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Pharmaceutics
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Semisolid Dosage (Volume III)
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Semisolid Dosage (Volume III)

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

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 28288

Special Issue Editor

Prof. Dr. Dominique Lunter

E-Mail Website
Guest Editor
Pharmaceutical Technology, Eberhard Karls University Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany
Interests: semi-solid dosage forms; topical delivery; confocal Raman spectroscopy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Already in ancient times, semi-solid preparations for cutaneous application, popularly known as ointments, played an important role in human society. An advanced scientific investigation of “ointments” as dosage forms was set off in the late fifties of the previous century. It was only from then on that the intensive physico-chemical characterization of ointments as well as the inclusion of dermatological aspects was leading to a comprehensive understanding of the various interactions between the vehicle, the active ingredient and the skin.

From then on, many researchers were involved in optimizing semi-solid formulations with respect to the continuously changing therapeutic and patient needs. Aspects that have been dealt with were the optimization of dermato-biopharmaceutical properties and many different issues related to patient’s compliance, such as skin tolerance, applicability, and cosmetic appeal. Moreover, processing technology has been improved and analytical techniques were developed and refined in order to enable improved characterization of the formulation itself as well as its interaction with the skin.

This special issue serves to highlight and capture the contemporary progress and current research on semi-solid formulations as dermal drug delivery systems. We invite articles on all aspects of semi-solid formulations highlighting the research currently undertaken to improve and better understand these complex drug delivery systems in particular with respect to formulation, processing and characterization issues.

Prof. Dr. Dominique Lunter
Guest Editor

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Keywords

  • semi-solid
  • dermato-biopharmceutics
  • processing
  • characterization
  • quality control
  • formulation concept
  • rheology
  • particle sizing

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Related Special Issues

Published Papers (9 papers)

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Research

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23 pages, 6765 KiB  
Article
Influence of Manufacturing Process on the Microstructure, Stability, and Sensorial Properties of a Topical Ointment Formulation
by Pui Shan Chow, Ron Tau Yee Lim, Febin Cyriac, Jaymin C. Shah, Abu Zayed Md Badruddoza, Thean Yeoh, Chetan Kantilal Yagnik, Xin Yi Tee, Annie Bao Hua Wong, Vernissa Dilys Chia and Guan Wang
Pharmaceutics 2023, 15(9), 2219; https://doi.org/10.3390/pharmaceutics15092219 - 28 Aug 2023
Cited by 4 | Viewed by 3935
Abstract
The manufacturing process for ointments typically involves a series of heating, cooling, and mixing steps. Precise control of the level of mixing through homogenization and the cooling rate, as well as temperature at different stages, is important in delivering ointments with the desired [...] Read more.
The manufacturing process for ointments typically involves a series of heating, cooling, and mixing steps. Precise control of the level of mixing through homogenization and the cooling rate, as well as temperature at different stages, is important in delivering ointments with the desired quality attributes, stability, and performance. In this work, we investigated the influence of typical plant processing conditions on the microstructure, stability, and sensorial properties of a model ointment system through a Design of Experiments (DoE) approach. Homogenization speed at the cooling stage after the addition of the solvent (propylene glycol, PG) was found to be the critical processing parameter that affects stability and the rheological and sensorial properties of the ointment. A lower PG addition temperature was also found to be beneficial. The stabilization of the ointment at a lower PG addition temperature was hypothesized to be due to more effective encapsulation by crystallizing mono- and diglycerides at the lower temperature. The in vitro release profiles were found to be not influenced by the processing parameters, suggesting that for the ointment platform studied, processing affects the microstructure, but the effects do not translate into the release profile, a key performance indicator. Our systematic study represents a Quality-by-Design (QbD) approach to the design of a robust manufacturing process for delivering stable ointments with the desired performance attributes and properties. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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14 pages, 3368 KiB  
Article
Fast-Embeddable Grooved Microneedles by Shear Actuation for Accurate Transdermal Drug Delivery
by Sang-Gu Yim, Keum-Yong Seong, Akash Thamarappalli, Hyeseon Lee, Seungsoo Lee, Sanha Lee, Semin Kim and Seung-Yun Yang
Pharmaceutics 2023, 15(7), 1966; https://doi.org/10.3390/pharmaceutics15071966 - 17 Jul 2023
Cited by 5 | Viewed by 1766
Abstract
Percutaneous drug delivery using microneedles (MNs) has been extensively exploited to increase the transdermal permeability of therapeutic drugs. However, it is difficult to control the precise dosage with existing MNs and they need to be attached for a long time, so a more [...] Read more.
Percutaneous drug delivery using microneedles (MNs) has been extensively exploited to increase the transdermal permeability of therapeutic drugs. However, it is difficult to control the precise dosage with existing MNs and they need to be attached for a long time, so a more simple and scalable method is required for accurate transdermal drug delivery. In this study, we developed grooved MNs that can be embedded into the skin by mechanical fracture following simple shear actuation. Grooved MNs are prepared from hyaluronic acid (HA), which is a highly biocompatible and biodegradable biopolymer. By adjusting the aspect ratio (length:diameter) of the MN and the position of the groove, the MN tip inserted into the skin can be easily broken by shear force. In addition, it was demonstrated that it is possible to deliver the desired amount of triamcinolone acetonide (TCA) for alopecia areata by controlling the position of the groove structure and the concentration of TCA loaded in the MN. It was also confirmed that the tip of the TCA MN can be accurately delivered into the skin with a high probability (98% or more) by fabricating an easy-to-operate applicator to provide adequate shear force. The grooved MN platform has proven to be able to load the desired amount of a drug and deliver it at the correct dose. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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34 pages, 3631 KiB  
Article
Rheology of Complex Topical Formulations: An Analytical Quality by Design Approach to Method Optimization and Validation
by Lucas Chiarentin, Catarina Cardoso, Margarida Miranda and Carla Vitorino
Pharmaceutics 2023, 15(7), 1810; https://doi.org/10.3390/pharmaceutics15071810 - 24 Jun 2023
Cited by 10 | Viewed by 3656
Abstract
Analytical method validation ensures that a method provides trustworthy information about a particular sample when applied in accordance with the predefined protocol. According to regulatory standards, the rheological characteristics of topically applied semisolid formulations are one of the key elements involved in microstructure [...] Read more.
Analytical method validation ensures that a method provides trustworthy information about a particular sample when applied in accordance with the predefined protocol. According to regulatory standards, the rheological characteristics of topically applied semisolid formulations are one of the key elements involved in microstructure equivalence documentation. Therefore, for generic drug product manufacturers, it is a dire need to take a step forward in rheology method development and validation procedures. This paper aims to apply Analytical Quality by Design (AQbD) principles towards the development and validation of rheology methods for topical creams, as complex semisolid formulations. Risk assessment was carried out through an Ishikawa diagram and an estimate failure mode, effects, and criticality analysis (FMECA). Sample application, peltier temperature control, and sample rest time were identified as critical method variables (CMVs), and a 23 full factorial design was applied to understand their impact on rotational, creep recovery and, oscillatory measurements. The development of the method was carried out as per the ICH Q8-Q10, and Q14 guidelines and validated according to ICH Q2 (R2) guideline. The method demonstrated adequate precision (RSD < 15%), as well as selectivity. AQbD provided a comprehensive framework for developing a reliable and effective rheology method for this type of formulation. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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17 pages, 3073 KiB  
Article
Spruce Balm-Based Semisolid Vehicles for Wound Healing: Effect of Excipients on Rheological Properties and Ex Vivo Skin Permeation
by Elisabeth Eichenauer, Martina Jozić, Sabine Glasl and Victoria Klang
Pharmaceutics 2023, 15(6), 1678; https://doi.org/10.3390/pharmaceutics15061678 - 8 Jun 2023
Cited by 3 | Viewed by 2056
Abstract
The treatment of chronic wounds, an important issue with the growing elderly population, is increasingly hindered by antibiotic resistance. Alternative wound care approaches involve the use of traditional plant-derived remedies, such as purified spruce balm (PSB), with antimicrobial effects and the promotion of [...] Read more.
The treatment of chronic wounds, an important issue with the growing elderly population, is increasingly hindered by antibiotic resistance. Alternative wound care approaches involve the use of traditional plant-derived remedies, such as purified spruce balm (PSB), with antimicrobial effects and the promotion of cell proliferation. However, spruce balm is difficult to formulate due to its stickiness and high viscosity; dermal products with satisfying technological properties and the scientific literature on this topic are scarce. Thus, the aim of the present work was to develop and rheologically characterize a range of PSB-based dermal formulations with different hydrophilic/lipophilic compositions. Mono- and biphasic semisolid formulations based on different compounds (petrolatum, paraffin oil, wool wax, castor oil, and water) were developed and characterized by their organoleptic and rheological measurements. A chromatographic method of analysis was established, and skin permeation data were collected for pivotal compounds. The results showed that the dynamic viscosity ranged from 10 to 70 Pas at 10/s for the different shear-thinning systems. The best formulation properties were observed for water-free wool wax/castor oil systems with 20% w/w PSB followed by different water-in-oil cream systems. Skin permeation through porcine skin was observed for different PSB compounds (e.g., pinoresinol, dehydroabietic acid, and 15-hydroxy-dehydroabietic acid) using Franz-type diffusion cells. The permeation potential of wool wax/castor oil- and lard-based formulations was shown for all the analyzed substance classes. The varying content of pivotal compounds in different PSB batches collected at different timepoints from different spruce individuals might have contributed to observed differences in vehicle performance. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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19 pages, 2735 KiB  
Article
Label-Free Quantification of Nanoencapsulated Piperonyl Esters in Cosmetic Hydrogels Using Raman Spectroscopy
by Suha Elderderi, Franck Bonnier, Xavier Perse, Hugh J. Byrne, Florent Yvergnaux, Igor Chourpa, Abdalla A. Elbashir and Emilie Munnier
Pharmaceutics 2023, 15(6), 1571; https://doi.org/10.3390/pharmaceutics15061571 - 23 May 2023
Cited by 1 | Viewed by 1825
Abstract
Raman spectroscopy is a well-established technique for the molecular characterisation of samples and does not require extensive pre-analytical processing for complex cosmetic products. As an illustration of its potential, this study investigates the quantitative performance of Raman spectroscopy coupled with partial least squares [...] Read more.
Raman spectroscopy is a well-established technique for the molecular characterisation of samples and does not require extensive pre-analytical processing for complex cosmetic products. As an illustration of its potential, this study investigates the quantitative performance of Raman spectroscopy coupled with partial least squares regression (PLSR) for the analysis of Alginate nanoencapsulated Piperonyl Esters (ANC-PE) incorporated into a hydrogel. A total of 96 ANC-PE samples covering a 0.4% w/w–8.3% w/w PE concentration range have been prepared and analysed. Despite the complex formulation of the sample, the spectral features of the PE can be detected and used to quantify the concentrations. Using a leave-K-out cross-validation approach, samples were divided into a training set (n = 64) and a test set, samples that were previously unknown to the PLSR model (n = 32). The root mean square error of cross-validation (RMSECV) and prediction (RMSEP) was evaluated to be 0.142% (w/w PE) and 0.148% (w/w PE), respectively. The accuracy of the prediction model was further evaluated by the percent relative error calculated from the predicted concentration compared to the true value, yielding values of 3.58% for the training set and 3.67% for the test set. The outcome of the analysis demonstrated the analytical power of Raman to obtain label-free, non-destructive quantification of the active cosmetic ingredient, presently PE, in complex formulations, holding promise for future analytical quality control (AQC) applications in the cosmetics industry with rapid and consumable-free analysis. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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13 pages, 4227 KiB  
Article
Transdermal Delivery of α-Aminophosphonates as Semisolid Formulations—An In Vitro-Ex Vivo Study
by Dorottya Kocsis, Petra Regina Varga, Rusul Keshwan, Mina Nader, Miléna Lengyel, Pál Szabó, István Antal, Károly Kánai, György Keglevich and Franciska Erdő
Pharmaceutics 2023, 15(5), 1464; https://doi.org/10.3390/pharmaceutics15051464 - 11 May 2023
Cited by 5 | Viewed by 1824
Abstract
α-Aminophosphonates are organophosphorus compounds with an obvious similarity with α-amino acids. Owing to their biological and pharmacological characteristics, they have attracted the attention of many medicinal chemists. α-Aminophosphonates are known to exhibit antiviral, antitumor, antimicrobial, antioxidant and antibacterial activities, which can all be [...] Read more.
α-Aminophosphonates are organophosphorus compounds with an obvious similarity with α-amino acids. Owing to their biological and pharmacological characteristics, they have attracted the attention of many medicinal chemists. α-Aminophosphonates are known to exhibit antiviral, antitumor, antimicrobial, antioxidant and antibacterial activities, which can all be important in pathological dermatological conditions. However, their ADMET properties are not well studied. The aim of the current study was to provide preliminary information about the skin penetration of three preselected α-aminophosphonates when applying them as topical cream formulations in static and dynamic diffusion chambers. The results indicate that aminophosphonate 1a, without any substituent in the para position, shows the best release from the formulation and the highest absorption through the excised skin. However, based on our previous study, the in vitro pharmacological potency was higher in the case of para-substituted molecules 1b and 1c. The particle size and rheological studies revealed that the 2% cream of aminophosphonate 1a was the most homogenous formulation. In conclusion, the most promising molecule was 1a, but further experiments are proposed to uncover the possible transporter interactions in the skin, optimize the topical formulations and improve PK/PD profiles in case of transdermal delivery. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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14 pages, 2790 KiB  
Article
Solid Lipid Nanoparticles Hydroquinone-Based for the Treatment of Melanoma: Efficacy and Safety Studies
by Sonia Trombino, Rocco Malivindi, Giuseppe Barbarossa, Roberta Sole, Federica Curcio and Roberta Cassano
Pharmaceutics 2023, 15(5), 1375; https://doi.org/10.3390/pharmaceutics15051375 - 29 Apr 2023
Cited by 7 | Viewed by 1957
Abstract
Classical melanoma therapy has several side effects that are responsible for a decrease in the final therapeutic efficacy. It is possible that the drug is degraded before reaching the target site and is metabolized by the body itself, resulting in repeated doses being [...] Read more.
Classical melanoma therapy has several side effects that are responsible for a decrease in the final therapeutic efficacy. It is possible that the drug is degraded before reaching the target site and is metabolized by the body itself, resulting in repeated doses being administered throughout the day and a decrease in patient compliance. Drug delivery systems avoid degradation of the active ingredient, improve release kinetics, prevent the drug from being metabolized before reaching the site of action, and improve the safety and efficacy profiles of adjuvant cancer therapy. The solid lipid nanoparticles (SLNs) based on hydroquinone esterified with stearic acid realized in this work represent a chemotherapeutic drug delivery system that is useful in the treatment of melanoma. The starting materials were characterized by FT-IR and 1H-NMR, while the SLNs were characterized by dynamic light scattering. In efficacy studies, their ability to influence anchorage-dependent cell proliferation was tested on COLO-38 human melanoma cells. Furthermore, the expression levels of proteins belonging to apoptotic mechanisms were determined by analyzing the role of SLNs in modulating the expression of p53 and p21WAF1/Cip1. Safety tests were conducted to determine not only the pro-sensitizing potential but also the cytotoxicity of SLNs, and studies were conducted to assess the antioxidant and anti-inflammatory activity of these drug delivery. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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22 pages, 4004 KiB  
Article
Design, Development, and Evaluation of Treprostinil Embedded Adhesive Transdermal Patch
by Ibrahim Alissa, Anroop B. Nair, Bandar Aldhubiab, Hiral Shah, Jigar Shah, Vivek Mewada, Rashed M. Almuqbil and Shery Jacob
Pharmaceutics 2023, 15(4), 1226; https://doi.org/10.3390/pharmaceutics15041226 - 12 Apr 2023
Cited by 1 | Viewed by 2484
Abstract
Clinical application of treprostinil in pulmonary arterial hypertension is hampered by adverse effects caused by its high dosing frequency. The objective of this investigation was to Formulate an adhesive-type transdermal patch of treprostinil and evaluate it both in vitro and in vivo. A [...] Read more.
Clinical application of treprostinil in pulmonary arterial hypertension is hampered by adverse effects caused by its high dosing frequency. The objective of this investigation was to Formulate an adhesive-type transdermal patch of treprostinil and evaluate it both in vitro and in vivo. A 32-factorial design was utilized to optimize the selected independent variables (X1: drug amount, X2: enhancer concentration) on the response variables (Y1: drug release, Y2: transdermal flux). The optimized patch was evaluated for various pharmaceutical properties, skin irritation, and pharmacokinetics in rats. Optimization results signify considerable influence (p < 0.0001) of X1 on both Y1 and Y2, as compared to X2. The optimized patch possesses higher drug content (>95%), suitable surface morphology, and an absence of drug crystallization. FTIR analysis revealed compatibility of the drug with excipients, whereas DSC thermograms indicate that the drug exists as amorphous in the patch. The adhesive properties of the prepared patch confirm adequate adhesion and painless removal, while the skin irritation study confirms its safety. A steady drug release via Fickian diffusion and greater transdermal delivery (~23.26 µg/cm2/h) substantiate the potential of the optimized patch. Transdermal therapy resulted in higher treprostinil absorption (p < 0.0001) and relative bioavailability (237%) when compared to oral administration. Overall, the results indicate that the developed drug in the adhesive patch can effectively deliver treprostinil through the skin and could be a promising treatment option for pulmonary arterial hypertension. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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Review

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24 pages, 2077 KiB  
Review
Rational Design of Topical Semi-Solid Dosage Forms-How Far Are We?
by Michael E. Herbig, Dirk-Heinrich Evers, Sascha Gorissen and Melanie Köllmer
Pharmaceutics 2023, 15(7), 1822; https://doi.org/10.3390/pharmaceutics15071822 - 26 Jun 2023
Cited by 12 | Viewed by 7735
Abstract
Specific aspects of semi-solid dosage forms for topical application include the nature of the barrier to be overcome, aspects of susceptibility to physical and chemical instability, and a greater influence of sensory perception. Advances in understanding the driving forces of skin penetration as [...] Read more.
Specific aspects of semi-solid dosage forms for topical application include the nature of the barrier to be overcome, aspects of susceptibility to physical and chemical instability, and a greater influence of sensory perception. Advances in understanding the driving forces of skin penetration as well as the design principles and inner structure of formulations, provide a good basis for the more rational design of such dosage forms, which still often follow more traditional design approaches. This review analyses the opportunities and constraints of rational formulation design approaches in the industrial development of new topical drugs. As the selection of drug candidates with favorable physicochemical properties increases the speed and probability of success, models for drug selection based on theoretical and experimental approaches are discussed. This paper reviews how progress in the scientific understanding of mechanisms and vehicle-influence of skin penetration can be used for rational formulation design. The characterization of semi-solid formulations is discussed with a special focus on modern rheological approaches and analytical methods for investigating and optimizing the chemical stability of active ingredients in consideration of applicable guidelines. In conclusion, the combination of a good understanding of scientific principles combined with early consideration of regulatory requirements for product quality are enablers for the successful development of innovative and robust semi-solid formulations for topical application. Full article
(This article belongs to the Special Issue Semisolid Dosage (Volume III))
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