Strategy for the Development of a Thermodynamically Stable Oral Microemulsion

Agatonović-Kuštrin, Snežana; Glass, B. D.; Wisch, M. H.

doi:10.2174/1570163043335126

Cited by 3 publications

(1 citation statement)

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“…These properties are not suitable for topical administration, leading to low permeation, and low bioavailability. Therefore, in this study, the o/w microemulsion was chosen as a promising vehicle due to the fact of its increased solubility as well as thermodynamic stability [35,36]. Furthermore, the microemulsion demonstrated ease of manufacturing and scale-up after optimizing formulations.…”

Section: Discussionmentioning

confidence: 99%

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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Section: Discussionmentioning

confidence: 99%