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Dear Colleagues,

Natural active principles still attract interest regarding their therapeutic purposes due to their lack of side effects, which makes them particularly appealing for the treatment of chronic diseases (e.g., hypertension and atherosclerosis).

However, strategies for optimising the delivery of natural compounds and enhancing their efficacy are still needed. Natural compounds, in fact, are often affected by low bioavailability, low stability or fast degradation.

Different strategies can be proposed, encompassing, for example, nano- or micro-carriers, polymer-based, lipid-based or oxide-based particles or hybrid systems, and specific formulations.

The present Special Issue aims to collect original research articles, review papers, or reviews regarding systems and approaches to delivering natural compounds, protecting them or enhancing their properties, with particular attention to oral and topical delivery.

Authors are encouraged to share their research on both the synthesis of new systems and their characterization. Works including in vitro and in vivo tests are welcome.

Potential topics concern, but are not limited to, the following:

Role of organic/inorganic carriers in natural active principle delivery;
Natural active principles to treat skin diseases (e.g., infection, cancer and psoriasis);
Delivery systems to improve natural active principles’ bioavailability and pharmacokinetics.

Dr. Marta Miola
Dr. Marta Gallo
Guest Editors

Manuscript Submission Information

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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.

Related Special Issue

Published Papers (2 papers)

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Research

8 pages, 666 KiB

Open AccessCommunication

Mesoporous Silica as an Alternative Vehicle to Overcome Solubility Limitations

by Tim Becker, Jan Heitkötter, Anna K. Krome, Andrea Schiefer, Kenneth Pfarr, Alexandra Ehrens, Miriam Grosse, Birthe Sandargo, Ingo Stammberger, Marc Stadler, Marc P. Hübner, Stefan Kehraus, Achim Hoerauf and Karl G. Wagner

Pharmaceutics 2024, 16(3), 386; https://doi.org/10.3390/pharmaceutics16030386 - 12 Mar 2024

Viewed by 1377

Abstract

Toxicological studies are a part of the drug development process and the preclinical stages, for which suitable vehicles ensuring easy and safe administration are crucial. However, poor aqueous solubility of drugs complicates vehicle screening for oral administration since non-aqueous solvents are often not tolerable. In the case of the anti-infective corallopyronin A, currently undergoing preclinical investigation for filarial nematode and bacterial infections, commonly used vehicles such as polyethylene glycol 200, aqueous solutions combined with cosolvents or solubilizers, or aqueous suspension have failed due to insufficient tolerability, solubility, or the generation of a non-homogeneous suspension. To this end, the aim of the study was to establish an alternative approach which offers suitable tolerability, dissolution, and ease of handling. Thus, a corallopyronin A-mesoporous silica formulation was successfully processed and tested in a seven-day toxicology study focused on Beagle dogs, including a toxicokinetic investigation on day one. Sufficient tolerability was confirmed by the vehicle control group. The vehicle enabled high-dose levels resulting in a low-, middle-, and high-dose of 150, 450, and 750 mg/kg. Overall, it was possible to achieve high plasma concentrations and exposures, leading to a valuable outcome of the toxicology study and establishing mesoporous silica as a valuable contender for challenging drug candidates. Full article

(This article belongs to the Special Issue Drug Delivery of Natural Active Principles: Focus on Topical and Oral Applications, 2nd Edition)

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Graphical abstract

18 pages, 3684 KiB

Open AccessArticle

Preparation of trans-Crocetin with High Solubility, Stability, and Oral Bioavailability by Incorporation into Three Types of Cyclodextrins

by Nan Liu, Jie Xiao, Ling-He Zang, Peng Quan and Dong-Chun Liu

Pharmaceutics 2023, 15(12), 2790; https://doi.org/10.3390/pharmaceutics15122790 - 16 Dec 2023

Viewed by 1094

Abstract

Crocetin (CRT), an active compound isolated from saffron, exhibits several pharmacological activities, including anti-tumor and immune-regulatory activities, and is effective against myocardial ischemia and coronary heart disease; however, its low stability and solubility limit its clinical application. Therefore, we investigated CRT inclusion complexes (ICs) with three cyclodextrins—α-CD, HP-β-CD, and γ-CD—suitable for oral administration prepared using an ultrasonic method. Fourier transform infrared spectroscopy and powder X-ray diffraction indicated that the crystalline state of CRT in ICs disappeared, and intermolecular interactions were observed between CRT and CDs. ¹H nuclear magnetic resonance and phase solubility studies confirmed CRT encapsulation in the CD cavity and the formation of ICs. In addition, we observed the morphology of ICs using scanning electron microscopy. All ICs showed a high drug encapsulation efficiency (approximately 90%) with 6500–10,000 times better solubilities than those of the pure drug. CRT showed rapid dissolution, whereas pure CRT was water-insoluble. The formation of ICs significantly improved the storage stability of CRT under heat, light, and moisture conditions. Further, the peak time of CRT in rats significantly decreased, and the relative bioavailability increased by approximately 3–4 times. In addition, the oral bioavailability of CRT IC was evaluated. Notably, the absorption rate and degree of the drug in rats were improved. This study illustrated the potential applications of CRT/CD ICs in the food, healthcare, and pharmaceutical industries, owing to their favorable dissolution, solubility, stability, and oral bioavailability. Full article

(This article belongs to the Special Issue Drug Delivery of Natural Active Principles: Focus on Topical and Oral Applications, 2nd Edition)

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