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18 pages, 14694 KiB

Open AccessArticle

Nanostructured Poly-l-lactide and Polyglycerol Adipate Carriers for the Encapsulation of Usnic Acid: A Promising Approach for Hepatoprotection

by Benedetta Brugnoli, Greta Perna, Sara Alfano, Antonella Piozzi, Luciano Galantini, Eleni Axioti, Vincenzo Taresco, Alessia Mariano, Anna Scotto d’Abusco, Stefano Vecchio Ciprioti and Iolanda Francolini

Polymers 2024, 16(3), 427; https://doi.org/10.3390/polym16030427 - 03 Feb 2024

Viewed by 869

Abstract

The present study investigates the utilization of nanoparticles based on poly-l-lactide (PLLA) and polyglycerol adipate (PGA), alone and blended, for the encapsulation of usnic acid (UA), a potent natural compound with various therapeutic properties including antimicrobial and anticancer activities. The development of these [...] Read more.

The present study investigates the utilization of nanoparticles based on poly-l-lactide (PLLA) and polyglycerol adipate (PGA), alone and blended, for the encapsulation of usnic acid (UA), a potent natural compound with various therapeutic properties including antimicrobial and anticancer activities. The development of these carriers offers an innovative approach to overcome the challenges associated with usnic acid’s limited aqueous solubility, bioavailability, and hepatotoxicity. The nanosystems were characterized according to their physicochemical properties (among others, size, zeta potential, thermal properties), apparent aqueous solubility, and in vitro cytotoxicity. Interestingly, the nanocarrier obtained with the PLLA-PGA 50/50 weight ratio blend showed both the lowest size and the highest UA apparent solubility as well as the ability to decrease UA cytotoxicity towards human hepatocytes (HepG2 cells). This research opens new avenues for the effective utilization of these highly degradable and biocompatible PLLA-PGA blends as nanocarriers for reducing the cytotoxicity of usnic acid. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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12 pages, 2930 KiB

Open AccessArticle

Hydroxyapatite/Poly (Butylene Succinate)/Metoprolol Tartrate Composites with Controllable Drug Release and a Porous Structure for Bone Scaffold Application

by Hongming Yang, Rui Pan, Yuan Zhou, Guiting Liu, Rong Chen and Shaoyun Guo

Polymers 2023, 15(21), 4205; https://doi.org/10.3390/polym15214205 - 24 Oct 2023

Viewed by 799

Abstract

Nowadays, it is a challenge for a bone scaffold to achieve controllable drug release and a porous structure at the same time. Herein, we fabricated hydroxyapatite/poly (butylene succinate)/metoprolol tartrate (HA/PBS/MPT) composites via melt blending, aiming to provide the option of an in situ [...] Read more.

Nowadays, it is a challenge for a bone scaffold to achieve controllable drug release and a porous structure at the same time. Herein, we fabricated hydroxyapatite/poly (butylene succinate)/metoprolol tartrate (HA/PBS/MPT) composites via melt blending, aiming to provide the option of an in situ pore-forming strategy. The introduction of HA not only significantly improved the hydrophilicity of the PBS matrix by reducing the hydrophilic contact angle by approximately 36% at a 10% content, but also damaged the integrity of the PBS crystal. Both were beneficial for the penetration of phosphate-buffered saline solution into matrix and the acceleration of MPT release. Accompanied with MPT release, porous structures were formed in situ, and the HA inside the matrix was exposed. With the increase in HA content, the MPT release rate accelerated and the pore size became larger. The in vitro cytocompatibility evaluation indicated that HA/PBS/MPT composites were conductive to the adhesion, growth, and proliferation of MC3T3-E1 cells due to the HA being exposed around the pores. Thus, the MPT release rate, pore size, and cell induction ability of the HA/PBS/MPT composites were flexibly and effectively adjusted by the composition at the same time. By introducing HA, we innovatively achieved the construction of porous structures during the drug release process, without the addition of pore-forming agents. This approach allows the drug delivery system to combine controllable drug release and biocompatibility effectively, offering a novel method for bone repair material preparation. This work might provide a convenient and robust strategy for the fabrication of bone scaffolds with controllable drug release and porous structures. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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10 pages, 2529 KiB

Open AccessArticle

Study on Nanomaterials with Inhibitory Effects on the Growth of Aspergillus niger

by Ziqi Qin, Yiyuan Peng, Yiting Pu, Tao Liu, Kun Qian and Huan Tang

Polymers 2023, 15(18), 3820; https://doi.org/10.3390/polym15183820 - 19 Sep 2023

Cited by 1 | Viewed by 722

Abstract

In this paper, the inhibitory effect of various nanomaterials on the growth of Aspergillus niger was studied. Among them, copper nanorods had the most obvious inhibitory effect on the growth of Aspergillus niger. The phase of copper nanorods was modified by chitosan, [...] Read more.

In this paper, the inhibitory effect of various nanomaterials on the growth of Aspergillus niger was studied. Among them, copper nanorods had the most obvious inhibitory effect on the growth of Aspergillus niger. The phase of copper nanorods was modified by chitosan, and its inhibitory effect on the expansion of Aspergillus niger was measured. 1. Preparation of copper nanorods and chitosan@copper nanorods: Copper nanorods with a diameter of about 300–350 nm and a length of about 100–800 nm were prepared by the liquid-phase reduction method. The chitosan solution was prepared by using the characteristics of chitosan dissolved in dilute acid to prepare chitosan@copper nanorods and modify the phase of copper nanorods. 2. Determination of the inhibitory effect of various copper nanomaterials on the growth of Aspergillus niger, including Cuprous Oxide nanoparticles, copper nanorods, nano copper oxide, and copper hydroxide, which have certain inhibitory effects on the growth of Aspergillus niger. Among them, copper nanorods have a better effect. On this basis, chitosan@copper nanorods are obtained by modifying the phase of copper nanorods with chitosan. The measured antibacterial effect is that the EC₅₀ value is 344 mg/L. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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15 pages, 3372 KiB

Open AccessArticle

Well-Defined Shell-Sheddable Core-Crosslinked Micelles with pH and Oxidation Dual-Response for On-Demand Drug Delivery

by Xinfeng Cheng, Qiyang Li, Xiaomeng Sun, Yuxin Ma, Huanping Xie, Weiguang Kong, Xianchao Du, Zhenghui Zhang, Dongfang Qiu and Yong Jin

Polymers 2023, 15(9), 1990; https://doi.org/10.3390/polym15091990 - 23 Apr 2023

Cited by 2 | Viewed by 1433

Abstract

Micellar-nanocarrier-based drug delivery systems possessing characteristics such as an excellent circulation stability, inhibited premature release and on-demand site-specific release are urgently needed for enhanced therapeutic efficacy. Therefore, a novel kind of shell-sheddable core-crosslinked polymeric micelles with pH and oxidation dual-triggered on-demand drug release [...] Read more.

Micellar-nanocarrier-based drug delivery systems possessing characteristics such as an excellent circulation stability, inhibited premature release and on-demand site-specific release are urgently needed for enhanced therapeutic efficacy. Therefore, a novel kind of shell-sheddable core-crosslinked polymeric micelles with pH and oxidation dual-triggered on-demand drug release behavior was facilely constructed. The multifunctional micelles were self-assembled from a carefully designed amphiphilic triblock PEGylated polyurethane (PEG-acetal-PUBr-acetal-PEG) employing an acid-labile acetal linker at the hydrophilic–hydrophobic interface and pendant reactive bromo-containing polyurethane (PU) as the hydrophobic block, followed by a post-crosslinking via oxidation-cleavable diselenide linkages. These well-defined micelles exhibited an enhanced structural stability against dilution, achieved through the incorporation of diselenide crosslinkers. As expected, they were found to possess dual pH- and oxidation-responsive dissociation behaviors when exposure to acid pH (~5.0) and 50 mM H₂O₂ conditions, as evidenced using dynamic light-scattering (DLS) and atomic force microscopy (AFM) analyses. An in vitro drug release investigation showed that the drug indomethacin (IND) could be efficiently encapsulated in the micelles, which demonstrated an inhibited premature release compared to the non-crosslinked ones. It is noteworthy that the resulting micelles could efficiently release entrapped drugs at a fast rate in response to either pH or oxidation stimuli. Moreover, the release could be significantly accelerated in the presence of both acid pH and oxidation conditions, relative to a single stimulus, owing to the synergetic degradation of micelles through pH-induced dePEGylation and oxidation-triggered decrosslinking processes. The proposed shell-sheddable core-crosslinked micelles with a pH and oxidation dual-response could be potential candidates as drug carriers for on-demand drug delivery. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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14 pages, 3449 KiB

Open AccessArticle

Construction and Performance Evaluation of Nicandra physalodes (Linn.) Gaertn. Polysaccharide-Based Nanogel

by Fangyan Liu, Chen Shen, Xuelian Chen, Fei Gao and Yin Chen

Polymers 2023, 15(8), 1933; https://doi.org/10.3390/polym15081933 - 19 Apr 2023

Cited by 1 | Viewed by 1138

Abstract

The nanogels made from these polysaccharides and their derivatives are often used to construct drug delivery systems owing to their biocompatible, biodegradable, non-toxic, water-soluble, and bioactive characteristics. In this work, a novel pectin with unique gelling properties was extracted from the seed of [...] Read more.

The nanogels made from these polysaccharides and their derivatives are often used to construct drug delivery systems owing to their biocompatible, biodegradable, non-toxic, water-soluble, and bioactive characteristics. In this work, a novel pectin with unique gelling properties was extracted from the seed of Nicandra physalodes (NPGP). The structural research indicated that NPGP was a low methoxyl pectin with a high content of galacturonic acid. NPGP-based nanogels (NGs) were accomplished employing the water in oil (W/O) nano-emulsion method. The cysteamine containing reduction-responsive bond and integrin-targeting RGD peptide were also grafted onto NPGP. The anti-tumor drug doxorubicin hydrochloride (DOX) was loaded during the formation of NGs, and the performance of DOX delivery was studied. The NGs were characterized by UV-vis, DLS, TEM, FT-IR, and XPS. The results showed that the prepared NGs were nanosized (167.6 ± 53.86 nm), had excellent encapsulation efficiency (91.61 ± 0.85%), and possessed a fine drug loading capacity (8.40 ± 0.16%). The drug release experiment showed that DOX@NPGP-SS-RGD had good redox-responsive performance. Furthermore, the results of cell experiments revealed good biocompatibility of prepared NGs, along with selective absorption by HCT-116 cells through integrin receptor-mediated endocytosis to play an anti-tumor effect. These studies indicated the potential application of NPGP-based NGs as targeted drug delivery systems. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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Review

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26 pages, 3788 KiB

Open AccessReview

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

by Agus Rusdin, Amirah Mohd Gazzali, Nur Ain Thomas, Sandra Megantara, Diah Lia Aulifa, Arif Budiman and Muchtaridi Muchtaridi

Polymers 2024, 16(2), 286; https://doi.org/10.3390/polym16020286 - 20 Jan 2024

Viewed by 1041

Abstract

Background: The current challenge in drug development lies in addressing the physicochemical issues that lead to low drug effectiveness. Solubility, a crucial physicochemical parameter, greatly influences various biopharmaceutical aspects of a drug, including dissolution rate, absorption, and bioavailability. Amorphous solid dispersion (ASD) has [...] Read more.

Background: The current challenge in drug development lies in addressing the physicochemical issues that lead to low drug effectiveness. Solubility, a crucial physicochemical parameter, greatly influences various biopharmaceutical aspects of a drug, including dissolution rate, absorption, and bioavailability. Amorphous solid dispersion (ASD) has emerged as a widely explored approach to enhance drug solubility. Objective: The objective of this review is to discuss and summarize the development of polyvinylpyrrolidone (PVP)-based amorphous solid dispersion in improving the physicochemical properties of drugs, with a focus on the use of PVP as a novel approach. Methodology: This review was conducted by examining relevant journals obtained from databases such as Scopus, PubMed, and Google Scholar, since 2018. The inclusion and exclusion criteria were applied to select suitable articles. Results: This study demonstrated the versatility and efficacy of PVP in enhancing the solubility and bioavailability of poorly soluble drugs. Diverse preparation methods, including solvent evaporation, melt quenching, electrospinning, coprecipitation, and ball milling are discussed for the production of ASDs with tailored characteristics. Conclusion: PVP-based ASDs could offer significant advantages in the formulation strategies, stability, and performance of poorly soluble drugs to enhance their overall bioavailability. The diverse methodologies and findings presented in this review will pave the way for further advancements in the development of effective and tailored amorphous solid dispersions. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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30 pages, 2984 KiB

Open AccessReview

Application of Starch, Cellulose, and Their Derivatives in the Development of Microparticle Drug-Delivery Systems

by Paolina Lukova, Plamen Katsarov and Bissera Pilicheva

Polymers 2023, 15(17), 3615; https://doi.org/10.3390/polym15173615 - 31 Aug 2023

Cited by 7 | Viewed by 2913

Abstract

Micro- and nanotechnologies have been intensively studied in recent years as novel platforms for targeting and controlling the delivery of various pharmaceutical substances. Microparticulate drug delivery systems for oral, parenteral, or topical administration are multiple unit formulations, considered as powerful therapeutic tools for [...] Read more.

Micro- and nanotechnologies have been intensively studied in recent years as novel platforms for targeting and controlling the delivery of various pharmaceutical substances. Microparticulate drug delivery systems for oral, parenteral, or topical administration are multiple unit formulations, considered as powerful therapeutic tools for the treatment of various diseases, providing sustained drug release, enhanced drug stability, and precise dosing and directing the active substance to specific sites in the organism. The properties of these pharmaceutical formulations are highly dependent on the characteristics of the polymers used as drug carriers for their preparation. Starch and cellulose are among the most preferred biomaterials for biomedical applications due to their biocompatibility, biodegradability, and lack of toxicity. These polysaccharides and their derivatives, like dextrins (maltodextrin, cyclodextrins), ethylcellulose, methylcellulose, hydroxypropyl methylcellulose, carboxy methylcellulose, etc., have been widely used in pharmaceutical technology as excipients for the preparation of solid, semi-solid, and liquid dosage forms. Due to their accessibility and relatively easy particle-forming properties, starch and cellulose are promising materials for designing drug-loaded microparticles for various therapeutic applications. This study aims to summarize some of the basic characteristics of starch and cellulose derivatives related to their potential utilization as microparticulate drug carriers in the pharmaceutical field. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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35 pages, 2091 KiB

Open AccessReview

Cyclodextrin-Based Polymeric Drug Delivery Systems for Cancer Therapy

by Xuebing Li, Junda Liu and Neng Qiu

Polymers 2023, 15(6), 1400; https://doi.org/10.3390/polym15061400 - 11 Mar 2023

Cited by 6 | Viewed by 2055

Abstract

Cyclodextrins (CDs) are one of the most extensively studied cyclic-oligosaccharides due to their low toxicity, good biodegradability and biocompatibility, facile chemical modification, and unique inclusion capacity. However, problems such as poor pharmacokinetics, plasma membrane disruption, hemolytic effects and a lack of target specificity [...] Read more.

Cyclodextrins (CDs) are one of the most extensively studied cyclic-oligosaccharides due to their low toxicity, good biodegradability and biocompatibility, facile chemical modification, and unique inclusion capacity. However, problems such as poor pharmacokinetics, plasma membrane disruption, hemolytic effects and a lack of target specificity still exist for their applications as drug carriers. Recently, polymers have been introduced into CDs to combine the advantages of both biomaterials for the superior delivery of anticancer agents in cancer treatment. In this review, we summarize four types of CD-based polymeric carriers for the delivery of chemotherapeutics or gene agents for cancer therapy. These CD-based polymers were classified based on their structural properties. Most of the CD-based polymers were amphiphilic with the introduction of hydrophobic/hydrophilic segments and were able to form nanoassemblies. Anticancer drugs could be included in the cavity of CDs, encapsulated in the nanoparticles or conjugated on the CD-based polymers. In addition, the unique structures of CDs enable the functionalization of targeting agents and stimuli-responsive materials to realize the targeting and precise release of anticancer agents. In summary, CD-based polymers are attractive carriers for anticancer agents. Full article

(This article belongs to the Special Issue Polymeric Materials for Drug Delivery II)

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