Special Issue "Drug Delivery of Natural Active Principles: Focus on Topical and Oral Applications"

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 31 May 2022 | Viewed by 4296

Special Issue Editors

Dr. Marta Gallo
E-Mail Website
Guest Editor
DISAT Department, Politecnico di Torino, Corso Duca degli Abruzzi 29, 10129 Torino, Italy
Interests: drug delivery; biomaterials; mesoporous silica; synthesis and characterization of biomaterials; drug adsorption; natural active principles; topical delivery
Prof. Dr. Marta Miola
E-Mail Website1 Website2
Guest Editor
Politecnico di Torino, Department of Applied Science and Technology, Torino, Italy
Interests: bioactive glasses/glass-ceramics; antibacterial materials; composites; magnetic materials; inorganic nanoparticles; natural active principles; materials functionalization
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Special Issue Information

Dear Colleagues,

Natural active principles still attract interest regarding their therapeutic purposes thanks to the 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:

  • Role of organic/inorganic carrier in the 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 Gallo
Prof. Dr. Marta Miola
Guest Editors

Manuscript Submission Information

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Keywords

  • natural compounds
  • topical drug delivery
  • oral drug delivery
  • micro- and nano-particles
  • polymer-, lipid-, oxide-based and hybrid systems
  • synthesis and characterization
  • in vitro, in vivo tests

Published Papers (4 papers)

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Research

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Article
Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture
Pharmaceutics 2022, 14(4), 742; https://doi.org/10.3390/pharmaceutics14040742 - 29 Mar 2022
Viewed by 503
Abstract
Arnica tincture is a traditional herbal medicine used to treat blunt injuries, e.g., bruises and squeezes. In addition, a potential new use in the treatment of cutaneous leishmaniasis is currently under investigation. Therefore, detailed information about the dermal absorption of the tincture and [...] Read more.
Arnica tincture is a traditional herbal medicine used to treat blunt injuries, e.g., bruises and squeezes. In addition, a potential new use in the treatment of cutaneous leishmaniasis is currently under investigation. Therefore, detailed information about the dermal absorption of the tincture and especially its bioactive constituents, sesquiterpene lactones (STLs) of the helenalin- and 11α,13-dihydrohelenalin type, is mandatory. Consequently, this article reports on dermal absorption studies of Arnica tincture using diffusion cells and porcine skin as well as two human skin samples with different permeability. The amounts of STLs on the skin surfaces, in skin extracts and in the receptor fluids were quantified by ultra-high-performance liquid chromatography with high-resolution mass spectrometry (UHPLC-HRMS). It was found that Arnica STLs permeated into the receptor fluid already 4 h after the application, but the amount was rather low. Within 48 h, a maximum of 8.4%, 14.6% and 36.4% of STLs permeated through porcine skin, human skin A (trans-epidermal water loss (TEWL) = 11.518 g·m−2·h−1) and the more permeable human skin B (TEWL = 17.271 g·m−2·h−1), respectively. The majority of STLs was absorbed (penetrated into the skin; 97.6%, 97.8% and 99.3%) after 48 h but a huge portion could not be extracted from skin and is expected to be irreversibly bound to skin proteins. To better visualize the analytes in different skin layers, a fluorescence-labeled STL, helenalin 3,4-dimethoxycinnamate, was synthesized. Fluorescence microscopic images depict an accumulation of the fluorescent derivative in the epidermis. For the treatment of local, cutaneous complaints, an enrichment of the bioactive substances in the skin may be considered beneficial. Full article
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Article
Crystal Structure, Solubility, and Pharmacokinetic Study on a Hesperetin Cocrystal with Piperine as Coformer
Pharmaceutics 2022, 14(1), 94; https://doi.org/10.3390/pharmaceutics14010094 - 01 Jan 2022
Cited by 2 | Viewed by 453
Abstract
Hesperetin (HES) is a key biological active ingredient in citrus peels, and is one of the natural flavonoids that attract the attention of researchers due to its numerous therapeutic bioactivities that have been identified in vitro. As a bioenhancer, piperine (PIP) can effectively [...] Read more.
Hesperetin (HES) is a key biological active ingredient in citrus peels, and is one of the natural flavonoids that attract the attention of researchers due to its numerous therapeutic bioactivities that have been identified in vitro. As a bioenhancer, piperine (PIP) can effectively improve the absorption of insoluble drugs in vivo. In the present study, a cocrystal of HES and PIP was successfully obtained through solution crystallization. The single-crystal structure was illustrated and comprehensive characterization of the cocrystal was conducted. The cocrystal was formed by two drug molecules at a molar ratio of 1:1, which contained O–H–O hydrogen bonds between the carbonyl and ether oxygen of PIP and the phenolic hydroxyl group of HES. In addition, a solubility experiment was performed on powder cocrystal in simulated gastrointestinal fluid, and the result revealed that the cocrystal improves the dissolution behavior of HES compared with that of the pure substance. Furthermore, HES’s bioavailability in the cocrystal was six times higher than that of pristine drugs. These results may provide an efficient oral formulation for HES. Full article
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Article
Cholesterol-Based Nanovesicles Enhance the In Vitro Cytotoxicity, Ex Vivo Intestinal Absorption, and In Vivo Bioavailability of Flutamide
Pharmaceutics 2021, 13(11), 1741; https://doi.org/10.3390/pharmaceutics13111741 - 20 Oct 2021
Viewed by 1131
Abstract
Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an [...] Read more.
Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an endeavor to maximize its therapeutic efficacy and minimize undesired adverse effects. Draper–Lin small composite design was used to optimize the critical quality attributes of FLT-loaded niosomes and ensure the desired product quality. The influence of the selected four independent variables on mean particle size (Y1), zeta potential (Y2), drug entrapment efficiency (Y3), and the cumulative drug release after 24 h (Y4) was examined. The optimized nanovesicles were assessed for their in vitro cytotoxicity, ex-vivo absorption via freshly excised rabbit intestine as well as in vivo pharmacokinetics on male rats. TEM confirmed nanovescicles’ spherical shape with bilayer structure. Values of dependent variables were 748.6 nm, −48.60 mV, 72.8% and 72.2% for Y1, Y2, Y3 and Y4, respectively. The optimized FLT-loaded niosomes exerted high cytotoxic efficacy against human prostate cancer cell line (PC-3) with an IC50 value of 0.64 ± 0.04 µg/mL whilst, it was 1.88 ± 0.16 µg/mL for free FLT. Moreover, the IC50 values on breast cancer cell line (MCF-7) were 0.27 ± 0.07 µg/mL and 4.07 ± 0.74 µg/mL for FLT-loaded niosomes and free FLT, respectively. The permeation of the optimized FLT-loaded niosomes through the rabbit intestine showed an enhancement ratio of about 1.5 times that of the free FLT suspension. In vivo pharmacokinetic study displayed an improvement in oral bioavailability of the optimized niosomal formulation with AUC and Cmax values of 741.583 ± 33.557 μg/mL × min and 6.950 ± 0.45 μg/mL compared to 364.536 ± 45.215 μg/mL × min and 2.650 ± 0.55 μg/mL for the oral FLT suspension. With these promising findings, we conclude that encapsulation of FLT in cholesterol-loaded nanovesicles enhanced its anticancer activity and oral bioavailability which endorse its use in the management of prostate cancer. Full article
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Review

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Review
Phytosomes as an Emerging Nanotechnology Platform for the Topical Delivery of Bioactive Phytochemicals
Pharmaceutics 2021, 13(9), 1475; https://doi.org/10.3390/pharmaceutics13091475 - 15 Sep 2021
Cited by 9 | Viewed by 1359
Abstract
The emergence of phytosome nanotechnology has a potential impact in the field of drug delivery and could revolutionize the current state of topical bioactive phytochemicals delivery. The main challenge facing the translation of the therapeutic activity of phytochemicals to a clinical setting is [...] Read more.
The emergence of phytosome nanotechnology has a potential impact in the field of drug delivery and could revolutionize the current state of topical bioactive phytochemicals delivery. The main challenge facing the translation of the therapeutic activity of phytochemicals to a clinical setting is the extremely low absorption rate and poor penetration across biological barriers (i.e., the skin). Phytosomes as lipid-based nanocarriers play a crucial function in the enhancement of pharmacokinetic and pharmacodynamic properties of herbal-originated polyphenolic compounds, and make this nanotechnology a promising tool for the development of new topical formulations. The implementation of this nanosized delivery system could enhance the penetration of phytochemicals across biological barriers due to their unique physiochemical characteristics, improving their bioavailability. In this review, we provide an outlook on the current knowledge of the biological barriers of phytoconstituents topical applications. The great potential of the emerging nanotechnology in the delivery of bioactive phytochemicals is reviewed, with particular focus on phytosomes as an innovative lipid-based nanocarrier. Additionally, we compared phytosomes with liposomes as the gold standard of lipid-based nanocarriers for the topical delivery of phytochemicals. Finally, the advantages of phytosomes in topical applications are discussed. Full article
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