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Pharmaceutics
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Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release
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Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release

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 (31 December 2024) | Viewed by 9510

Special Issue Editor

Dr. Ivalina Trendafilova

E-Mail Website
Guest Editor
1. Laboratory of Inorganic Materials Chemistry, Namur Institute of Structured Matter (NISM), University of Namur, 5000 Namur, Belgium
2. Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
Interests: materials science; porous silica; surface modification; surface interactions; drug delivery systems; drug release; nanotheranostics

Special Issue Information

Dear Colleagues,

Porous silica materials and composites on their bases attract increasing interest as carriers in drug delivery systems due to their unique properties, such as high specific surface area, controllable porosity, easy-to-modify surface, low cytotoxicity, etc. These properties allow the loading of significant amounts of drugs and can solve problems related to low solubility by modifying drug release, resulting in bioavailability enhancement and greater treatment effectiveness.

This Special Issue is focused on the design and development of novel drug delivery systems on the basis of porous silica or porous silica-containing materials, as well as the characterisation of their physico-chemical and biopharmaceutical properties. Studies on the synthesis of new porous silica materials as carriers in delivery systems, investigations of carrier–drug molecule interactions, and evaluations of the drug release rate and biocompatibility of the obtained systems are welcome to contribute to this SI.    

As a Guest Editor of a Special Issue titled "Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release" in Pharmaceutics (IF 5.4, ranks Q1 in the category of Pharmacology & Pharmacy) I am pleased to invite you to contribute a research article, or review paper, and I look forward to receiving your contributions.

Dr. Ivalina Trendafilova
Guest Editor

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • porous silica
  • silica-based composites
  • drug delivery system design
  • controlled release
  • target drug delivery
  • nanotheranostics

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Published Papers (5 papers)

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Research

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12 pages, 2398 KiB  
Article
Mesoporous Silica-Based Membranes in Transdermal Drug Delivery: The Role of Drug Loss in the Skin
by Frank Baumann, Theresa Paul, Susann Ossmann, Dirk Enke and Achim Aigner
Pharmaceutics 2024, 16(8), 995; https://doi.org/10.3390/pharmaceutics16080995 - 26 Jul 2024
Cited by 1 | Viewed by 1045
Abstract
Compared to other forms of drug administration, the use of Transdermal Drug Delivery Systems (TDDSs) offers significant advantages, including uniform drug release profiles that contribute to lower side effects and higher tolerability, avoidance of direct exposure to the gastrointestinal tract, better patient compliance [...] Read more.
Compared to other forms of drug administration, the use of Transdermal Drug Delivery Systems (TDDSs) offers significant advantages, including uniform drug release profiles that contribute to lower side effects and higher tolerability, avoidance of direct exposure to the gastrointestinal tract, better patient compliance due to their non-invasive means of application and others. Mesoporous silica membranes are of particular interest in this regard, due to their chemical stability and their tunable porous system, with adjustable pore sizes, pore volumes and surface chemistries. While this allows for fine-tuning and, thus, the development of optimized TDDSs with high loading capacities and the desired release profile of a given drug, its systemic availability also relies on skin penetration. In this paper, using a TDDS based on mesoporous silica membranes in Franz cell experiments on porcine skin, we demonstrate surprisingly substantial drug loss during skin penetration. Drug passage through porcine skin was found to be dependent on the age and pre-treatment of the skin. pH and temperature were major determinants of drug recovery rates as well, indicating drug loss in the skin by enzymatic metabolization. Regarding the TDDS, higher loading obtained by SO3H surface modification of the mesoporous silica membranes reduced drug loss. Still, high loss rates in the skin were determined for different drugs, including anastrozole, xylazine and imiquimod. We conclude that, beyond the fine-tuned drug release profiles from the mesoporous silica membrane TDDS, remarkably high drug loss in the skin is a major issue for achieving desired skin penetration and, thus, the systemic availability of drugs. This also poses critical requirements for defining an optimal TDDS based on mesoporous silica membranes. Full article
(This article belongs to the Special Issue Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release)
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23 pages, 6324 KiB  
Article
Investigating the Influence of Processing Conditions on Dissolution and Physical Stability of Solid Dispersions with Fenofibrate and Mesoporous Silica
by Ana Baumgartner, Nina Dobaj and Odon Planinšek
Pharmaceutics 2024, 16(5), 575; https://doi.org/10.3390/pharmaceutics16050575 - 24 Apr 2024
Cited by 5 | Viewed by 1478
Abstract
The study aimed to enhance the solubility of the poorly water-soluble drug, fenofibrate, by loading it onto mesoporous silica, forming amorphous solid dispersions. Solid dispersions with 30% fenofibrate were prepared using the solvent evaporation method with three solvents (ethyl acetate, acetone, and isopropanol) [...] Read more.
The study aimed to enhance the solubility of the poorly water-soluble drug, fenofibrate, by loading it onto mesoporous silica, forming amorphous solid dispersions. Solid dispersions with 30% fenofibrate were prepared using the solvent evaporation method with three solvents (ethyl acetate, acetone, and isopropanol) at different temperatures (40 °C, boiling point temperature). Various characteristics, including solid-state properties, particle morphology, and drug release, were evaluated by different methods and compared to a pure drug and a physical mixture of fenofibrate and silica. Results revealed that higher solvent temperatures facilitated complete amorphization and rapid drug release, with solvent choice having a lesser impact. The optimal conditions for preparation were identified as ethyl acetate at boiling point temperature. Solid dispersions with different fenofibrate amounts (20%, 25%, 35%) were prepared under these conditions. All formulations were fully amorphous, and their dissolution profiles were comparable to the formulation with 30% fenofibrate. Stability assessments after 8 weeks at 40 °C and 75% relative humidity indicated that formulations prepared with ethyl acetate and at 40 °C were physically stable. Interestingly, some formulations showed improved dissolution profiles compared to initial tests. In conclusion, mesoporous silica-based solid dispersions effectively improved fenofibrate dissolution and demonstrated good physical stability if prepared under appropriate conditions. Full article
(This article belongs to the Special Issue Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release)
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14 pages, 5767 KiB  
Article
Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation
by Rafaela de Andrade, Rita de Cássia dos Reis Schmidt, Leonardo Santos Gomes, Legna Colina-Vegas, Ruth Hinrichs, Marcos Antônio Zen Vasconcellos, Tania Maria Haas Costa, Monique Deon, Wilmer Villarreal and Edilson Valmir Benvenutti
Pharmaceutics 2024, 16(3), 357; https://doi.org/10.3390/pharmaceutics16030357 - 3 Mar 2024
Cited by 4 | Viewed by 2241
Abstract
Malaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein, magnetic mesoporous [...] Read more.
Malaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein, magnetic mesoporous silica (magMCM) was synthesized using iron oxide particles dispersed in the silica structure for magnetically driven behavior. The X-ray diffractogram (XRD) and Mössbauer spectra show patterns corresponding to magnetite and maghemite. Furthermore, Mössbauer spectroscopy revealed superparamagnetic behavior, attributed to single magnetic domains in particles smaller than 10 nm. Even in the presence of iron oxide particles, the hexagonal structure of MCM is clearly identified in XRD (low-angle region) and the channels are visible in TEM images. The drug chloroquine (CQ) was encapsulated by incipient wetness impregnation (magMCM-CQ). The N2 adsorption–desorption isotherms show that CQ molecules were encapsulated in the pores, without completely filling the mesopores. BET surface area values were 630 m2 g−1 (magMCM) and 467 m2 g−1 (magMCM-CQ). Encapsulated CQ exhibited rapid delivery (99% in 3 h) in buffer medium and improved solubility compared to the non-encapsulated drug, attributed to CQ encapsulation in amorphous form. The biocompatibility assessment of magMCM, magMCM-CQ, and CQ against MRC5 non-tumoral lung fibroblasts using the MTT assay after 24 h revealed no toxicity associated with magMCM. On the other hand, the non-encapsulated CQ and magMCM-CQ exhibited comparable dose–response activity, indicating a similar cytotoxic effect. Full article
(This article belongs to the Special Issue Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release)
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22 pages, 5846 KiB  
Article
In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen
by Aisha Rashid, Muhammad Irfan, Yousaf Kamal, Sajid Asghar, Syed Haroon Khalid, Ghulam Hussain, Abdulrahman Alshammari, Thamer H. Albekairi, Metab Alharbi, Hafeez Ullah Khan, Zunera Chauhdary, Thierry F. Vandamme and Ikram Ullah Khan
Pharmaceutics 2024, 16(2), 164; https://doi.org/10.3390/pharmaceutics16020164 - 24 Jan 2024
Cited by 3 | Viewed by 2502
Abstract
Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous administration of H2 receptor antagonists such [...] Read more.
Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous administration of H2 receptor antagonists such as ranitidine hydrochloride (RHCl) is obligatory. Here, we developed composite oral fast-disintegrating films (ODFs) containing FBP along with RHCl to provide a gastroprotective effect as well as to enhance the solubility and bioavailability of FBP. The ternary solid dispersion (TSD) of FBP was fabricated with Syloid® 244FP and poloxamer® 188 using the solvent evaporation technique. The synthesized FBP-TSD (coded as TSD) was loaded alone (S1) and in combination with plain RHCl (S2) in the composite ODFs based on hydroxypropyl methyl cellulose E5 (HPMC E5). The synthesized composite ODFs were evaluated by in vitro (thickness, folding endurance, tensile strength, disintegration, SEM, FTIR, XRD and release study) and in vivo (analgesic, anti-inflammatory activity, pro-inflammatory cytokines and gastroprotective assay) studies. The in vitro characterization revealed that TSD preserved its integrity and was effectively loaded in S1 and S2 with optimal compatibility. The films were durable and flexible with a disintegration time ≈15 s. The release profile at pH 6.8 showed that the solid dispersion of FBP improved the drug solubility and release when compared with pure FBP. After in vitro studies, it was observed that the analgesic and anti-inflammatory activity of S2 was higher than that of pure FBP and other synthesized formulations (TSD and S1). Similarly, the level of cytokines (TNF-α and IL-6) was also markedly reduced by S2. Furthermore, a gastroprotective assay confirmed that S2 has a higher safety profile in comparison to pure FBP and other synthesized formulations (TSD and S1). Thus, composite ODF (S2) can effectively enhance the FBP solubility and its therapeutic efficacy, along with its gastroprotective effect. Full article
(This article belongs to the Special Issue Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release)
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Review

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28 pages, 4534 KiB  
Review
Porous Silica Nanomaterials as Carriers of Biologically Active Natural Polyphenols: Effect of Structure and Surface Modification
by Ivalina Trendafilova and Margarita Popova
Pharmaceutics 2024, 16(8), 1004; https://doi.org/10.3390/pharmaceutics16081004 - 29 Jul 2024
Cited by 2 | Viewed by 1356
Abstract
For centuries, humans have relied on natural products to prevent and treat numerous health issues. However, biologically active compounds from natural sources, such as polyphenols, face considerable challenges, due to their low solubility, rapid metabolism, and instability, which hinder their effectiveness. Advances in [...] Read more.
For centuries, humans have relied on natural products to prevent and treat numerous health issues. However, biologically active compounds from natural sources, such as polyphenols, face considerable challenges, due to their low solubility, rapid metabolism, and instability, which hinder their effectiveness. Advances in the nanotechnologies have provided solutions to overcoming these problems through the use of porous silica materials as polyphenol carriers. These materials possess unique properties, such as a high specific surface area, adjustable particle and pore sizes, and a surface that can be easily and selectively modified, which favor their application in delivery systems of polyphenols. In this review, we summarize and discuss findings on how the pore and particle size, structure, and surface modification of silica materials influence the preparation of efficient delivery systems for biologically active polyphenols from natural origins. The available data demonstrate how parameters such as adsorption capacity, release and antioxidant properties, bioavailability, solubility, stability, etc., of the studied delivery systems could be affected by the structural and chemical characteristics of the porous silica carriers. Results in the literature confirm that by regulating the structure and selecting the appropriate surface modifications, the health benefits of the loaded bioactive molecules can be significantly improved. Full article
(This article belongs to the Special Issue Mesoporous Silica-Based Materials in Drug Delivery and Controlled Release)
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