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Pharmaceutics
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Semisolid Dosage
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Semisolid Dosage

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (31 December 2019) | Viewed by 66961

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Prof. Dr. Rolf Daniels

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, University of Tübingen, 72076 Tubingen, Germany
Interests: semi-solids; oleogels; surfactant-free; foams; process analytical technology; electro-spinning
Special Issues, Collections and Topics in MDPI journals
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. Rolf Daniels
Dr. Dominique Lunter
Guest Editors

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Keywords

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

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Published Papers (14 papers)

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Editorial

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4 pages, 182 KiB  
Editorial
Semisolid Dosage
by Dominique Jasmin Lunter and Rolf Daniels
Pharmaceutics 2020, 12(4), 315; https://doi.org/10.3390/pharmaceutics12040315 - 1 Apr 2020
Viewed by 2534
Abstract
Already in ancient times, semisolid preparations for cutaneous application, popularly known as ointments, played an important role in human society [...] Full article
(This article belongs to the Special Issue Semisolid Dosage)

Research

Jump to: Editorial, Other

16 pages, 5049 KiB  
Article
Systematic Investigation of the Effect of Non-Ionic Emulsifiers on Skin by Confocal Raman Spectroscopy—A Comprehensive Lipid Analysis
by Yali Liu and Dominique Jasmin Lunter
Pharmaceutics 2020, 12(3), 223; https://doi.org/10.3390/pharmaceutics12030223 - 2 Mar 2020
Cited by 26 | Viewed by 4101
Abstract
Non-ionic emulsifiers are commonly found in existing pharmaceutical and cosmetic formulations and have been widely employed to enhance the penetration and permeation of active ingredients into the skin. With the potential of disrupting skin barrier function and increasing fluidity of stratum corneum (SC) [...] Read more.
Non-ionic emulsifiers are commonly found in existing pharmaceutical and cosmetic formulations and have been widely employed to enhance the penetration and permeation of active ingredients into the skin. With the potential of disrupting skin barrier function and increasing fluidity of stratum corneum (SC) lipids, we herein examined the effects of two kinds of non-ionic emulsifiers on intercellular lipids of skin, using confocal Raman spectroscopy (CRS) with lipid signals on skin CRS spectrum. Non-ionic emulsifiers of polyethylene glycol alkyl ethers and sorbitan fatty acid esters were studied to obtain a deep understanding of the mechanism between non-ionic emulsifiers and SC lipids. Emulsifier solutions and dispersions were prepared and applied onto excised porcine skin. Water and sodium laureth sulfate solution (SLS) served as controls. SC lipid signals were analysed by CRS regarding lipid content, conformation and lateral packing order. Polyethylene glycol (PEG) sorbitan esters revealed no alteration of intercellular lipid properties while PEG-20 ethers appeared to have the most significant effects on reducing lipid content and interrupting lipid organization. In general, the polyoxyethylene chain and alkyl chain of PEG derivative emulsifiers might indicate their ability of interaction with SC components. HLB values remained critical for complete explanation of emulsifier effects on skin lipids. With this study, it is possible to characterize the molecular effects of non-ionic emulsifiers on skin lipids and further deepen the understanding of enhancing substance penetration with reduced skin barrier properties and increased lipid fluidity. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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12 pages, 1044 KiB  
Article
Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis
by Antonella Casiraghi, Chiara Grazia Gennari, Umberto Maria Musazzi, Marco Aldo Ortenzi, Susanna Bordignon and Paola Minghetti
Pharmaceutics 2020, 12(3), 211; https://doi.org/10.3390/pharmaceutics12030211 - 1 Mar 2020
Cited by 20 | Viewed by 3799
Abstract
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal inflammatory disease for which off-label topical corticosteroids (e.g., budesonide) are widely used in clinic. In general, thickening excipients are mixed with industrial products to improve the residence time of the drug on the esophageal mucosa. [...] Read more.
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal inflammatory disease for which off-label topical corticosteroids (e.g., budesonide) are widely used in clinic. In general, thickening excipients are mixed with industrial products to improve the residence time of the drug on the esophageal mucosa. The compounding procedures are empirical and the composition is not supported by real physicochemical and technological characterization. The current study aimed to propose a standardized budesonide oral formulation intended to improve the resistance time of the drug on the esophageal mucosa for EE treatment. Different placebo and drug-loaded (0.025% w/w) formulations were prepared by changing the percentage of xanthan gum alone or in ratio 1:1 with guar gum. Both excipients were added in the composition for their mucoadhesive properties. The formulative space was rationalized based on the drug physicochemical stability and the main critical quality attributes of the formulation, e.g., rheological properties, syringeability, mucoadhesiveness and in vitro penetration of budesonide in porcine esophageal tissue. The obtained results demonstrated that gums allowed a prolonged residence time. However, the concentration of the mucoadhesive polymer has to be rationalized appropriately to permit the syringeability of the formulation and, therefore, easy dosing by the patient/caregiver. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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10 pages, 3908 KiB  
Article
Oleogels with Birch Bark Dry Extract: Extract Saving Formulations through Gelation Enhancing Additives
by Kashif Ahmad Ghaffar and Rolf Daniels
Pharmaceutics 2020, 12(2), 184; https://doi.org/10.3390/pharmaceutics12020184 - 21 Feb 2020
Cited by 9 | Viewed by 3543
Abstract
Triterpenes from the outer bark of birch have many beneficial biological and pharmacological activities. In particular, its wound healing efficacy is of paramount importance. Apart from that, particles of a birch bark dry extract aggregate into a three dimensional network when they are [...] Read more.
Triterpenes from the outer bark of birch have many beneficial biological and pharmacological activities. In particular, its wound healing efficacy is of paramount importance. Apart from that, particles of a birch bark dry extract aggregate into a three dimensional network when they are dispersed in lipids yielding a semi-solid oleogel. However, gel formation requires high amounts of the extract, which then acts at once as the active ingredient and the gelling agent. Infrared spectra of the respective mixtures proved that hydrogen bonds play a crucial role in the formation of the gel network. Dicarboxylic acids had almost no effect on gel strength. Monoalcohols increased the firmness of the oleogel with a decreasing effect from methanol > ethanol > butanol > octanol. All tested terminal diols increased the gel strength whereas vicinal diols affected the gel strength negatively. The effect was highly dependent on their concentration. The different effects of the diols are linked to their structure and polarity. The most pronounced enhancement of gelation was found for 1,6-hexanediol, which reduced the amount of triterpene extract (TE), which is necessary for the formation of an oleogel by a factor of 10. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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16 pages, 3767 KiB  
Article
Topical Amphotericin B Semisolid Dosage Form for Cutaneous Leishmaniasis: Physicochemical Characterization, Ex Vivo Skin Permeation and Biological Activity
by Diana Berenguer, Maria Magdalena Alcover, Marcella Sessa, Lyda Halbaut, Carme Guillén, Antoni Boix-Montañés, Roser Fisa, Ana Cristina Calpena-Campmany, Cristina Riera and Lilian Sosa
Pharmaceutics 2020, 12(2), 149; https://doi.org/10.3390/pharmaceutics12020149 - 12 Feb 2020
Cited by 25 | Viewed by 4067
Abstract
Amphotericin B (AmB) is a potent antifungal successfully used intravenously to treat visceral leishmaniasis but depending on the Leishmania infecting species, it is not always recommended against cutaneous leishmaniasis (CL). To address the need for alternative topical treatments of CL, the aim of [...] Read more.
Amphotericin B (AmB) is a potent antifungal successfully used intravenously to treat visceral leishmaniasis but depending on the Leishmania infecting species, it is not always recommended against cutaneous leishmaniasis (CL). To address the need for alternative topical treatments of CL, the aim of this study was to elaborate and characterize an AmB gel. The physicochemical properties, stability, rheology and in vivo tolerance were assayed. Release and permeation studies were performed on nylon membranes and human skin, respectively. Toxicity was evaluated in macrophage and keratinocyte cell lines, and the activity against promastigotes and intracellular amastigotes of Leishmania infantum was studied. The AmB gel remained stable for a period of two months, with optimal properties for topical use and no apparent toxic effect on the cell lines. High amounts of AmB were found in damaged and non-damaged skin (1230.10 ± 331.52 and 2484.57 ± 439.12 µg/g/cm2, respectively) and they were above the IC50 of AmB for amastigotes. Although there were no differences in the in vitro anti-leishmanial activity between the AmB solution and gel, the formulation resulted in a higher amount of AmB being retained in the skin, and is therefore a candidate for further studies of in vivo efficacy. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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14 pages, 790 KiB  
Article
A Validated IVRT Method to Assess Topical Creams Containing Metronidazole Using a Novel Approach
by Seeprarani Rath and Isadore Kanfer
Pharmaceutics 2020, 12(2), 119; https://doi.org/10.3390/pharmaceutics12020119 - 3 Feb 2020
Cited by 18 | Viewed by 5687
Abstract
An IVRT method was developed and validated to confirm its reproducibility, precision, sensitivity, selectivity, accuracy, robustness, and reliability. A novel approach was used to demonstrate the appropriateness of the IVRT method to accurately assess “sameness” between topical products and to confirm that the [...] Read more.
An IVRT method was developed and validated to confirm its reproducibility, precision, sensitivity, selectivity, accuracy, robustness, and reliability. A novel approach was used to demonstrate the appropriateness of the IVRT method to accurately assess “sameness” between topical products and to confirm that the methodology applied also possesses the requisite discriminatory power to detect differences should such differences exist between products. In the first instance, the reference product (Metrocreme®) containing 0.75% metronidazole (MTZ) was tested against itself as a positive control, to accurately demonstrate “sameness”, where the results met the relevant acceptance criteria falling within the limits of 75–133.33% in accordance with the FDA’s SUPAC-SS guidance. In addition, two specially prepared creams containing 25% less and 26% more MTZ, i.e., 0.563% and 0.945%, served as negative controls and were compared against the reference product. Neither of these creams fell within the “sameness” acceptance criteria, thereby confirming the discriminatory ability of the IVRT method to detect differences between MTZ products. Furthermore, another cream containing 0.75% MTZ tested against the reference product was shown to be pharmaceutically equivalent to the reference product. These results confirm the appropriateness of the IVRT method as a valuable tool for use in the development of topical MTZ products intended for local action and indicate the potential for general use with other topical products. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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14 pages, 2237 KiB  
Article
Curcumin-In-Deformable Liposomes-In-Chitosan-Hydrogel as a Novel Wound Dressing
by Selenia Ternullo, Laura Victoria Schulte Werning, Ann Mari Holsæter and Nataša Škalko-Basnet
Pharmaceutics 2020, 12(1), 8; https://doi.org/10.3390/pharmaceutics12010008 - 20 Dec 2019
Cited by 60 | Viewed by 6763
Abstract
A liposomes-in-hydrogel system as an advanced wound dressing for dermal delivery of curcumin was proposed for improved chronic wound therapy. Curcumin, a multitargeting poorly soluble active substance with known beneficial properties for improved wound healing, was incorporated in deformable liposomes to overcome its [...] Read more.
A liposomes-in-hydrogel system as an advanced wound dressing for dermal delivery of curcumin was proposed for improved chronic wound therapy. Curcumin, a multitargeting poorly soluble active substance with known beneficial properties for improved wound healing, was incorporated in deformable liposomes to overcome its poor solubility. Chitosan hydrogel served as a vehicle providing superior wound healing properties. The novel system should assure sustained skin delivery of curcumin, and increase its retention at the skin site, utilizing both curcumin and chitosan to improve the therapy outcome. To optimize the properties of the formulation and determine the effect of the liposomal charge on the hydrogel properties, curcumin-containing deformable liposomes (DLs) with neutral (NDLs), cationic (CDLs), and anionic (ADLs) surface properties were incorporated in chitosan hydrogel. The charged DLs affected the hydrogel’s hardness, cohesiveness, and adhesiveness. Importantly, the incorporation of DLs, regardless of their surface charge, in chitosan hydrogel did not decrease the system’s bioadhesion to human skin. Stability testing revealed that the incorporation of CDLs in hydrogel preserved hydrogel´s bioadhesiveness to a higher degree than both NDLs and ADLs. In addition, CDLs-in-hydrogel enabled the most sustained skin penetration of curcumin. The proposed formulation should be further evaluated in a chronic wound model. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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13 pages, 2521 KiB  
Article
Topical Delivery of Niacinamide: Influence of Binary and Ternary Solvent Systems
by Yanling Zhang, Chin-Ping Kung, Bruno C. Sil, Majella E. Lane, Jonathan Hadgraft, Michael Heinrich and Balint Sinko
Pharmaceutics 2019, 11(12), 668; https://doi.org/10.3390/pharmaceutics11120668 - 10 Dec 2019
Cited by 12 | Viewed by 6201
Abstract
Niacinamide (NIA) is the amide form of vitamin B3 and has been widely used in pharmaceutical and personal care formulations. Previously, we reported a comparative study of NIA permeation from neat solvents using the Skin Parallel Artificial Membrane Permeability Assay (PAMPA) and mammalian [...] Read more.
Niacinamide (NIA) is the amide form of vitamin B3 and has been widely used in pharmaceutical and personal care formulations. Previously, we reported a comparative study of NIA permeation from neat solvents using the Skin Parallel Artificial Membrane Permeability Assay (PAMPA) and mammalian skin. A good correlation between NIA permeation in the different models was found. In the present work, ten binary and ternary systems were evaluated for their ability to promote NIA delivery in the Skin PAMPA model, porcine skin and human epidermis. Penetration enhancement was evident for binary systems composed of propylene glycol and fatty acids in human skin studies. However, propylene glycol and oleic acid did not promote enhancement of NIA compared with other systems in the Skin PAMPA model. A good correlation was obtained for permeation data from Skin PAMPA and porcine skin. However, data from the Skin PAMPA model and from human skin could only be correlated when the PG-fatty acid systems were excluded. These findings add to our knowledge of the potential applications of Skin PAMPA for screening dermal/transdermal preparations. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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14 pages, 2787 KiB  
Article
Preparation, Characterization and Dermal Delivery of Methadone
by Chin-Ping Kung, Bruno C. Sil, Jonathan Hadgraft, Majella E. Lane, Bhumik Patel and Renée McCulloch
Pharmaceutics 2019, 11(10), 509; https://doi.org/10.3390/pharmaceutics11100509 - 2 Oct 2019
Cited by 10 | Viewed by 6036
Abstract
The use of methadone for the management of pain has received great interest in recent years. Currently, oral and intravenous formulations are available for clinical use. Dermal delivery represents an attractive alternative route of administration for this drug as it is associated with [...] Read more.
The use of methadone for the management of pain has received great interest in recent years. Currently, oral and intravenous formulations are available for clinical use. Dermal delivery represents an attractive alternative route of administration for this drug as it is associated with comparatively fewer side effects. The first stage of the work was the preparation of methadone free base as this form of the drug is expected to permeate the skin to a greater extent than the hydrochloride salt. Subsequently the molecule was characterized with Nuclear Magnetic Resonance (NMR) and thermal analysis, the distribution coefficient was determined and solubility studies were conducted in a range of solvents. In vitro permeation and mass balance studies were conducted under finite dose conditions (5 μL/cm2) in porcine skin. The results confirmed the more favorable penetration of methadone free base compared with the salt. The highest cumulative amount of methadone (41 ± 5 μg/cm2) permeated from d-limonene (LIM). Ethyl oleate (EO), Transcutol® P (TC) and octyl salicylate (OSAL) also appear to be promising candidate components of dermal formulations for methadone base. Future work will focus on further formulation optimization with the objective of progressing to evaluation of prototype dosage forms in clinical trials. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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18 pages, 5429 KiB  
Article
In Situ Hydrogel-Forming/Nitric Oxide-Releasing Wound Dressing for Enhanced Antibacterial Activity and Healing in Mice with Infected Wounds
by Juho Lee, Shwe Phyu Hlaing, Jiafu Cao, Nurhasni Hasan, Hye-Jin Ahn, Ki-Won Song and Jin-Wook Yoo
Pharmaceutics 2019, 11(10), 496; https://doi.org/10.3390/pharmaceutics11100496 - 27 Sep 2019
Cited by 56 | Viewed by 6055
Abstract
The eradication of bacteria from wound sites and promotion of healing are essential for treating infected wounds. Nitric oxide (NO) is desirable for these purposes due to its ability to accelerate wound healing and its broad-spectrum antibacterial effects. We developed an in situ [...] Read more.
The eradication of bacteria from wound sites and promotion of healing are essential for treating infected wounds. Nitric oxide (NO) is desirable for these purposes due to its ability to accelerate wound healing and its broad-spectrum antibacterial effects. We developed an in situ hydrogel-forming/NO-releasing powder dressing (NO/GP), which is a powder during storage and forms a hydrogel when applied to wounds, as a novel NO-releasing formulation to treat infected wounds. An NO/GP fine powder (51.5 μm) was fabricated by blending and micronizing S-nitrosoglutathione (GSNO), alginate, pectin, and polyethylene glycol (PEG). NO/GP remained stable for more than four months when stored at 4 or 37 °C. When applied to wounds, NO/GP absorbed wound fluid and immediately converted to a hydrogel. Additionally, wound fluid triggered a NO release from NO/GP for more than 18 h. The rheological properties of hydrogel-transformed NO/GP indicated that NO/GP possesses similar adhesive properties to marketed products (Vaseline). NO/GP resulted in a 6-log reduction in colony forming units (CFUs) of methicillin resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, which are representative drug-resistant gram-positive and -negative bacteria, respectively. The promotion of wound healing by NO/GP was demonstrated in mice with full-thickness wounds challenged with MRSA and P. aeruginosa. Thus, NO/GP is a promising formulation for the treatment of infected wounds. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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14 pages, 2026 KiB  
Article
Dermal Delivery of the High-Molecular-Weight Drug Tacrolimus by Means of Polyglycerol-Based Nanogels
by Fiorenza Rancan, Hildburg Volkmann, Michael Giulbudagian, Fabian Schumacher, Jessica Isolde Stanko, Burkhard Kleuser, Ulrike Blume-Peytavi, Marcelo Calderón and Annika Vogt
Pharmaceutics 2019, 11(8), 394; https://doi.org/10.3390/pharmaceutics11080394 - 5 Aug 2019
Cited by 22 | Viewed by 4738
Abstract
Polyglycerol-based thermoresponsive nanogels (tNGs) have been shown to have excellent skin hydration properties and to be valuable delivery systems for sustained release of drugs into skin. In this study, we compared the skin penetration of tacrolimus formulated in tNGs with a commercial 0.1% [...] Read more.
Polyglycerol-based thermoresponsive nanogels (tNGs) have been shown to have excellent skin hydration properties and to be valuable delivery systems for sustained release of drugs into skin. In this study, we compared the skin penetration of tacrolimus formulated in tNGs with a commercial 0.1% tacrolimus ointment. The penetration of the drug was investigated in ex vivo abdominal and breast skin, while different methods for skin barrier disruption were investigated to improve skin permeability or simulate inflammatory conditions with compromised skin barrier. The amount of penetrated tacrolimus was measured in skin extracts by liquid chromatography tandem-mass spectrometry (LC-MS/MS), whereas the inflammatory markers IL-6 and IL-8 were detected by enzyme-linked immunosorbent assay (ELISA). Higher amounts of tacrolimus penetrated in breast as compared to abdominal skin or in barrier-disrupted as compared to intact skin, confirming that the stratum corneum is the main barrier for tacrolimus skin penetration. The anti-proliferative effect of the penetrated drug was measured in skin tissue/Jurkat cells co-cultures. Interestingly, tNGs exhibited similar anti-proliferative effects as the 0.1% tacrolimus ointment. We conclude that polyglycerol-based nanogels represent an interesting alternative to paraffin-based formulations for the treatment of inflammatory skin conditions. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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13 pages, 1515 KiB  
Article
Optimization of Rheological Behaviour and Skin Penetration of Thermogelling Emulsions with Enhanced Substantivity for Potential Application in Treatment of Chronic Skin Diseases
by Markus Schmidberger, Ines Nikolic, Ivana Pantelic and Dominique Lunter
Pharmaceutics 2019, 11(8), 361; https://doi.org/10.3390/pharmaceutics11080361 - 24 Jul 2019
Cited by 9 | Viewed by 3388
Abstract
Topical formulations are an important pillar in the therapy of skin diseases. Nevertheless, after application the formulation will be exposed to environmental effects. Contact with other surfaces will reduce the available amount of formulation and drug substance. The resulting consequences for therapy range [...] Read more.
Topical formulations are an important pillar in the therapy of skin diseases. Nevertheless, after application the formulation will be exposed to environmental effects. Contact with other surfaces will reduce the available amount of formulation and drug substance. The resulting consequences for therapy range from reduced effects to therapeutic failure. The removed active ingredient also contaminates patients’ environment. The aim of this work was to develop preparations that remain at the application site. These will enhance safety and efficiency and thus improve of skin disease therapies. Therefore, we developed polymer-stabilised emulsions that show thermogelling properties. Emulsions with different methyl cellulose concentrations and macrogols of different molecular weights were investigated. The dispersed phase consisted of nonivamide as the active pharmaceutical ingredient, dissolved in medium-chain triglycerides. Rheological properties, droplet size, substantivity and ex vivo penetration experiments were performed to characterise the developed formulations. Droplet size and rheological parameters were affected by the composition of the preparations. The tested formulations showed benefits in their substantivity compared to a conventional semi-solid cream. We found a residual amount of up to 100% at the application site. The drug levels in viable epidermis were in a therapeutic range. The developed emulsions are a promising vehicle to improve therapy for chronic skin diseases. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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11 pages, 2256 KiB  
Article
Nanostructured Lipid Carrier Gel for the Dermal Application of Lidocaine: Comparison of Skin Penetration Testing Methods
by Stella Zsikó, Kendra Cutcher, Anita Kovács, Mária Budai-Szűcs, Attila Gácsi, Gabriella Baki, Erzsébet Csányi and Szilvia Berkó
Pharmaceutics 2019, 11(7), 310; https://doi.org/10.3390/pharmaceutics11070310 - 2 Jul 2019
Cited by 33 | Viewed by 5330
Abstract
The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured lipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test the penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin penetration [...] Read more.
The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured lipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test the penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin penetration modeling methods. The formulations were characterized by laser diffraction, rheological measurements and microscopic examinations. Various in vitro methods were used to study drug release, diffusion and penetration. Two types of vertical Franz diffusion cells with three different membranes, including cellulose, Strat-M®, and heat separated human epidermis were used and compared to the Skin-parallel artificial membrane permeability assay (PAMPA) method. Results indicated that the nanostructured lipid carrier dispersion had to be gelified as soon as possible for proper stability. Both the Skin-PAMPA model and Strat-M® membranes correlated favorably with heat separated human epidermis in this research, with the Strat-M® membranes sharing the most similar drug permeability profile to an ex vivo human skin model. Our experimental findings suggest that even when the best available in vitro experiment is selected for modeling human skin penetration to study nanostructured lipid carrier gel systems, relevant in vitro/in vivo correlation should be made to calculate the drug release/permeation in vivo. Future investigations in this field are still needed to demonstrate the influence of membranes and equipment from other classes on other drug candidates. Full article
(This article belongs to the Special Issue Semisolid Dosage)
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Other

Jump to: Editorial, Research

2 pages, 171 KiB  
Reply
Reply to “Comment on Casiraghi et al. ‘Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis’ 2020, 12, 211”
by Antonella Casiraghi, Chiara Grazia Gennari, Umberto Maria Musazzi, Marco Aldo Ortenzi, Susanna Bordignon and Paola Minghetti
Pharmaceutics 2020, 12(9), 822; https://doi.org/10.3390/pharmaceutics12090822 - 28 Aug 2020
Cited by 8 | Viewed by 2009
Abstract
The paper entitled “Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis Pharmaceutics 2020, 12, 211” discusses the physicochemical and technological characterization of a formulation to treat eosinophilic esophagitis [...] Full article
(This article belongs to the Special Issue Semisolid Dosage)
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