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Pharmaceutics
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Controlled Release of Nanostructured Drug Systems
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Controlled Release of Nanostructured Drug Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (10 November 2021) | Viewed by 72033

Special Issue Editors

Prof. Dr. Maria Luisa García

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Guest Editor
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain
Interests: drug delivery systems; nanoparticles; nanomedicines; nanobiomedicine; ocular drug delivery
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Elena Sánchez-López

E-Mail Website
Guest Editor
1. Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain
2. Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, Barcelona, Spain
Interests: drug delivery systems; nanoparticles; biodegradable nanoparticles; neurodegenerative diseases; ocular drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Controlled-release formulations are aimed to modulate a drug pharmacokinetic profile by maintaining steady concentrations of the drug in the blood or target tissues. These nanostructured systems are able to improve drugs’ therapeutic efficacy and reduce their toxicity and adverse effects. In addition, nanocarriers have shown to possess unique physical and chemical features and have been recently used in medicine for drug delivery and targeting.

This Special Issue “Controlled drug release of nanostructured drug systems” of Pharmaceutics addresses this multidisciplinary field and aims to discuss innovative advances in the design and applications of nanostructured systems for diagnosis, therapeutics, and cosmetics, among other relevant fields. Colleagues are invited to participate by proposing original and review papers that deal with new strategies and approaches for nanostructured systems applied in pharmaceutical and biomedical sciences, with a special focus on functionalized nanostructured systems.

Prof. Dr. Maria Luisa García
Prof. Dr. Elena Sánchez-López
Guest Editors

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Keywords

  • controlled drug release
  • nanocarriers
  • drug delivery
  • nanomedicine
  • nanobiotechnology
  • nanoparticles
  • targeting strategies

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Published Papers (17 papers)

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Research

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17 pages, 3372 KiB  
Article
Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation
by Ruth Galindo, Elena Sánchez-López, María José Gómara, Marta Espina, Miren Ettcheto, Amanda Cano, Isabel Haro, Antoni Camins and María Luisa García
Pharmaceutics 2022, 14(2), 285; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020285 - 26 Jan 2022
Cited by 14 | Viewed by 3784
Abstract
Licochalcone-A is a natural compound with anti-inflammatory properties. However, it possesses low water solubility, making its application for the treatment of ocular inflammation difficult. To overcome this drawback, biodegradable nanoparticles incorporating Licochalcone-A have been developed. Additionally, to avoid fast clearance and increase cellular [...] Read more.
Licochalcone-A is a natural compound with anti-inflammatory properties. However, it possesses low water solubility, making its application for the treatment of ocular inflammation difficult. To overcome this drawback, biodegradable nanoparticles incorporating Licochalcone-A have been developed. Additionally, to avoid fast clearance and increase cellular internalization into the ocular tissues, PLGA nanoparticles have been functionalized using PEG and cell penetrating peptides (Tet-1 and B6). To optimize the formulations, a factorial design was carried out and short-term stability of the nanoparticles was studied. Moreover, morphology was also observed by transmission electron microcopy and in vitro drug release was carried out. Ocular tolerance of the formulations was ensured in vitro and in vivo and anti-inflammatory therapeutic efficacy was also assessed. Surface functionalized nanoparticles loading Licochalcone-A were developed with an average size below 200 nm, a positive surface charge, and a monodisperse population. The formulations were non-irritant and showed a prolonged Licochalcone-A release. Despite the fact that both Licochalcone-A Tet-1 and B6 functionalized nanoparticles demonstrated to be suitable for the treatment of ocular inflammation, B6 targeted nanoparticles provided greater therapeutic efficacy in in vivo assays. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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19 pages, 2294 KiB  
Article
Optimization of Hemoglobin Encapsulation within PLGA Nanoparticles and Their Investigation as Potential Oxygen Carriers
by Clara Coll-Satue, Michelle Maria Theresia Jansman, Peter Waaben Thulstrup and Leticia Hosta-Rigau
Pharmaceutics 2021, 13(11), 1958; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13111958 - 18 Nov 2021
Cited by 10 | Viewed by 2587
Abstract
Hemoglobin (Hb)-based oxygen carriers (HBOCs) display the excellent oxygen-carrying properties of red blood cells, while overcoming some of the limitations of donor blood. Various encapsulation platforms have been explored to prepare HBOCs which aim to avoid or minimize the adverse effects caused by [...] Read more.
Hemoglobin (Hb)-based oxygen carriers (HBOCs) display the excellent oxygen-carrying properties of red blood cells, while overcoming some of the limitations of donor blood. Various encapsulation platforms have been explored to prepare HBOCs which aim to avoid or minimize the adverse effects caused by the administration of free Hb. Herein, we entrapped Hb within a poly(lactide-co-glycolide) (PLGA) core, prepared by the double emulsion solvent evaporation method. We study the effect of the concentrations of Hb, PLGA, and emulsifier on the size, polydispersity (PDI), loading capacity (LC), and entrapment efficiency (EE) of the resulting Hb-loaded PLGA nanoparticles (HbNPs). Next, the ability of the HbNPs to reversibly bind and release oxygen was thoroughly evaluated. When needed, trehalose, a well-known protein stabilizer that has never been explored for the fabrication of HBOCs, was incorporated to preserve Hb’s functionality. The optimized formulation had a size of 344 nm, a PDI of 0.172, a LC of 26.9%, and an EE of 40.7%. The HbNPs were imaged by microscopy and were further characterized by FTIR and CD spectroscopy to assess their chemical composition and structure. Finally, the ability of the encapsulated Hb to bind and release oxygen over several rounds was demonstrated, showing the preservation of its functionality. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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19 pages, 11410 KiB  
Article
Development of Lactoferrin-Loaded Liposomes for the Management of Dry Eye Disease and Ocular Inflammation
by Ana López-Machado, Natalia Díaz-Garrido, Amanda Cano, Marta Espina, Josefa Badia, Laura Baldomà, Ana Cristina Calpena, Eliana B. Souto, María Luisa García and Elena Sánchez-López
Pharmaceutics 2021, 13(10), 1698; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13101698 - 15 Oct 2021
Cited by 26 | Viewed by 3697
Abstract
Dry eye disease (DED) is a high prevalent multifactorial disease characterized by a lack of homeostasis of the tear film which causes ocular surface inflammation, soreness, and visual disturbance. Conventional ophthalmic treatments present limitations such as low bioavailability and side effects. Lactoferrin (LF) [...] Read more.
Dry eye disease (DED) is a high prevalent multifactorial disease characterized by a lack of homeostasis of the tear film which causes ocular surface inflammation, soreness, and visual disturbance. Conventional ophthalmic treatments present limitations such as low bioavailability and side effects. Lactoferrin (LF) constitutes a promising therapeutic tool, but its poor aqueous stability and high nasolacrimal duct drainage hinder its potential efficacy. In this study, we incorporate lactoferrin into hyaluronic acid coated liposomes by the lipid film method, followed by high pressure homogenization. Pharmacokinetic and pharmacodynamic profiles were evaluated in vitro and ex vivo. Cytotoxicity and ocular tolerance were assayed both in vitro and in vivo using New Zealand rabbits, as well as dry eye and anti-inflammatory treatments. LF loaded liposomes showed an average size of 90 nm, monomodal population, positive surface charge and a high molecular weight protein encapsulation of 53%. Biopharmaceutical behaviour was enhanced by the nanocarrier, and any cytotoxic effect was studied in human corneal epithelial cells. Developed liposomes revealed the ability to reverse dry eye symptoms and possess anti-inflammatory efficacy, without inducing ocular irritation. Hence, lactoferrin loaded liposomes could offer an innovative nanotechnological tool as suitable approach in the treatment of DED. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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23 pages, 8062 KiB  
Article
Surface-Modified Multifunctional Thymol-Loaded Biodegradable Nanoparticles for Topical Acne Treatment
by Camila Folle, Natalia Díaz-Garrido, Elena Sánchez-López, Ana Maria Marqués, Josefa Badia, Laura Baldomà, Marta Espina, Ana Cristina Calpena and María Luisa García
Pharmaceutics 2021, 13(9), 1501; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13091501 - 18 Sep 2021
Cited by 15 | Viewed by 3170
Abstract
The present work is focused on the development of novel surface-functionalized poly(lactic-co-glycolic acid) nanoparticles loaded with thymol (TH-NPs) for topical administration enhancing thymol anti-inflammatory, antioxidant and wound healing activities against acne. TH-NPs were prepared by solvent evaporation method using different surface functionalization strategies [...] Read more.
The present work is focused on the development of novel surface-functionalized poly(lactic-co-glycolic acid) nanoparticles loaded with thymol (TH-NPs) for topical administration enhancing thymol anti-inflammatory, antioxidant and wound healing activities against acne. TH-NPs were prepared by solvent evaporation method using different surface functionalization strategies and obtaining suitable physicochemical parameters and a good short-term stability at 4 °C. Moreover, TH-NPs skin penetration and antioxidant activity were assessed in ex vivo pig skin models. Skin penetration of TH-NPs followed the follicular route, independently of the surface charge and they were able to enhance antioxidant capacity. Furthermore, antimicrobial activity against Cutibacterium acnes was evaluated in vitro by the suspension test showing improved antibacterial performance. Using human keratinocyte cells (HaCat), cytotoxicity, cellular uptake, antioxidant, anti-inflammatory and wound healing activities were studied. TH-NPs were non-toxic and efficiently internalized inside the cells. In addition, TH-NPs displayed significant anti-inflammatory, antioxidant and wound healing activities, which were highly influenced by TH-NPs surface modifications. Moreover, a synergic activity between TH-NPs and their surface functionalization was demonstrated. To conclude, surface-modified TH-NPs had proven to be suitable to be used as anti-inflammatory, antioxidant and wound healing agents, constituting a promising therapy for treating acne infection and associated inflammation. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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14 pages, 2837 KiB  
Article
Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin
by Peipei Huo, Xinxu Han, Wenyu Zhang, Jing Zhang, Parveen Kumar and Bo Liu
Pharmaceutics 2021, 13(8), 1228; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13081228 - 09 Aug 2021
Cited by 37 | Viewed by 3428
Abstract
The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these [...] Read more.
The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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23 pages, 6812 KiB  
Article
Thermo-Responsive PLGA-PEG-PLGA Hydrogels as Novel Injectable Platforms for Neuroprotective Combined Therapies in the Treatment of Retinal Degenerative Diseases
by José Javier López-Cano, Sigen A., Vanessa Andrés-Guerrero, Hongyun Tai, Irene Bravo-Osuna, Irene Teresa Molina-Martínez, Wenxin Wang and Rocío Herrero-Vanrell
Pharmaceutics 2021, 13(2), 234; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13020234 - 07 Feb 2021
Cited by 26 | Viewed by 4044
Abstract
The present study aims to develop a thermo-responsive-injectable hydrogel (HyG) based on PLGA-PEG-PLGA (PLGA = poly-(DL-lactic acid co-glycolic acid); PEG = polyethylene glycol) to deliver neuroprotective agents to the retina over time. Two PLGA-PEG PLGA copolymers with different PEG:LA:GA ratios (1:1.54:23.1 and 1:2.25:22.5) [...] Read more.
The present study aims to develop a thermo-responsive-injectable hydrogel (HyG) based on PLGA-PEG-PLGA (PLGA = poly-(DL-lactic acid co-glycolic acid); PEG = polyethylene glycol) to deliver neuroprotective agents to the retina over time. Two PLGA-PEG PLGA copolymers with different PEG:LA:GA ratios (1:1.54:23.1 and 1:2.25:22.5) for HyG-1 and HyG-2 development respectively were synthetized and characterized by different techniques (gel permeation chromatography (GPC), nuclear magnetic resonance (NMR), dynamic light scattering (DLS), critical micelle concentration (CMC), gelation and rheological behaviour). According to the physicochemical characterization, HyG-1 was selected for further studies and loaded with anti-inflammatory drugs: dexamethasone (0.2%), and ketorolac (0.5%), alone or in combination with the antioxidants idebenone (1 µM) and D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) (0.002%). In vitro drug release and cytotoxicity studies were performed for the active substances and hydrogels (loaded and drug-free). A cellular model based on oxidative stress was optimized for anti-inflammatory and antioxidant screening of the formulations by using retinal-pigmented epithelial cell line hTERT (RPE-1). The copolymer 1, used to prepare thermo-responsive HyG-1, showed low polydispersity (PDI = 1.22) and a strong gel behaviour at 25% (w/v) in an isotonic buffer solution close to the vitreous temperature (31–34 °C). Sustained release of dexamethasone and ketorolac was achieved between 47 and 62 days, depending on the composition. HyG-1 was well tolerated (84.5 ± 3.2%) in retinal cells, with values near 100% when the anti-inflammatory and antioxidant agents were included. The combination of idebenone and dexamethasone promoted high oxidative protection in the cells exposed to H2O2, with viability values of 86.2 ± 14.7%. Ketorolac and dexamethasone-based formulations ameliorated the production of TNF-α, showing significant results (p ≤ 0.0001). The hydrogels developed in the present study entail a novel biodegradable tool to treat neurodegenerative processes of the retina overtime. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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18 pages, 4169 KiB  
Article
Doxorubicin-Loaded PLGA Nanoparticles for Cancer Therapy: Molecular Weight Effect of PLGA in Doxorubicin Release for Controlling Immunogenic Cell Death
by Yongwhan Choi, Hong Yeol Yoon, Jeongrae Kim, Suah Yang, Jaewan Lee, Ji Woong Choi, Yujeong Moon, Jinseong Kim, Seungho Lim, Man Kyu Shim, Sangmin Jeon, Ick Chan Kwon and Kwangmeyung Kim
Pharmaceutics 2020, 12(12), 1165; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12121165 - 29 Nov 2020
Cited by 39 | Viewed by 4379
Abstract
Direct local delivery of immunogenic cell death (ICD) inducers to a tumor site is an attractive approach for leading ICD effectively, due to enabling the concentrated delivery of ICD inducers to the tumor site. Herein, we prepared doxorubicin (DOX)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles [...] Read more.
Direct local delivery of immunogenic cell death (ICD) inducers to a tumor site is an attractive approach for leading ICD effectively, due to enabling the concentrated delivery of ICD inducers to the tumor site. Herein, we prepared doxorubicin (DOX)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) using different molecular weight PLGA (7000 g/mol and 12,000 g/mol), showing different drug release kinetics. The different release kinetics of DOX might differently stimulate a tumor cell-specific immune response by releasing damage-associated molecular patterns (DAMPs), resulting in showing a different antitumor response in the living body. DOX-PLGA7K NPs showed faster DOX release kinetics than DOX-PLGA12K NPs in the physiological condition. DOX-PLGA7K NPs and DOX-PLGA12K NPs were successfully taken up by the CT-26 tumor cells, subsequently showing different DOX localization times at the nucleus. Released DOX successfully lead to cytotoxicity and HMGB1 release in vitro. Although the DOX-PLGA7K NPs and DOX-PLGA12K NPs showed different sustained DOX release kinetics in vitro, tumor growth of the CT-26 tumor was similarly inhibited for 28 days post-direct tumor injection. Furthermore, the immunological memory effect was successfully established by the ICD-based tumor-specific immune responses, including DC maturation and tumor infiltration of cytotoxic T lymphocytes (CTLs). We expect that the controlled release of ICD-inducible chemotherapeutic agents, using different types of nanomedicines, can provide potential in precision cancer immunotherapy by controlling the tumor-specific immune responses, thus improving the therapeutic efficacy. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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22 pages, 3350 KiB  
Article
Self-Nanoemulsifying System Loaded with Sildenafil Citrate and Incorporated within Oral Lyophilized Flash Tablets: Preparation, Optimization, and In Vivo Evaluation
by Khaled M. Hosny, Nabil A. Alhakamy, Maeen A. Almodhwahi, Mallesh Kurakula, Alshaimaa M. Almehmady and Samar S. Elgebaly
Pharmaceutics 2020, 12(11), 1124; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12111124 - 21 Nov 2020
Cited by 17 | Viewed by 3284
Abstract
Sildenafil citrate is a drug used throughout the world primarily to treat erectile dysfunction. Several problems with the commercially available product decrease its efficacy, such as limited solubility, delayed onset of action, and low bioavailability with a large variability in the absorption profile. [...] Read more.
Sildenafil citrate is a drug used throughout the world primarily to treat erectile dysfunction. Several problems with the commercially available product decrease its efficacy, such as limited solubility, delayed onset of action, and low bioavailability with a large variability in the absorption profile. This study aimed to develop an optimized self-nanoemulsifying lyophilized tablet for the drug to conquer the foresaid problems. Sildenafil solubility in various surfactants, oils, and cosurfactants was attempted. An optimized formulation of a loaded self-nanoemulsion with a small droplet size was developed by applying a special cubic model of the mixture design. Sixteen formulations were prepared and characterized for droplet size. On the basis of solubility studies, a clove oil/oleic acid mixture, polysorbate 20 (Tween 20), and propylene glycol were selected as the proposed oil, surfactant, and cosurfactant, respectively. On the basis of desirability, an optimized sildenafil citrate-loaded self-nanoemulsifying delivery system containing 10% of the oil mixture, 60% of the surfactant, and 30% of the cosurfactant had a droplet size of 65 nm. Subsequently, the tablet form was fabricated with optimum ratios of 0.4% fumed silica, 0.1% hydroxypropyl methylcellulose, and 0.4% sodium starch glycolate. This formula showed satisfactory results in both disintegration and dissolution studies. In vivo pharmacokinetic studies indicated a higher bioavailability (1.44 times) and rapid absorption profile for the study’s tablets compared with commercially available tablets. In conclusion, highly bioavailable oral lyophilized flash tablets of sildenafil were successfully prepared. They will be a good alternative to the conventional solid-dosage form. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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19 pages, 5778 KiB  
Article
The Design of Anionic Surfactant-Based Amino-Functionalized Mesoporous Silica Nanoparticles and their Application in Transdermal Drug Delivery
by Aliyah Almomen, Ahmed M. El-Toni, Mohammed Badran, Adel Alhowyan, Mohd Abul Kalam, Aws Alshamsan and Musaed Alkholief
Pharmaceutics 2020, 12(11), 1035; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12111035 - 29 Oct 2020
Cited by 29 | Viewed by 3124
Abstract
Melanoma remains the most lethal form of skin cancer and most challenging to treat despite advances in the oncology field. Our work describes the utilization of nanotechnology to target melanoma locally in an attempt to provide an advanced and efficient quality of therapy. [...] Read more.
Melanoma remains the most lethal form of skin cancer and most challenging to treat despite advances in the oncology field. Our work describes the utilization of nanotechnology to target melanoma locally in an attempt to provide an advanced and efficient quality of therapy. Amino-functionalized mesoporous silica nanoparticles (MSN-NH2) were developed in situ through the utilization of anionic surfactant and different volumes of 3-aminopropyltriethoxysilane (APTES) as a co-structure directing agent (CSDA). Prepared particles were characterized for their morphology, particles size, 5-flurouracol (5-FU) and dexamethasone (DEX) loading capacity and release, skin penetration, and cytotoxicity in vitro in HT-144 melanoma cells. Results of transmission electron microscopy (TEM) and nitrogen adsorption–desorption isotherm showed that using different volumes of APTES during the functionalization process had an impact on the internal and external morphology of the particles, as well as particle size. However, changing the volume of APTES did not affect the diameter of formed mesochannels, which was about 4 nm. MSN-NH2 showed a relatively high loading capacity of 5-FU (12.6 ± 5.5) and DEX (44.72 ± 4.21) when using drug: MSN-NH2 ratios of 5:1 for both drugs. The release profile showed that around 83% of 5-FU and 21% of DEX were released over 48 h in pH 7.4. The skin permeability study revealed that enhancement ratio of 5-Fu and DEX using MSN-NH2 were 4.67 and 5.68, respectively, relative to their free drugs counterparts. In addition, the accumulation of drugs in skin layers where melanoma cells usually reside were enhanced approximately 10 times with 5-FU and 5 times with DEX when delivering drugs using MSN-NH2 compared to control. MSN-NH2 alone was nontoxic to melanoma cells when incubated for 48 h in the range of 0 to 468 µg/mL. The combination of 5-FU MSN-NH2 and DEX MSN-NH2 showed significant increase in toxicity compared to their free dug counterparts and exhibited a synergetic effect as well as the ability to circumvent DEX induced 5-FU resistance in melanoma cells. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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15 pages, 788 KiB  
Article
Direct Quantification of Drug Loading Content in Polymeric Nanoparticles by Infrared Spectroscopy
by Guzmán Carissimi, Mercedes G. Montalbán, Gloria Víllora and Andreas Barth
Pharmaceutics 2020, 12(10), 912; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12100912 - 23 Sep 2020
Cited by 16 | Viewed by 3563
Abstract
Nanotechnology has enabled the development of novel therapeutic strategies such as targeted nanodrug delivery systems, control and stimulus-responsive release mechanisms, and the production of theranostic agents. As a prerequisite for the use of nanoparticles as drug delivery systems, the amount of loaded drug [...] Read more.
Nanotechnology has enabled the development of novel therapeutic strategies such as targeted nanodrug delivery systems, control and stimulus-responsive release mechanisms, and the production of theranostic agents. As a prerequisite for the use of nanoparticles as drug delivery systems, the amount of loaded drug must be precisely quantified, a task for which two approaches are currently used. However, both approaches suffer from the inefficiencies of drug extraction and of the solid-liquid separation process, as well as from dilution errors. This work describes a new, reliable, and simple method for direct drug quantification in polymeric nanoparticles using attenuated total reflection Fourier transform infrared spectroscopy, which can be adapted for a wide variety of drug delivery systems. Silk fibroin nanoparticles and naringenin were used as model polymeric nanoparticle carrier and drug, respectively. The specificity, linearity, detection limit, precision, and accuracy of the spectroscopic approach were determined in order to validate the method. A good linear relation was observed within 0.00 to 7.89% of naringenin relative mass with an R2 of 0.973. The accuracy was determined by the spike and recovery method. The results showed an average 104% recovery. The limit of detection and limit of quantification of the drug loading content were determined to be 0.3 and 1.0%, respectively. The method’s robustness is demonstrated by the notable similarities between the calibrations carried out using two different equipment setups at two different institutions. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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17 pages, 903 KiB  
Article
Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide
by Elena Sánchez-López, Anna Paús, Ignacio Pérez-Pomeda, Ana Calpena, Isabel Haro and María José Gómara
Pharmaceutics 2020, 12(6), 502; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12060502 - 31 May 2020
Cited by 9 | Viewed by 2714
Abstract
The effective use of fusion inhibitor peptides against cervical and colorectal infections requires the development of sustained release formulations. In this work we comparatively study two different formulations based on polymeric nanoparticles and lipid vesicles to propose a suitable delivery nanosystem for releasing [...] Read more.
The effective use of fusion inhibitor peptides against cervical and colorectal infections requires the development of sustained release formulations. In this work we comparatively study two different formulations based on polymeric nanoparticles and lipid vesicles to propose a suitable delivery nanosystem for releasing an HIV-1 fusion inhibitor peptide in vaginal mucosa. Polymeric nanoparticles of poly-d,l-lactic-co-glycolic acid (PLGA) and lipid large unilamellar vesicles loaded with the inhibitor peptide were prepared. Both formulations showed average sizes and polydispersity index values corresponding to monodisperse systems appropriate for vaginal permeation. High entrapment efficiency of the inhibitor peptide was achieved in lipid vesicles, which was probably due to the peptide’s hydrophobic nature. In addition, both nanocarriers remained stable after two weeks stored at 4 °C. While PLGA nanoparticles (NPs) did not show any delay in peptide release, lipid vesicles demonstrated favorably prolonged release of the peptide. Lipid vesicles were shown to improve the retention of the peptide on ex vivo vaginal tissue in a concentration sufficient to exert its pharmacological effect. Thus, the small size of lipid vesicles, their lipid-based composition as well as their ability to enhance peptide penetration on vaginal tissue led us to consider this formulation as a better nanosystem than polymeric nanoparticles for the sustained delivery of the HIV-1 fusion inhibitor peptide in vaginal tissues. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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Review

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30 pages, 3228 KiB  
Review
Lipid Nanoparticles for the Posterior Eye Segment
by Lorena Bonilla, Marta Espina, Patricia Severino, Amanda Cano, Miren Ettcheto, Antoni Camins, Maria Luisa García, Eliana B. Souto and Elena Sánchez-López
Pharmaceutics 2022, 14(1), 90; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14010090 - 31 Dec 2021
Cited by 25 | Viewed by 4555
Abstract
This review highlights the application of lipid nanoparticles (Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, or Lipid Drug Conjugates) as effective drug carriers for pathologies affecting the posterior ocular segment. Eye anatomy and the most relevant diseases affecting the posterior segment will be summarized. [...] Read more.
This review highlights the application of lipid nanoparticles (Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, or Lipid Drug Conjugates) as effective drug carriers for pathologies affecting the posterior ocular segment. Eye anatomy and the most relevant diseases affecting the posterior segment will be summarized. Moreover, preparation methods and different types and subtypes of lipid nanoparticles will also be reviewed. Lipid nanoparticles used as carriers to deliver drugs to the posterior eye segment as well as their administration routes, pharmaceutical forms and ocular distribution will be discussed emphasizing the different targeting strategies most recently employed for ocular drug delivery. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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54 pages, 7151 KiB  
Review
Lipid Nanocarriers for Anti-HIV Therapeutics: A Focus on Physicochemical Properties and Biotechnological Advances
by Maria J. Faria, Carla M. Lopes, José das Neves and Marlene Lúcio
Pharmaceutics 2021, 13(8), 1294; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13081294 - 19 Aug 2021
Cited by 11 | Viewed by 3763
Abstract
Since HIV was first identified, and in a relatively short period of time, AIDS has become one of the most devastating infectious diseases of the 21st century. Classical antiretroviral therapies were a major step forward in disease treatment options, significantly improving the survival [...] Read more.
Since HIV was first identified, and in a relatively short period of time, AIDS has become one of the most devastating infectious diseases of the 21st century. Classical antiretroviral therapies were a major step forward in disease treatment options, significantly improving the survival rates of HIV-infected individuals. Even though these therapies have greatly improved HIV clinical outcomes, antiretrovirals (ARV) feature biopharmaceutic and pharmacokinetic problems such as poor aqueous solubility, short half-life, and poor penetration into HIV reservoir sites, which contribute to the suboptimal efficacy of these regimens. To overcome some of these issues, novel nanotechnology-based strategies for ARV delivery towards HIV viral reservoirs have been proposed. The current review is focused on the benefits of using lipid-based nanocarriers for tuning the physicochemical properties of ARV to overcome biological barriers upon administration. Furthermore, a correlation between these properties and the potential therapeutic outcomes has been established. Biotechnological advancements using lipid nanocarriers for RNA interference (RNAi) delivery for the treatment of HIV infections were also discussed. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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54 pages, 2955 KiB  
Review
Novel Approaches for the Treatment of Pulmonary Tuberculosis
by Zhi Ming Tan, Gui Ping Lai, Manisha Pandey, Teerapol Srichana, Mallikarjuna Rao Pichika, Bapi Gorain, Subrat Kumar Bhattamishra and Hira Choudhury
Pharmaceutics 2020, 12(12), 1196; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12121196 - 10 Dec 2020
Cited by 28 | Viewed by 5767
Abstract
Tuberculosis (TB) is a contagious airborne disease caused by Mycobacterium tuberculosis, which primarily affects human lungs. The progression of drug-susceptible TB to drug-resistant strains, MDR-TB and XDR-TB, has become worldwide challenge in eliminating TB. The limitations of conventional TB treatment including frequent [...] Read more.
Tuberculosis (TB) is a contagious airborne disease caused by Mycobacterium tuberculosis, which primarily affects human lungs. The progression of drug-susceptible TB to drug-resistant strains, MDR-TB and XDR-TB, has become worldwide challenge in eliminating TB. The limitations of conventional TB treatment including frequent dosing and prolonged treatment, which results in patient’s noncompliance to the treatment because of treatment-related adverse effects. The non-invasive pulmonary drug administration provides the advantages of targeted-site delivery and avoids first-pass metabolism, which reduced the dose requirement and systemic adverse effects of the therapeutics. With the modification of the drugs with advanced carriers, the formulations may possess sustained released property, which helps in reducing the dosing frequency and enhanced patients’ compliances. The dry powder inhaler formulation is easy to handle and storage as it is relatively stable compared to liquids and suspension. This review mainly highlights the aerosolization properties of dry powder inhalable formulations with different anti-TB agents to understand and estimate the deposition manner of the drug in the lungs. Moreover, the safety profile of the novel dry powder inhaler formulations has been discussed. The results of the studies demonstrated that dry powder inhaler formulation has the potential in enhancing treatment efficacy. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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20 pages, 1925 KiB  
Review
Mechanisms of Resistance to Chemotherapy in Breast Cancer and Possible Targets in Drug Delivery Systems
by Patrícia de Faria Lainetti, Antonio Fernando Leis-Filho, Renee Laufer-Amorim, Alexandre Battazza and Carlos Eduardo Fonseca-Alves
Pharmaceutics 2020, 12(12), 1193; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12121193 - 09 Dec 2020
Cited by 33 | Viewed by 3575
Abstract
Breast cancer (BC) is one of the most important cancers worldwide, and usually, chemotherapy can be used in an integrative approach. Usually, chemotherapy treatment is performed in association with surgery, radiation or hormone therapy, providing an increased outcome to patients. However, tumors can [...] Read more.
Breast cancer (BC) is one of the most important cancers worldwide, and usually, chemotherapy can be used in an integrative approach. Usually, chemotherapy treatment is performed in association with surgery, radiation or hormone therapy, providing an increased outcome to patients. However, tumors can develop resistance to different drugs, progressing for a more aggressive phenotype. In this scenario, the use of nanocarriers could help to defeat tumor cell resistance, providing a new therapeutic perspective for patients. Thus, this systematic review aims to bring the molecular mechanisms involved in BC chemoresistance and extract from the previous literature information regarding the use of nanoparticles as potential treatment for chemoresistant breast cancer. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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45 pages, 6030 KiB  
Review
Hydrogels as Drug Delivery Systems: A Review of Current Characterization and Evaluation Techniques
by Margaux Vigata, Christoph Meinert, Dietmar W. Hutmacher and Nathalie Bock
Pharmaceutics 2020, 12(12), 1188; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12121188 - 07 Dec 2020
Cited by 199 | Viewed by 11389
Abstract
Owing to their tunable properties, controllable degradation, and ability to protect labile drugs, hydrogels are increasingly investigated as local drug delivery systems. However, a lack of standardized methodologies used to characterize and evaluate drug release poses significant difficulties when comparing findings from different [...] Read more.
Owing to their tunable properties, controllable degradation, and ability to protect labile drugs, hydrogels are increasingly investigated as local drug delivery systems. However, a lack of standardized methodologies used to characterize and evaluate drug release poses significant difficulties when comparing findings from different investigations, preventing an accurate assessment of systems. Here, we review the commonly used analytical techniques for drug detection and quantification from hydrogel delivery systems. The experimental conditions of drug release in saline solutions and their impact are discussed, along with the main mathematical and statistical approaches to characterize drug release profiles. We also review methods to determine drug diffusion coefficients and in vitro and in vivo models used to assess drug release and efficacy with the goal to provide guidelines and harmonized practices when investigating novel hydrogel drug delivery systems. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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25 pages, 5756 KiB  
Review
Recent Advances and Challenges in Controlling the Spatiotemporal Release of Combinatorial Anticancer Drugs from Nanoparticles
by Moon Sup Yoon, Yu Jin Lee, Hee Ji Shin, Chun-Woong Park, Sang-Bae Han, Jae-Kyung Jung, Jin-Seok Kim and Dae Hwan Shin
Pharmaceutics 2020, 12(12), 1156; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics12121156 - 27 Nov 2020
Cited by 17 | Viewed by 3525
Abstract
To overcome cancer, various chemotherapeutic studies are in progress; among these, studies on nano-formulated combinatorial drugs (NFCDs) are being actively pursued. NFCDs function via a fusion technology that includes a drug delivery system using nanoparticles as a carrier and a combinatorial drug therapy [...] Read more.
To overcome cancer, various chemotherapeutic studies are in progress; among these, studies on nano-formulated combinatorial drugs (NFCDs) are being actively pursued. NFCDs function via a fusion technology that includes a drug delivery system using nanoparticles as a carrier and a combinatorial drug therapy using two or more drugs. It not only includes the advantages of these two technologies, such as ensuring stability of drugs, selectively transporting drugs to cancer cells, and synergistic effects of two or more drugs, but also has the additional benefit of enabling the spatiotemporal and controlled release of drugs. This spatial and temporal drug release from NFCDs depends on the application of nanotechnology and the composition of the combination drug. In this review, recent advances and challenges in the control of spatiotemporal drug release from NFCDs are provided. To this end, the types of combinatorial drug release for various NFCDs are classified in terms of time and space, and the detailed programming techniques used for this are described. In addition, the advantages of the time and space differences in drug release in terms of anticancer efficacy are introduced in depth. Full article
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
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