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

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 49942

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Dr. Rakesh Tiwari

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Department of Basic Medical Sciences, College of Osteopathic Medicine of the Pacific-Northwest, Western University of Health Sciences, 200 Mullins Drive, Lebanon, OR 97355, USA
Interests: peptide-based drug delivery; siRNA; anticancer drug; peptide therapeutics; peptide-drug conjugate; antimicrobial peptides; neurotherapeutics
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Dear Colleagues,

Peptides are natural components of our biological system. They are building blocks of proteins and are involved in several biological processes to regulate the functioning of our complex biological system. Peptides are very specific to their targets. Thus, they are used in targeting the drugs to specific cells and tissues. This strategy could reduce the various side effects of the drug. They are extensively used in various areas of biomedical, material, and pharmaceutical sciences. Various drugs and other pharmaceutical candidates fail to reach their target due to limitations to their cellular permeability and/or oral bioavailability. Peptides are found as an alternative candidate compared to other drug delivery systems due to their safety, easy functionalization with various pharmaceutical candidates, robustness of synthetic methodology, availability to use natural or unnatural amino acids, targeting with biomarker ligands, and use of peptidomimetics to improve pharmacokinetics property. Peptides also have the potential to be used to deliver biomaterials.

In connection with the above, this Special Issue aims to covered new approaches, methodologies, and prospectives towards recent development in the use of peptide-based drug delivery.

Dr. Rakesh Tiwari
Guest Editor

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Keywords

design and development of novel peptide-based drug delivery system
peptide-based oral drug delivery
peptide-based brain drug delivery system
peptide-based targeted delivery of therapeutics
delivery of biomaterials using peptide-based drug delivery systems

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Published Papers (11 papers)

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21 pages, 5780 KiB

Open AccessArticle

Oleyl Conjugated Histidine-Arginine Cell-Penetrating Peptides as Promising Agents for siRNA Delivery

by Muhammad Imran Sajid, Dindyal Mandal, Naglaa Salem El-Sayed, Sandeep Lohan, Jonathan Moreno and Rakesh Kumar Tiwari

Pharmaceutics 2022, 14(4), 881; https://doi.org/10.3390/pharmaceutics14040881 - 18 Apr 2022

Cited by 15 | Viewed by 3691

Abstract

Recent approvals of siRNA-based products motivated the scientific community to explore siRNA as a treatment option for several intractable ailments, especially cancer. The success of approved siRNA therapy requires a suitable and safer drug delivery agent. Herein, we report a series of oleyl conjugated histidine–arginine peptides as a promising nonviral siRNA delivery tool. The conjugated peptides were found to bind with the siRNA at N/P ratio ≥ 2 and demonstrated complete protection for the siRNA from early enzymatic degradation at N/P ratio ≥ 20. Oleyl-conjugated peptide -siRNA complexes were found to be noncytotoxic in breast cancer cells (MCF-7 and MDA-MB-231) and normal breast epithelial cells (MCF 10A) at N/P ratio of ~40. The oleyl-R₃-(HR)₄ and oleyl-R₄-(HR)₄ showed ~80-fold increased cellular uptake in MDA-MB-231 cells at N/P 40. Moreover, the conjugated peptides-siRNA complexes form nanocomplexes (~115 nm in size) and have an appropriate surface charge to interact with the cell membrane and cause cellular internalization. Furthermore, this study provides a proof-of-concept that oleyl-R₅-(HR)₄ can efficiently silence STAT-3 gene (~80% inhibition) in MDA-MB-231 cells with similar effectiveness to Lipofectamine. Further exploration of this approach holds a great promise in discovering a successful in vivo siRNA delivery agent with a favorable pharmacokinetic profile. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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18 pages, 1591 KiB

Open AccessArticle

New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets

by Wioletta Brankiewicz, Joanna Okońska, Katarzyna Serbakowska, Jan Lica, Marek Drab, Natalia Ptaszyńska, Anna Łęgowska, Krzysztof Rolka and Piotr Szweda

Pharmaceutics 2022, 14(4), 693; https://doi.org/10.3390/pharmaceutics14040693 - 23 Mar 2022

Cited by 7 | Viewed by 3152

Abstract

Infections of Candida spp. etiology are frequently treated with azole drugs. Among azoles, the most widely used in the clinical scenario remains fluconazole (FLC). Promising results in treatment of dangerous, systemic Candida infections demonstrate the advantages of combined therapies carried out with combinations of at least two different antifungal agents. Here, we report five conjugates composed of covalently linked FLC and cell penetrating or antimicrobial peptide: TP10-7-NH₂, TP10-NH₂, LFcinB(2-11)-NH₂, LFcinB[Nle^1,11]-NH₂, and HLopt2-NH₂, with aspects of design, chemical synthesis and their biological activities. Two of these compounds, namely FLCpOH-TP10-NH₂ and FLCpOH-TP10-7-NH₂, exhibit high activity against reference strains and fluconazole-resistant clinical isolates of C. albicans, including strains overproducing drug transporters. Moreover, both of them demonstrate higher fungicidal effects compared to fluconazole. Analysis performed with fluorescence and scanning electron microscopy as well as flow cytometry indicated the cell membrane as a molecular target of synthesized conjugates. An important advantage of FLCpOH-TP10-NH₂ and FLCpOH-TP10-7-NH₂ is their low cytotoxicity. The IC₉₀ value for the human cells after 72 h treatment was comparable to the MIC₅₀ value after 24 h treatment for most strains of C. albicans. In reported conjugates, FLC was linked to the peptide by its hydroxyl group. It is worth noting that conjugation of FLC by the nitrogen atom of the triazole ring led to practically inactive compounds. Two compounds produced by us and reported herein appear to be potential candidates for novel antifungal agents. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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13 pages, 1957 KiB

Open AccessArticle

pH-Sensitive Peptide Hydrogels as a Combination Drug Delivery System for Cancer Treatment

by Yuanfen Liu, Yingchun Ran, Yu Ge, Faisal Raza, Shasha Li, Hajra Zafar, Yiqun Wu, Ana Cláudia Paiva-Santos, Chenyang Yu, Meng Sun, Ying Zhu and Fei Li

Pharmaceutics 2022, 14(3), 652; https://doi.org/10.3390/pharmaceutics14030652 - 16 Mar 2022

Cited by 44 | Viewed by 4307

Abstract

Conventional antitumor chemotherapeutics generally have shortcomings in terms of dissolubility, selectivity and drug action time, and it has been difficult to achieve high antitumor efficacy with single-drug therapy. At present, combination therapy with two or more drugs is widely used in the treatment of cancer, but a shortcoming is that the drugs do not reach the target at the same time, resulting in a reduction in efficacy. Therefore, it is necessary to design a carrier that can release two drugs at the same site. We designed an injectable pH-responsive OE peptide hydrogel as a carrier material for the antitumor drugs gemcitabine (GEM) and paclitaxel (PTX) that can release drugs at the tumor site simultaneously to achieve the antitumor effect. After determining the optimal gelation concentration of the OE polypeptide, we conducted an in vitro release study to prove its pH sensitivity. The release of PTX from the OE hydrogel in the medium at pH 5.8 and pH 7.4 was 96.90% and 38.98% in 7 days. The release of GEM from the OE hydrogel in media with pH of 5.8 and 7.4 was 99.99% and 99.63% in 3 days. Transmission electron microscopy (TEM) and circular dichroism (CD) experiments were used to observe the microstructure of the peptides. The circular dichroism of OE showed a single negative peak shape when under neutral conditions, indicating a β-folded structure, while under acidic conditions, it presented characteristics of a random coil. Rheological experiments were used to investigate the mechanical strength of this peptide hydrogel. Furthermore, the treatment effect of the drug-loaded peptide hydrogel was demonstrated through in vitro and in vivo experiments. The results show that the peptide hydrogels have different structures at different pH values and are highly sensitive to pH. They can reach the tumor site by injection and are induced by the tumor microenvironment to release antitumor drugs slowly and continuously. This biologically functional material has a promising future in drug delivery for combination drugs. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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23 pages, 5149 KiB

Open AccessArticle

NGIWY-Amide: A Bioinspired Ultrashort Self-Assembled Peptide Gelator for Local Drug Delivery Applications

by Nikoleta F. Theodoroula, Christina Karavasili, Manos C. Vlasiou, Alexandra Primikyri, Christia Nicolaou, Alexandra V. Chatzikonstantinou, Aikaterini-Theodora Chatzitaki, Christos Petrou, Nikolaos Bouropoulos, Constantinos K. Zacharis, Eleftheria Galatou, Yiannis Sarigiannis, Dimitrios G. Fatouros and Ioannis S. Vizirianakis

Pharmaceutics 2022, 14(1), 133; https://doi.org/10.3390/pharmaceutics14010133 - 6 Jan 2022

Cited by 9 | Viewed by 4158

Abstract

Fibrillar structures derived from plant or animal origin have long been a source of inspiration for the design of new biomaterials. The Asn-Gly-Ile-Trp-Tyr-NH₂ (NGIWY-amide) pentapeptide, isolated from the sea cucumber Apostichopus japonicus, which spontaneously self-assembles in water to form hydrogel, pertains to this category. In this study, we evaluated this ultra-short cosmetic bioinspired peptide as vector for local drug delivery applications. Combining nuclear magnetic resonance, circular dichroism, infrared spectroscopy, X-ray diffraction, and rheological studies, the synthesized pentapeptide formed a stiff hydrogel with a high β-sheet content. Molecular dynamic simulations aligned well with scanning electron and atomic-force microscopy studies, revealing a highly filamentous structure with the fibers adopting a helical-twisted morphology. Model dye localization within the supramolecular hydrogel provided insights on the preferential distribution of hydrophobic and hydrophilic compounds in the hydrogel network. That was further depicted in the diffusion kinetics of drugs differing in their aqueous solubility and molecular weight, namely, doxorubicin hydrochloride, curcumin, and octreotide acetate, highlighting its versatility as a delivery vector of both hydrophobic and hydrophilic compounds of different molecular weight. Along with the observed cytocompatibility of the hydrogel, the NGIWY-amide pentapeptide may offer new approaches for cell growth, drug delivery, and 3D bioprinting tissue-engineering applications. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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15 pages, 4319 KiB

Open AccessArticle

The Effects of a Short Self-Assembling Peptide on the Physical and Biological Properties of Biopolymer Hydrogels

by Sumit Chowdhuri, Moumita Ghosh, Lihi Adler-Abramovich and Debapratim Das

Pharmaceutics 2021, 13(10), 1602; https://doi.org/10.3390/pharmaceutics13101602 - 2 Oct 2021

Cited by 17 | Viewed by 3815

Abstract

Hydrogel scaffolds have attracted much interest in the last few years for applications in the field of bone and cartilage tissue engineering. These scaffolds serve as a convenient three-dimensional structure on which cells can grow while sensing the native environment. Natural polymer-based hydrogels are an interesting choice for such purposes, but they lack the required mechanical properties. In contrast, composite hydrogels formed by biopolymers and short peptide hydrogelators possess mechanical characteristics suitable for osteogenesis. Here, we describe how combining the short peptide hydrogelator, Pyrene-Lysine-Cysteine (PyKC), with other biopolymers, can produce materials that are suitable for tissue engineering purposes. The presence of PyKC considerably enhances the strength and water content of the composite hydrogels, and confers thixotropic behavior. The hyaluronic acid-PyKC composite hydrogels were shown to be biocompatible, with the ability to support osteogenesis, since MC3 T3-E1 osteoblast progenitor cells grown on the materials displayed matrix calcification and osteogenic differentiation. The osteogenesis results and the injectability of these composite hydrogels hold promise for their future utilization in tissue engineering. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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31 pages, 13231 KiB

Open AccessArticle

Atrial Natriuretic Peptide Antibody-Functionalised, PEGylated Multiwalled Carbon Nanotubes for Targeted Ischemic Stroke Intervention

by Patrick P. Komane, Pradeep Kumar and Yahya E. Choonara

Pharmaceutics 2021, 13(9), 1357; https://doi.org/10.3390/pharmaceutics13091357 - 28 Aug 2021

Cited by 7 | Viewed by 2684

Abstract

Stroke is one of the major causes of disability and the second major cause of death around the globe. There is a dire need for an ultrasensitive detection tool and an effective and efficient therapeutic system for both detection and treatment of stroke at its infancy stage. Carbon nanotubes are promising nanomaterials for tackling these challenges. The loading of dexamethasone and decoration of PEGylated multiwalled carbon nanotube with atrial natriuretic peptide (ANP) antibody and fluorescein isothiocyanate for targeting ischemic site in the rat stroke model is presented here. Functionalisation of carbon nanotubes with dexamethasone (DEX), polyethylene glycol (PEG), fluorescein isothiocyanate (FITC), and ANP antibody caused a 63-fold increase in the D band intensity as illustrated by Raman. The characteristic band intensity increase was observed at 1636 nm following functionalisation of carbon nanotubes with polyethylene glycol and dexamethasone as confirmed by Fourier Transform Infrared. These findings have demonstrated the coupling capability of atrial natriuretic peptide antibody to DEX-PEG-CNTs. The baseline plasma atrial natriuretic peptide levels were ranging from 118 to 135.70 pg/mL prior to surgery and from 522.09 to 552.37 following common carotid artery occlusion. A decrease in atrial natriuretic peptide levels to 307.77 was observed when the rats were treated with FITC-DEX-PEG-ANP-CNTs, PEG-CNTs and DEX with a significant drop in the FITC-DEX-PEG-ANP-CNTs treated group. Fluorescence was detected in FITC-DEX-PEG-CNTs and FITC-DEX-PEG-ANP-CNTs treated ischemic stroke rats. The highest fluorescence intensity was reported in plasma (2179) followed by the kidney (1563) and liver (1507). These findings suggest a beneficial role that is played by the FITC-DEX-PEG-ANP-CNTs in the reduction of inflammation in the ischemic stroke induced rats that could induce a successful treatment of ischemic stroke. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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18 pages, 2900 KiB

Open AccessArticle

Increased Carrier Peptide Stability through pH Adjustment Improves Insulin and PTH(1-34) Delivery In Vitro and In Vivo Rather than by Enforced Carrier Peptide-Cargo Complexation

by Mie Kristensen, Ragna Guldsmed Diedrichsen, Valeria Vetri, Vito Foderà and Hanne Mørck Nielsen

Pharmaceutics 2020, 12(10), 993; https://doi.org/10.3390/pharmaceutics12100993 - 20 Oct 2020

Cited by 13 | Viewed by 3205

Abstract

Oral delivery of therapeutic peptides is hampered by their large molecular size and labile nature, thus limiting their permeation across the intestinal epithelium. Promising approaches to overcome the latter include co-administration with carrier peptides. In this study, the cell-penetrating peptide penetratin was employed to investigate effects of co-administration with insulin and the pharmacologically active part of parathyroid hormone (PTH(1-34)) at pH 5, 6.5, and 7.4 with respect to complexation, enzymatic stability, and transepithelial permeation of the therapeutic peptide in vitro and in vivo. Complex formation between insulin or PTH(1-34) and penetratin was pH-dependent. Micron-sized complexes dominated in the samples prepared at pH-values at which penetratin interacts electrostatically with the therapeutic peptide. The association efficiency was more pronounced between insulin and penetratin than between PTH(1-34) and penetratin. Despite the high degree of complexation, penetratin retained its membrane activity when applied to liposomal structures. The enzymatic stability of penetratin during incubation on polarized Caco-2 cell monolayers was pH-dependent with a prolonged half-live determined at pH 5 when compared to pH 6.5 and 7.4. Also, the penetratin-mediated transepithelial permeation of insulin and PTH(1-34) was increased in vitro and in vivo upon lowering the sample pH from 7.4 or 6.5 to 5. Thus, the formation of penetratin-cargo complexes with several molecular entities is not prerequisite for penetratin-mediated transepithelial permeation a therapeutic peptide. Rather, a sample pH, which improves the penetratin stability, appears to optimize the penetratin-mediated transepithelial permeation of insulin and PTH(1-34). Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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18 pages, 1685 KiB

Open AccessArticle

Click-Free Synthesis of a Multivalent Tricyclic Peptide as a Molecular Transporter

by Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari and Keykavous Parang

Pharmaceutics 2020, 12(9), 842; https://doi.org/10.3390/pharmaceutics12090842 - 3 Sep 2020

Cited by 8 | Viewed by 4178

Abstract

The cellular delivery of cell-impermeable and water-insoluble molecules remains an ongoing challenge to overcome. Previously, we reported amphipathic cyclic peptides c[WR]₄ and c[WR]₅ consisting of alternate arginine and tryptophan residues as nuclear-targeting molecular transporters. These peptides contain an optimal balance of positive charge and hydrophobicity, which is required for interactions with the phospholipid bilayer to facilitate their application as a drug delivery system. To further optimize them, we synthesized and evaluated a multivalent tricyclic peptide as an efficient molecular transporter. The monomeric cyclic peptide building blocks were synthesized using Fmoc/tBu solid-phase chemistry and cyclization in the solution and conjugated with each other through an amide bond to afford the tricyclic peptide, which demonstrated modest antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli (E. coli) with a minimum inhibitory concentration (MIC) of 64–128 µg/mL. The tricyclic peptide was found to be nontoxic up to 30 µM in the breast cancer cell lines (MDA-MB-231). The presence of tricyclic peptide enhanced cellular uptakes of fluorescently-labeled phosphopeptide (F’-GpYEEI, 18-fold), anti-HIV drugs (lamivudine (F’-3TC), emtricitabine (F’-FTC), and stavudine (F’-d4T), 1.7–12-fold), and siRNA (3.3-fold) in the MDA-MB-231 cell lines. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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15 pages, 1614 KiB

Open AccessArticle

Cyclic Peptide-Gadolinium Nanoparticles for Enhanced Intracellular Delivery

by Amir Nasrolahi Shirazi, Shang Eun Park, Shirin Rad, Luiza Baloyan, Dindyal Mandal, Muhammad Imran Sajid, Ryley Hall, Sandeep Lohan, Khalid Zoghebi, Keykavous Parang and Rakesh Kumar Tiwari

Pharmaceutics 2020, 12(9), 792; https://doi.org/10.3390/pharmaceutics12090792 - 21 Aug 2020

Cited by 6 | Viewed by 6533

Abstract

A cyclic peptide containing one cysteine and five alternating tryptophan and arginine amino acids [(WR)₅C] was synthesized using Fmoc/tBu solid-phase methodology. The ability of the synthesized cyclic peptide to produce gadolinium nanoparticles through an in situ one-pot mixing of an aqueous solution of GdCl₃ with [(WR)₅C] peptide solution was evaluated. Transmission electron microscopy showed the formed peptide-Gd nanoparticles in star-shape morphology with a size of ~250 nm. Flow cytometry investigation showed that the cellular uptake of a cell-impermeable fluorescence-labeled phosphopeptide (F′-GpYEEI, where F′ = fluorescein) was approximately six times higher in the presence of [(WR)₅C]-Gd nanoparticles than those of F′-GpYEEI alone in human leukemia adenocarcinoma (CCRF-CEM) cells after 2 h incubation. The antiproliferative activities of cisplatin and carboplatin (5 µM) were increased in the presence of [(WR)₅C]-GdNPs (50 μM) by 41% and 18%, respectively, after 72-h incubation in CCRF-CEM cells. The intracellular release of epirubicin, an anticancer drug, from the complex showed that 15% and 60% of the drug was released intracellularly within 12 and 48 h, respectively. This report provides insight about using a non-toxic MRI agent, gadolinium nanoparticles, for the delivery of various types of molecular cargos. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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24 pages, 8455 KiB

Open AccessArticle

An Enteric-Coated Polyelectrolyte Nanocomplex Delivers Insulin in Rat Intestinal Instillations When Combined with a Permeation Enhancer

by Svenja Sladek, Fiona McCartney, Mena Eskander, David J. Dunne, Maria Jose Santos-Martinez, Federico Benetti, Lidia Tajber and David J. Brayden

Pharmaceutics 2020, 12(3), 259; https://doi.org/10.3390/pharmaceutics12030259 - 12 Mar 2020

Cited by 21 | Viewed by 4820

Abstract

The use of nanocarriers is being researched to achieve oral peptide delivery. Insulin-associated anionic polyelectrolyte nanoparticle complexes (PECs) were formed that comprised hyaluronic acid and chitosan in an optimum mass mixing ratio of 5:1 (MR 5), followed by coating with a pH-dependent polymer. Free insulin was separated from PECs by size exclusion chromatography and then measured by HPLC. The association efficiency of insulin in PECs was >95% and the loading was ~83 µg/mg particles. Dynamic light scattering and nanoparticle tracking analysis of PECs revealed low polydispersity, a negative zeta potential range of −40 to −50 mV, and a diameter range of 95–200 nm. Dissolution studies in simulated small intestinal fluid (FaSSIF-V2) revealed that the PECs were colloidally stable. PECs that were coated with Eudragit^® L-100 delayed insulin release in FaSSIF-V2 and protected insulin against pancreatin attack more than uncoated PECs. Uncoated anionic PECs interacted weakly with mucin in vitro and were non-cytotoxic to Caco-2 cells. The coated and uncoated PECs, both concentrated further by ultrafiltration, permitted dosing of 50 IU/kg in rat jejunal instillations, but they failed to reduce plasma glucose or deliver insulin to the blood. When ad-mixed with the permeation enhancer (PE), sucrose laurate (100 mM), the physicochemical parameters of coated PECs were relatively unchanged, however blood glucose was reduced by 70%. In conclusion, the use of a PE allowed for the PEC-released bioactive insulin to permeate the jejunum. This has implications for the design of orally delivered particles that can release the payload when formulated with enhancers. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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31 pages, 3013 KiB

Open AccessReview

Peptide-Based Strategies for Targeted Tumor Treatment and Imaging

by Abiodun Ayo and Pirjo Laakkonen

Pharmaceutics 2021, 13(4), 481; https://doi.org/10.3390/pharmaceutics13040481 - 2 Apr 2021

Cited by 42 | Viewed by 7913

Abstract

Cancer is one of the leading causes of death worldwide. The development of cancer-specific diagnostic agents and anticancer toxins would improve patient survival. The current and standard types of medical care for cancer patients, including surgery, radiotherapy, and chemotherapy, are not able to treat all cancers. A new treatment strategy utilizing tumor targeting peptides to selectively deliver drugs or applicable active agents to solid tumors is becoming a promising approach. In this review, we discuss the different tumor-homing peptides discovered through combinatorial library screening, as well as native active peptides. The different structure–function relationship data that have been used to improve the peptide’s activity and conjugation strategies are highlighted. Full article

(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems)

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