[go: up one dir, main page]
More Web Proxy on the site http://driver.im/
You seem to have javascript disabled. Please note that many of the page functionalities won't work as expected without javascript enabled.
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
7.9
4.9
Journals
Pharmaceutics
Special Issues
Pharmaceutical Excipients: Impact on Efficiency, Stability, and Solubility in Formulation
share announcement

Pharmaceutical Excipients: Impact on Efficiency, Stability, and Solubility in Formulation

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

Deadline for manuscript submissions: 31 July 2025 | Viewed by 920

Special Issue Editors

Prof. Dr. Laura Sbârcea

E-Mail Website
Guest Editor
Department of Drug Analysis, Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: drug solubility; cyclodextrin-based delivery systems; drug analysis and quality control; drug stability; drug–drug interactions; drug-excipient interactions
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Adriana Violeta Ledeți

E-Mail Website
Guest Editor
Department of Analytical Chemistry, Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: drug stability and stabilization techniques; instrumental analysis of active pharmaceutical ingredients; heterogenous degradation of drugs; solid-state kinetics; supramolecular systems with increased biopharmaceutical profile
Special Issues, Collections and Topics in MDPI journals
Dr. Denisa Laura Ivan

E-Mail Website
Guest Editor
Department of Analytical Chemistry , Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: stability of drugs and compounds with potential biological activity; instrumental analysis of drugs as pure APIs and in pharmaceutical dosage forms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmaceutical excipients are substances, other than the active pharmaceutical ingredient (API), of invaluable importance for the final dosage forms. They facilitate the manufacture, stability, patient compliance, and administration of pharmaceutical formulations and also possess various functional roles that include modulating the solubility and bioavailability of APIs, delivering APIs, maintaining the osmolarity and pH of the liquid formulations, and preventing aggregation and dissociation. Nowadays, pharmaceutical excipients have gained the attention of researchers due to the growth of novel drug delivery systems that led to an increase in the number of the excipients, the development of new co-processed excipient mixtures, and also because of their potential to alter the pharmacokinetic profile of drugs. The quality, efficiency, safety, and stability of the finished pharmaceutical formulations highly depend on the choice of excipients, their concentration, and their interaction with APIs and with each other.

This Special Issue aims to collect research dedicated to all aspects of the excipients in pharmaceutical and cosmetic formulations. In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following: drug–excipient compatibility studies; the effect of excipients on metabolic enzymes; the solubility of natural and synthetic active substances; drug release; and issues related to drug stability.

We look forward to receiving your contributions.

Prof. Dr. Laura Sbârcea
Prof. Dr. Adriana Violeta Ledeți
Dr. Denisa Laura Ivan
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. Pharmaceutics is an international peer-reviewed open access monthly 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 2900 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

  • excipient
  • drug-excipient interaction
  • drug solubility
  • cyclodextrins
  • solid-state kinetics
  • drug delivery systems
  • drug release
  • bioavailability

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • e-Book format: Special Issues with more than 10 articles can be published as dedicated e-books, ensuring wide and rapid dissemination.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (1 paper)

Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

25 pages, 9926 KiB  
Article
A Novel Natural Penetration Enhancer for Transdermal Drug Delivery: In Vitro/In Vivo Evaluation and Penetration Enhancement Mechanism
by Nanxi Zhao, Jiale Hao, Yucong Zhao, Bingqian Zhao, Jiayu Lin, Jian Song, Manli Wang and Zheng Luo
Pharmaceutics 2025, 17(2), 254; https://doi.org/10.3390/pharmaceutics17020254 - 14 Feb 2025
Viewed by 429
Abstract
Objectives: This study aimed to identify and develop a novel, safe, and effective transdermal penetration enhancer derived from the leaves of Perilla frutescens (L.) Britt, and to explore the underlying mechanisms of its penetration enhancement effects. Methods: To evaluate the safety [...] Read more.
Objectives: This study aimed to identify and develop a novel, safe, and effective transdermal penetration enhancer derived from the leaves of Perilla frutescens (L.) Britt, and to explore the underlying mechanisms of its penetration enhancement effects. Methods: To evaluate the safety profile of the penetration enhancer, both skin irritation tests and histopathological analyses were conducted. The transdermal enhancement capabilities of the penetration enhancer were assessed in vitro using five model drugs. Furthermore, to gain insights into the penetration enhancement mechanism of this novel penetration enhancer, a range of analytical methods were used, including a spectroscopic technique, differential scanning calorimetry, micro-optical techniques, and molecular docking simulations. Results: Perilla essential oil contained 93.70% perilla ketone (PEK), which exhibited a safety profile superior to that of azone. PEK significantly increased the cumulative skin permeation of all the model drugs (p < 0.05). PEK exhibited the most obvious impact on puerarin penetration, with quantitative enhancement ratios of 2.96 ± 0.07 and 3.39 ± 0.21 at concentrations of 3% and 5% (w/v), respectively. A strong correlation between the enhancement effect of PEK and the physicochemical properties of the drugs was observed. Mechanistic studies revealed that PEK facilitates drug distribution from the solution phase to the stratum corneum (SC). Conclusions: PEK, seldom discussed in former studies, was observed to show extensive penetration enhancement effects by inducing conformational changes in SC lipids and disrupting the tightly ordered bilayer arrangement of lipids. These findings highlight the potential of PEK as a promising and safe natural transdermal penetration enhancer. Full article
(This article belongs to the Special Issue Pharmaceutical Excipients: Impact on Efficiency, Stability, and Solubility in Formulation)
►▼ Show Figures

Graphical abstract

Graphical abstract
Full article ">Figure 1
<p>Chemical structures of the model drugs.</p> Full article ">Figure 2
<p>Flowchart for the PO preparation and evaluation processes. (GC-MS: gas chromatography–mass spectrometry; <sup>1</sup>H NMR: proton nuclear magnetic resonance; PEK: perilla ketone; SC: stratum corneum; ATR-FTIR: attenuated total reflectance–Fourier transform infrared spectroscopy; DSC: differential scanning calorimetry; CLSM: confocal laser scanning microscope; SEM: scanning electron microscope; MS: molecular dynamics simulation; MD: molecular docking; TEWL: transepidermal water loss).</p> Full article ">Figure 3
<p>Chemical structures of the three compounds in PO. (PO: perilla essential oil; PEK: perilla ketone; β-CP: β-caryophyllene; α-FE: (<span class="html-italic">Z</span>,<span class="html-italic">E</span>)-α-farnesene).</p> Full article ">Figure 4
<p>Dynamic skin irritation caused by penetration enhancers (<span class="html-italic">n</span> = 4, <span class="html-italic">EI</span>: erythema index; PEK: perilla ketone).</p> Full article ">Figure 5
<p>Histological pictures of the skin treated with penetration enhancers. (<b>a</b>) Skin without treatment. (<b>b</b>) Skin treated with azone. (<b>c</b>) Skin treated with 3% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<b>d</b>) Skin treated with 5% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (H&amp;E staining: 200×; PEK: perilla ketone).</p> Full article ">Figure 6
<p>Enhancement effects of PEK on different model drugs (mean ± SD, <span class="html-italic">n</span> = 4; * <span class="html-italic">p</span> &lt; 0.05 compared to the 3% PEK group; <span class="html-italic">QER</span>: quantitative enhancement ratio; PEK: perilla ketone).</p> Full article ">Figure 7
<p>Response surface plot illustrating the effects of <span class="html-italic">KER</span> and <span class="html-italic">PER</span> on <span class="html-italic">QER</span>. (<b>a</b>) The perilla ketone concentration was 3% (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<b>b</b>) The perilla ketone concentration was 5% (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<span class="html-italic">QER</span>: quantitative enhancement ratio; <span class="html-italic">PER</span>: enhancement ratio of the drug permeability coefficient; <span class="html-italic">KER</span>: partition enhancement ratio for drug distribution to the stratum corneum).</p> Full article ">Figure 8
<p>Response surface plot illustrating the effects of PSA and H-bond donor on <span class="html-italic">KER</span>. (<b>a</b>) The perilla ketone concentration was 3% (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<b>b</b>) The perilla ketone concentration was 5% (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<span class="html-italic">PSA</span>: polar surface area; <span class="html-italic">KER</span>: partition enhancement ratio for drug distribution to the stratum corneum).</p> Full article ">Figure 9
<p>The correlation between the <span class="html-italic">PER</span> and ∆<span class="html-italic">δ</span>. (<span class="html-italic">PER</span>: enhancement ratio of the drug permeability coefficient; PEK: perilla ketone; Δ<span class="html-italic">δ</span>: the difference in solubility parameters).</p> Full article ">Figure 10
<p>Mechanism by which PEK enhances a drug’s skin permeation (PEK: perilla ketone).</p> Full article ">Figure 11
<p>ATR-FTIR spectra with or without PEK (PEK: perilla ketone).</p> Full article ">Figure 12
<p>DSC curve of the SC with or without PEK (<span class="html-italic">T</span><sub>m</sub>: transition temperature; PEK: perilla ketone).</p> Full article ">Figure 13
<p>CLSM optical images of the skin at different depths after treatment with PEK. (<b>a</b>) Skin without treatment. (<b>b</b>) Skin treated with 3% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<b>c</b>) Skin treated with 5% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (PEK: perilla ketone).</p> Full article ">Figure 14
<p>Microstructure of the rat skin’s SC after treatment with PEK. (<b>a</b>) Skin without treatment. (<b>b</b>) Skin treated with donor vehicle IPP. (<b>c</b>) Skin treated with 3% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (<b>d</b>) Skin treated with 5% PEK (<span class="html-italic">w</span>/<span class="html-italic">v</span>). (IPP: isopropyl palmitate; PEK: perilla ketone).</p> Full article ">Figure 15
<p>Snapshots of the optimal binding sites for hydrogen bonds between each group of molecules. (<b>a</b>) Binding site between NP and NP. (<b>b</b>) Binding site between NP and PEK. (<b>c</b>) Binding site between NP and ferulic acid. (<b>d</b>) Binding site between NP-PEK and ferulic acid. (<b>e</b>) Binding site between NP and rutin. (<b>f</b>) Binding site between NP-PEK and rutin. (<b>g</b>) Binding site between NP and paeoniflorin. (<b>h</b>) Binding site between NP-PEK and paeoniflorin. (<b>i</b>) Binding site between NP and puerarin. (<b>j</b>) Binding site between NP-PEK and puerarin. (<b>k</b>) Binding site between NP and luteolin. (<b>l</b>) Binding site between NP-PEK and luteolin. (Gray: carbon; red: oxygen; blue: nitrogen; white: hydrogen. H-bonds are presented as light green dotted lines; H-bond energy values are described in orange letters; NP: ceramide NP; PEK: perilla ketone).</p> Full article ">Figure 16
<p>Snapshots of the simulated systems at the end stage of the MS. (<b>a</b>) PEK in NP box. (<b>b</b>) α-FE in NP box. (<b>c</b>) β-CP in NP box. (NP: ceramide NP; PEK: perilla ketone; β-CP: β-caryophyllene; α-FE: (<span class="html-italic">Z</span>,<span class="html-italic">E</span>)-α-farnesene).</p> Full article ">Figure 17
<p>TEWL of the rat skin after treatment with different penetration enhancers (<span class="html-italic">n</span> = 4, PEK: perilla ketone; TEWL: transepidermal water loss).</p> Full article ">
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-1
Back to TopTop