Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications

Theochari, Ioanna; Ilić, Tanja; Nicolic, Ines; Dobričić, Vladimir; Tenchiou, Alia; Papahatjis, Demetris P.; Savić, Snežana; Xenakis, Aristotelis; Papadimitriou, Vassiliki; Pletsa, Vasiliki

doi:10.3390/biomimetics6010010

Cited by 3 publications

(2 citation statements)

References 60 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Several carriers for improving the safety and efficacy of IMQ have been developed, such as complexes, micelles, liposomes, and nanostructured vehicles [ 7 , 8 , 12 ]. Among various skin delivery systems, nano- and microemulsion (ME) systems have gained recent popularity for their efficacies in delivering different active substances [ 1 , 13 , 14 , 15 , 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Phospholipid-Based Microemulsions for Cutaneous Imiquimod Delivery

et al. 2022

View full text Add to dashboard Cite

Imiquimod (IMQ) is a potent immune response modifier with antiviral and antitumor properties. IMQ’s low aqueous solubility and unsatisfactory cutaneous permeability limit its formulation into effective dosage forms. This work aimed to develop IMQ-loaded microemulsions (MEs) based on phospholipids and oleic acid to improve IMQ penetration into the epidermis. A pseudo-ternary phase diagram was constructed, and the microstructure of the formulations was examined by measuring the conductivity values. Selected MEs were characterized and studied for their ability to deliver IMQ into and through ex vivo human skin. ME1 with 1% IMQ (bicontinuous ME with Bingham rheology) delivered similar IMQ quantities to the human epidermis ex vivo as the commercial product while having a 5-fold lower IMQ dose. IMQ was not detected in the acceptor phase after the permeation experiment, suggesting a lower systemic absorption risk than the established product. Infrared spectroscopy of the stratum corneum revealed less ordered and less tightly packed lipids after ME1 application. The ME1-induced barrier disruption recovered within less than 5 h after the formulation removal, as detected by transepidermal water loss measurements. In conclusion, our findings demonstrate that phospholipid and oleic acid-based MEs could become a promising alternative for topical IMQ administration.

show abstract

Section: Introductionmentioning

confidence: 99%

Phospholipid-Based Microemulsions for Cutaneous Imiquimod Delivery

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Microemulsions (MEs) have been widely used as drug delivery systems owing to their advantages of enhanced permeation, improved drug solubility, and easy preparation (El Maghraby, 2012 ; Park et al, 2021 ; Theochari et al, 2021 ). However, the low viscosity of MEs makes topical administration difficult and inconvenient for patients (Heuschkel et al, 2008 ; Zhu et al, 2009 ; Scomoroscenco et al, 2021 ).…”

Section: Introductionmentioning

confidence: 99%

O/W microemulsion droplets diffuse through hydrogel network to achieve enhanced transdermal drug delivery

et al. 2021

View full text Add to dashboard Cite

To overcome the poor water solubility of total flavones of Arisaematis rhizoma , microemulsions (MEs) can be used as a carrier for transdermal administration to promote their solubilization and skin permeability. Here, we investigated the physical compatibility of MEs in hydrogels and their skin permeation-enhancing effects. Transparency of microemulsion-based hydrogels (MBGs) was analyzed to evaluate ME compatibility with different hydrogel matrices. Transmission electron microscopy (TEM) and Fourier transform infrared (FTIR) spectroscopy were used to explore the microstructures of MBGs and ME–hydrogel combinations. Uniform and transparent MBG was obtained by adding 1% sodium hyaluronate (SH) to the optimized ME. MBG prepared with SH as a matrix expressed pseudoplastic-fluid and shear-thinning characteristics, making it easy to apply in clinical settings. No new FTIR peak occurred in the MBG compared with ME and hydrogel matrix, indicating a physical combination of ME and the polymer network gel. Nanoscale droplets of ME migrated in the gel network, and the migration capacity and in vitro transdermal permeation flux negatively correlated with SH concentration in the gel system. In conclusion, in MBGs, ME can keep nanoscale droplets migrating in the hydrogel network, thereby enhancing transdermal drug delivery.

show abstract

Pain Management with Topical Aceclofenac Nanosuspension In-Vitro/In- Vivo and Proof of Concept Studies

Nagpal

Kumari

Saini

et al. 2022

CDTH

View full text Add to dashboard Cite

Introduction: Pain is one of the most common medical conditions and affects more than diabetes, heart disease, and cancer combined. Current pain treatments mainly rely on NSAIDs analgesics and remain unsatisfactory. Due to associated adverse effects such as gastrointestinal ulcers and bleeding and low solubility limits its uses. Objective: The present research focus on advance in the field of pain treatment by topical delivery of NSAIDs (aceclofenac) drugs via enhancing its solubility and diminishing related side effects. Materials and Methods: ACE-nanosuspension (ACE-NS) prepared by anti-solvent precipitation technique was characterized for particle size, PDI, zeta-potential, total drug content, DSC, FTIR, P-XRD and FESEM. Further spreadabilty, ex-vivo occlusivity, in-vitro release, ex-vivo skin permeation and retention and stability studies were performed. Dermal irritation and histopathological examinations were conducted in accordance to OECD guidelines. Proof of concept studies were accomplished using radiant tail flick and paw-licking animal model. Results: ACE-NS showed particle size of 148 ±15 nm with PDI: 0.170, zeta potential: 21.2 mV and total drug content of 86±0.23% respectively. DSC, FT-IR, P-XRD and FESEM studies revealed the thermal behavior, compatibility, solid state characterization and morphology of ACE-NS. ACE-NS loaded ointment showed a spreadability ratio of 0.23 and a drug content of 84±1.15%. In-vitro release of ACE from nano-ACE-ointment (88.07%) was higher than marketed formulation (70.55%) and free drug ointment (70.45%) after 24 hours. Release profile of nano-ACE-ointment fitted best for Higuchi model with r2 = 0.94 and n = 0.45 and its permeation flux was 9.2312 ± 0.8430 mg/cm2/h, which was significantly higher (p ≤0.05) than ACE marketed gel (2.6158 ± 0.4352 mg/cm2/h). Cutaneous irritation and histological studies revealed no inflammatory skin lesions post treatment with ACE-NS. Furthermore, ACE-NS-ointment showed better analgesic effect than marketed formulation in both radiant tail flick model (2.87 times) and paw-licking (2.73 times) animal model. Conclusion: Studies highlighted the potential of topical nano-ACE-ointment for pain management.

show abstract

Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications

Cited by 3 publications

References 60 publications

Phospholipid-Based Microemulsions for Cutaneous Imiquimod Delivery

Phospholipid-Based Microemulsions for Cutaneous Imiquimod Delivery

O/W microemulsion droplets diffuse through hydrogel network to achieve enhanced transdermal drug delivery

Pain Management with Topical Aceclofenac Nanosuspension In-Vitro/In- Vivo and Proof of Concept Studies

Contact Info

Product

Resources

About