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Molecules
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Role of Amphiphil tensides in pharmaceutical formulations
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Role of Amphiphil tensides in pharmaceutical formulations

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 July 2021) | Viewed by 20004

Special Issue Editors

Prof. Dr. Ildikó Bácskay

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Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: assessment of biocompatibility; drug delivery system formulation; application of macromolecules; characterization of dosage forms; in vitro dissolution studies; SEDDS
Special Issues, Collections and Topics in MDPI journals
Dr. Pálma Fehér

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Assistant Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary
Interests: topical drug delivery; semi-solid pharmaceutical dosage forms; self-emulsifying drug delivery systems; nanocarriers; surfactants; in vitro studies; pharmaceutical technology; drug release; skin permeation
Special Issues, Collections and Topics in MDPI journals
Dr. Zoltan Ujhelyi

E-Mail Website
Assistant Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary
Interests: pharmaceutical research and development; nanotechnology; permeability enhancement
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

Surface-active agents are widely used in new pharmaceutical dosage form development to improve the bioavailability of drugs which have low solubility in water. They can influence drug permeability and enhance APIs’ absorption. On the other hand, surfactants can cause local irritations, membrane damage, and cell death, and therefore, special biocompatibility investigations are performed to assess their level of harm.

Different types of amphiphil tensides are used in topical formulations, especially in ointments that have emulsion bases and in creams that are o/w emulsion type. The property of the emulsifying agent may also influence the penetration of active substance from topical dosage forms. However, it is very important to examine the biocompatibility of these surfactants and to determine the non-toxic concentration range of these excipients as well.

The aim of this Special Issue is to go deep into those pharmaceutical formulations which contain amphiphil tensides. A special point to consider is the assessment of the biocompatibility of these formulations. In this Special Issue we are also waiting for articles from topical pharmaceutical formulations which contain amphiphil tensides. To determine the biocompatibility of these surfactants alone and in topical formulations is an important point of view in this Special Issue.  

As Guest Editors, we cordially invite you to contribute a research paper or review on any aspect related to this topic.

Dr. Ildikó Bácskay
Dr. Zoltán Ujhelyi
Dr. Pálma Fehér
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Amphiphilic tensides
  • Biocompatibility
  • Innovative formulation

Published Papers (4 papers)

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Research

16 pages, 4282 KiB  
Article
Formulation of Novel Liquid Crystal (LC) Formulations with Skin-Permeation-Enhancing Abilities of Plantago lanceolata (PL) Extract and Their Assessment on HaCaT Cells
by Dóra Kósa, Ágota Pető, Ferenc Fenyvesi, Judit Váradi, Miklós Vecsernyés, Sándor Gonda, Gábor Vasas, Pálma Fehér, Ildikó Bácskay and Zoltán Ujhelyi
Molecules 2021, 26(4), 1023; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26041023 - 15 Feb 2021
Cited by 8 | Viewed by 3008
Abstract
Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can [...] Read more.
Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can be used to improve the effects of these phytopharmacons. The bioactive compounds of Plantago lanceolata (PL) possess different effects, such as anti-inflammatory, antioxidant, and bactericidal pharmacological effects. The objective of this study was to formulate novel liquid crystal (LC) compositions to protect Plantago lanceolata extract from hydrolysis and to improve its effect. Since safety is an important aspect of pharmaceutical formulations, the biological properties of applied excipients and blends were evaluated using assorted in vitro methods on HaCaT cells. According to the antecedent toxicity screening evaluation, three surfactants were selected (Gelucire 44/14, Labrasol, and Lauroglycol 90) for the formulation. The dissolution rate of PL from the PL-LC systems was evaluated using a Franz diffusion chamber apparatus. The antioxidant properties of the PL-LC systems were evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and malondialdehyde (MDA) assessments. Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum. These excipients can be safe and highly tolerable thus, they could improve the patient’s experience and promote adherence. Full article
(This article belongs to the Special Issue Role of Amphiphil tensides in pharmaceutical formulations)
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26 pages, 4702 KiB  
Article
Formulation of Topical Dosage Forms Containing Synthetic and Natural Anti-Inflammatory Agents for the Treatment of Rheumatoid Arthritis
by Tunde Jurca, Liza Józsa, Ramona Suciu, Annamaria Pallag, Eleonora Marian, Ildikó Bácskay, Mariana Mureșan, Roxana Liana Stan, Mariana Cevei, Felicia Cioară, Laura Vicaș and Pálma Fehér
Molecules 2021, 26(1), 24; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26010024 - 23 Dec 2020
Cited by 11 | Viewed by 5479
Abstract
Topical anti-inflammatory and analgesic effect for the treatment of rheumatoid arthritis is of major interest because of their fewer side effects compared to oral therapy. The purpose of this study was to prepare different types of topical formulations (ointments and gels) containing synthetic [...] Read more.
Topical anti-inflammatory and analgesic effect for the treatment of rheumatoid arthritis is of major interest because of their fewer side effects compared to oral therapy. The purpose of this study was to prepare different types of topical formulations (ointments and gels) containing synthetic and natural anti-inflammatory agents with different excipients (e.g.,: surfactants, gel-forming) for the treatment of rheumatoid arthritis. The combination of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), diclofenac sodium, a topical analgesic agent methyl salicylate, and a lyophilized extract of Calendula officinalis with antioxidant effect were used in our formulations. The aim was to select the appropriate excipients and dosage form for the formulation in order to enhance the diffusion of active substances and to certify the antioxidant, analgesic, and anti-inflammatory effects of these formulations. To characterize the physicochemical properties of the formulations, rheological studies, and texture profile analysis were carried out. Membrane diffusion and permeability studies were performed with Franz-diffusion method. The therapeutic properties of the formulations have been proven by an antioxidant assay and a randomized prospective study that was carried out on 115 patients with rheumatoid arthritis. The results showed that the treatment with the gel containing diclofenac sodium, methyl salicylate, and lyophilized Calendula officinalis as active ingredients, 2-propenoic acid homopolymer (Synthalen K) as gel-forming excipient, distilled water, triethanolamine, and glycerol had a beneficial analgesic and local anti-inflammatory effect. Full article
(This article belongs to the Special Issue Role of Amphiphil tensides in pharmaceutical formulations)
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14 pages, 2380 KiB  
Article
Effects of Sucrose Palmitate on the Physico-Chemical and Mucoadhesive Properties of Buccal Films
by András Kelemen, Bálint Katona, Szilvia Módra, Zoltán Aigner, István Sebe, Klára Pintye-Hódi, Romána Zelkó, Géza Regdon, Jr. and Katalin Kristó
Molecules 2020, 25(22), 5248; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25225248 - 11 Nov 2020
Cited by 8 | Viewed by 2182
Abstract
In our current research, sucrose palmitate (SP) was applied as a possible permeation enhancer for buccal use. This route of administration is a novelty as there is no literature on the use of SP in buccal mucoadhesive films. Films containing SP were prepared [...] Read more.
In our current research, sucrose palmitate (SP) was applied as a possible permeation enhancer for buccal use. This route of administration is a novelty as there is no literature on the use of SP in buccal mucoadhesive films. Films containing SP were prepared at different temperatures, with different concentrations of SP and different lengths of hydroxypropyl methylcellulose (HPMC) chains. The mechanical, structural, and in vitro mucoadhesive properties of films containing SP were investigated. Tensile strength and mucoadhesive force were measured with a device and software developed in our Institute. Positron annihilation lifetime spectroscopy (PALS) and X-ray powder diffractometry (XRPD) were applied for the structure analysis of the films. Mucoadhesive work was calculated in two ways: from the measured contact angle and compared with direct mucoadhesive work, which measured mucoadhesive force, which is direct mucoadhesion work. These results correlate linearly with a correlation coefficient of 0.98. It is also novel because it is a new method for the determination of mucoadhesive work. Full article
(This article belongs to the Special Issue Role of Amphiphil tensides in pharmaceutical formulations)
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23 pages, 2951 KiB  
Article
Formulation of Creams Containing Spirulina Platensis Powder with Different Nonionic Surfactants for the Treatment of Acne Vulgaris
by Liza Józsa, Zoltán Ujhelyi, Gábor Vasvári, Dávid Sinka, Dániel Nemes, Ferenc Fenyvesi, Judit Váradi, Miklós Vecsernyés, Judit Szabó, Gergő Kalló, Gábor Vasas, Ildikó Bácskay and Pálma Fehér
Molecules 2020, 25(20), 4856; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25204856 - 21 Oct 2020
Cited by 13 | Viewed by 8616
Abstract
Natural products used in the treatment of acne vulgaris may be promising alternative therapies with fewer side effects and without antibiotic resistance. The objective of this study was to formulate creams containing Spirulina (Arthrospira) platensis to be used in acne therapy. Spirulina platensis [...] Read more.
Natural products used in the treatment of acne vulgaris may be promising alternative therapies with fewer side effects and without antibiotic resistance. The objective of this study was to formulate creams containing Spirulina (Arthrospira) platensis to be used in acne therapy. Spirulina platensis belongs to the group of micro algae and contains valuable active ingredients. The aim was to select the appropriate nonionic surfactants for the formulations in order to enhance the diffusion of the active substance and to certify the antioxidant and antibacterial activity of Spirulina platensis-containing creams. Lyophilized Spirulina platensis powder (SPP) was dissolved in Transcutol HP (TC) and different types of nonionic surfactants (Polysorbate 60 (P60), Cremophor A6:A25 (CR) (1:1), Tefose 63 (TFS), or sucrose ester SP 70 (SP70)) were incorporated in creams as emulsifying agents. The drug release was evaluated by the Franz diffusion method and biocompatibility was tested on HaCaT cells. In vitro antioxidant assays were also performed, and superoxide dismutase (SOD) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays were executed. Antimicrobial activities of the selected compositions were checked against Staphylococcus aureus (S. aureus) and Cutibacteriumacnes (C. acnes) (formerly Propionibacterium acnes) with the broth microdilution method. Formulations containing SP 70 surfactant with TC showed the most favorable dissolution profiles and were found to be nontoxic. This composition also showed significant increase in free radical scavenger activity compared to the blank sample and the highest SOD enzyme activity was also detected after treatment with the cream samples. In antibacterial studies, significant differences were observed between the treated and control groups after an incubation time of 6 h. Full article
(This article belongs to the Special Issue Role of Amphiphil tensides in pharmaceutical formulations)
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