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Dosage Form Design and Delivery Therapy for Skin Disorders

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 20 February 2025 | Viewed by 2826

Special Issue Editors


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Guest Editor
Center for Studies in Bio-Pharmacy, Postgraduate Program in Pharmaceutical Sciences, Federal University of Paraná, Curitiba, Brazil
Interests: nanotechnology; drug delivery; skin disorders; topical formulations; natural products
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Postgraduate Program of Pharmaceutical Sciences, Federal University of Santa Maria, UFSM, Santa Maria, RS 97105-900, Brazil
Interests: nano-based formulations; cutaneous drug delivery; inflammation; polymeric films;topical drug delivery; hydrogels.
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Skin disorders affect millions of individuals globally, presenting a significant challenge in dermatological therapy. These conditions require effective and innovative therapeutic approaches for their management and treatment. The design of dosage forms and advanced drug delivery systems are crucial for enhancing the efficacy, safety, and patient compliance of dermatological treatments. Pharmaceutical forms designed for skin applications, especially those utilizing natural active ingredients, are gaining prominence due to their therapeutic benefits and biocompatibility. These forms enhance hydration, improve barrier function, and control the release of active compounds. Natural agents—including gums, polysaccharides, vegetable oils, and bioactive compounds—are increasingly incorporated into these formulations due to their ability to provide anti-inflammatory, antioxidant, and antimicrobial effects, which are crucial for treating skin disorders. The integration of these natural ingredients into advanced delivery systems, such as nano-based formulations, further enhances their efficacy by improving skin penetration and ensuring a sustained release of active agents.

In this regard, we are pleased to invite you to this Special Issue, titled “Dosage Form Design and Delivery Therapy for Skin Disorders.” This Special Issue aims to provide a comprehensive platform for disseminating the latest research and innovations in the design and development of dosage forms and drug delivery systems for managing skin disorders. We encourage the submission of research that provides new insights into the formulation science, biopharmaceutical considerations, and clinical applications of skin disorder treatments.

In this Special Issue, original research articles and reviews focusing on the design and development of dosage forms and drug delivery systems for managing skin disorders are welcome, as well as the following: contributions that cover a broad range of topics within this theme—including dosage forms such as emulsions, creams, hydrogels, polymeric films, and nano-based formulations tailored specifically for skin applications; advanced drug delivery systems, particularly those designed to enhance drug penetration, retention, and targeted delivery to affected skin areas; and formulations incorporating natural ingredients (such as gums, polysaccharides, vegetable oils, and bioactive compounds), which are of interest due to their therapeutic potential and biocompatibility. This Issue seeks to highlight therapeutic applications in treating skin disorders, including acne, eczema, psoriasis, skin infections, and wound healing. Mechanistic studies that elucidate the mechanisms of drug action, skin absorption, and the interaction of formulations with skin tissues are also welcome. Additionally, the safety, efficacy, and stability of new dosage forms and delivery systems will be assessed through comprehensive in vitro and in vivo models, ensuring their potential for clinical use.

We look forward to receiving your contributions.

Prof. Dr. Luana Mota Ferreira
Dr. Marcel Henrique Marcondes Sari
Guest Editors

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Keywords

  • skin therapy
  • skin dosage forms
  • skin delivery
  • formulations design
  • natural agents
  • polysaccharides
  • vegetable oils
  • bioactive compounds
  • antioxidant activity
  • anti-inflammatory activity
  • antimicrobial effect
  • dosage safety and efficacy

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Published Papers (2 papers)

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Research

29 pages, 5701 KiB  
Article
Polysaccharide-Stabilized Semisolid Emulsion with Vegetable Oils for Skin Wound Healing: Impact of Composition on Physicochemical and Biological Properties
by Giovanna Araujo de Morais Trindade, Laiene Antunes Alves, Raul Edison Luna Lazo, Kamila Gabrieli Dallabrida, Jéssica Brandão Reolon, Juliana Sartori Bonini, Karine Campos Nunes, Francielle Pelegrin Garcia, Celso Vataru Nakamura, Fabiane Gomes de Moraes Rego, Roberto Pontarolo, Marcel Henrique Marcondes Sari and Luana Mota Ferreira
Pharmaceutics 2024, 16(11), 1426; https://doi.org/10.3390/pharmaceutics16111426 - 8 Nov 2024
Viewed by 738
Abstract
Background/Objectives: The demand for natural-based formulations in chronic wound care has increased, driven by the need for biocompatible, safe, and effective treatments. Natural polysaccharide-based emulsions enriched with vegetable oils present promising benefits for skin repair, offering structural support and protective barriers suitable for [...] Read more.
Background/Objectives: The demand for natural-based formulations in chronic wound care has increased, driven by the need for biocompatible, safe, and effective treatments. Natural polysaccharide-based emulsions enriched with vegetable oils present promising benefits for skin repair, offering structural support and protective barriers suitable for sensitive wound environments. This study aimed to develop and evaluate semisolid polysaccharide-based emulsions for wound healing, incorporating avocado (Persea gratissima) and blackcurrant (Ribes nigrum) oils (AO and BO, respectively). Both gellan gum (GG) and kappa-carrageenan (KC) were used as stabilizers due to their biocompatibility and gel-forming abilities. Methods: Four formulations were prepared (F1-GG-AO; F2-KC-AO; F3-GG-BO; F4-KC-BO) and evaluated for physicochemical properties, spreadability, rheology, antioxidant activity, occlusive and bioadhesion potential, biocompatibility, and wound healing efficacy using an in vitro scratch assay. Results: The pH values (4.74–5.06) were suitable for skin application, and FTIR confirmed excipient compatibility. The formulations showed reduced occlusive potential, pseudoplastic behavior with thixotropy, and adequate spreadability (7.13–8.47 mm2/g). Lower bioadhesion indicated ease of application and removal, enhancing user comfort. Formulations stabilized with KC exhibited superior antioxidant activity (DPPH scavenging) and fibroblast biocompatibility (CC50% 390–589 µg/mL) and were non-hemolytic. Both F2-KC-AO and F4-KC-BO significantly improved in vitro wound healing by promoting cell migration compared to other formulations. Conclusions: These findings underscore the potential of these emulsions for effective wound treatment, providing a foundation for developing skin care products that harness the therapeutic properties of polysaccharides and plant oils in a natural approach to wound care. Full article
(This article belongs to the Special Issue Dosage Form Design and Delivery Therapy for Skin Disorders)
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Figure 1

Figure 1
<p>Flowchart of the formulation and characterization procedures. The preparation of the semisolid emulsion involves several sequential steps (<b>A</b>): weighing the individual components for the oil phase (OP) and aqueous phase (AP), heating each phase separately to 70 °C to ensure proper dissolution and mixing, combining the phases by gradually pouring the aqueous phase (AP) into the oil phase (OP) under constant stirring to form a uniform emulsion, and obtaining the final gel–cream formulation. The emulsion was subsequently characterized through various analyses (<b>B</b>): Fourier-transform infrared spectroscopy (FTIR) to assess molecular interactions and confirm compatibility among components, centrifugation to evaluate physical stability and detect any phase separation, spreadability and reology testing to determine ease of application and coverage on the skin, density measurement to assess formulation consistency, pH measurement with a pH meter to ensure suitability for skin application, bioadhesion and occlusion potential, antioxidant activity, cytotoxicity testing using cell cultures to evaluate biocompatibility and potential safety for skin use, and wound healing assay to determine efficacy.</p>
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<p>Macroscopic (<b>A</b>) and microscopic (<b>B</b>) images of polysaccharide-based semisolid emulsions containing vegetable oils. Overall, the formulations have a whitish color, homogeneous aspect, and shiny texture. The microscopic evaluation indicates that the system effectively dispersed the oil, keeping it stable within the semisolid structure. Abbreviations: GG—Gellan gum; KC—<span class="html-italic">Kappa</span>-carrageenan; BO—Blackcurrant Oil; AO—Avocado Oil.</p>
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<p>Infrared spectra of raw materials (<b>A</b>) and semisolid emulsions (<b>B</b>). The spectra exhibit characteristic peaks corresponding to the functional groups present in the substances. Additionally, these spectra support the compatibility among the components, as the absence of significant new peaks suggests no chemical interaction altering the molecular structure of the excipients.</p>
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<p>PCA model. In (<b>A</b>,<b>B</b>) are the eigenvalues graphs, which indicate that these three principal components encompass most of the chemical information in the raw materials. The red circles represent the principal components selected for the model. In (<b>C</b>,<b>D</b>) are the score plot graphs that reveal a distinct differentiation is observable between the formulations containing GG and KC, emphasizing these polysaccharides’ influence on the formulations’ ultimate chemical composition.</p>
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<p>Spreadability profile (<b>A</b>), spreadability factor (<b>B</b>), and viscosity (<b>C</b>) of semisolid emulsions. The developed emulsions demonstrated an increased spreading area with the application of more weight, suggesting they can expand more easily under pressure. Moreover, rheological measurements supported this behavior, as the complex viscosity (η*) of all formulations decreased with increasing angular frequency, which is a characteristic of pseudoplastic materials.</p>
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<p>Storage modulus (G′) and loss modulus (G″) as functions of angular frequency (ω). In (<b>A</b>,<b>B</b>) formulations containing AO stabilized with GG and KC, respectively. In (<b>C</b>,<b>D</b>) formulations prepared with BO stabilized with GG and KC, respectively. Data indicates that elastic and viscous behaviors become more pronounced at higher frequencies, suggesting a predominantly elastic rather than viscous behavior.</p>
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<p>Thixotropy evaluation of F1-GG-AO (<b>A</b>), F2-KC-AO (<b>B</b>), F3-GG-BO (<b>C</b>), and (<b>D</b>) F4-KC-BO. The data show that the material’s structure is temporarily disrupted under shear, but it recovers gradually when the shear is removed, which is characteristic of thixotropic materials.</p>
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<p>Antioxidant activity. The @ denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) between formulations and their respective blank forms (F1-GG-AO versusF5-GG-B, and F3-GG-BO versus F5-GG-B); # represents the significant difference (<span class="html-italic">p</span> &lt; 0.05) between polysaccharides (F1-GG-AO versus F2-KC-AO, and F5-GG-B versus F6-KC-B). NS means “not significant”. Both oils significantly enhanced the antioxidant potential of GG emulsions compared to the placebo semisolid, while emulsions stabilized with KC demonstrated higher antioxidant properties than those stabilized with GG.</p>
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<p>Occlusion potential. The @ denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) between formulations and their respective blank forms (F2-KC-AO versusF6-KC-B, and F4-KC-BO versus F6-KC-B); # represents the significant difference (<span class="html-italic">p</span> &lt; 0.05) between polysaccharides (F5-GG-B versus F6-KC-B). NS means “not significant”. Similar occlusion potential was observed among the formulations. Data also suggests that the oily components may negatively affect the KC formulations.</p>
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<p>Bioadhesion potential in intact and injured skin. The @ denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) between formulations and their respective blank forms; # represents the significant difference (<span class="html-italic">p</span> &lt; 0.05) between polysaccharides with the same oil (F1-GG-AO versusF2-KC-AO, or F3-GG-BO versus F4-KC-BO); * denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) between oils with the same polysaccharide (F1-GG-AO versus F3-GG-BO or F2-KC-AO versus F4-KC-BO); and <span>$</span> represents the significant difference (<span class="html-italic">p</span> &lt; 0.05) between intact and injured skin. NS means “not significant”. All formulations presented significantly higher bioadhesion in intact skin than in injured skin.</p>
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<p>Effect of F1-GG-AO (<b>A</b>), F2-KC-AO (<b>B</b>), F3-GG-BO (<b>C</b>), F4-KC-BO (<b>D</b>), F5-GG-B (<b>E</b>), and F6-KC-B (<b>F</b>) (1–1000 µg/mL) on the viability of L-929 cells by MTT assay. A negative control (non–treated cells) was conducted and considered 100% viability. Mean values were calculated from 3 independent results. The * denotes the significative difference from the negative control (<span class="html-italic">p</span> &lt; 0.05). NS means “not significant”. In all formulations examined, the viability of cells is observed to decline as the concentration increases.</p>
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<p>Hemolytic assay of KC semisolid emulsions. The results showed a hemolytic potential of less than 1% for all tested concentrations of the KC-based emulsions.</p>
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<p>Representative images showing the progression of healing over time (<b>A</b>) and percentage of open wound area at different times (0, 6, and 24 h) (<b>B</b>) for the F2-KC-AO, F4-KC-BO, and F6-KC-B, compared to the negative control. The * denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) with time zero in the same group, and # denotes the significant difference (<span class="html-italic">p</span> &lt; 0.05) with negative control at the same time. There is a consistent reduction in the area of open wounds over time, with formulations containing oils exhibiting a more pronounced degree of cell migration, which suggests an effective healing process.</p>
Full article ">
25 pages, 6758 KiB  
Article
Comprehensive Advanced Physicochemical Characterization and In Vitro Human Cell Culture Assessment of BMS-202: A Novel Inhibitor of Programmed Cell Death Ligand
by Hasham Shafi, Andrea J. Lora, Haley M. Donow, Sally E. Dickinson, Georg T. Wondrak, H.-H. Sherry Chow, Clara Curiel-Lewandrowski and Heidi M. Mansour
Pharmaceutics 2024, 16(11), 1409; https://doi.org/10.3390/pharmaceutics16111409 - 1 Nov 2024
Viewed by 1399
Abstract
Background/Objectives: BMS-202, is a potent small molecule with demonstrated antitumor activity. The study aimed to comprehensively characterize the physical and chemical properties of BMS-202 and evaluate its suitability for topical formulation, focusing on uniformity, stability and safety profiles. Methods: A range of analytical [...] Read more.
Background/Objectives: BMS-202, is a potent small molecule with demonstrated antitumor activity. The study aimed to comprehensively characterize the physical and chemical properties of BMS-202 and evaluate its suitability for topical formulation, focusing on uniformity, stability and safety profiles. Methods: A range of analytical techniques were employed to characterize BMS-202. Scanning Electron Microscopy (SEM) was used to assess morphology, Differential Scanning Calorimetry (DSC) provided insights of thermal behavior, and Hot-Stage Microscopy (HSM) corroborated these thermal behaviors. Molecular fingerprinting was conducted using Raman spectroscopy and Fourier Transform Infrared (FTIR) spectroscopy, with chemical uniformity of the batch further validated by mapping through FTIR and Raman microscopies. The residual water content was measured using Karl Fisher Coulometric titration, and vapor sorption isotherms examined moisture uptake across varying relative humidity levels. In vitro safety assessments involved testing with skin epithelial cell lines, such as HaCaT and NHEK, and Transepithelial Electrical Resistance (TEER) to evaluate barrier integrity. Results: SEM revealed a distinctive needle-like morphology, while DSC indicated a sharp melting point at 110.90 ± 0.54 ℃ with a high enthalpy of 84.41 ± 0.38 J/g. HSM confirmed the crystalline-to-amorphous transition at the melting point. Raman and FTIR spectroscopy, alongside chemical imaging, confirmed chemical uniformity as well as validated the batch consistency. A residual water content of 2.76 ± 1.37 % (w/w) and minimal moisture uptake across relative humidity levels demonstrated its low hygroscopicity and suitability for topical formulations. Cytotoxicity testing showed dose-dependent reduction in skin epithelial cell viability at high concentrations (100 µM and 500 µM), with lower doses (0.1 µM to 10 µM) demonstrating acceptable safety. TEER studies indicated that BMS-202 does not disrupt the HaCaT cell barrier function. Conclusions: The findings from this study establish that BMS-202 has promising physicochemical and in vitro characteristics at therapeutic concentrations for topical applications, providing a foundation for future formulation development focused on skin-related cancers or localized immune modulation. Full article
(This article belongs to the Special Issue Dosage Form Design and Delivery Therapy for Skin Disorders)
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Figure 1

Figure 1
<p>BMS-202 structures drawn using ChemDraw<sup>®</sup> ver. 21.0.0 (ChemOffice, Cambridge, MA, USA): (<b>a</b>) chemical structure; and (<b>b</b>) wire-frame 3D model; and Molecular Modeling Pro Plus<sup>®</sup> ver. 8.0.4 (Norgwyn Montgomery Software Inc., North Wales, PA, USA): (<b>c</b>) chemical structure; and (<b>d</b>) ball-and-stick 3D model.</p>
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<p>Representative SEM images of BMS-202 showing powder morphology at different magnifications: (<b>a</b>) 910×, (<b>b</b>) 1500×, (<b>c</b>) 2500×, and (<b>d</b>) 10,000×.</p>
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<p>(<b>a</b>) Representative SEM micrograph taken at 2400× magnification, depicting the elemental spot analysis of the BMS-202 particle surface using EDX spectroscopy. (<b>b</b>) Representative EDX spectrum of the analyzed spot on the powder sample, indicated by the blue crosshair, illustrating the elemental composition of the BMS-202 particle, comprising C, N and O (with the N symbol overlapped by the O symbol). The inset table presents the atomic and weight concentrations of the identified elements.</p>
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<p>Representative DSC thermogram of BMS-202 showing main thermal transitions of the compound.</p>
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<p>Representative HSM images of BMS-202 powder taken at different temperatures (scale 100 µm). The interference colors, particularly as the powder begins to melt, indicate birefringence.</p>
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<p>Representative Raman spectrum of BMS-202 powder showing characteristic Raman vibrational modes.</p>
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<p>(<b>a</b>) Raman map of BMS-202 powders showing spectra obtained from nine distinct points on the sample. The Y-axis of each overlay map is presented on an offset scale for clarity. (<b>b</b>) 2D Raman area contour map of the highlighted red square region (as shown in (<b>c</b>)), indicating the position coordinates of each spectrum. (<b>c</b>) 2D Raman area map depicting the sample surface under a 10× objective, with a red square highlighting the specific region analyzed. Each spectrum in the overlay corresponds to one of the nine points within the highlighted red square, captured using a 785 nm laser, and is color-coded according to the spectrum obtained based on position coordinates.</p>
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<p>Representative ATR-FTIR spectrum illustrating the characteristic molecular fingerprints of BMS-202 powder.</p>
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<p>(<b>a</b>) FTIR map of BMS-202 powders showing the spectra obtained from nine distinct points on the sample. Y-axis of each overlay map is represented on an offset scale. (<b>b</b>) 2D area contour map of the highlighted red square region (as shown in (<b>c</b>)), displaying the position coordinates of each spectrum. (<b>c</b>) 2D area map displaying the sample surface under a 10× objective, with a highlighted red square indicating the specific region analyzed. Each spectrum in the overlay corresponds to one of the nine points within the highlighted red square and color-coded according to the spectrum obtained.</p>
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<p>Gravimetric water vapor sorption isotherm of BMS-202 powder (weight change % vs. RH) at room temperature (25 °C). The green line represents the average of three individual experiments. Each circle represents the percent weight change when exposed to different levels of the humidity.</p>
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<p>Dose-dependent in vitro cell viability of BMS-202 powder after 48 h of exposure on skin epithelial cells. (<b>a</b>) HaCaT (mean ± SD, n = 6), Control: 100.00 ± 3.54, 0.1 µM: 98.14 ± 3.88, 1 µM: 98.85 ± 5.07, 10 µM: 97.08 ± 3.81, 100 µM: 35.15 ± 6.37, and 500 µM; 11.25 ± 0.57 (<b>b</b>) NHEK (mean ± SD, n = 7), Control: 100.00 ± 2.98, 0.1 µM: 103.46 ± 2.73, 1 µM: 84.84 ± 5.84, 10 µM: 81.73 ± 8.74, 100 µM: 15.98 ± 2.35, and 500 µM: 12.87 ± 1.34. Each small circle represents a data point, and the vertical bars on each column indicate the standard deviation of the data. One-way ANOVA was used to compare different dose treatments with control (no treatment) using Dunnett’s multiple comparison test (α = 0.05, *** <span class="html-italic">p</span> &lt; 0.001, and **** <span class="html-italic">p</span> &lt; 0.0001).</p>
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<p>Transepithelial electric resistance (TEER) values (% of control) recorded at various time points using a STX4 open-ended electrode connected to an EVOM™ TEER measurement meter. Measurements were taken across HaCaT cells in Transwells<sup>®</sup> under air–liquid interface (ALI) conditions after exposure to 100 µM BMS-202. TEER values were also recorded for naïve (non-treated) and vehicle-treated Transwells<sup>®</sup>. Each time point represents <span class="html-italic">n</span> = 4 replicates. Statistical analysis was conducted using a two-way ANOVA with Dunnett’s multiple comparison test (<span class="html-italic">p</span> &lt; 0.05) to compare the means across different time points.</p>
Full article ">
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