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Polymeric Nanocapsules in Drug Delivery

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

Deadline for manuscript submissions: closed (30 November 2021) | Viewed by 33928

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Prof. Dr. Vanessa Carla Furtado Mosqueira

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School of Pharmacy, Federal University of Ouro Preto, Department of Pharmacy - Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Campus Universitário Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Interests: polymeric nanoparticles; biodistribution; oral lipid-based nanosystems; efficacy; pharmaceutical nanotechnology; functionalized polymer synthesis
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Prof. Dr. Raquel Silva Araújo

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College of Pharmacy, Department of Biological and Health Sciences, Federal University of Amapá, Rod. Juscelino Kubitschek, km 02 - Jardim Marco Zero, Macapá 68903-419, AP, Brazil
Interests: nanobiotechnology; pharmaceutical technology; nanocarriers; polymeric nanoparticles; natural products; radiopharmaceuticals
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The development of nanostructured drug carriers has been the subject of intense research in the pharmaceutical field to optimize efficacy and reduce drug toxicity.

Polymeric nanocapsules (NCs) are widely used as drug nanocarriers for the delivery of diverse lipophilic molecules and some hydrophilic macromolecules. Nanocapsules are vesicular systems, containing in general a lipid-based core (liquid, semi-solid, or solid) surrounded by a polymeric wall. Their ability to modify the drug release and pharmacokinetic properties of active substances is associated with their size and chemical nature of the polymer. Many research projects have enabled the modification of nanocapsule surfaces, improving long-circulating properties, increasing immune stimulation, and particularly, decorating the surface with ligands such as small molecules, antibodies, peptides, and aptamers, with the aim to increase site-specific drug delivery.

Furthermore, nanocapsules have been demonstrating outstanding physicochemical characteristics, including biocompatibility, stability, and versatility as delivery systems to load a plethora of substances and macromolecules. NCs allow fine-tuning of surface hydrophilicity, easy production, and scalability. All of these attributes contribute to making nanocapsules one of the most important and efficient drug delivery systems under consideration in the pharmaceutical area.

The scope of this Special Issue aims to cover the major features of polymeric nanocapsules systems in drug delivery including:

Processes of preparation
Characterization methods
Raw materials and physicochemistry
Surface modification
Drug release and delivery properties
Biodistribution
Efficacy studies
Their applicability for the diagnosis and therapeutics as nanomedicines for human and in the veterinary area
Technologies of nanocapsules drying
Scale-up technologies

Prof. Dr. Vanessa Carla Furtado Mosqueira
Prof. Dr. Raquel Silva Araújo
Guest Editors

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Published Papers (9 papers)

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Research

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19 pages, 18771 KiB

Open AccessArticle

Toltrazuril-Loaded Polymeric Nanocapsules as a Promising Approach for the Preventive Control of Coccidiosis in Poultry

by Lana Flávia Baron, Francisco Noé da Fonseca, Shaiana Salete Maciag, Franciana Aparecida Volpato Bellaver, Adriana Mércia Guaratini Ibeli, Marcos Antônio Zanella Mores, Gabryelle Furtado de Almeida, Silvia Stanisçuaski Guterres, Ana Paula Almeida Bastos and Karina Paese

Pharmaceutics 2022, 14(2), 392; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020392 - 10 Feb 2022

Cited by 4 | Viewed by 2029

Abstract

Coccidiosis is a disease caused by intracellular protozoan parasites of the genus Eimeria that affect the intestinal tract of poultry. However, strain resistance and drug residue in the carcass have drawn the attention of the productive sector. The nanotechnology can improve the biological effect of drugs, reducing of administered doses and toxic effects. Due to this, toltrazuril-load polymeric nanoparticles based on Eudragit^® S100 (NCt) or poly-ε-caprolactone (LNCt) were developed to prevent coccidiosis in broilers. Nanoformulations were produced and showed homogeneous particle diameter distribution in the nanometer range (z-average and D (4.3) < 200 nm), negative zeta potential (<−8.93 mV), drug content ~100%, and encapsulation efficiency >90%. Cell viability assays using avian fibroblasts showed that LNCt presented no relevant toxicity up to 72 h. LNCt was then prophylactically administrated to chicken followed by challenge with Eimeria oocysts. The evaluation of the small intestine and cecum showed that the treatment with LNCt (3.5 mg/kg/day) in drinking water reduced the lesion scores and oocysts excretion, similar to the reference medicine containing toltrazuril (Baycox^®, 7 mg/kg/day). The current study shows the potential protective use of nanoencapsulating anticoccidial drugs as a promising approach for the control of coccidiosis in poultry. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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13 pages, 1931 KiB

Open AccessArticle

Polylactide Nanocapsules Attenuate Adverse Cardiac Cellular Effects of Lyso-7, a Pan-PPAR Agonist/Anti-Inflammatory New Thiazolidinedione

by Giani M. Garcia, Jérôme Roy, Ivan R. Pitta, Dulcinéia S. P. Abdalla, Andrea Grabe-Guimarães, Vanessa C. F. Mosqueira and Sylvain Richard

Pharmaceutics 2021, 13(9), 1521; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13091521 - 20 Sep 2021

Cited by 3 | Viewed by 2176

Abstract

Lyso-7 is a novel synthetic thiazolidinedione, which is a receptor (pan) agonist of PPAR α,β/δ,γ with anti-inflammatory activity. We investigated the cardiotoxicity of free Lyso-7 in vitro (4.5–450 nM), and Lyso-7 loaded in polylactic acid nanocapsules (NC) in vivo (Lyso-7-NC, 1.6 mg/kg). In previous work, we characterized Lyso-7-NC. We administered intravenously Lyso-7, Lyso-7-NC, control, and blank-NC once a day for seven days in mice. We assessed cell contraction and intracellular Ca²⁺ transients on single mice cardiomyocytes enzymatically isolated. Lyso-7 reduced cell contraction and accelerated relaxation while lowering diastolic Ca²⁺ and reducing Ca²⁺ transient amplitude. Lyso-7 also promoted abnormal ectopic diastolic Ca²⁺ events, which isoproterenol dramatically enhanced. Incorporation of Lyso-7 in NC attenuated drug effects on cell contraction and prevented its impact on relaxation, diastolic Ca²⁺, Ca²⁺ transient amplitude, Ca²⁺ transient decay kinetics, and promotion of diastolic Ca²⁺ events. Acute effects of Lyso-7 on cardiomyocytes in vitro at high concentrations (450 nM) were globally similar to those observed after repeated administration in vivo. In conclusion, we show evidence for off-target effects of Lyso-7, seen during acute exposure of cardiomyocytes to high concentrations and after repeated treatment in mice. Nano-encapsulation of Lyso-7 in polymeric NC attenuated the unwanted effects, particularly ectopic Ca²⁺ events known to support life-threatening arrhythmias favored by stress or exercise. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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24 pages, 7749 KiB

Open AccessArticle

Microencapsulated Chitosan-Based Nanocapsules: A New Platform for Pulmonary Gene Delivery

by Estefanía Fernández-Paz, Lucía Feijoo-Siota, Maria Manuela Gaspar, Noemi Csaba and Carmen Remuñán-López

Pharmaceutics 2021, 13(9), 1377; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13091377 - 31 Aug 2021

Cited by 7 | Viewed by 2225

Abstract

In this work, we propose chitosan (CS)-based nanocapsules (NCs) for pulmonary gene delivery. Hyaluronic acid (HA) was incorporated in the NCs composition (HA/CS NCs) aiming to promote gene transfection in the lung epithelium. NCs were loaded with a model plasmid (pCMV-βGal) to easily evaluate their transfection capacity. The plasmid encapsulation efficiencies were of approx. 90%. To facilitate their administration to the lungs, the plasmid-loaded NCs were microencapsulated in mannitol (Ma) microspheres (MS) using a simple spray-drying technique, obtaining dry powders of adequate properties. In vivo, the MS reached the deep lung, where the plasmid-loaded CS-based NCs were released and transfected the alveolar cells more homogeneously than the control formulation of plasmid directly microencapsulated in Ma MS. The HA-containing formulation achieved the highest transfection efficiency, in a more extended area and more homogeneously distributed than the rest of tested formulations. The new micro-nanostructured platform proposed in this work represents an efficient strategy for the delivery of genetic material to the lung, with great potential for the treatment of genetic lung diseases. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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11 pages, 2938 KiB

Open AccessArticle

A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery

by Jin Sil Lee, Hyeryeon Oh, Sunghyun Kim, Jeung-Hoon Lee, Yong Chul Shin and Won Il Choi

Pharmaceutics 2021, 13(9), 1329; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13091329 - 25 Aug 2021

Cited by 7 | Viewed by 2266

Abstract

Transepidermal drug delivery achieves high drug concentrations at the action site and ensures continuous drug delivery and better patient compliance with fewer adverse effects. However, drug delivery through topical application is still limited in terms of drug penetration. Chitosan is a promising enhancer to overcome this constraint, as it can enhance drug diffusion by opening the tight junctions of the stratum corneum. Therefore, here, we developed a novel chitosan nanosponge (CNS) with an optimal ratio and molecular weight of chitosan to improve drug penetration through skin. To prepare the CNS, two types of chitosan (3 and 10 kDa) were each conjugated with poloxamer 407 using para-nitrophenyl chloroformate, and the products were mixed with poloxamer 407 at ratios of 5:5, 8:2, and 10:0. The resulting mixtures were molded to produce flexible soft nanosponges by simple nanoprecipitation. The CNSs were highly stable in biological buffer for four weeks and showed no toxicity in human dermal fibroblasts. The CNSs increased drug permeability through human cadaver skin in a Franz-type diffusion cell, with substantially higher permeability with 3 kDa chitosan at a ratio of 8:2. This suggests the applicability of the novel CNS as a promising carrier for efficient transepidermal drug delivery. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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25 pages, 7547 KiB

Open AccessArticle

Repositioning of Tamoxifen in Surface-Modified Nanocapsules as a Promising Oral Treatment for Visceral Leishmaniasis

by Débora Faria Silva, Levi Eduardo Soares Reis, Marina Guimarães Carvalho Machado, Douglas Daniel Dophine, Vinicius Roberto de Andrade, Wanderson Geraldo de Lima, Margareth Spangler Andrade, José Mário Carneiro Vilela, Alexandre Barbosa Reis, Gwenaelle Pound-Lana, Simone Aparecida Rezende and Vanessa Carla Furtado Mosqueira

Pharmaceutics 2021, 13(7), 1061; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13071061 - 10 Jul 2021

Cited by 3 | Viewed by 2627

Abstract

Standards of care for human visceral leishmaniasis (VL) are based on drugs used parenterally, and oral treatment options are urgently needed. In the present study, a repurposing strategy was used associating tamoxifen (TMX) with polyethylene glycol-block-polylactide nanocapsules (NC) and its anti-leishmanial efficacy was reported in vivo. Stable surface modified-NC (5 mg/mL of TMX) exhibited 200 nm in size, +42 mV of zeta potential, and 98% encapsulation efficiency. Atomic force microscopy evidenced core-shell-NC. Treatment with TMX-NC reduced parasite-DNA quantified in liver and spleen compared to free-TMX; and provided a similar reduction of parasite burden compared with meglumine antimoniate in mice and hamster models. Image-guided biodistribution showed accumulation of NC in liver and spleen after 30 min post-administration. TMX-NC reduced the number of liver granulomas and restored the aspect of capsules and trabeculae in the spleen of infected animals. TMX-NC was tested for the first time against VL models, indicating a promising formulation for oral treatment. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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20 pages, 5024 KiB

Open AccessArticle

Nanoformulation Shows Cytotoxicity against Glioblastoma Cell Lines and Antiangiogenic Activity in Chicken Chorioallantoic Membrane

by Danieli Rosane Dallemole, Thatiana Terroso, Aline de Cristo Soares Alves, Juliete Nathali Scholl, Giovana Ravizzoni Onzi, Rodrigo Cé, Karina Paese, Ana Maria Oliveira Battastini, Silvia Stanisçuaski Guterres, Fabrício Figueiró and Adriana Raffin Pohlmann

Pharmaceutics 2021, 13(6), 862; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13060862 - 11 Jun 2021

Cited by 2 | Viewed by 3203

Abstract

Glioblastoma (GB) is a histological and genetically heterogeneous brain tumor that is highly proliferative and vascularized. The prognosis is poor with currently available treatment. In this study, we evaluated the cytotoxicity and antiangiogenic activity of doxorubicin-loaded-chitosan-coated-arginylglycylaspartic acid-functionalized-poly(ε-caprolactone)-alpha bisabolol-LNC (AB-DOX-LNC-L-C-RGD). The nanoformulation was prepared by self-assembling followed by interfacial reactions, physicochemically characterized and evaluated in vitro against GB cell lines (U87MG and U138MG) and in vivo using the chicken chorioallantoic membrane assay (CAM). Spherical shape nanocapsules had a hydrodynamic mean diameter of 138 nm, zeta potential of +13.4 mV, doxorubicin encapsulation of 65%, and RGD conjugation of 92%. After 24 h of treatment (U87MG and U138MG), the median inhibition concentrations (IC₅₀) were 520 and 490 nmol L⁻¹ doxorubicin-equivalent concentrations, respectively. The treatment induced antiproliferative activity with S-phase cell-cycle arrest and apoptosis in the GB cells. Furthermore, after 48 h of exposure, evaluation of antiangiogenic activity (CAM) showed that the relative vessel growth following treatment with the nanocapsules was 5.4 times lower than that with the control treatment. The results support the therapeutic potential of the nanoformulation against GB and, thereby, pave the way for future preclinical studies. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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22 pages, 4423 KiB

Open AccessArticle

Nanoparticle-Mediated Angiotensin-(1-9) Drug Delivery for the Treatment of Cardiac Hypertrophy

by Sabrina Sepúlveda-Rivas, Matías S. Leal, Zully Pedrozo, Marcelo J. Kogan, María Paz Ocaranza and Javier O. Morales

Pharmaceutics 2021, 13(6), 822; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13060822 - 01 Jun 2021

Cited by 4 | Viewed by 2389

Abstract

Ang-(1-9) peptide is a bioactive vasodilator peptide that prevents cardiomyocyte hypertrophy in vitro and in vivo as well as lowers blood pressure and pathological cardiovascular remodeling; however, it has a reduced half-life in circulation, requiring a suitable carrier for its delivery. In this work, hybrid nanoparticles composed of polymeric nanoparticles (pNPs) based on Eudragit^® E/Alginate (EE/Alg), and gold nanospheres (AuNS), were developed to evaluate their encapsulation capacity and release of Ang-(1-9) under different experimental conditions. Hybrid pNPs were characterized by dynamic light scattering, zeta potential, transmission and scanning electron microscopy, size distribution, and concentration by nanoparticle tracking analysis. Nanometric pNPs, with good polydispersity index and colloidally stable, produced high association efficiency of Ang-(1-9) and controlled release. Finally, the treatment of neonatal cardiomyocytes in culture with EE/Alg/AuNS 2% + Ang-(1-9) 20% pNPs decreased the area and perimeter, demonstrating efficacy in preventing norepinephrine-induced cardiomyocyte hypertrophy. On the other hand, the incorporation of AuNS did not cause negative effects either on the cytotoxicity or on the association capacity of Ang-(1-9), suggesting that the hybrid carrier EE/Alg/AuNS pNPs could be used for the delivery of Ang-(1-9) in the treatment of cardiovascular hypertrophy. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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Review

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27 pages, 32922 KiB

Open AccessReview

Polymeric Lipid Hybrid Nanoparticles (PLNs) as Emerging Drug Delivery Platform—A Comprehensive Review of Their Properties, Preparation Methods, and Therapeutic Applications

by Durgaramani Sivadasan, Muhammad Hadi Sultan, Osama Madkhali, Yosif Almoshari and Neelaveni Thangavel

Pharmaceutics 2021, 13(8), 1291; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13081291 - 18 Aug 2021

Cited by 40 | Viewed by 7175

Abstract

Polymeric lipid hybrid nanoparticles (PLNs) are core–shell nanoparticles made up of a polymeric kernel and lipid/lipid–PEG shells that have the physical stability and biocompatibility of both polymeric nanoparticles and liposomes. PLNs have emerged as a highly potent and promising nanocarrier for a variety of biomedical uses, including drug delivery and biomedical imaging, owing to recent developments in nanomedicine. In contrast with other forms of drug delivery systems, PLNs have been regarded as seamless and stable because they are simple to prepare and exhibit excellent stability. Natural, semi-synthetic, and synthetic polymers have been used to make these nanocarriers. Due to their small scale, PLNs can be used in a number of applications, including anticancer therapy, gene delivery, vaccine delivery, and bioimaging. These nanoparticles are also self-assembled in a reproducible and predictable manner using a single or two-step nanoprecipitation process, making them significantly scalable. All of these positive attributes therefore make PLNs an attractive nanocarrier to study. This review delves into the fundamentals and applications of PLNs as well as their formulation parameters, several drug delivery strategies, and recent advancements in clinical trials, giving a comprehensive insight into the pharmacokinetic and biopharmaceutical aspects of these hybrid nanoparticles. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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26 pages, 5757 KiB

Open AccessReview

Lyophilization of Nanocapsules: Instability Sources, Formulation and Process Parameters

by Ghania Degobert and Dunya Aydin

Pharmaceutics 2021, 13(8), 1112; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13081112 - 21 Jul 2021

Cited by 29 | Viewed by 8201

Abstract

Polymeric nanocapsules have gained more and more interest in the medical sciences. Their core-shell structure offers numerous advantages, especially regarding their use as drug delivery systems. This review begins by presenting the different intrinsic sources of the instability of nanocapsules. The physical and chemical potential instabilities of nanocapsules reduce their shelf-life and constitute a barrier to their clinical use and to their commercialization. To overcome these issues, lyophilization is often used as a process of choice in the pharmaceutical industry especially when labile compounds are used. The state of the art of lyophilization nanocapsules is reviewed. The formulation properties and the process parameters are discussed for a complete understanding of their impact on the stability and storage of the final dried product. To assess the quality of the dried product, various characterization methods are also discussed. Full article

(This article belongs to the Special Issue Polymeric Nanocapsules in Drug Delivery)

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