Advances in Drug Delivery Systems Using Polymeric Nanocarriers

Topic Information

Dear Colleagues,

Nanotechnology has revolutionized the way we treat and diagnose several diseases, particularly cancer. Among the many types of nanoscale drug delivery systems, polymeric nanocarriers remain the most versatile. They can be applied in multiple formats such as nanospheres, micelles, prodrug conjugates, and nanogels, and may be customized to deliver a variety of therapeutic agents including small drug molecules and biologics. Furthermore, they can be tailored to impart spatiotemporal control over drug release according to the desired therapeutic goal. Despite the long history of drug delivery research using polymeric nanocarriers, pertinent issues such as the clinical translation of in vitro and animal studies and the scale-up of nanoparticle formulations are just a few challenges that need to be overcome for these highly promising therapeutics to reach the market.

We are pleased to invite you to contribute to this Special Issue, which aims to highlight the latest advances in polymer-based nanoscale drug delivery systems, with particular emphasis on innovative approaches that address the challenges of clinical translation and scalability of polymeric nanocarriers. In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

• Polymeric nanocarriers for cancer targeting
• Polymeric nanocarriers for immunomodulation and vaccine formulations
• Polymeric nanocarriers for inflammatory disorders
• Scalable fabrication techniques for polymeric nanocarriers
• Green synthesis of polymers and polymeric nanocarriers

We look forward to receiving your contributions.

Dr. Suhair Sunoqrot
Dr. Sara A. Abdel Gaber
Topic Editors

Keywords

Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Biomedicines biomedicines	3.9	5.2	2013	14.6 Days	CHF 2600
Cancers cancers	4.5	8.0	2009	17.4 Days	CHF 2900
Future Pharmacology futurepharmacol	-	-	2021	19.2 Days	CHF 1000
Journal of Clinical Medicine jcm	3.0	5.7	2012	16 Days	CHF 2600
Journal of Nanotheranostics jnt	-	-	2020	18.2 Days	CHF 1000
Pharmaceutics pharmaceutics	4.9	7.9	2009	15.5 Days	CHF 2900

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Published Papers (6 papers)

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All Biomedicines Cancers Future Pharmacology JCM JNT Pharmaceutics

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24 pages, 5913 KiB  

Open AccessArticle

Human Serum Albumin Grafted by Monomeric and Polymeric β-Cyclodextrin as Drug Delivery System for Levofloxacin with Improved Pharmacological Properties

by Tatiana Yu Kopnova, Linara R. Yakupova, Natalya Georgievna Belogurova and Elena Vadimovna Kudryashova

Future Pharmacol. 2024, 4(1), 139-162; https://doi.org/10.3390/futurepharmacol4010010 - 13 Feb 2024

Viewed by 1809

Abstract

Human serum albumin (HSA) is a multifunctional protein, known to be a natural carrier for a number of endogenous and exogenous compounds, including drugs. HSA-based drugs formulation is a clinically validated approach to improve pharmacological properties and biodistribution (such as in Abraxane). Based [...] Read more.

Human serum albumin (HSA) is a multifunctional protein, known to be a natural carrier for a number of endogenous and exogenous compounds, including drugs. HSA-based drugs formulation is a clinically validated approach to improve pharmacological properties and biodistribution (such as in Abraxane). Based on this, one might like to modify HSA in a way that its distribution is more favorable for certain therapeutic purposes. Levofloxacin (LV), a broad-spectrum antibiotic drug, could benefit from extended systemic exposure, and stronger interactions with plasma proteins could be useful for this purpose. We engrafted monomeric or polymeric cyclodextrins (CDs) on the surface of HSA molecules to strengthen the LV adsorption (the CD−LV dissociation constant is three orders of magnitude lower than that of HSA−LV). We found that (HSA−HPolS)_conj+LV exhibited the highest activity against E. coli, whereas (HSA−HPCD)_conj+LV was the most effective against B. subtilis, and both HSA conjugates were more potent than LV alone or LV with HSA. Further fine-tuning of HSA could yield an improvement in biodistribution and thus a more favorable risk/benefit ratio. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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21 pages, 1480 KiB  

Open AccessReview

The Use of Photoactive Polymeric Nanoparticles and Nanofibers to Generate a Photodynamic-Mediated Antimicrobial Effect, with a Special Emphasis on Chronic Wounds

by Mohamed A. Abdel Khalek, Amr M. Abdelhameed and Sara A. Abdel Gaber

Pharmaceutics 2024, 16(2), 229; https://doi.org/10.3390/pharmaceutics16020229 - 5 Feb 2024

Cited by 6 | Viewed by 2733

Abstract

This review is concerned with chronic wounds, with an emphasis on biofilm and its complicated management process. The basics of antimicrobial photodynamic therapy (PDT) and its underlying mechanisms for microbial eradication are presented. Intrinsically active nanocarriers (polydopamine NPs, chitosan NPs, and polymeric micelles) [...] Read more.

This review is concerned with chronic wounds, with an emphasis on biofilm and its complicated management process. The basics of antimicrobial photodynamic therapy (PDT) and its underlying mechanisms for microbial eradication are presented. Intrinsically active nanocarriers (polydopamine NPs, chitosan NPs, and polymeric micelles) that can further potentiate the antimicrobial photodynamic effect are discussed. This review also delves into the role of photoactive electrospun nanofibers, either in their eluting or non-eluting mode of action, in microbial eradication and accelerating the healing of wounds. Synergic strategies to augment the PDT-mediated effect of photoactive nanofibers are reviewed. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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13 pages, 6945 KiB  

Open AccessArticle

Gastroprotective Chitosan Nanoparticles Loaded with Oleuropein: An In Vivo Proof of Concept

by Hend Abd-Allah, John Youshia, Gehad A. Abdel Jaleel, Azza Hassan, Mevidette El Madani and Maha Nasr

Pharmaceutics 2024, 16(1), 153; https://doi.org/10.3390/pharmaceutics16010153 - 22 Jan 2024

Cited by 3 | Viewed by 2193

Abstract

Oleuropein is the main constituent of olive leaf extract, and it has shown antioxidant and gastroprotective properties against gastric ulcers. Chitosan nanoparticles are known for their mucoadhesive abilities, and consequently, they can increase the retention time of drugs in the gastrointestinal tract. Therefore, [...] Read more.

Oleuropein is the main constituent of olive leaf extract, and it has shown antioxidant and gastroprotective properties against gastric ulcers. Chitosan nanoparticles are known for their mucoadhesive abilities, and consequently, they can increase the retention time of drugs in the gastrointestinal tract. Therefore, loading oleuropein onto chitosan nanoparticles is expected to enhance its biological efficiency. Oleuropein-loaded chitosan nanoparticles were prepared and characterized for particle size, surface charge, in vitro release, and anti-inflammatory activity. Their in vivo efficacy was assessed by measuring specific inflammatory and protective biomarkers, along with histopathological examination. The optimum oleuropein chitosan nanoparticles were cationic, had a size of 174.3 ± 2.4 nm and an entrapment efficiency of 92.81%, and released 70% of oleuropein within 8 h. They recorded a lower IC50 in comparison to oleuropein solutions for membrane stabilization of RBCs (22.6 vs. 25.6 µg/mL) and lipoxygenase inhibition (7.17 vs. 15.6 µg/mL). In an ethanol-induced gastric ulcer in vivo model, they decreased IL-1β, TNF-α, and TBARS levels by 2.1, 1.7, and 1.3 fold, respectively, in comparison to increments caused by exposure to ethanol. Moreover, they increased prostaglandin E2 and catalase enzyme levels by 2.4 and 3.8 fold, respectively. Immunohistochemical examination showed that oleuropein chitosan nanoparticles markedly lowered the expression of IL-6 and caspase-3 in gastric tissues in comparison to oleuropein solution. Overall, oleuropein chitosan nanoparticles showed superior gastroprotective effects to oleuropein solution since comparable effects were demonstrated at a 12-fold lower drug dose, delineating that chitosan nanoparticles indeed enhanced the potency of oleuropein as a gastroprotective agent. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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14 pages, 2688 KiB  

Open AccessArticle

Development and Characterization of Thiolated Cyclodextrin-Based Nanoparticles for Topical Delivery of Minoxidil

by Ammara Akhtar, Muhammad Khurram Waqas, Arshad Mahmood, Saira Tanvir, Talib Hussain, Mohsin Kazi, Muhammad Ijaz and Mulazim Hussain Asim

Pharmaceutics 2023, 15(12), 2716; https://doi.org/10.3390/pharmaceutics15122716 - 1 Dec 2023

Cited by 1 | Viewed by 1895

Abstract

Purpose: The aim of this research was to prepare adhesive nanoparticles for the topical application of Minoxidil (MXD). Methods: Thiolated β-CDs were prepared via conjugation of cysteamine with oxidized CDs. MXD was encapsulated within thiolated and unmodified β-CDs. Ionic gelation method was used [...] Read more.

Purpose: The aim of this research was to prepare adhesive nanoparticles for the topical application of Minoxidil (MXD). Methods: Thiolated β-CDs were prepared via conjugation of cysteamine with oxidized CDs. MXD was encapsulated within thiolated and unmodified β-CDs. Ionic gelation method was used to prepare nanoparticles (Thio-NP and blank NP) of CDs with chitosan. Nanoparticles were analyzed for size and zetapotential. Inclusion complexes were characterized via FTIR. Drug dissolution studies were carried out. An in vitro adhesion study over human hair was performed. An in vivo skin irritation study was performed. Ex vivo drug uptake was evaluated by using a Franz diffusion cell. Results: Thiolated β-CDs presented 1804.68 ± 25 μmol/g thiol groups and 902.34 ± 25 μmol/g disulfide bonds. Nanoparticles displayed particle sizes within a range of 231 ± 07 nm to 354 ± 13 nm. The zeta potential was in the range of −8.1 ± 02 mV, +16.0 ± 05 mV. FTIR analyses confirmed no interaction between the excipients and drug. Delayed drug release was observed from Thio-NP. Thio-NP retained over hair surfaces for a significantly longer time. Similarly, drug retention was significantly improved. Thio-NP displayed no irritation over rabbit skin. Conclusion: Owing to the above results, nanoparticles developed with MXD-loaded thiolated β-CDs might be a potential drug delivery system for topical scalp diseases. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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17 pages, 7257 KiB  

Open AccessArticle

A Closed Loop Stimuli-Responsive Concanavalin A-Loaded Chitosan–Pluronic Hydrogel for Glucose-Responsive Delivery of Short-Acting Insulin Prototyped in RIN-5F Pancreatic Cells

by Shazia Mansoor, Samson A. Adeyemi, Pierre P. D. Kondiah and Yahya E. Choonara

Biomedicines 2023, 11(9), 2545; https://doi.org/10.3390/biomedicines11092545 - 15 Sep 2023

Cited by 5 | Viewed by 1808

Abstract

The optimal treatment of diabetes (in particular, type 1 diabetes—T1D) remains a challenge. Closed-loop systems (implants/inserts) provide significant advantages for glucose responsivity and providing real-time sustained release of rapid-acting insulin. Concanavalin A (ConA), a glucose affinity agent, has been used to design closed-loop [...] Read more.

The optimal treatment of diabetes (in particular, type 1 diabetes—T1D) remains a challenge. Closed-loop systems (implants/inserts) provide significant advantages for glucose responsivity and providing real-time sustained release of rapid-acting insulin. Concanavalin A (ConA), a glucose affinity agent, has been used to design closed-loop insulin delivery systems but not without significant risk of leakage of ConA from the matrices and poor mechanical strength of the hydrogels impacting longevity and control of insulin release. Therefore, this work focused on employing a thermoresponsive co-forming matrix between Pluronic F-127 (PL) and structurally robust chitosan (CHT) via EDC/NHS coupling (i.e., covalent linkage of -NH₂ from CHT and ConA to the -COOH of PL). The system was characterized for its chemical structure stability and integrity (FTIR, XRD and TGA), injectability, rheological parameters and hydrogel morphology (Texture Analysis, Elastosens TM Bio2 and SEM). The prepared hydrogels demonstrated shear-thinning for injectability with a maximum force of 4.9 ± 8.3 N in a 26G needle with sol–gel transitioning from 25 to 38 °C. The apparent yield stress value of the hydrogel was determined to be 67.47 Pa. The insulin loading efficiency within the hydrogel matrix was calculated to be 46.8%. Insulin release studies revealed glucose responsiveness in simulated glycemic media (4 and 10 mg/mL) over 7 days (97%) (305 nm via fluorescence spectrophotometry). The MTT studies were performed over 72 h on RIN-5F pancreatic cells with viability results >80%. Results revealed that the thermoresponsive hydrogel is a promising alternative to current closed-loop insulin delivery systems. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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15 pages, 2484 KiB  

Open AccessArticle

Targeted Anticancer Agent with Original Mode of Action Prepared by Supramolecular Assembly of Antibody Oligonucleotide Conjugates and Cationic Nanoparticles

by Victor Lehot, Patrick Neuberg, Manon Ripoll, François Daubeuf, Stéphane Erb, Igor Dovgan, Sylvain Ursuegui, Sarah Cianférani, Antoine Kichler, Guilhem Chaubet and Alain Wagner

Pharmaceutics 2023, 15(6), 1643; https://doi.org/10.3390/pharmaceutics15061643 - 2 Jun 2023

Cited by 3 | Viewed by 3174

Abstract

Despite their clinical success, Antibody-Drug Conjugates (ADCs) are still limited to the delivery of a handful of cytotoxic small-molecule payloads. Adaptation of this successful format to the delivery of alternative types of cytotoxic payloads is of high interest in the search for novel [...] Read more.

Despite their clinical success, Antibody-Drug Conjugates (ADCs) are still limited to the delivery of a handful of cytotoxic small-molecule payloads. Adaptation of this successful format to the delivery of alternative types of cytotoxic payloads is of high interest in the search for novel anticancer treatments. Herein, we considered that the inherent toxicity of cationic nanoparticles (cNP), which limits their use as oligonucleotide delivery systems, could be turned into an opportunity to access a new family of toxic payloads. We complexed anti-HER2 antibody-oligonucleotide conjugates (AOC) with cytotoxic cationic polydiacetylenic micelles to obtain Antibody-Toxic-Nanoparticles Conjugates (ATNPs) and studied their physicochemical properties, as well as their bioactivity in both in vitro and in vivo HER2 models. After optimising their AOC/cNP ratio, the small (73 nm) HER2-targeting ATNPs were found to selectively kill antigen-positive SKBR-2 cells over antigen-negative MDA-MB-231 cells in serum-containing medium. Further in vivo anti-cancer activity was demonstrated in an SKBR-3 tumour xenograft model in BALB/c mice in which stable 60% tumour regression could be observed just after two injections of 45 pmol of ATNP. These results open interesting prospects in the use of such cationic nanoparticles as payloads for ADC-like strategies. Full article

(This article belongs to the Topic Advances in Drug Delivery Systems Using Polymeric Nanocarriers)

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