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Pharmaceutics
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PLGA Nanoparticles for Drug Delivery
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PLGA Nanoparticles for Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (10 January 2024) | Viewed by 11196

Special Issue Editor

Prof. Dr. Jin-Wook Yoo

E-Mail Website
Guest Editor
College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea
Interests: nanomedicine; colon-targeted delivery; wound healing; nitric oxide delivery; infectious diseases
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polymeric nanoparticles have long been investigated as a drug delivery system to resolve the intrinsic problems of free drugs such as low solubility, poor stability and unwanted side effects caused by lack of targeting ability. Among various medical polymers, poly(d, l-lactide-co-glycolide), PLGA, is one of the most widely used polymers in the field of nanoparticle-based drug delivery. PLGA nanoparticles have advantages of excellent biocompatibility, biodegradability with the ability to encapsulate drugs and adaptive versatile surface functionalities such as targetability. For the reasons, PLGA nanoparticles have been exploited for the development of various drug delivery systems and are still evolving for more effective delivery function. Therefore, this Special Issue aims to present the latest advances in the development of drug delivery systems based on PLGA nanoparticles.

Prof. Dr. Jin-Wook Yoo
Guest Editor

Manuscript Submission Information

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Keywords

  • PLGA
  • nanoparticles
  • drug delivery
  • targeting
  • encapsulation

Published Papers (5 papers)

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Research

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13 pages, 3256 KiB  
Article
Core-Shell Structured PLGA Particles Having Highly Controllable Ketoprofen Drug Release
by Norbert Varga, Rita Bélteki, Ádám Juhász and Edit Csapó
Pharmaceutics 2023, 15(5), 1355; https://doi.org/10.3390/pharmaceutics15051355 - 28 Apr 2023
Cited by 3 | Viewed by 1184
Abstract
The non-steroid anti-inflammatory drug ketoprofen (KP) as a model molecule is encapsulated in different poly(lactide-co-glycolide) (PLGA) nanostructured particles, using Tween20 (TWEEN) and Pluronic F127 (PLUR) as stabilizers to demonstrate the design of a biocompatible colloidal carrier particles with highly controllable drug release feature. [...] Read more.
The non-steroid anti-inflammatory drug ketoprofen (KP) as a model molecule is encapsulated in different poly(lactide-co-glycolide) (PLGA) nanostructured particles, using Tween20 (TWEEN) and Pluronic F127 (PLUR) as stabilizers to demonstrate the design of a biocompatible colloidal carrier particles with highly controllable drug release feature. Based on TEM images the formation of well-defined core-shell structure is highly favorable using nanoprecipitation method. Stabile polymer-based colloids with ~200–210 nm hydrodynamic diameter can be formed by successful optimization of the KP concentration with the right choice of stabilizer. Encapsulation efficiency (EE%) of 14–18% can be achieved. We clearly confirmed that the molecular weight of the stabilizer thus its structure greatly controls the drug release from the PLGA carrier particles. It can be determined that ~20% and ~70% retention is available with the use of PLUR and TWEEN, respectively. This measurable difference can be explained by the fact that the non-ionic PLUR polymer provides a steric stabilization of the carrier particles in the form of a loose shell, while the adsorption of the non-ionic biocompatible TWEEN surfactant results in a more compact and well-ordered shell around the PLGA particles. In addition, the release property can be further tuned by decreasing the hydrophilicity of PLGA by changing the monomer ratio in the range of ~20–60% (PLUR) and 70–90% (TWEEN). Full article
(This article belongs to the Special Issue PLGA Nanoparticles for Drug Delivery)
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19 pages, 6231 KiB  
Article
Targeted Two-Step Delivery of Oncotheranostic Nano-PLGA for HER2-Positive Tumor Imaging and Therapy In Vivo: Improved Effectiveness Compared to One-Step Strategy
by Victoria O. Shipunova, Elena N. Komedchikova, Polina A. Kotelnikova, Maxim P. Nikitin and Sergey M. Deyev
Pharmaceutics 2023, 15(3), 833; https://doi.org/10.3390/pharmaceutics15030833 - 03 Mar 2023
Cited by 6 | Viewed by 1914
Abstract
Therapy for aggressive metastatic breast cancer remains a great challenge for modern biomedicine. Biocompatible polymer nanoparticles have been successfully used in clinic and are seen as a potential solution. Specifically, researchers are exploring the development of chemotherapeutic nanoagents targeting the membrane-associated receptors of [...] Read more.
Therapy for aggressive metastatic breast cancer remains a great challenge for modern biomedicine. Biocompatible polymer nanoparticles have been successfully used in clinic and are seen as a potential solution. Specifically, researchers are exploring the development of chemotherapeutic nanoagents targeting the membrane-associated receptors of cancer cells, such as HER2. However, there are no targeting nanomedications that have been approved for human cancer therapy. Novel strategies are being developed to alter the architecture of agents and optimize their systemic administration. Here, we describe a combination of these approaches, namely, the design of a targeted polymer nanocarrier and a method for its systemic delivery to the tumor site. Namely, PLGA nanocapsules loaded with a diagnostic dye, Nile Blue, and a chemotherapeutic compound, doxorubicin, are used for two-step targeted delivery using the concept of tumor pre-targeting through the barnase/barstar protein “bacterial superglue”. The first pre-targeting component consists of an anti-HER2 scaffold protein, DARPin9_29 fused with barstar, Bs-DARPin9_29, and the second component comprises chemotherapeutic PLGA nanocapsules conjugated to barnase, PLGA-Bn. The efficacy of this system was evaluated in vivo. To this aim, we developed an immunocompetent BALB/c mouse tumor model with a stable expression of human HER2 oncomarkers to test the potential of two-step delivery of oncotheranostic nano-PLGA. In vitro and ex vivo studies confirmed HER2 receptor stable expression in the tumor, making it a feasible tool for HER2-targeted drug evaluation. We demonstrated that two-step delivery was more effective than one-step delivery for both imaging and tumor therapy: two-step delivery had higher imaging capabilities than one-step and a tumor growth inhibition of 94.9% in comparison to 68.4% for the one-step strategy. The barnase*barstar protein pair has been proven to possess excellent biocompatibility, as evidenced by the successful completion of biosafety tests assessing immunogenicity and hemotoxicity. This renders the protein pair a highly versatile tool for pre-targeting tumors with various molecular profiles, thereby enabling the development of personalized medicine. Full article
(This article belongs to the Special Issue PLGA Nanoparticles for Drug Delivery)
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19 pages, 17879 KiB  
Article
PLGA Nanoparticles Containing VCAM-1 Inhibitor Succinobucol and Chemotherapeutic Doxorubicin as Therapy against Primary Tumors and Their Lung Metastases
by Jie Wang, Fengling Wang, Dandan Xie, Min Zhou, Jiaxing Liao, Hongliang Wu, Yue Dai, Jingbin Huang and Yu Zhao
Pharmaceutics 2023, 15(2), 349; https://doi.org/10.3390/pharmaceutics15020349 - 20 Jan 2023
Cited by 1 | Viewed by 1649
Abstract
The treatment of malignant tumors is usually accompanied by poor prognosis due to metastasis of tumor cells. Hence, it is crucial to enhance anti-metastasis efficacy when anti-tumor treatments are conducted. It has been reported that the vascular cell adhesion molecule-1 (VCAM-1) is highly [...] Read more.
The treatment of malignant tumors is usually accompanied by poor prognosis due to metastasis of tumor cells. Hence, it is crucial to enhance anti-metastasis efficacy when anti-tumor treatments are conducted. It has been reported that the vascular cell adhesion molecule-1 (VCAM-1) is highly expressed on the surface of tumor cells and plays an essential role in the metastasis of tumor cells. Thus, reducing VCAM-1 expression offers hope for inhibiting the metastasis of tumor cells. Evidence has shown that succinobucol (Suc) can selectively and efficiently inhibit VCAM-1 expression. Inspired by these, we designed dual drug-loaded PLGA nanoparticles (Co-NPs) to co-deliver VCAM-1 inhibitor Suc and the chemotherapeutic doxorubicin (Dox) which could both effectively suppress primary melanoma and its lung metastases. Co-NPs were composed of PLGA encapsulated Suc and Dox as hydrophobic cores and DSPE-mPEG2000 as surface modification materials. With an appropriate particle size (122.4 nm) and a negatively charged surface (−6.77 mV) we could achieve prolonged blood circulation. The in vitro experiments showed that Co-NPs had potent cytotoxicity against B16F10 cells and could significantly inhibit VCAM-1 expression and migration of B16F10 cells. Additionally, the in vivo experiments showed that Co-NPs could efficiently suppress not only primary melanoma but also its lung metastases. In conclusion, PLGA nanoparticles containing VCAM-1 inhibitor Suc and chemotherapeutic Dox as therapy against primary tumors and their lung metastases provides a promising drug delivery strategy for the treatment of metastatic malignant tumors. Full article
(This article belongs to the Special Issue PLGA Nanoparticles for Drug Delivery)
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18 pages, 3211 KiB  
Article
Hyaluronic Acid-Conjugated PLGA Nanoparticles Alleviate Ulcerative Colitis via CD44-Mediated Dual Targeting to Inflamed Colitis Tissue and Macrophages
by Shwe Phyu Hlaing, Jiafu Cao, Juho Lee, Jihyun Kim, Aruzhan Saparbayeva, Dongmin Kwak, Hyunwoo Kim, Seonghwan Hwang, Hwayoung Yun, Hyung Ryong Moon, Yunjin Jung and Jin-Wook Yoo
Pharmaceutics 2022, 14(10), 2118; https://doi.org/10.3390/pharmaceutics14102118 - 05 Oct 2022
Cited by 12 | Viewed by 2939
Abstract
Although various local anti-inflammatory therapies for ulcerative colitis have been developed, rapid drug elimination from inflamed colitis tissue and off-target side effects reduce their therapeutic efficacy. In this study, we synthesized curcumin (Cur)-loaded hyaluronic acid (HA)-conjugated nanoparticles (Cur-HA-PLGA-NPs) that target inflamed colitis tissue [...] Read more.
Although various local anti-inflammatory therapies for ulcerative colitis have been developed, rapid drug elimination from inflamed colitis tissue and off-target side effects reduce their therapeutic efficacy. In this study, we synthesized curcumin (Cur)-loaded hyaluronic acid (HA)-conjugated nanoparticles (Cur-HA-PLGA-NPs) that target inflamed colitis tissue via HA-CD44 interaction with resident colonic epithelial cells and subsequently target activated macrophages for ulcerative colitis therapy. The synthesized spherical Cur-HA-PLGA-NPs showed physicochemical properties similar to those of non-HA-conjugated Cur-PLGA-NPs. HA-PLGA-NPs exhibited selective accumulation in inflamed colitis tissue with minimal accumulation in healthy colon tissue. HA functionalization enhanced targeted drug delivery to intestinal macrophages, significantly increasing HA-PLGA-NP cellular uptake. Importantly, the rectal administration of Cur-HA-PLGA-NPs exhibited better therapeutic efficacy than Cur-PLGA-NPs in animal studies. Histological examination revealed that Cur-HA-PLGA-NPs reduced inflammation with less inflammatory cell infiltration and accelerated recovery with re-epithelialization signs. Our results suggest that Cur-HA-PLGA-NPs are a promising delivery platform for treating ulcerative colitis. Full article
(This article belongs to the Special Issue PLGA Nanoparticles for Drug Delivery)
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Review

Jump to: Research

35 pages, 2038 KiB  
Review
Use of Poly Lactic-co-glycolic Acid Nano and Micro Particles in the Delivery of Drugs Modulating Different Phases of Inflammation
by Chiara Puricelli, Casimiro Luca Gigliotti, Ian Stoppa, Sara Sacchetti, Deepika Pantham, Anna Scomparin, Roberta Rolla, Stefania Pizzimenti, Umberto Dianzani, Elena Boggio and Salvatore Sutti
Pharmaceutics 2023, 15(6), 1772; https://doi.org/10.3390/pharmaceutics15061772 - 20 Jun 2023
Cited by 6 | Viewed by 2784
Abstract
Chronic inflammation contributes to the pathogenesis of many diseases, including apparently unrelated conditions such as metabolic disorders, cardiovascular diseases, neurodegenerative diseases, osteoporosis, and tumors, but the use of conventional anti-inflammatory drugs to treat these diseases is generally not very effective given their adverse [...] Read more.
Chronic inflammation contributes to the pathogenesis of many diseases, including apparently unrelated conditions such as metabolic disorders, cardiovascular diseases, neurodegenerative diseases, osteoporosis, and tumors, but the use of conventional anti-inflammatory drugs to treat these diseases is generally not very effective given their adverse effects. In addition, some alternative anti-inflammatory medications, such as many natural compounds, have scarce solubility and stability, which are associated with low bioavailability. Therefore, encapsulation within nanoparticles (NPs) may represent an effective strategy to enhance the pharmacological properties of these bioactive molecules, and poly lactic-co-glycolic acid (PLGA) NPs have been widely used because of their high biocompatibility and biodegradability and possibility to finely tune erosion time, hydrophilic/hydrophobic nature, and mechanical properties by acting on the polymer’s composition and preparation technique. Many studies have been focused on the use of PLGA-NPs to deliver immunosuppressive treatments for autoimmune and allergic diseases or to elicit protective immune responses, such as in vaccination and cancer immunotherapy. By contrast, this review is focused on the use of PLGA NPs in preclinical in vivo models of other diseases in which a key role is played by chronic inflammation or unbalance between the protective and reparative phases of inflammation, with a particular focus on intestinal bowel disease; cardiovascular, neurodegenerative, osteoarticular, and ocular diseases; and wound healing. Full article
(This article belongs to the Special Issue PLGA Nanoparticles for Drug Delivery)
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