence: 59%

“…Both O/W and W/O microemulsions are transparent, isotropic, and thermodynamically stable systems that are spontaneously formed in nano‐sized droplets by mixing a suitable proportion of oil, water, and surfactant, or in combination of co‐surfactants . Microemulsions can be used as nano‐structured delivery vehicles for poorly water‐soluble drugs that have better water solubility, higher bioavailability, and greater drug skin permeation than conventional formulations . In our study, an O/W microemulsion was observed in a phase diagram at a region of 18–22% AITC (or oil), 47–52% surfactant/cosurfactants (Tween 80:Tween 20:Span 80 = 33:2:1), and 28–32% water.…”

Section: Resultsmentioning

confidence: 99%

Preparation of allyl isothiocyanate nanoparticles, their anti‐inflammatory activity towards RAW 264.7 macrophage cells and anti‐proliferative effect on HT1376 bladder cancer cells

et al. 2019

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BACKGROUND Allyl isothiocyanate (AITC), a volatile and water‐insoluble compound present in several cruciferous vegetables, has been shown to possess several biological qualities such as anti‐bacterial, anti‐fungal, and anti‐cancer activity. In this study, water‐soluble allyl isothiocyanate nanoparticles (AITC‐NPs) were prepared by oil dispersed in water (O/W) microemulsion and complex coacervation techniques and evaluated for their anti‐inflammatory activity towards macrophage cell RAW 264.7 and anti‐cancer effect on human bladder cancer cell HT1376. RESULTS The AITC‐NPs with a particle size of 9.4 nm were stable during heating up to 110 °C or three freeze‐thawing cycles. No significant cytotoxicity was shown on Caco‐2 and intestine epithelial IEC‐6 cells at AITC‐NP doses ranging from 0.25 to 2 g L−1 (8.75–70 mg L−1 AITC). However, at 2 g L−1 dosage, AITC‐NPs could inhibit the growth of human bladder cancer cells HT1376 by 90%, while their low dosage at 0.25 g L−1 could inhibit migration ability by 83.7, 71.3, 58.4 and 31.4% after 4, 8, 12, and 24 h of incubation, respectively. Compared to AITC and NPs, AITC‐NPs showed a better inhibition on lipopolysaccharide (LPS)‐induced TNF‐α, IL‐6, NO and iNOS production in RAW 264.7 macrophage cells. CONCLUSION The results demonstrate the potential of AITC‐NPs as therapeutic agents for the treatment of bladder cancer and the enhancement of immune function. © 2018 Society of Chemical Industry

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Topical Nano and Microemulsions for Skin Delivery

Cited by 285 publications

References 98 publications

Topical delivery of vismodegib using ablative fractional laser and micro‐emulsion formulation in vitro

Topical delivery of vismodegib using ablative fractional laser and micro‐emulsion formulation in vitro

Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration

Preparation of allyl isothiocyanate nanoparticles, their anti‐inflammatory activity towards RAW 264.7 macrophage cells and anti‐proliferative effect on HT1376 bladder cancer cells

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