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Biopolymer-Based Nanosystem for Drug Delivery

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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 (20 April 2023) | Viewed by 29139

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Prof. Dr. János Borbély

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Doctoral School of Clinical Medicine, University of Debrecen, Nagyerdei krt. 94., 4032 Debrecen, Hungary
Interests: biopolymer expression and modification; chemical structure determination; biopolymer-drug conjugation; drug release; in vitro and in vivo studies; design of nano-formulated drugs; contrast agents for MRI; SPECT and PET multimodal imaging
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Ildikó Bácskay

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Guest Editor

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: assessment of biocompatibility; drug delivery system formulation; application of macromolecules; characterization of dosage forms; in vitro dissolution studies; SEDDS
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The enhanced permeability and retention (EPR) effect was discovered more than three decades ago (Y. Matsumura, H. Maeda 1986). This discovery is now cited as a new wave of nanomedicine for tumor-targeted drug delivery, a new concept in cancer chemotherapy. As of now, more than 50 nanomedicine formulations have been approved for clinical use. In the anticancer agent class, the flagship formulation is the biopolymer-based drug Abraxane (nanoparticle albumin-bound paclitaxel). ADCs represent another anticancer class, in which specific biopolymers serve as antibodies to target moieties when they are conjugated to a highly toxic warhead drug, making them an effective anticancer agent. These drugs combine chemotherapy and immunotherapy, providing a better patient outcome. The encapsulation of other biopolymer ingredients, such as RNA and DNA, or, in other words, active biomacromolecular therapeutic agents, results in the formation of nanosystems. Nowadays, the priority is the development of new vaccines. Recently, nanoformulated vaccines have saved and are are continuing to save the lives of hundreds millions of people during the COVID pandemic.

Researchers have to find new appropriate biopolymers that are biodegradable, biocompatible, non-immunogenic, improve the bioavailability of active cargos, and protect the active ingredient in the bloodstream. Depending on the formulation, the nature of the release of the active ingredient is a key factor. The main value is the precise targeting of the “cargo” to the cancer cells and the avoidance of healthy cells. This goal can be achieved by developing nanoformulation systems. The economic strength of this subdivision within the pharmaceutical industry is well known; however, R&D innovation in the biotech segment requires more time and effort compared to in other fields. This is why a professional risk analysis will be taken into consideration.

Scientists are encouraged to send relevant research for submission in this Special Issue.

Prof. Dr. János Borbély
Prof. Dr. Ildikó Bácskay
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.

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Keywords

nano-formulations of drugs
antibody drug conjugation (ADC)
nanoformulated vaccines
delivery of biologics
biotech risk analysis
assessment of biocompatibility
drug delivery system formulation
characterization of dosage forms
in vitro dissolution studies
SEDDS

Published Papers (10 papers)

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Research

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14 pages, 2173 KiB

Open AccessArticle

Effect of Copolymer Properties on the Phase Behavior of Ibuprofen–PLA/PLGA Mixtures

by Anton Iemtsev, Martin Klajmon, Fatima Hassouna and Michal Fulem

Pharmaceutics 2023, 15(2), 645; https://doi.org/10.3390/pharmaceutics15020645 - 14 Feb 2023

Cited by 4 | Viewed by 1599

Abstract

Prediction of compatibility of the active pharmaceutical ingredient (API) with the polymeric carrier plays an essential role in designing drug delivery systems and estimating their long-term physical stability. A key element in deducing API–polymer compatibility is knowledge of a complete phase diagram, i.e., the solubility of crystalline API in polymer and mutual miscibility of API and polymer. In this work, the phase behavior of ibuprofen (IBU) with different grades of poly(D,L-lactide-co-glycolide) (PLGA) and polylactide (PLA), varying in composition of PLGA and molecular weight of PLGA and PLA, was investigated experimentally using calorimetry and computationally by the perturbed-chain statistical associating fluid theory (PC-SAFT) equation of state (EOS). The phase diagrams constructed based on a PC-SAFT EOS modeling optimized using the solubility data demonstrated low solubility at typical storage temperature (25 °C) and limited miscibility (i.e., presence of the amorphous–amorphous phase separation region) of IBU with all polymers studied. The ability of PC-SAFT EOS to capture the experimentally observed trends in the phase behavior of IBU–PLA/PLGA systems with respect to copolymer composition and molecular weight was thoroughly investigated and evaluated. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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14 pages, 3219 KiB

Open AccessArticle

Low-Density Lipoprotein Pathway Is a Ubiquitous Metabolic Vulnerability in High Grade Glioma Amenable for Nanotherapeutic Delivery

by Adenike O. Adekeye, David Needham and Ruman Rahman

Pharmaceutics 2023, 15(2), 599; https://doi.org/10.3390/pharmaceutics15020599 - 10 Feb 2023

Cited by 1 | Viewed by 2442

Abstract

Metabolic reprogramming, through increased uptake of cholesterol in the form of low-density lipoproteins (LDL), is one way by which cancer cells, including high grade gliomas (HGG), maintain their rapid growth. In this study, we determined LDL receptor (LDLR) expression in HGGs using immunohistochemistry on tissue microarrays from intra- and inter tumour regions of 36 adult and 133 paediatric patients to confirm LDLR as a therapeutic target. Additionally, we analysed expression levels in three representative cell line models to confirm their future utility to test LDLR-targeted nanoparticle uptake, retention, and cytotoxicity. Our data show widespread LDLR expression in adult and paediatric cohorts, but with significant intra-tumour variation observed between the core and either rim or invasive regions of adult HGG. Expression was independent of paediatric tumour grade or identified clinicopathological factors. LDLR-expressing tumour cells localized preferentially within perivascular niches, also with significant adult intra-tumour variation. We demonstrated variable levels of LDLR expression in all cell lines, confirming their suitability as models to test LDLR-targeted nanotherapy delivery. Overall, our study reveals the LDLR pathway as a ubiquitous metabolic vulnerability in high grade gliomas across all ages, amenable to future consideration of LDL-mediated nanoparticle/drug delivery to potentially circumvent tumour heterogeneity. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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19 pages, 2643 KiB

Open AccessArticle

Selective Targeting and Eradication of Various Human Non-Small Cell Lung Cancer Cell Lines Using Self-Assembled Aptamer-Decorated Nanoparticles

by Daniel Barak, Shira Engelberg, Yehuda G. Assaraf and Yoav D. Livney

Pharmaceutics 2022, 14(8), 1650; https://doi.org/10.3390/pharmaceutics14081650 - 08 Aug 2022

Cited by 1 | Viewed by 1839

Abstract

The leading cause of cancer mortality remains lung cancer (LC), of which non-small cell lung cancer (NSCLC) is the predominant type. Chemotherapy achieves only low response rates while inflicting serious untoward toxicity. Herein, we studied the binding and internalization of S15-aptamer (S15-APT)-decorated polyethylene glycol-polycaprolactone (PEG-PCL) nanoparticles (NPs) by various human NSCLC cell lines. All the NSCLC cell lines were targeted by S15-APT-decorated NPs. Confocal microscopy revealed variable levels of NP binding and uptake amongst these NSCLC cell lines, decreasing in the following order: Adenocarcinoma (AC) A549 cells > H2228 (AC) > H1299 (large cell carcinoma) > H522 (AC) > H1975 (AC). Flow cytometry analysis showed a consistent variation between these NSCLC cell lines in the internalization of S15-APT-decorated quantum dots. We obtained a temperature-dependent NP uptake, characteristic of active internalization. Furthermore, cytotoxicity assays with APT-NPs entrapping paclitaxel, revealed that A549 cells had the lowest IC₅₀ value of 0.03 µM PTX (determined previously), whereas H2228, H1299, H522 and H1975 exhibited higher IC₅₀ values of 0.38 µM, 0.92 µM, 2.31 µM and 2.59 µM, respectively (determined herein). Cytotoxicity was correlated with the binding and internalization of APT-NPs in the various NSCLC cells, suggesting variable expression of the putative S15 target receptor. These findings support the development of APT-targeted NPs in precision nanomedicine for individual NSCLC patient treatment. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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Review

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18 pages, 1051 KiB

Open AccessFeature PaperReview

Business Risk Mitigation in the Development Process of New Monoclonal Antibody Drug Conjugates for Cancer Treatment

by Balázs Kiss and János Borbély

Pharmaceutics 2023, 15(6), 1761; https://doi.org/10.3390/pharmaceutics15061761 - 18 Jun 2023

Cited by 1 | Viewed by 2332

Abstract

Recent developments aim to extend the cytotoxic effect and therapeutic window of mAbs by constructing antibody–drug conjugates (ADCs), in which the targeting moiety is the mAb that is linked to a highly toxic drug. According to a report from mid of last year, the global ADCs market accounted for USD 1387 million in 2016 and was worth USD 7.82 billion in 2022. It is estimated to increase in value to USD 13.15 billion by 2030. One of the critical points is the linkage of any substituent to the functional group of the mAb. Increasing the efficacy against cancer cells’ highly cytotoxic molecules (warheads) are connected biologically. The connections are completed by different types of linkers, or there are efforts to add biopolymer-based nanoparticles, including chemotherapeutic agents. Recently, a combination of ADC technology and nanomedicine opened a new pathway. To fulfill the scientific knowledge for this complex development, our aim is to write an overview article that provides a basic introduction to ADC which describes the current and future opportunities in therapeutic areas and markets. Through this approach, we show which development directions are relevant both in terms of therapeutic area and market potential. Opportunities to reduce business risks are presented as new development principles. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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25 pages, 5787 KiB

Open AccessReview

Intranasal Drug Administration in Alzheimer-Type Dementia: Towards Clinical Applications

by Raquel Taléns-Visconti, Jesus Vicente de Julián-Ortiz, Ofelia Vila-Busó, Octavio Diez-Sales and Amparo Nácher

Pharmaceutics 2023, 15(5), 1399; https://doi.org/10.3390/pharmaceutics15051399 - 03 May 2023

Cited by 6 | Viewed by 6736

Abstract

Alzheimer-type dementia (ATD) treatments face limitations in crossing the blood–brain barrier and systemic adverse effects. Intranasal administration offers a direct route to the brain via the nasal cavity’s olfactory and trigeminal pathways. However, nasal physiology can hinder drug absorption and limit bioavailability. Therefore, the physicochemical characteristics of formulations must be optimized by means of technological strategies. Among the strategies that have been explored, lipid-based nanosystems, particularly nanostructured lipid carriers, are promising in preclinical investigations with minimal toxicity and therapeutic efficacy due to their ability to overcome challenges associated with other nanocarriers. We review the studies of nanostructured lipid carriers for intranasal administration in the treatment of ATD. Currently, no drugs for intranasal administration in ATD have marketing approval, with only three candidates, insulin, rivastigmine and APH-1105, being clinically investigated. Further studies with different candidates will eventually confirm the potential of the intranasal route of administration in the treatment of ATD. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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27 pages, 2135 KiB

Open AccessReview

Advances in Xanthan Gum-Based Systems for the Delivery of Therapeutic Agents

by Mahima Jadav, Deep Pooja, David J. Adams and Hitesh Kulhari

Pharmaceutics 2023, 15(2), 402; https://doi.org/10.3390/pharmaceutics15020402 - 25 Jan 2023

Cited by 20 | Viewed by 4186

Abstract

In the last three decades, polymers have contributed significantly to the improvement of drug delivery technologies by enabling the controlled and sustained release of therapeutic agents, versatility in designing different delivery systems, and feasibility of encapsulation of both hydrophobic and hydrophilic molecules. Both natural and synthetic polymers have been explored for the delivery of various therapeutic agents. However, due to the disadvantages of synthetic polymers, such as lack of intrinsic biocompatibility and bioactivity, hydrophobicity, and expensive and complex procedure of synthesis, there is a move toward the use of naturally occurring polymers. The biopolymers are generally derived from either plants or microorganisms and have shown a wide range of applications in drug administration due to their hydrophilic nature, biodegradability, biocompatibility, no or low toxicity, abundance, and readily available, ease of chemical modification, etc. This review describes the applications of a biopolymer, xanthan gum (XG), in the delivery of various therapeutic agents such as drugs, genetic materials, proteins, and peptides. XG is a high molecular weight, microbial heteropolysaccharide and is produced as a fermented product of Gram-negative bacteria, Xanthomonas campestris. Traditionally, it has been used as a thickener in liquid formulations and an emulsion stabiliser. XG has several favourable properties for designing various forms of drug delivery systems. Furthermore, the structure of XG can be easily modified using different temperature and pH conditions. Therefore, XG and its derivatives have been explored for various applications in the food, pharmaceutical, and cosmetic industries. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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38 pages, 1879 KiB

Open AccessReview

Delivery of Therapeutic Biopolymers Employing Silica-Based Nanosystems

by Zoila Gándara, Noelia Rubio and Rafael R. Castillo

Pharmaceutics 2023, 15(2), 351; https://doi.org/10.3390/pharmaceutics15020351 - 20 Jan 2023

Viewed by 1448

Abstract

The use of nanoparticles is crucial for the development of a new generation of nanodevices for clinical applications. Silica-based nanoparticles can be tailored with a wide range of functional biopolymers with unique physicochemical properties thus providing several advantages: (1) limitation of interparticle interaction, (2) preservation of cargo and particle integrity, (3) reduction of immune response, (4) additional therapeutic effects and (5) cell targeting. Therefore, the engineering of advanced functional coatings is of utmost importance to enhance the biocompatibility of existing biomaterials. Herein we will focus on the most recent advances reported on the delivery and therapeutic use of silica-based nanoparticles containing biopolymers (proteins, nucleotides, and polysaccharides) with proven biological effects. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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18 pages, 1822 KiB

Open AccessReview

Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer

by Md Abdus Subhan and Vladimir P. Torchilin

Pharmaceutics 2023, 15(1), 153; https://doi.org/10.3390/pharmaceutics15010153 - 01 Jan 2023

Cited by 3 | Viewed by 2621

Abstract

Nanobiopolymers such as chitosan, gelatin, hyaluronic acid, polyglutamic acid, lipids, peptides, exosomes, etc., delivery systems have prospects to help overwhelmed physiological difficulties allied with the delivery of siRNA drugs to solid tumors, including breast cancer cells. Nanobiopolymers have favorable stimuli-responsive properties and therefore can be utilized to improve siRNA delivery platforms to undruggable MDR metastatic cancer cells. These biopolymeric siRNA drugs can shield drugs from pH degradation, extracellular trafficking, and nontargeted binding sites and are consequently suitable for drug internalization in a controlled-release fashion. In this review, the utilization of numerous biopolymeric compounds such as siRNA drug delivery systems for MDR solid tumors, including breast cancers, will be discussed. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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33 pages, 4874 KiB

Open AccessReview

Polymeric Biomaterials for Topical Drug Delivery in the Oral Cavity: Advances on Devices and Manufacturing Technologies

by Paula de Freitas Rosa Remiro, Mariana Harue Taniguchi Nagahara, Rafael Abboud Azoubel, Michelle Franz-Montan, Marcos Akira d’Ávila and Ângela Maria Moraes

Pharmaceutics 2023, 15(1), 12; https://doi.org/10.3390/pharmaceutics15010012 - 20 Dec 2022

Cited by 5 | Viewed by 2359

Abstract

There are several routes of drug administration, and each one has advantages and limitations. In the case of the topical application in the oral cavity, comprising the buccal, sublingual, palatal, and gingival regions, the advantage is that it is painless, non-invasive, allows easy application of the formulation, and it is capable of avoiding the need of drug swallowing by the patient, a matter of relevance for children and the elderly. Another advantage is the high permeability of the oral mucosa, which may deliver very high amounts of medication rapidly to the bloodstream without significant damage to the stomach. This route also allows the local treatment of lesions that affect the oral cavity, as an alternative to systemic approaches involving injection-based methods and oral medications that require drug swallowing. Thus, this drug delivery route has been arousing great interest in the pharmaceutical industry. This review aims to condense information on the types of biomaterials and polymers used for this functionality, as well as on production methods and market perspectives of this topical drug delivery route. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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14 pages, 1696 KiB

Open AccessReview

Tailoring Lipid-Based Drug Delivery Nanosystems by Synchrotron Small Angle X-ray Scattering

by Barbara Sartori and Benedetta Marmiroli

Pharmaceutics 2022, 14(12), 2704; https://doi.org/10.3390/pharmaceutics14122704 - 02 Dec 2022

Cited by 2 | Viewed by 1797

Abstract

Thanks to specific physico-chemical properties, drug delivery systems based on nanoparticles have proven to effectively transport delicate molecules for therapeutic purposes, protecting them from degradation, increasing their stability in the blood circulation and allowing to convey and release the transported substances in specific areas of the body. Nanoparticles obtained from biopolymers for applications in medicine and pharmaceutics have become particularly popular in recent years due to the enormous research effort in the field of vaccines to respond to the pandemic emergency. Among the various types of biopolymers used to produce nanoparticles for therapeutics, lipids have characteristics that make them biocompatible, with low toxicity and ease of clearance. They can be synthesized by designing their characteristics according to the foreseen administration path, or to the target of the transported drug. The analytical methods mostly used to evaluate the characteristics of lipid nanosytems for drug delivery involve studying their effects on cells, in vitro and in vivo. Although it is often considered a “niche technique“ for research in the bio-related sciences, Small Angle X-ray Scattering (SAXS) is a versatile tool to study the structure of nanosystems based on lipids, both ex situ and in situ. Therefore, it allows to evaluate both the effect of the different synthesis parameters and of the exposure of lipid nanoparticles to physiological conditions, which is of fundamental importance to design efficient drug delivery systems. In this mini-review, we will report some recent examples of characterization and design of nanoparticles based on lipids, where SAXS has been a fundamental step both to guide the synthesis of nanomaterials with tailored characteristics, and to understand the interaction between nanomaterials and cells. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery)

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