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  • 1
    Online Resource
    Online Resource
    Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 5 ( 2022-05-11), p. 1039-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 5 ( 2022-05-11), p. 1039-
    Abstract: (1) Background: The study systematically investigated the influence of dispersed particles within a topical formulation on the dermal penetration efficacy of active compounds that are dissolved in the water phase of this formulation. The aim was to prove or disprove if particle-assisted dermal penetration can be used for improved dermal drug delivery. (2) Methods: Fluorescein was used as a surrogate for a hydrophilic active ingredient (AI). It was dissolved in the water phase of different formulations with and without particles. Two different types of particles (titanium dioxide and nanostructured lipid carriers (NLC)) were used. The influence of particle size and number of particles and the influence of skin hydrating excipients was also investigated. (3) Results demonstrate that the addition of particles can strongly increase the dermal penetration efficacy of AI. The effect depends on the size of the particles and the number of particles in the formulation, where smaller sizes and higher numbers resulted in higher penetration parameters. Formulations with NLC that contained 20% w/w or 40% w/w particles resulted in an about 2-fold higher amount of penetrated AI and increased the penetration depth about 2.5-fold. The penetration-enhancing effect was highly significant (p 〈 0.001) and allowed for an efficient delivery of the AI in the viable dermis. In contrast, the penetration-enhancing effect of excipients that increase the skin hydration was found to be very limited and not significant (≤5%, p 〉 0.05). (4) Conclusions: Based on the results, it can be concluded that particle-assisted dermal penetration can be considered to be a simple but highly efficient and industrially feasible formulation principle for improved and tailor-made dermal drug delivery of active compounds.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14051039
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
    SSG: 15,3
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  • 2
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    Online Resource
    Improved Dermal and Transdermal Delivery of Curcumin with SmartFilms and Nanocrystals
    MDPI AG ; 2021
    In:  Molecules Vol. 26, No. 6 ( 2021-03-15), p. 1633-
    Details
    In: Molecules, MDPI AG, Vol. 26, No. 6 ( 2021-03-15), p. 1633-
    Abstract: Poor aqueous solubility of active compounds is a major issue in today’s drug delivery. In this study the smartFilm-technology was exploited to improve the dermal penetration efficacy of a poorly soluble active compound (curcumin). Results were compared to the dermal penetration efficacy of curcumin from curcumin bulk suspensions and nanocrystals, respectively. The smartFilms enabled an effective dermal and transdermal penetration of curcumin, whereas curcumin bulk- and nanosuspensions were less efficient when the curcumin content was similar to the curcumin content in the smartFilms. Interestingly, it was found that increasing numbers of curcumin particles within the suspensions increased the passive dermal penetration of curcumin. The effect is caused by an aqueous meniscus that is created between particle and skin if the dispersion medium evaporates. The connecting liquid meniscus causes a local swelling of the stratum corneum and maintains a high local concentration gradient between drug particles and skin. Thus, leading to a high local passive dermal penetration of curcumin. The findings suggest a new dermal penetration mechanism for active compounds from nano-particulate drug delivery systems, which can be the base for the development of topical drug products with improved penetration efficacy in the future.
    Type of Medium: Online Resource
    ISSN: 1420-3049
    URL: Article
    DOI: 10.3390/molecules26061633
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
    detail.hit.zdb_id: 2008644-1
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  • 3
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    Online Resource
    Are lipid nanoparticles really superior? A holistic proof of concept study
    Springer Science and Business Media LLC ; 2022
    In:  Drug Delivery and Translational Research Vol. 12, No. 6 ( 2022-06), p. 1433-1444
    Details
    In: Drug Delivery and Translational Research, Springer Science and Business Media LLC, Vol. 12, No. 6 ( 2022-06), p. 1433-1444
    Abstract: Lipid nanoparticles are a successful carrier system for dermal drug delivery. They possess various beneficial properties, i.e., increased chemical stability for chemically labile compounds, increased dermal penetration of active compounds, or skin carrying properties after dermal application due to the formation of a so-called “invisible patch.” Despite manifold studies showing these properties individually, a study that investigates if one lipid nanoparticle formulation can really combine all the above-mentioned benefits at once is not yet available. In the present study, lipid nanoparticles (NLC) were produced and characterized regarding their physico-chemical properties. The chemical stability of the incorporated active ingredient (AI) was determined, as well as the dermal penetration efficacy of the AI, and the skin carrying properties of the NLC after dermal penetration. The properties of the NLC were compared to classical formulations, i.e., AI dissolved in pure oil, an o/w cream base and a nanoemulsion. All formulations contained similar lipids and emulsifiers, which allowed for a direct comparison of the different properties. NLC were shown to provide most efficient chemical stabilization and most efficient dermal penetration for the AI. The formation of the invisible patch was shown for the NLC but not for the other formulations. Skin hydration and skin carrying properties were also most pronounced for the NLC. Results provide evidence that NLC can combine all beneficial effects that were previously described in one formulation. Thus, providing evidence that NLC are a holistically superior formulation principle when compared to other formulation principles. Graphical abstract
    Type of Medium: Online Resource
    ISSN: 2190-393X , 2190-3948
    URL: Article
    DOI: 10.1007/s13346-021-01021-5
    Language: English
    Publisher: Springer Science and Business Media LLC
    Publication Date: 2022
    detail.hit.zdb_id: 2590155-2
    SSG: 15,3
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  • 4
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    Online Resource
    Fingerprint of Nature—Skin Penetration Analysis of a Stinging Nettle PlantCrystals Formulation
    MDPI AG ; 2021
    In:  Cosmetics Vol. 8, No. 1 ( 2021-03-10), p. 21-
    Details
    In: Cosmetics, MDPI AG, Vol. 8, No. 1 ( 2021-03-10), p. 21-
    Abstract: Background: PlantCrystals are a new concept to produce plant-based formulations. Their principle is based on the diminution of parts of or whole plants. In this study, the effect of a surfactant on stinging nettle leaf PlantCrystals was investigated. Secondly, the contents of bulk material and the PlantCrystals formulation were compared. In addition, for the very first time, the skin penetration of PlantCrystals was investigated. Methods: Stinging nettle leaves were milled with high-pressure homogenization. Sizes were analyzed via light microscopy and static light scattering. To investigate the effect of the milling, the flavonoid and total carotenoid content were determined, and the antioxidant capacity of the formulation was measured via total polyphenol content and DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Finally, the impact on skin penetration was investigated. Results: Size analysis showed a stabilizing effect of the surfactant, and the chemical analysis revealed higher flavonoid and polyphenol contents for PlantCrystals. The penetration of the formulation into the stratum corneum was shown to be promising; PlantCrystals possessed a visually perceived higher fluorescence and homogeneity compared to the bulk material. Conclusion: The concept of PlantCrystals improved the availability of valuable constituents and the penetration efficacy. The utilization of the natural chlorophyll fluorescence for skin penetration analysis of plant-based formulations proved itself highly effective.
    Type of Medium: Online Resource
    ISSN: 2079-9284
    URL: Article
    DOI: 10.3390/cosmetics8010021
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
    detail.hit.zdb_id: 2720868-0
    SSG: 15,3
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  • 5
    Online Resource
    Online Resource
    State of knowledge about information sources and health care centres for rare diseases among affected people in Germany
    National Institute of Public Health ; 2020
    In:  Central European Journal of Public Health Vol. 28, No. 1 ( 2020-3-30), p. 82-84
    Details
    In: Central European Journal of Public Health, National Institute of Public Health, Vol. 28, No. 1 ( 2020-3-30), p. 82-84
    Type of Medium: Online Resource
    ISSN: 1210-7778 , 1803-1048
    URL: Article
    DOI: 10.21101/cejph.a5652
    Language: Unknown
    Publisher: National Institute of Public Health
    Publication Date: 2020
    detail.hit.zdb_id: 2560743-1
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  • 6
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    Online Resource
    Cucumber-Derived Exosome-like Vesicles and PlantCrystals for Improved Dermal Drug Delivery
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 3 ( 2022-02-22), p. 476-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 3 ( 2022-02-22), p. 476-
    Abstract: (1) Background: Extracellular vesicles (EVs) are considered to be efficient nanocarriers for improved drug delivery and can be derived from mammalian or plant cells. Cucumber-derived EVs are not yet described in the literature. Therefore, the aim of this study was to produce and characterize cucumber-derived EVs and to investigate their suitability to improve the dermal penetration efficacy of a lipophilic active ingredient (AI) surrogate. (2) Methods: The EVs were obtained by classical EVs isolation methods and by high pressure homogenization (HPH). They were characterized regarding their physico-chemical and biopharmaceutical properties. (3) Results: Utilization of classical isolation and purification methods for EVs resulted in cucumber-derived EVs. Their dermal penetration efficacy for the AI surrogate was 2-fold higher when compared to a classical formulation and enabled a pronounced transdermal penetration into the viable dermis. HPH resulted in submicron sized particles composed of a mixture of disrupted plant cells. A successful isolation of pure EVs from this mixture was not possible with classical EVs isolation methods. The presence of EVs was, therefore, proven indirectly. For this, the lipophilic drug surrogate was admixed to the cucumber juice either prior to or after HPH. Admixing of the drug surrogate to the cucumber prior to the HPH resulted in a 1.5-fold increase in the dermal penetration efficacy, whereas the addition of the AI surrogate to the cucumber after HPH was not able to improve the penetration efficacy. (4) Conclusions: Results, therefore, indicate that HPH causes the formation of EVs in which AI can be incorporated. The formation of plant EVs by HPH was also indicated by zeta potential analysis.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14030476
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
    SSG: 15,3
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  • 7
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    Online Resource
    Assessing the Dermal Penetration Efficacy of Chemical Compounds with the Ex-Vivo Porcine Ear Model
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 3 ( 2022-03-19), p. 678-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 3 ( 2022-03-19), p. 678-
    Abstract: (1) Background: The ex vivo porcine ear model is often used for the determination of the dermal penetration efficacy of chemical compounds. This study investigated the influence of the post-slaughter storage time of porcine ears on the dermal penetration efficacy of chemical compounds. (2) Methods: Six different formulations (curcumin and different fluorescent dyes in different vehicles and/or nanocarriers) were tested on ears that were (i) freshly obtained, (ii) stored for 24 or 48 h at 4 °C after slaughter before use and (iii) freshly frozen and defrosted 12 h before use. (3) Results: Results showed that porcine ears undergo post-mortem changes. The changes can be linked to rigor mortis and all other well-described phenomena that occur with carcasses after slaughter. The post-mortem changes modify the skin properties of the ears and affect the penetration efficacy. The onset of rigor mortis causes a decrease in the water-holding capacity of the ears, which leads to reduced penetration of chemical compounds. The water-holding capacity increases once the rigor is released and results in an increased penetration efficacy for chemical compounds. Despite different absolute penetration values, no differences in the ranking of penetration efficacies between the different formulations were observed between the differently aged ears. (4) Conclusions: All different types of ears can be regarded to be suitable for dermal penetration testing of chemical compounds. The transepidermal water loss (TEWL) and/or skin hydration of the ears were not correlated with the ex vivo penetration efficacy because both an impaired skin barrier and rigor mortis cause elevated skin hydration and TEWL values but an opposite penetration efficacy. Other additional values (for example, pH and/or autofluorescence of the skin) should, therefore, be used to select suitable and non-suitable skin areas for ex vivo penetration testing. Finally, data from this study confirmed that smartFilms and nanostructured lipid carriers (NLC) represent superior formulation strategies for efficient dermal and transdermal delivery of curcumin.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14030678
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
    SSG: 15,3
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  • 8
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    Online Resource
    Methodology to Reach Full Spectral Photo-Protection by Selecting the Best Combination of Physical Filters and Antioxidants
    MDPI AG ; 2022
    In:  Cosmetics Vol. 10, No. 1 ( 2022-12-20), p. 1-
    Details
    In: Cosmetics, MDPI AG, Vol. 10, No. 1 ( 2022-12-20), p. 1-
    Abstract: Antioxidants can reduce free radical formation in deeper skin layers where typical sunscreen filters may no longer be effective. Here, a general method is presented to pre-select optimum combinations of antioxidants and physical filters. The radical production of selected common physical filters after UV irradiation, the capacity of different antioxidants and the interaction between these compounds was investigated in solution by optical measurement of DPPH scavenging, allowing a theoretical calculation of the antioxidant amount necessary to scavenge UV-induced radicals. Furthermore, the antioxidant capacity and the scattering properties were determined. All physical filters induced different amounts of radicals in suspensions depending on the coating. ZnO coated with polydimethylsiloxane and myristic acid (ZnOpolymyr) showed the lowest radical formation. Epigallocatechin-gallate (EGCG) provided the highest antioxidant capacity. Different formulations with different ratios of selected physical filters and antioxidants were prepared. It turned out that the high radical protection factor (RPF) of cream formulations, which originally did not contain any physical filters, was reduced when such filters were added. The data demonstrates that the addition of physical filters to antioxidant-containing formulations lowers their reduction capacity, but to varying degrees. An optimal combination of physical filters and antioxidants must be pre-selected in order to incorporate them into a formulation and verify their effect on skin.
    Type of Medium: Online Resource
    ISSN: 2079-9284
    URL: Article
    DOI: 10.3390/cosmetics10010001
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2720868-0
    SSG: 15,3
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  • 9
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    Online Resource
    Oral Health-Related Quality of Life in People with Achalasia
    MDPI AG ; 2020
    In:  Medicina Vol. 56, No. 6 ( 2020-06-11), p. 286-
    Details
    In: Medicina, MDPI AG, Vol. 56, No. 6 ( 2020-06-11), p. 286-
    Abstract: Background and Objective: The oral health-related quality of life (OHRQoL) of patients with achalasia has not been evaluated to date. Therefore, the aim of this study was to assess the OHRQoL of patients with achalasia and to get information about the time taken for diagnosis and oral symptoms. Materials and Methods: The study was conceived of as an anonymous epidemiological survey study in people with achalasia in order to assess their OHRQoL in each case. For this, a questionnaire was developed consisting of free-text questions and of the standardized German version of the OHIP-14 questionnaire. Results: In total, forty-four questionnaires were analyzed including 31 female and 13 male participants. Regardless of gender, the mean age was 50.57 years (range: 17–78). Of the surveyed individuals, seventy-nine-point-five-five percent had been diagnosed between 25 and 60 years of age. The period from the first signs of the disease to diagnosis was 6.15 years, irrespective of gender. The overall OHIP-14 score without gender differentiation was 8.72 points (range 0–48); the mean score of female participants was 11.13 (range: 0–48), and the OHIP score of male participants was 3.15 on average. Two participants reported oral symptoms. Conclusions: The already known problem of the delayed diagnosis of rare diseases was also confirmed in the case of achalasia. Females with achalasia seemed to be significantly affected by lower OHRQoL than males with achalasia and women of the general population. Demineralization of the tooth structure was described in two participants.
    Type of Medium: Online Resource
    ISSN: 1648-9144
    URL: Article
    DOI: 10.3390/medicina56060286
    Language: English
    Publisher: MDPI AG
    Publication Date: 2020
    detail.hit.zdb_id: 2088820-X
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  • 10
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    Online Resource
    Influence of Dose, Particle Size and Concentration on Dermal Penetration Efficacy of Curcumin
    MDPI AG ; 2023
    In:  Pharmaceutics Vol. 15, No. 11 ( 2023-11-20), p. 2645-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 15, No. 11 ( 2023-11-20), p. 2645-
    Abstract: The influence of size, particle concentration and applied dose (finite vs. infinite dose) on the dermal penetration efficacy of curcumin was investigated in this study. For this, curcumin suspensions with different particle sizes (approx. 20 µm and approx. 250 nm) were produced in different concentrations (0.625–5% (w/w)). The dermal penetration efficacy was determined semi-quantitatively on the ex vivo porcine ear model. The results demonstrated that the presence of particles increases the dermal penetration efficacy of the active compounds being dissolved in the water phase of the formulation. The reason for this is the formation of an aqueous meniscus that develops between particles and skin due to the partial evaporation of water from the vehicle after topical application. The aqueous meniscus contains dissolved active ingredients, and therefore creates a small local spot with a locally high concentration gradient that leads to improved dermal penetration. The increase in penetration efficacy depends on the number of particles in the vehicle, i.e., higher numbers of particles and longer contact times lead to higher penetration efficacy. Therefore, nanocrystals with a high particle concentration were found to be the most suitable formulation principle for efficient and deep dermal penetration of poorly water-soluble active ingredients.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics15112645
    Language: English
    Publisher: MDPI AG
    Publication Date: 2023
    detail.hit.zdb_id: 2527217-2
    SSG: 15,3
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