Porous Micro and Nanoparticles for Drug Delivery

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 (30 October 2021) | Viewed by 20516

Special Issue Editors

Instituto Interuniversitario de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat de València, Doctor Moliner 50, Burjassot, 46100, Valencia, Spain
Interests: gated mesoporous materials; drug delivery; molecular sensing; chromo and fluorogenic chemosensors and probes; molecular recognition
Instituto Interuniversitario de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat de València, Doctor Moliner 50, Burjassot, 46100 Valencia, Spain
Interests: gated mesoporous materials; drug delivery; molecular sensing; chromo and fluorogenic chemosensors and probes; molecular recognition
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Special Issue Information

Dear Colleagues,

Although the fields of molecular, biomolecular, and supramolecular chemistry and inorganic materials have traditionally been poorly interrelated, research into this cross-disciplinary region has recently emerged almost exponentially and has resulted in a many novel hybrid materials with advanced functions in a surprisingly short time. Among the different inorganic solids, much attention has been given to porous materials in both fundamental and applied research. In this scenario, gated nanochemistry is a highly topical tool that has been applied to the design of new advanced functions by means of mass transport control in nanometric terms. In recent years, gated supports have proven excellent candidates for designing controlled-release systems for different applications, including drug delivery and sensing.

This Special Issue aims to collect the latest advances and state-of-the-art in the field of controlled drug delivery, using porous nano- or microparticles as drug carriers. The combination of these materials with selective molecular gates, which open only on the site of action as a result of some target stimulus, is expected to improve drug bioavailability and reduce drug toxicity.

Prof. Dr. Pablo Gaviña
Prof. Dr. Margarita Parra
Guest Editors

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Keywords

  • porous materials
  • gated materials
  • micro and nanoparticles
  • drug delivery
  • controlled release
  • biomedical applications

Published Papers (5 papers)

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Research

12 pages, 4809 KiB  
Article
Plate-like Alginate Microparticles with Disulfiram–SPIO–Coencapsulation: An In Vivo Study for Combined Therapy on Ovarian Cancer
by Meng-Yi Bai, Mu-Hsien Yu, Ting-Teng Wang, Shiu-Hsin Chen and Yu-Chi Wang
Pharmaceutics 2021, 13(9), 1348; https://doi.org/10.3390/pharmaceutics13091348 - 27 Aug 2021
Cited by 6 | Viewed by 1877
Abstract
Disulfiram is a drug used to support the treatment of chronic alcoholism. Recently, it has been found to have an off-label ability to inhibit the growth of ovarian cancer cells. However, the original formulation was designed for use via oral administration, which is [...] Read more.
Disulfiram is a drug used to support the treatment of chronic alcoholism. Recently, it has been found to have an off-label ability to inhibit the growth of ovarian cancer cells. However, the original formulation was designed for use via oral administration, which is not suitable to be given by a direct spray on the affected area. Therefore, in this study, we designed and prepared alginate (ALG) microparticles loaded with disulfiram and superparamagnetic iron oxide (cross-linking disulfiram/SPIO/ALG MPs), which have great potential application for inhibiting the growth of ovarian cancer simultaneously via two treatments, i.e., chemotherapy and hyperthermia. The drug-encapsulating alginate microparticles were prepared using an electrospray system and then cross-linked with calcium chloride ions. The particles were observed by optical microscopy and scanning electron microscopy, and found to be approximately 200 μm in diameter. The disc-shape morphology of the microparticles could be controlled by up to 95%. The drug-encapsulation efficiency of the microparticles reached 98%, and the suppression of tumor growth for the free-form disulfiram-treated group and disulfiram/SPIO/ALG MPs-treated group were 48.2% and 55.9% of tumor volume reduction, respectively, compared with a cisplatin-treated group. A hyperthermic effect can be achieved by applying a magnetic field to oscillate SPIO. The results of this study showed that these cross-linking disulfiram/SPIO/ALG MPs are potential drug carriers for the treatment of ovarian cancer. Full article
(This article belongs to the Special Issue Porous Micro and Nanoparticles for Drug Delivery)
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21 pages, 4629 KiB  
Article
Development of a Hydrophobicity-Controlled Delivery System Containing Levodopa Methyl Ester Hydrochloride Loaded into a Mesoporous Silica
by Tamás Kiss, Gábor Katona, László Mérai, László Janovák, Ágota Deák, Gábor Kozma, Zoltán Kónya and Rita Ambrus
Pharmaceutics 2021, 13(7), 1039; https://doi.org/10.3390/pharmaceutics13071039 - 07 Jul 2021
Cited by 3 | Viewed by 2381
Abstract
Background: The drug release of antiparkinsonian drugs is an important issue during the formulation process because proper release kinetics can help to reduce the off periods of Parkinson’s disease. A 2-factor, 3-level (32) full-factorial design was conducted to evaluate statistically the [...] Read more.
Background: The drug release of antiparkinsonian drugs is an important issue during the formulation process because proper release kinetics can help to reduce the off periods of Parkinson’s disease. A 2-factor, 3-level (32) full-factorial design was conducted to evaluate statistically the influence of the hydrophobicity of mesoporous silica on drug release. Methods: Hydrophobization was evaluated by different methods, such as contact angle measurement, infrared spectroscopy and charge titration. After loading the drug (levodopa methyl ester hydrochloride, melevodopa hydrochloride, LDME) into the mesopores, drug content, particle size, specific surface area and homogeneity of the products were also analyzed. The amorphous state of LDME was verified by X-ray diffractometry and differential scanning calorimetry. Results: Drug release was characterized by a model-independent method using the so-called initial release rate parameter, as detailed in the article. The adaptability of this method was verified; the model fitted closely to the actual release results according to the similarity factor, independently of the release kinetics. Conclusions: The API was successfully loaded into the silica, resulting in a reduced surface area. The release studies indicated that the release rate significantly decreased (p < 0.05) with increasing hydrophobicity. The products with controlled release can reduce the off period frequency. Full article
(This article belongs to the Special Issue Porous Micro and Nanoparticles for Drug Delivery)
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20 pages, 4458 KiB  
Article
Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation
by Joshua H. Santos, Mark Tristan J. Quimque, Allan Patrick G. Macabeo, Mary Jho-Anne T. Corpuz, Yun-Ming Wang, Tsai-Te Lu, Chia-Her Lin and Oliver B. Villaflores
Pharmaceutics 2020, 12(5), 437; https://doi.org/10.3390/pharmaceutics12050437 - 09 May 2020
Cited by 18 | Viewed by 4202
Abstract
Bioavailability plays an important role in drug activity in the human body, as certain drug amounts should be present to elicit activity. However, low bioavailability of drugs leads to negligible use for human benefit. In this study, the diversely active neolignan, magnolol, was [...] Read more.
Bioavailability plays an important role in drug activity in the human body, as certain drug amounts should be present to elicit activity. However, low bioavailability of drugs leads to negligible use for human benefit. In this study, the diversely active neolignan, magnolol, was impregnated onto a Zr-based organometallic framework [Uio-66(Zr)] to increase its low bioavailability (4–5%) and to test its potential acute oral toxicity. Synthesis of Uio-66(Zr) was done through the solvothermal method while simple impregnation at different time points was used to incorporate magnolol. The loading capacity of Uio-66(Zr) at 36 h was found to be significantly higher at 72.16 ± 2.15% magnolol than in other incubation time. Based on the OECD 425 (limit test), toxicity was not observed at 2000 mg kg−1 dose of mag@Uio-66(Zr) in female Sprague Dawley rats. The area under the curve (AUC) at 0–720 min of mag@Uio-66(Zr) was significantly higher than the AUC of free magnolol. Moreover, relative bioavailability increased almost two-folds using Uio-66(Zr). Unconjugated magnolol was found in the liver, kidney, and brain of rats in all treatment groups. Collectively, Uio-66(Zr) provided a higher magnolol bioavailability when used as drug carrier. Thus, utilization of Uio-66(Zr) as drug carrier is of importance for maximal use for poorly soluble and lowly bioavailable drugs. Full article
(This article belongs to the Special Issue Porous Micro and Nanoparticles for Drug Delivery)
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16 pages, 3712 KiB  
Article
Poly(ε-caprolactone) (PCL) Hollow Nanoparticles with Surface Sealability and On-Demand Pore Generability for Easy Loading and NIR Light-Triggered Release of Drug
by Ju Hyang Park, Da In Kim, Sang Gi Hong, Hojun Seo, Jongbok Kim, Geon Dae Moon and Dong Choon Hyun
Pharmaceutics 2019, 11(10), 528; https://doi.org/10.3390/pharmaceutics11100528 - 13 Oct 2019
Cited by 7 | Viewed by 4155
Abstract
A new system for the easy loading and NIR light-triggered release of drugs is introduced. It consists of poly(ε-caprolactone) (PCL) hollow nanoparticles with surface openings containing a biodegradable fatty acid with phase-change ability and a biocompatible photothermal agent. These openings, which can enhance [...] Read more.
A new system for the easy loading and NIR light-triggered release of drugs is introduced. It consists of poly(ε-caprolactone) (PCL) hollow nanoparticles with surface openings containing a biodegradable fatty acid with phase-change ability and a biocompatible photothermal agent. These openings, which can enhance the connectivity between the interior and the exterior, enable the easy loading of drug molecules into the interior voids, and their successive sealing ensures a stable encapsulation of the drug. Upon exposure to an external NIR light irradiation, the photothermal agent generates heat that raises the local temperature of the hollow particles above the melting point of the fatty acid, leading to the formation of nanopores on their shells, and consequently, the instant release of the encapsulated drug molecules through the pores. The synergistic activity of the hyperthermia effect from the photothermal agent and the NIR-triggered release of the drug molecules results in noticeable anticancer efficacy. Full article
(This article belongs to the Special Issue Porous Micro and Nanoparticles for Drug Delivery)
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16 pages, 2012 KiB  
Article
Rationally Designed Dendritic Silica Nanoparticles for Oral Delivery of Exenatide
by Muhammad Mustafa Abeer, Anand Kumar Meka, Naisarg Pujara, Tushar Kumeria, Ekaterina Strounina, Rute Nunes, Ana Costa, Bruno Sarmento, Sumaira Z. Hasnain, Benjamin P. Ross and Amirali Popat
Pharmaceutics 2019, 11(8), 418; https://doi.org/10.3390/pharmaceutics11080418 - 19 Aug 2019
Cited by 43 | Viewed by 6799
Abstract
Type 2 diabetes makes up approximately 85% of all diabetic cases and it is linked to approximately one-third of all hospitalisations. Newer therapies with long-acting biologics such as glucagon-like peptide-1 (GLP-1) analogues have been promising in managing the disease, but they cannot reverse [...] Read more.
Type 2 diabetes makes up approximately 85% of all diabetic cases and it is linked to approximately one-third of all hospitalisations. Newer therapies with long-acting biologics such as glucagon-like peptide-1 (GLP-1) analogues have been promising in managing the disease, but they cannot reverse the pathology of the disease. Additionally, their parenteral administration is often associated with high healthcare costs, risk of infections, and poor patient adherence associated with phobia of needles. Oral delivery of these compounds would significantly improve patient compliance; however, poor enzymatic stability and low permeability across the gastrointestinal tract makes this task challenging. In the present work, large pore dendritic silica nanoparticles (DSNPs) with a pore size of ~10 nm were prepared, functionalized, and optimized in order to achieve high peptide loading and improve intestinal permeation of exenatide, a GLP-1 analogue. Compared to the loading capacity of the most popular, Mobil Composition of Matter No. 41 (MCM-41) with small pores, DSNPs showed significantly high loading owing to their large and dendritic pore structure. Among the tested DSNPs, pristine and phosphonate-modified DSNPs (PDSNPs) displayed remarkable loading of 40 and 35% w/w, respectively. Furthermore, particles successfully coated with positively charged chitosan reduced the burst release of exenatide at both pH 1.2 and 6.8. Compared with free exenatide, both chitosan-coated and uncoated PDSNPs enhanced exenatide transport through the Caco-2 monolayer by 1.7 fold. Interestingly, when a triple co-culture model of intestinal permeation was used, chitosan-coated PDSNPs performed better compared to both PDSNPs and free exenatide, which corroborated our hypothesis behind using chitosan to interact with mucus and improve permeation. These results indicate the emerging role of large pore silica nanoparticles as promising platforms for oral delivery of biologics such as exenatide. Full article
(This article belongs to the Special Issue Porous Micro and Nanoparticles for Drug Delivery)
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