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Pharmaceutics
Special Issues
Novel Drug Delivery Systems of Phytomedicines
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Novel Drug Delivery Systems of Phytomedicines

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

Deadline for manuscript submissions: 30 April 2024 | Viewed by 8309

Special Issue Editors

Dr. Xingwang Zhang

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Guest Editor
Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou 511436, China
Interests: modern TCM preparations; micro/nanoparticle-based drug delivery systems; nanotherapy with phytomedicines
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Wei Wu

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Guest Editor
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201203, China
Interests: dug delivery; pharmaceutics; oral delivery; controlled and sustained release; pharmaceutical technology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Phytomedicines coming from medicinal plants or herbs are an important medical resource that plays a crucial role in the prevention and treatment of a diversity of diseases. Unfortunately, most phytomedicines, including extracts and monomers, are plagued with usage due to poor solubility/permeability, bitter taste, gastrointestinal irritability, or latent cytotoxicity. However, once encapsulated into or conjugated onto suitable carriers, the untoward physicochemical properties of therapeutic molecules can be properly modified. As a result, synergism and attenuation emerge in formulated phytomedicines with the help of novel drug delivery systems. Novel drug delivery systems refer to a set of smart formulations that can ameliorate the pharmacokinetics and pharmacodynamics of laden drugs.

Given the many merits of novel delivery systems in potentiating phytomedicines, we have launched a Special Issue “Novel Drug Delivery Systems of Phytomedicines”. This Special Issue will cover broad interests in wielding diverse novel delivery systems to achieve PK/PD optimization of phytomedicines, including but not limited to lipid-based formulations, nanoparticles, nanovesicles, micelles, micro/nanoemulsions, and micro/nanocapsules.

Dr. Xingwang Zhang
Prof. Dr. Wei Wu
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

  • phytomedicines
  • encapsulation
  • conjugation
  • lipid formulation
  • nanocarriers
  • nanoparticles
  • micro/nanoemulsions
  • vesicles
  • micelles
  • phytosomes
  • liposomes
  • niosomes
  • bilosomes
  • exosomes
  • pharmacokinetics
  • pharmacodynamics
 

Published Papers (5 papers)

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Research

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22 pages, 7560 KiB  
Article
In Situ Preparation of Tannic Acid-Modified Poly(N-isopropylacrylamide) Hydrogel Coatings for Boosting Cell Response
by Jufei Xu, Xiangzhe Liu, Pengpeng Liang, Hailong Yuan and Tianyou Yang
Pharmaceutics 2024, 16(4), 538; https://doi.org/10.3390/pharmaceutics16040538 - 13 Apr 2024
Viewed by 303
Abstract
The improvement of the capability of poly(N-isopropylacrylamide) (PNIPAAm) hydrogel coating in cell adhesion and detachment is critical to efficiently prepare cell sheets applied in cellular therapies and tissue engineering. To enhance cell response on the surface, the amine group-modified PNIPAAm (PNIPAAm-APTES) [...] Read more.
The improvement of the capability of poly(N-isopropylacrylamide) (PNIPAAm) hydrogel coating in cell adhesion and detachment is critical to efficiently prepare cell sheets applied in cellular therapies and tissue engineering. To enhance cell response on the surface, the amine group-modified PNIPAAm (PNIPAAm-APTES) nanohydrogels were synthesized and deposited spontaneously on tannic acid (TA)-modified polyethylene (PE) plates. Subsequently, TA was introduced onto PNIPAAm-APTES nanohydrogels to fabricate coatings composed of TA-modified PNIPAAm-APTES (PNIPAAm-APTES-TA). Characterization techniques, including TEM, SEM, XPS, and UV-Vis spectroscopy, confirmed the effective deposition of hydrogels of PNIPAAm as well as the morphologies, content of chemical bonding-TA, and stability of various coatings. Importantly, the porous hydrogel coatings exhibited superhydrophilicity at 20 °C and thermo-responsive behavior. The fluorescence measurement demonstrated that the coating’s stability effectively regulated protein behavior, influencing cell response. Notably, cell response tests revealed that even without precise control over the chain length/thickness of PNIPAAm during synthesis, the coatings enhanced cell adhesion and detachment, facilitating efficient cell culture. This work represented a novel and facile approach to preparing bioactive PNIPAAm for cell culture. Full article
(This article belongs to the Special Issue Novel Drug Delivery Systems of Phytomedicines)
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19 pages, 5361 KiB  
Article
Selenized Polymer-Lipid Hybrid Nanoparticles for Oral Delivery of Tripterine with Ameliorative Oral Anti-Enteritis Activity and Bioavailability
by Yuehong Ren, Chunli Qi, Shuxian Ruan, Guangshang Cao, Zhiguo Ma and Xingwang Zhang
Pharmaceutics 2023, 15(3), 821; https://doi.org/10.3390/pharmaceutics15030821 - 02 Mar 2023
Cited by 4 | Viewed by 1501
Abstract
The oral delivery of insoluble and enterotoxic drugs has been largely plagued by gastrointestinal irritation, side effects, and limited bioavailability. Tripterine (Tri) ranks as the hotspot of anti-inflammatory research other than inferior water-solubility and biocompatibility. This study was intended to develop selenized polymer-lipid [...] Read more.
The oral delivery of insoluble and enterotoxic drugs has been largely plagued by gastrointestinal irritation, side effects, and limited bioavailability. Tripterine (Tri) ranks as the hotspot of anti-inflammatory research other than inferior water-solubility and biocompatibility. This study was intended to develop selenized polymer-lipid hybrid nanoparticles loading Tri (Se@Tri-PLNs) for enteritis intervention by improving its cellular uptake and bioavailability. Se@Tri-PLNs were fabricated by a solvent diffusion-in situ reduction technique and characterized by particle size, ζ potential, morphology, and entrapment efficiency (EE). The cytotoxicity, cellular uptake, oral pharmacokinetics, and in vivo anti-inflammatory effect were evaluated. The resultant Se@Tri-PLNs were 123 nm around in particle size, with a PDI of 0.183, ζ potential of −29.70 mV, and EE of 98.95%. Se@Tri-PLNs exhibited retardant drug release and better stability in the digestive fluids compared with the unmodified counterpart (Tri-PLNs). Moreover, Se@Tri-PLNs manifested higher cellular uptake in Caco-2 cells as evidenced by flow cytometry and confocal microscopy. The oral bioavailability of Tri-PLNs and Se@Tri-PLNs was up to 280% and 397% relative to Tri suspensions, respectively. Furthermore, Se@Tri-PLNs demonstrated more potent in vivo anti-enteritis activity, which resulted in a marked resolution of ulcerative colitis. Polymer-lipid hybrid nanoparticles (PLNs) enabled drug supersaturation in the gut and the sustained release of Tri to facilitate absorption, while selenium surface engineering reinforced the formulation performance and in vivo anti-inflammatory efficacy. The present work provides a proof-of-concept for the combined therapy of inflammatory bowel disease (IBD) using phytomedicine and Se in an integrated nanosystem. Selenized PLNs loading anti-inflammatory phytomedicine may be valuable for the treatment of intractable inflammatory diseases. Full article
(This article belongs to the Special Issue Novel Drug Delivery Systems of Phytomedicines)
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19 pages, 6828 KiB  
Article
Spanlastics as a Potential Approach for Enhancing the Nose-To-Brain Delivery of Piperine: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Management of Epilepsy
by Isha Gupta, Syeda Nashvia Adin, Md Abdur Rashid, Yahya Alhamhoom, Mohd. Aqil and Mohd. Mujeeb
Pharmaceutics 2023, 15(2), 641; https://doi.org/10.3390/pharmaceutics15020641 - 14 Feb 2023
Cited by 10 | Viewed by 3228
Abstract
The present study delineates the preparation of piperine-loaded spanlastics (PIP-SPL) to improve piperine (PIP) solubility, bioavailability, and permeation through nasal mucosa for intranasal delivery. PIP-SPL was formulated using the thin-film hydration method and optimization was performed using Box–Behnken design (BBD). PIP-SPL optimized formulation [...] Read more.
The present study delineates the preparation of piperine-loaded spanlastics (PIP-SPL) to improve piperine (PIP) solubility, bioavailability, and permeation through nasal mucosa for intranasal delivery. PIP-SPL was formulated using the thin-film hydration method and optimization was performed using Box–Behnken design (BBD). PIP-SPL optimized formulation (PIP-SPLopt) was characterized for polydispersity index (PDI), vesicle size, entrapment efficiency, zeta potential, and in vitro PIP release. For further evaluation, blood–brain distribution study, transmission electron microscopy (TEM), nasal permeation study, and confocal scanning laser microscopy (CLSM) were performed withal. The PIP-SPLopt presented spherical and sealed shape vesicles with a small vesicle size of 152.4 nm, entrapment efficiency of 72.93%, PDI of 0.1118, and in vitro release of 82.32%. The CLSM study unveiled that the developed formulation has greater permeation of PIP across the nasal mucosa in comparison with the PIP suspension. The blood–brain distribution study demonstrated higher Cmax and AUC0–24h of PIP-SPL via the intranasal route in comparison to PIP-SPL via oral administration. The in vivo study revealed that the PIP-SPL has good antiepileptic potential in comparison with the standard diazepam, which was evinced by seizure activity, neuromuscular coordination by rotarod test, biochemical estimation of oxidative stress markers, and histopathological studies. Furthermore, nasal toxicity study confirm that the developed PIP-SPL formulation is safer for intranasal application. The current investigation corroborated that the prepared spanlastic vesicle formulation is a treasured carrier for the PIP intranasal delivery for the management of epilepsy. Full article
(This article belongs to the Special Issue Novel Drug Delivery Systems of Phytomedicines)
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Review

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22 pages, 7119 KiB  
Review
Delivery Strategies for Colchicine as a Critical Dose Drug: Reducing Toxicity and Enhancing Efficacy
by Yaran Lei, Yulu Yang, Guobao Yang, Ao Li, Yang Yang, Yuli Wang and Chunsheng Gao
Pharmaceutics 2024, 16(2), 222; https://doi.org/10.3390/pharmaceutics16020222 - 03 Feb 2024
Viewed by 1200
Abstract
Colchicine (COL), a widely used natural drug, has potent anti-inflammatory effects; however, as a narrow therapeutic index drug, its clinical application is limited by its serious gastrointestinal adverse effects, and only oral formulations are currently marketed worldwide. Recent studies have shown that transdermal, [...] Read more.
Colchicine (COL), a widely used natural drug, has potent anti-inflammatory effects; however, as a narrow therapeutic index drug, its clinical application is limited by its serious gastrointestinal adverse effects, and only oral formulations are currently marketed worldwide. Recent studies have shown that transdermal, injection, and oral drug delivery are the three main delivery strategies for COL. This article elaborates on the research progress of different delivery strategies in terms of toxicity reduction and efficacy enhancement, depicting that the transdermal drug delivery route can avoid the first-pass effect and the traumatic pain associated with the oral and injection routes, respectively. Therefore, such a dosage form holds a significant promise that requires the development of further research to investigate effective COL delivery formulations. In addition, the permeation-promoting technologies utilized for transdermal drug delivery systems are briefly discussed. This article is expected to provide scientific ideas and theoretical guidance for future research and the exploration of COL delivery strategies. Full article
(This article belongs to the Special Issue Novel Drug Delivery Systems of Phytomedicines)
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18 pages, 1940 KiB  
Review
Research Progress on the Mechanism of Nanoparticles Crossing the Intestinal Epithelial Cell Membrane
by Yunjie He, Meng Cheng, Ruyue Yang, Haocheng Li, Zhiyang Lu, Yi Jin, Jianfang Feng and Liangxing Tu
Pharmaceutics 2023, 15(7), 1816; https://doi.org/10.3390/pharmaceutics15071816 - 25 Jun 2023
Cited by 3 | Viewed by 1338
Abstract
Improving the stability of drugs in the gastrointestinal tract and their penetration ability in the mucosal layer by implementing a nanoparticle delivery strategy is currently a research focus in the pharmaceutical field. However, for most drugs, nanoparticles failed in enhancing their oral absorption [...] Read more.
Improving the stability of drugs in the gastrointestinal tract and their penetration ability in the mucosal layer by implementing a nanoparticle delivery strategy is currently a research focus in the pharmaceutical field. However, for most drugs, nanoparticles failed in enhancing their oral absorption on a large scale (4 folds or above), which hinders their clinical application. Recently, several researchers have proved that the intestinal epithelial cell membrane crossing behaviors of nanoparticles deeply influenced their oral absorption, and relevant reviews were rare. In this paper, we systematically review the behaviors of nanoparticles in the intestinal epithelial cell membrane and mainly focus on their intracellular mechanism. The three key complex intracellular processes of nanoparticles are described: uptake by intestinal epithelial cells on the apical side, intracellular transport and basal side exocytosis. We believe that this review will help scientists understand the in vivo performance of nanoparticles in the intestinal epithelial cell membrane and assist in the design of novel strategies for further improving the bioavailability of nanoparticles. Full article
(This article belongs to the Special Issue Novel Drug Delivery Systems of Phytomedicines)
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