Functional Ingredients in Topical and Transdermal Delivery Systems

A special issue of Scientia Pharmaceutica (ISSN 2218-0532).

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 43201

Special Issue Editors

CBIOS - Research Center for Biosciences and Health Technologies, Lusófona University, Lisboa, Portugal
Interests: transdermal drug delivery; efficacy and safety testing; topical biomaterials; transdermal and cosmetic ingredients; nutrition and skin
Special Issues, Collections and Topics in MDPI journals
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo 05508-900, Brazil
Interests: photoprotection; dermocosmetics; efficacy tests; cutaneous attributes
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Topical and transdermal delivery systems are used to address regional and systemic pathologies and to improve the delivery of dermocosmetic active substances. Their efficacy is highly dependant on their stability and the extension of permeation across the skin of the bioactive compounds, which, in turn, depends on appropriate partition to the stratum corneum and facilitated diffusion through this impermeable layer. Different components of the formulation and technological strategies can beneficially influence this, either by increasing the solubility or stability or by promoting transcutaneous penetration. Innovative ingredients have been introduced to tackle these challenges, and one of the current trends is the use of materials from natural sources or even industrial by-products. Another interesting area is the development of innovative strategies to assess the safety and efficacy of these formulations.

This Special Issue, “Functional Ingredients in Topical and Transdermal Drug Delivery Systems”, will cover a selection of recent research topics and current review articles focusing on efficacious skin delivery systems.

Prof. Dr. Catarina Rosado
Prof. Dr. André Rolim Baby
Guest Editors

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Keywords

  • topical and transdermal formulations
  • ingredients of natural origin
  • efficacy and safety assessment
  • byproduct valorization
  • cosmetic and pharmaceutical product technology

Published Papers (5 papers)

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Research

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8 pages, 900 KiB  
Communication
Preliminary Protocol Development of a HPLC-TBARS-EVSC (Ex Vivo Stratum Corneum) Assay for Skin Research: Application in a Sunscreen System
by Rafael Sauce, Claudinéia Aparecida Sales de Oliveira Pinto, Carmen Ayala-Jara, Zulita Adriana Prieto, Maria Valéria Robles Velasco and André Rolim Baby
Sci. Pharm. 2021, 89(2), 17; https://0-doi-org.brum.beds.ac.uk/10.3390/scipharm89020017 - 27 Apr 2021
Cited by 10 | Viewed by 4940
Abstract
Considering the importance of the cutaneous tissue investigation and the need for the development of new protocols to non-invasively establish the safety and efficacy of dermocosmetics and topical products, we aimed at developing an HPLC-TBARS-EVSC (high performance liquid chromatography–thiobarbituric acid reactive species–ex vivo [...] Read more.
Considering the importance of the cutaneous tissue investigation and the need for the development of new protocols to non-invasively establish the safety and efficacy of dermocosmetics and topical products, we aimed at developing an HPLC-TBARS-EVSC (high performance liquid chromatography–thiobarbituric acid reactive species–ex vivo stratum corneum) assay for the lipid peroxidation measurement on subjects’ stratum corneum (SC) obtained by tape stripping; additionally, we applied the HPLC-TBARS-EVSC assay in an emulsified sunscreen system containing ethylhexyl triazone and bemotrizinol as UV filters. HPLC analysis was performed in isocratic mode with 35% methanol/65% phosphate buffer (pH 7.0) as the mobile phase. The diode detector was set at 532 nm to quantify the malondialdehyde (MDA)-TBA adduct. An ex vivo tape stripping method was applied in 10 volunteers in three pre-defined regions of the volar forearms: the control; the irradiated; and the site containing the sunscreen (2.0 mg·cm−2). Ten adhesive tapes per region were used for SC removal. An exclusive ex vivo protocol to measure SC lipid peroxidation was preliminarily developed with linearity and selectivity. The protocol suggested the use of an artificial irradiation dose (5506 KJ·m−2) to improve the assay response from the SC. The sunscreen system had a significative decrease in SC lipoperoxidative damage compared to the control. Our protocol can aid in the efficacy establishment of anti-UV and antioxidant agents, for instance, in studies that aim at elucidating the level of SC lipid peroxidation and even in carrying out baseline investigations characterizing different ethnicities and genders. Full article
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
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9 pages, 1696 KiB  
Communication
Is the Botryococcus braunii Dry Biomass an Adjuvant for Anti-UVB Topical Formulations?
by Maíra Bueno Ariede, Ana Lucia Morocho-Jácome, Thalita Marcílio Candido, Felipe Rebello Lourenço, Edna Tomiko Myiake Kato, Fabiana Vieira Lima, Catarina Rosado, Maria Valéria Robles Velasco, João Carlos Monteiro de Carvalho and André Rolim Baby
Sci. Pharm. 2020, 88(2), 22; https://0-doi-org.brum.beds.ac.uk/10.3390/scipharm88020022 - 26 Apr 2020
Cited by 6 | Viewed by 4501
Abstract
Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) radiation, such as sunscreens. Research for actives from natural sources is increasing due to the fact that chemical filters could induce adverse events. The microalgae Botryococcus braunii has potential [...] Read more.
Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) radiation, such as sunscreens. Research for actives from natural sources is increasing due to the fact that chemical filters could induce adverse events. The microalgae Botryococcus braunii has potential interest in cosmetic applications. Specialized literature reported that B. braunii aqueous extract induced a reduction in skin dehydration and collagen production and promoted antioxidant activity. This research aimed to produce B. braunii biomass and to investigate its contribution regarding photoprotection. Formulations containing B. braunii dry biomass, with or without UV filters into vehicles composed of an emulsifying polymer or a self-emulsifying base, were evaluated in vitro by means of photoprotective activity and photostability. B. braunii dry biomass did not provide adequate photoprotection efficacy; however, it was observed that the self-emulsifying base promoted better sun protection factor (SPF) in comparison with the emulsifying polymer. Full article
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
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13 pages, 1547 KiB  
Article
Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems
by Fotis Iliopoulos, A. S. M. Monjur Al Hossain, Bruno C. Sil, David J. Moore, Robert A. Lucas and Majella E. Lane
Sci. Pharm. 2020, 88(2), 19; https://0-doi-org.brum.beds.ac.uk/10.3390/scipharm88020019 - 01 Apr 2020
Cited by 9 | Viewed by 12523
Abstract
3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6–7.5% of the applied EA was delivered through the skin over 24 [...] Read more.
3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6–7.5% of the applied EA was delivered through the skin over 24 h. In this work, we designed complex formulations using combinations of solvents that may act synergistically and examined their impact on EA permeation in porcine skin in vitro under finite dose conditions. Binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML) were effective in enhancing skin permeation of EA compared with individual solvents (p < 0.05). Combining PGML with 1,2-hexanediol (HEX) did not result in significantly higher EA permeation compared with the neat solvents (p > 0.05). Addition of the volatile solvent isopropyl alcohol (IPA) to PG solutions also did not improve EA skin delivery compared with neat PG. Ternary solvent systems containing PG:PGML were subsequently prepared by the addition of a lipophilic solvent, either isopropyl myristate (IPM), medium-chain triglycerides (MCT) or isostearyl isostearate (ISIS). The optimum vehicle, PG:PGML:IPM, promoted up to 70.9% skin delivery of EA. The PG:PGML:ISIS vehicles also promoted EA permeation across the skin, but to a significantly lesser extent than the IPM-containing vehicles. No enhancement of EA delivery was noted for the PG:PGML:MCT mixtures. These results will inform the development of targeted formulations for EA in the future. Full article
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
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Review

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17 pages, 3555 KiB  
Review
Contribution of Topical Antioxidants to Maintain Healthy Skin—A Review
by Tércio Elyan Azevedo Martins, Claudinéia Aparecida Sales de Oliveira Pinto, Andressa Costa de Oliveira, Maria Valéria Robles Velasco, Arilmí Rosa Gorriti Guitiérrez, Martha Francisca Cosquillo Rafael, Jossimar Paúl Huamaní Tarazona and Mónica Guadalupe Retuerto-Figueroa
Sci. Pharm. 2020, 88(2), 27; https://0-doi-org.brum.beds.ac.uk/10.3390/scipharm88020027 - 03 Jun 2020
Cited by 19 | Viewed by 9945
Abstract
The skin is constantly exposed to various environmental stresses, in particular to the damage caused by pollution and ultraviolet radiation (UV), and as a consequence, the horny extract can be negatively impacted by the harmful influence of some of its surface components. The [...] Read more.
The skin is constantly exposed to various environmental stresses, in particular to the damage caused by pollution and ultraviolet radiation (UV), and as a consequence, the horny extract can be negatively impacted by the harmful influence of some of its surface components. The mechanisms involved in the degradation processes promoted by UV radiation are driven by the direct absorption of radiation via cellular chromophores, the formation of excited states and the consequent chemical reactions, or even by the photosensitization mechanisms, in which UV light is absorbed by the sensitizers that are excited and their reactions promote the formation of reactive oxygen species (ROS). The mechanisms of polluting agents are not yet fully understood, however, they indicate that one of the main mechanisms involved is oxidative stress by lipid peroxidation, with the ability to promote damage to the composition of sebum, the quality of the stratum corneum and also, promote aging skin. Recent studies demonstrate the potential of antioxidant agents, with an emphasis on products of natural origin, which try to promote the maintenance of the physiological balance of the skin. Full article
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
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24 pages, 2470 KiB  
Review
Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected
by Daniélle van Staden, Jeanetta du Plessis and Joe Viljoen
Sci. Pharm. 2020, 88(2), 17; https://0-doi-org.brum.beds.ac.uk/10.3390/scipharm88020017 - 27 Mar 2020
Cited by 20 | Viewed by 10510
Abstract
Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing [...] Read more.
Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected. Full article
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
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