Editorial

4 pages, 221 KiB

Open AccessEditorial

New Horizons in Dermal and Transdermal Drug Delivery Systems

by Joana Marto and Sandra Simões

Pharmaceuticals 2023, 16(12), 1654; https://doi.org/10.3390/ph16121654 - 28 Nov 2023

Viewed by 738

Dermal and transdermal drug delivery represents an important strategy to target drugs towards the site of action or to noninvasively enhance treatment activity, circumventing the hepatic first passage and reducing toxicity [...] Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

Research

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17 pages, 2043 KiB

Open AccessArticle

Assessing the Oxidative State of the Skin by Combining Classical Tape Stripping with ORAC Assay

by Reem M. Alnemari, Jana Brüßler and Cornelia M. Keck

Pharmaceuticals 2022, 15(5), 520; https://doi.org/10.3390/ph15050520 - 23 Apr 2022

Cited by 1 | Viewed by 2401

Abstract

The antioxidant barrier system of the skin acts as the main defence against environmental pro-oxidants. Impaired skin oxidative state is linked to unhealthy conditions such as skin autoimmune diseases and cancer. Thus, the evaluation of the overall oxidative state of the skin plays [...] Read more.

The antioxidant barrier system of the skin acts as the main defence against environmental pro-oxidants. Impaired skin oxidative state is linked to unhealthy conditions such as skin autoimmune diseases and cancer. Thus, the evaluation of the overall oxidative state of the skin plays a key role in further understanding and prevention of these disorders. This study aims to present a novel ex vivo model to evaluate the skin oxidative state by the measurement of its antioxidant capacity (AOC). For this the ORAC assay was combined with classical tape stripping and infrared densitometry to evaluate the oxidative state of the stratum corneum (SC). Outcomes implied the suitability of the used model to determine the intrinsic antioxidant capacity (iAOC) of the skin. The average iAOC of untreated skin was determined as 140 ± 7.4 µM TE. Skin exposure to UV light for 1 h reduced the iAOC by about 17%, and exposure for 2 h decreased the iAOC by about 30%. Treatment with ascorbic acid (AA) increased the iAOC in a dose-dependent manner and reached an almost two-fold iAOC when 20% AA solution was applied on the skin. The application of coenzyme Q10 resulted in an increase in the iAOC at low doses but decreased the iAOC when doses > 1% were applied on the skin. The results show that the combination of classical tape stripping and ORAC assay is a cost-effective and versatile method to evaluate the skin oxidative state and the pro-oxidate and antioxidative effects of topical skin treatments on the iAOC of the skin. Therefore, the model can be considered to be a valuable tool in skin research. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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13 pages, 1780 KiB

Open AccessArticle

Phospholipid-Based Microemulsions for Cutaneous Imiquimod Delivery

by Eleni Panoutsopoulou, Jarmila Zbytovská, Kateřina Vávrová and Georgios Paraskevopoulos

Pharmaceuticals 2022, 15(5), 515; https://doi.org/10.3390/ph15050515 - 22 Apr 2022

Cited by 5 | Viewed by 2153

Abstract

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 [...] Read more.

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. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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22 pages, 14856 KiB

Open AccessArticle

Electrospun Biomimetic Multifunctional Nanofibers Loaded with Ferulic Acid for Enhanced Antimicrobial and Wound-Healing Activities in STZ-Induced Diabetic Rats

by Sneha Anand, Prashant Pandey, Mohammed Yasmin Begum, Kumarappan Chidambaram, Dilip Kumar Arya, Ravi Kr. Gupta, Ruchi Sankhwar, Shweta Jaiswal, Sunita Thakur and Paruvathanahalli Siddalingam Rajinikanth

Pharmaceuticals 2022, 15(3), 302; https://doi.org/10.3390/ph15030302 - 28 Feb 2022

Cited by 32 | Viewed by 3809

Abstract

Diabetic foot ulceration is the most distressing complication of diabetes having no standard therapy. Nanofibers are an emerging and versatile nanotechnology-based drug-delivery system with unique wound-healing properties. This study aimed to prepare and evaluate silk-sericin based hybrid nanofibrous mats for diabetic foot ulcer. [...] Read more.

Diabetic foot ulceration is the most distressing complication of diabetes having no standard therapy. Nanofibers are an emerging and versatile nanotechnology-based drug-delivery system with unique wound-healing properties. This study aimed to prepare and evaluate silk-sericin based hybrid nanofibrous mats for diabetic foot ulcer. The nanofibrous mats were prepared by electrospinning using silk sericin mixed with different proportions of polycaprolactone (PCL) and cellulose acetate (CA) loaded with ferulic acid (FA). The in vitro characterizations, such as surface morphology, mechanical properties, swelling behavior, biodegradability, scanning electron microscopy, and drug release were carried out. The SEM images indicated that nanofibers formed with varied diameters, ranging from 100 to 250 nm, and their tensile strength was found to range from 7 to 15 MPa. In vitro release demonstrated that the nanofibers sustained FA release over an extended time of period. In vitro cytotoxicity showed that the nanofibers possessed a lower cytotoxicity in HaCaT cells. The in vivo wound-healing studies demonstrated an excellent wound-healing efficiency of the nanofibers in diabetic rats. Furthermore, the histopathological studies showed the nanofibers’ ability to restore the skin’s normal structure. Therefore, it was concluded that the prepared silk-sericin-based hybrid nanofibers loaded with FA could be a promising drug-delivery platform for the effective treatment of diabetic foot ulcers. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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17 pages, 2042 KiB

Open AccessArticle

Hesperidin-Loaded Lipid Polymer Hybrid Nanoparticles for Topical Delivery of Bioactive Drugs

by Rajendra Jangde, Gamal Osman Elhassan, Sulekha Khute, Deependra Singh, Manju Singh, Ram Kumar Sahu and Jiyauddin Khan

Pharmaceuticals 2022, 15(2), 211; https://doi.org/10.3390/ph15020211 - 10 Feb 2022

Cited by 17 | Viewed by 3271

Abstract

Hesperidin is a bioflavonoid constituent that among many other biological activities shows significant wound healing properties. However, the bioavailability of hesperidin when applied topically is limited due to its low solubility and systemic absorption, so novel dosage forms are needed to improve its [...] Read more.

Hesperidin is a bioflavonoid constituent that among many other biological activities shows significant wound healing properties. However, the bioavailability of hesperidin when applied topically is limited due to its low solubility and systemic absorption, so novel dosage forms are needed to improve its therapeutic efficacy. The objectives of this study were to develop hesperidin-loaded lipid-polymer hybrid nanoparticles (HLPHNs) to enhance the delivery of hesperidin to endogenous sites in the wound bed and promote the efficacy of hesperidin. HLPHNs were optimized by response surface methodology (RSM) using the Box-Behnken design. HLPHNs were prepared using an emulsion-solvent evaporation method based on a double emulsion of water-in-oil-in-water (w/o/w) followed by freeze-drying to obtain nanoparticles. The prepared formulations were characterized using various evaluation parameters. In addition, the antioxidant activity of HLPHN 4 was investigated in vitro using the DPPH model. Seventeen different HLPHNs were prepared and the HLPHN4 exhibited the best mean particle size distribution, zeta potential, drug release and entrapment efficiency. The values are 91.43 nm, +23 mV, 79.97% and 92.8%, respectively. Transmission electron microscope showed similar spherical morphology as HLPHN4. Differential scanning calorimetry verified the physical stability of the loaded drug in a hybrid system. In vitro release studies showed uniform release of the drug over 24 h. HLPHN4 showed potent antioxidant activity in vitro in the DPPH model. The results of this study suggest that HLPHNs can achieve sustained release of the drug at the wound site and exhibit potent in vitro antioxidant activity. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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14 pages, 4207 KiB

Open AccessArticle

Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers

by Quoc Lam Vu, Chih-Wun Fang, Muhammad Suhail and Pao-Chu Wu

Pharmaceuticals 2021, 14(12), 1233; https://doi.org/10.3390/ph14121233 - 27 Nov 2021

Cited by 8 | Viewed by 2459

Abstract

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using [...] Read more.

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm²·h up to 20.00 μg/cm²·h and 4.90 up to 53.52 μg/cm², respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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Review

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25 pages, 1597 KiB

Open AccessReview

Cannabis-Based Products for the Treatment of Skin Inflammatory Diseases: A Timely Review

by Ana M. Martins, Ana L. Gomes, Inês Vilas Boas, Joana Marto and Helena M. Ribeiro

Pharmaceuticals 2022, 15(2), 210; https://doi.org/10.3390/ph15020210 - 09 Feb 2022

Cited by 23 | Viewed by 7985 | Correction

Abstract

The use of natural products in dermatology is increasingly being pursued due to sustainability and ecological issues, and as a possible way to improve the therapeutic outcome of chronic skin diseases, relieving the burden for both patients and healthcare systems. The legalization of [...] Read more.

The use of natural products in dermatology is increasingly being pursued due to sustainability and ecological issues, and as a possible way to improve the therapeutic outcome of chronic skin diseases, relieving the burden for both patients and healthcare systems. The legalization of cannabis by a growing number of countries has opened the way for researching the use of cannabinoids in therapeutic topical formulations. Cannabinoids are a diverse class of pharmacologically active compounds produced by Cannabis sativa (phytocannabinoids) and similar molecules (endocannabinoids, synthetic cannabinoids). Humans possess an endocannabinoid system involved in the regulation of several physiological processes, which includes naturally-produced endocannabinoids, and proteins involved in their transport, synthesis and degradation. The modulation of the endocannabinoid system is a promising therapeutic target for multiple diseases, including vascular, mental and neurodegenerative disorders. However, due to the complex nature of this system and its crosstalk with other biological systems, the development of novel target drugs is an ongoing challenging task. The discovery of a skin endocannabinoid system and its role in maintaining skin homeostasis, alongside the anti-inflammatory actions of cannabinoids, has raised interest in their use for the treatment of skin inflammatory diseases, which is the focus of this review. Oral treatments are only effective at high doses, having considerable adverse effects; thus, research into plant-based or synthetic cannabinoids that can be incorporated into high-quality, safe topical products for the treatment of inflammatory skin conditions is timely. Previous studies revealed that such products are usually well tolerated and showed promising results for example in the treatment of atopic dermatitis, psoriasis, and contact dermatitis. However, further controlled human clinical trials are needed to fully unravel the potential of these compounds, and the possible side effects associated with their topical use. Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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Other

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1 pages, 203 KiB

Open AccessCorrection

Correction: Martins et al. Cannabis-Based Products for the Treatment of Skin Inflammatory Diseases: A Timely Review. Pharmaceuticals 2022, 15, 210

by Ana M. Martins, Ana L. Gomes, Inês Vilas Boas, Joana Marto and Helena M. Ribeiro

Pharmaceuticals 2022, 15(7), 849; https://doi.org/10.3390/ph15070849 - 11 Jul 2022

Cited by 2 | Viewed by 874

Abstract

The authors would like to make the following corrections about the published paper [...] Full article

(This article belongs to the Special Issue New Horizons in Dermal and Transdermal Drug Delivery Systems)

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