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22 pages, 4061 KiB

Open AccessEditor’s ChoiceArticle

Cinnamyl-Modified Polyglycidol/Poly(ε-Caprolactone) Block Copolymer Nanocarriers for Enhanced Encapsulation and Prolonged Release of Cannabidiol

by Natalia Toncheva-Moncheva, Erik Dimitrov, Georgi Grancharov, Denitsa Momekova, Petar Petrov and Stanislav Rangelov

Pharmaceutics 2023, 15(8), 2128; https://doi.org/10.3390/pharmaceutics15082128 - 13 Aug 2023

Cited by 1 | Viewed by 1137

Abstract

The present study describes the development of novel block copolymer nanocarriers of the phytocannabinoid cannabidiol (CBD), designed to enhance the solubility of the drug in water while achieving high encapsulation efficiency and prolonged drug release. Firstly, a well-defined amphiphilic block copolymer consisting of [...] Read more.

The present study describes the development of novel block copolymer nanocarriers of the phytocannabinoid cannabidiol (CBD), designed to enhance the solubility of the drug in water while achieving high encapsulation efficiency and prolonged drug release. Firstly, a well-defined amphiphilic block copolymer consisting of two outer hydrophilic polyglycidol (PG) blocks and a middle hydrophobic block of poly(ε-caprolactone) bearing pendant cinnamyl moieties (P(CyCL-co-CL)) were synthesized by the click coupling reaction of PG-monoalkyne and P(CyCL-co-CL)-diazide functional macroreagents. A non-modified polyglycidol/poly(ε-caprolactone) amphiphilic block copolymer was obtained as a referent system. Micellar carriers based on the two block copolymers were formed via the solvent evaporation method and loaded with CBD following two different protocols—loading during micelle formation and loading into preformed micelles. The key parameters/characteristics of blank and CBD-loaded micelles such as size, size distribution, zeta potential, molar mass, critical micelle concentration, morphology, and encapsulation efficiency were determined by using dynamic and static multiangle and electrophoretic light scattering, transmission electron microscopy, and atomic force microscopy. Embedding CBD into the micellar carriers affected their hydrodynamic radii to some extent, while the spherical morphology of particles was not changed. The nanoformulation based on the copolymer bearing cinnamyl moieties possessed significantly higher encapsulation efficiency and a slower rate of drug release than the non-modified copolymer. The comparative assessment of the antiproliferative effect of micellar CBD vs. the free drug against the acute myeloid leukemia-derived HL-60 cell line and Sezary Syndrome HUT-78 demonstrated that the newly developed systems have pronounced antitumor activity. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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18 pages, 9751 KiB

Open AccessArticle

Novel Fluorescent Benzimidazole-Hydrazone-Loaded Micellar Carriers for Controlled Release: Impact on Cell Toxicity, Nuclear and Microtubule Alterations in Breast Cancer Cells

by Rayna Bryaskova, Nikolai Georgiev, Nikoleta Philipova, Ventsislav Bakov, Kameliya Anichina, Maria Argirova, Sonia Apostolova, Irina Georgieva and Rumiana Tzoneva

Pharmaceutics 2023, 15(6), 1753; https://doi.org/10.3390/pharmaceutics15061753 - 16 Jun 2023

Cited by 2 | Viewed by 1212

Abstract

Fluorescent micellar carriers with controlled release of a novel anticancer drug were developed to enable intracellular imaging and cancer treatment simultaneously. The nanosized fluorescent micellar systems were embedded with a novel anticancer drug via the self-assembling behavior of well-defined block copolymers based on [...] Read more.

Fluorescent micellar carriers with controlled release of a novel anticancer drug were developed to enable intracellular imaging and cancer treatment simultaneously. The nanosized fluorescent micellar systems were embedded with a novel anticancer drug via the self-assembling behavior of well-defined block copolymers based on amphiphilic poly(acrylic acid)-block-poly(n-butyl acrylate) (PAA-b-PnBA) copolymer obtained by Atom Transfer Radical Polymerization (ATRP) and hydrophobic anticancer benzimidazole-hydrazone drug (BzH). Through this method, well-defined nanosized fluorescent micelles were obtained consisting of a hydrophilic PAA shell and a hydrophobic PnBA core embedded with the BzH drug due to the hydrophobic interactions, thus reaching very high encapsulation efficiency. The size, morphology, and fluorescent properties of blank and drug-loaded micelles were investigated using dynamic light scattering (DLS), transmission electron microscopy (TEM), and fluorescent spectroscopy, respectively. Additionally, after 72 h of incubation, drug-loaded micelles released 3.25 μM of BzH, which was spectrophotometrically determined. The BzH drug-loaded micelles were found to exhibit enhanced antiproliferative and cytotoxic effects on MDA-MB-231 cells, with long-lasting effects on microtubule organization, with apoptotic alterations and preferential localization in the perinuclear space of cancer cells. In contrast, the antitumor effect of BzH alone or incorporated in micelles on non-cancerous cells MCF-10A was relatively weak. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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15 pages, 3620 KiB

Open AccessArticle

Double-Loaded Doxorubicin/Resveratrol Polymeric Micelles Providing Low Toxicity on Cardiac Cells and Enhanced Cytotoxicity on Lymphoma Cells

by Lyubomira Radeva, Yordan Yordanov, Ivanka Spassova, Daniela Kovacheva, Virginia Tzankova and Krassimira Yoncheva

Pharmaceutics 2023, 15(4), 1287; https://doi.org/10.3390/pharmaceutics15041287 - 19 Apr 2023

Cited by 2 | Viewed by 1261

Abstract

The anthracycline antibiotic doxorubicin is a well-known antitumour agent, however its cardiotoxicity is a significant obstacle to therapy. The aim of the present study was to improve the safety of doxorubicin through its simultaneous encapsulation with a cardioprotective agent (resveratrol) in Pluronic micelles. [...] Read more.

The anthracycline antibiotic doxorubicin is a well-known antitumour agent, however its cardiotoxicity is a significant obstacle to therapy. The aim of the present study was to improve the safety of doxorubicin through its simultaneous encapsulation with a cardioprotective agent (resveratrol) in Pluronic micelles. The formation and double-loading of the micelles was performed via the film hydration method. Infrared spectroscopy proved the successful incorporation of both drugs. X-ray diffraction analyses revealed that resveratrol was loaded in the core, whereas doxorubicin was included in the shell. The double-loaded micelles were characterised by a small diameter (26 nm) and narrow size distribution, which is beneficial for enhanced permeability and retention effects. The in vitro dissolution tests showed that the release of doxorubicin depended on the pH of the medium and was faster than that of resveratrol. In vitro studies on cardioblasts showed the opportunity to reduce the cytotoxicity of doxorubicin through the presence of resveratrol in double-loaded micelles. Higher cardioprotection was observed when the cells were treated with the double-loaded micelles compared with referent solutions with equal concentrations of both drugs. In parallel, treatments of L5178 lymphoma cells with the double-loaded micelles revealed that the cytotoxic effect of doxorubicin was enhanced. Thus, the study demonstrated that the simultaneous delivery of doxorubicin and resveratrol via the micellar system enabled the cytotoxicity of doxorubicin in lymphoma cells and lowered its cardiotoxicity in cardiac cells. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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22 pages, 4481 KiB

Open AccessArticle

Influence of Molecular Structure and Physicochemical Properties of Immunosuppressive Drugs on Micelle Formulation Characteristics and Cutaneous Delivery

by Julie Quartier, Maria Lapteva, Younes Boulaguiem, Stéphane Guerrier and Yogeshvar N. Kalia

Pharmaceutics 2023, 15(4), 1278; https://doi.org/10.3390/pharmaceutics15041278 - 19 Apr 2023

Cited by 3 | Viewed by 1408

Abstract

The aim of this study was to investigate whether subtle differences in molecular properties affected polymeric micelle characteristics and their ability to deliver poorly water-soluble drugs into the skin. D-α-tocopherol-polyethylene glycol 1000 was used to prepare micelles containing ascomycin-derived immunosuppressants—sirolimus (SIR), pimecrolimus (PIM) [...] Read more.

The aim of this study was to investigate whether subtle differences in molecular properties affected polymeric micelle characteristics and their ability to deliver poorly water-soluble drugs into the skin. D-α-tocopherol-polyethylene glycol 1000 was used to prepare micelles containing ascomycin-derived immunosuppressants—sirolimus (SIR), pimecrolimus (PIM) and tacrolimus (TAC)—which have similar structures and physicochemical properties and have dermatological applications. Micelle formulations were prepared by thin-film hydration and extensively characterized. Cutaneous delivery and biodistribution were determined and compared. Sub-10 nm micelles were obtained for the three immunosuppressants with incorporation efficiencies >85%. However, differences were observed for drug loading, stability (at the highest concentration), and their in vitro release kinetics. These were attributed to differences in drug aqueous solubility and lipophilicity. Differences between the cutaneous biodistribution profiles and drug deposition in the different skin compartments pointed to the impact of differences in thermodynamic activity. Therefore, despite their structural similarities, SIR, TAC and PIM did not demonstrate the same behaviour either in the micelles or when applied to the skin. These outcomes indicate that polymeric micelles should be optimized even for closely related drug molecules and support the hypothesis that drugs are released from micelles prior to skin penetration. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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20 pages, 5112 KiB

Open AccessArticle

Synergistic Encapsulation of Paclitaxel and Sorafenib by Methoxy Poly(Ethylene Glycol)-b-Poly(Caprolactone) Polymeric Micelles for Ovarian Cancer Therapy

by Chae Eun Jin, Moon Sup Yoon, Min Jeong Jo, Seo Yeon Kim, Jae Min Lee, Su Jeong Kang, Chun-Woong Park, Jin-Seok Kim and Dae Hwan Shin

Pharmaceutics 2023, 15(4), 1206; https://doi.org/10.3390/pharmaceutics15041206 - 10 Apr 2023

Cited by 5 | Viewed by 1953

Abstract

Ovarian cancer has a high mortality rate due to difficult detection at an early stage. It is necessary to develop a novel anticancer treatment that demonstrates improved efficacy while reducing toxicity. Here, using the freeze-drying method, micelles encapsulating paclitaxel (PTX) and sorafenib (SRF) [...] Read more.

Ovarian cancer has a high mortality rate due to difficult detection at an early stage. It is necessary to develop a novel anticancer treatment that demonstrates improved efficacy while reducing toxicity. Here, using the freeze-drying method, micelles encapsulating paclitaxel (PTX) and sorafenib (SRF) with various polymers were prepared, and the optimal polymer (mPEG-b-PCL) was selected by measuring drug loading (%), encapsulation efficiency (%), particle size, polydispersity index, and zeta potential. The final formulation was selected based on a molar ratio (PTX:SRF = 1:2.3) with synergistic effects on two ovarian cancer cell lines (SKOV3-red-fluc, HeyA8). In the in vitro release assay, PTX/SRF micelles showed a slower release than PTX and SRF single micelles. In pharmacokinetic evaluation, PTX/SRF micelles showed improved bioavailability compared to PTX/SRF solution. In in vivo toxicity assays, no significant differences were observed in body weight between the micellar formulation and the control group. The anticancer effect of PTX/SRF combination therapy was improved compared to the use of a single drug. In the xenografted BALB/c mouse model, the tumor growth inhibition rate of PTX/SRF micelles was 90.44%. Accordingly, PTX/SRF micelles showed improved anticancer effects compared to single-drug therapy in ovarian cancer (SKOV3-red-fluc). Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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18 pages, 2836 KiB

Open AccessArticle

Ciprofloxacin-Loaded Mixed Polymeric Micelles as Antibiofilm Agents

by Rumena Stancheva, Tsvetelina Paunova-Krasteva, Tanya Topouzova-Hristova, Stoyanka Stoitsova, Petar Petrov and Emi Haladjova

Pharmaceutics 2023, 15(4), 1147; https://doi.org/10.3390/pharmaceutics15041147 - 04 Apr 2023

Cited by 2 | Viewed by 1332

Abstract

In this work, mixed polymeric micelles (MPMs) based on a cationic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA₂₉-b-PCL₇₀-b-PDMAEMA₂₉) and a non-ionic poly(ethylene oxide)–b-poly(propylene oxide)–b-poly(ethylene oxide) (PEO₉₉-b-PPO₆₇-b-PEO₉₉) triblock copolymers, blended at different molar ratios, were [...] Read more.

In this work, mixed polymeric micelles (MPMs) based on a cationic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA₂₉-b-PCL₇₀-b-PDMAEMA₂₉) and a non-ionic poly(ethylene oxide)–b-poly(propylene oxide)–b-poly(ethylene oxide) (PEO₉₉-b-PPO₆₇-b-PEO₉₉) triblock copolymers, blended at different molar ratios, were developed. The key physicochemical parameters of MPMs, including size, size distribution, and critical micellar concentration (CMC), were evaluated. The resulting MPMs are nanoscopic with a hydrodynamic diameter of around 35 nm, and the ζ-potential and CMC values strongly depend on the MPM’s composition. Ciprofloxacin (CF) was solubilized by the micelles via hydrophobic interaction with the micellar core and electrostatic interaction between the polycationic blocks, and the drug localized it, to some extent, in the micellar corona. The effect of a polymer-to-drug mass ratio on the drug-loading content (DLC) and encapsulation efficiency (EE) of MPMs was assessed. MPMs prepared at a polymer-to-drug mass ratio of 10:1 exhibited very high EE and a prolonged release profile. All micellar systems demonstrated their capability to detach pre-formed Gram-positive and Gram-negative bacterial biofilms and significantly reduced their biomass. The metabolic activity of the biofilm was strongly suppressed by the CF-loaded MPMs indicating the successful drug delivery and release. The cytotoxicity of empty and CF-loaded MPMs was evaluated. The test reveals composition-dependent cell viability without cell destruction or morphological signs of cell death. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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16 pages, 3721 KiB

Open AccessArticle

Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential

by Maria Schröder, Maria Petrova, Georgi M. Dobrikov, Georgy Grancharov, Denitsa Momekova, Petar D. Petrov and Iva Ugrinova

Pharmaceutics 2023, 15(3), 791; https://doi.org/10.3390/pharmaceutics15030791 - 27 Feb 2023

Cited by 1 | Viewed by 1497

Abstract

The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine [...] Read more.

The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-b-poly(α-cinnamyl-ε-caprolactone-co-ε-caprolactone)-b-poly(ethylene oxide) triblock copolymer (PEO₁₁₃-b-P(CyCL₃-co-CL₄₆)-b-PEO₁₁₃), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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19 pages, 5209 KiB

Open AccessArticle

Lipopolyplex-Mediated Co-Delivery of Doxorubicin and FAK siRNA to Enhance Therapeutic Efficiency of Treating Colorectal Cancer

by Tilahun Ayane Debele, Chi-Kang Chen, Lu-Yi Yu and Chun-Liang Lo

Pharmaceutics 2023, 15(2), 596; https://doi.org/10.3390/pharmaceutics15020596 - 10 Feb 2023

Cited by 4 | Viewed by 1784

Abstract

Tumor metastasis is a major concern in cancer therapy. In this context, focal adhesion kinase (FAK) gene overexpression, which mediates cancer cell migration and invasion, has been reported in several human tumors and is considered a potential therapeutic target. However, gene-based treatment has [...] Read more.

Tumor metastasis is a major concern in cancer therapy. In this context, focal adhesion kinase (FAK) gene overexpression, which mediates cancer cell migration and invasion, has been reported in several human tumors and is considered a potential therapeutic target. However, gene-based treatment has certain limitations, including a lack of stability and low transfection ability. In this study, a biocompatible lipopolyplex was synthesized to overcome the aforementioned limitations. First, polyplexes were prepared using poly(2-Hydroxypropyl methacrylamide-co-methylacrylate-hydrazone-pyridoxal) (P(HPMA-co-MA-hyd-VB6)) copolymers, which bore positive charges at low pH value owing to protonation of pyridoxal groups and facilitated electrostatic interactions with negatively charged FAK siRNA. These polyplexes were then encapsulated into methoxy polyethylene glycol (mPEG)-modified liposomes to form lipopolyplexes. Doxorubicin (DOX) was also loaded into lipopolyplexes for combination therapy with siRNA. Experimental results revealed that lipopolyplexes successfully released DOX at low pH to kill cancer cells and induced siRNA out of endosomes to inhibit the translation of FAK proteins. Furthermore, the efficient accumulation of lipopolyplexes in the tumors led to excellent cancer therapeutic efficacy. Overall, the synthesized lipopolyplex is a suitable nanocarrier for the co-delivery of chemotherapeutic agents and genes to treat cancers. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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13 pages, 3992 KiB

Open AccessArticle

Stimuli-Responsive Triblock Terpolymer Conversion into Multi-Stimuli-Responsive Micelles with Dynamic Covalent Bonds for Drug Delivery through a Quick and Controllable Post-Polymerization Reaction

by Eva Hlavatovičová, Roberto Fernandez-Alvarez, Katarzyna Byś, Sami Kereïche, Tarun K. Mandal, Leonard Ionut Atanase, Miroslav Štěpánek and Mariusz Uchman

Pharmaceutics 2023, 15(1), 288; https://doi.org/10.3390/pharmaceutics15010288 - 14 Jan 2023

Cited by 5 | Viewed by 1869

Abstract

Stimuli-responsive copolymers are of great interest for targeted drug delivery. This study reports on a controllable post-polymerization quaternization with 2-bromomethyl-4-fluorophenylboronic acid of the poly(4-vinyl pyridine) (P4VP) block of a common poly(styrene)-b-poly(4-vinyl pyridine)-b-poly(ethylene oxide) (SVE) triblock terpolymer in order to [...] Read more.

Stimuli-responsive copolymers are of great interest for targeted drug delivery. This study reports on a controllable post-polymerization quaternization with 2-bromomethyl-4-fluorophenylboronic acid of the poly(4-vinyl pyridine) (P4VP) block of a common poly(styrene)-b-poly(4-vinyl pyridine)-b-poly(ethylene oxide) (SVE) triblock terpolymer in order to achieve a selective responsivity to various diols. For this purpose, a reproducible method was established for P4VP block quaternization at a defined ratio, confirming the reaction yield by ¹¹B, ¹H NMR. Then, a reproducible self-assembly protocol is designed for preparing stable micelles from functionalized stimuli-responsive triblock terpolymers, which are characterized by light scattering and by cryogenic transmission electron microscopy. In addition, UV-Vis spectroscopy is used to monitor the boron-ester bonding and hydrolysis with alizarin as a model drug and to study encapsulation and release of this drug, induced by sensing with three geminal diols: fructose, galactose and ascorbic acid. The obtained results show that only the latter, with the vicinal diol group on sp²-hybridized carbons, was efficient for alizarin release. Therefore, the post-polymerization method for triblock terpolymer functionalization presented in this study allows for preparation of specific stimuli-responsive systems with a high potential for targeted drug delivery, especially for cancer treatment. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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Review

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15 pages, 1330 KiB

Open AccessReview

Copolymer Micelles: A Focus on Recent Advances for Stimulus-Responsive Delivery of Proteins and Peptides

by Thomas Trimaille and Bernard Verrier

Pharmaceutics 2023, 15(10), 2481; https://doi.org/10.3390/pharmaceutics15102481 - 17 Oct 2023

Cited by 2 | Viewed by 1061

Abstract

Historically used for the delivery of hydrophobic drugs through core encapsulation, amphiphilic copolymer micelles have also more recently appeared as potent nano-systems to deliver protein and peptide therapeutics. In addition to ease and reproducibility of preparation, micelles are chemically versatile as hydrophobic/hydrophilic segments [...] Read more.

Historically used for the delivery of hydrophobic drugs through core encapsulation, amphiphilic copolymer micelles have also more recently appeared as potent nano-systems to deliver protein and peptide therapeutics. In addition to ease and reproducibility of preparation, micelles are chemically versatile as hydrophobic/hydrophilic segments can be tuned to afford protein immobilization through different approaches, including non-covalent interactions (e.g., electrostatic, hydrophobic) and covalent conjugation, while generally maintaining protein biological activity. Similar to many other drugs, protein/peptide delivery is increasingly focused on stimuli-responsive nano-systems able to afford triggered and controlled release in time and space, thereby improving therapeutic efficacy and limiting side effects. This short review discusses advances in the design of such micelles over the past decade, with an emphasis on stimuli-responsive properties for optimized protein/peptide delivery. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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31 pages, 3665 KiB

Open AccessReview

Polymeric-Micelle-Based Delivery Systems for Nucleic Acids

by Genada Sinani, Meltem Ezgi Durgun, Erdal Cevher and Yıldız Özsoy

Pharmaceutics 2023, 15(8), 2021; https://doi.org/10.3390/pharmaceutics15082021 - 26 Jul 2023

Viewed by 1684

Abstract

Nucleic acids can modulate gene expression specifically. They are increasingly being utilized and show huge potential for the prevention or treatment of various diseases. However, the clinical translation of nucleic acids faces many challenges due to their rapid clearance after administration, low stability [...] Read more.

Nucleic acids can modulate gene expression specifically. They are increasingly being utilized and show huge potential for the prevention or treatment of various diseases. However, the clinical translation of nucleic acids faces many challenges due to their rapid clearance after administration, low stability in physiological fluids and limited cellular uptake, which is associated with an inability to reach the intracellular target site and poor efficacy. For many years, tremendous efforts have been made to design appropriate delivery systems that enable the safe and effective delivery of nucleic acids at the target site to achieve high therapeutic outcomes. Among the different delivery platforms investigated, polymeric micelles have emerged as suitable delivery vehicles due to the versatility of their structures and the possibility to tailor their composition for overcoming extracellular and intracellular barriers, thus enhancing therapeutic efficacy. Many strategies, such as the addition of stimuli-sensitive groups or specific ligands, can be used to facilitate the delivery of various nucleic acids and improve targeting and accumulation at the site of action while protecting nucleic acids from degradation and promoting their cellular uptake. Furthermore, polymeric micelles can be used to deliver both chemotherapeutic drugs and nucleic acid therapeutics simultaneously to achieve synergistic combination treatment. This review focuses on the design approaches and current developments in polymeric micelles for the delivery of nucleic acids. The different preparation methods and characteristic features of polymeric micelles are covered. The current state of the art of polymeric micelles as carriers for nucleic acids is discussed while highlighting the delivery challenges of nucleic acids and how to overcome them and how to improve the safety and efficacy of nucleic acids after local or systemic administration. Full article

(This article belongs to the Special Issue Application of Polymeric Micelles for Drug and Gene Delivery)

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