Topic Editors

Institute of New Drug Development, China Medical University, No. 91 Hsueh-Shih Road, Taichung 40402, Taiwan
School of Pharmacy, Macau University of Science and Technology, Macau 999078, China
Neher's Biophysics Laboratory for Innovative Drug Discovery, Macau University of Science and Technology, Macao, China

Advances in Controlled Release and Targeting of Drugs

Abstract submission deadline
20 January 2025
Manuscript submission deadline
20 March 2025
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Topic Information

Dear Colleagues,

Drug delivery focuses on the approaches to improve pharmaceutical practices by enhancing drug molecule fractions that reach the target cells and receptors. The importance of this topic lies in the necessity of reducing the drug side effects and drug dosage. Drug delivery compounds consist of molecules (polymers, macromolecules, small molecules) capable of coordinating, transporting, and releasing drugs selectively to their targets. The coordination must be reversible to allow the subsequent release. The targeting can be active (through functional groups that interact with the targets) or passive (the delivery drug exploits the physical characteristics of the physical environment sorrounding the targets). Commercial systems include liposome compounds, cyclodextrins, and prodrug compounds. Recent research is trying to develop more sophisticated strategies by exploiting the progress in organic synthesis, supramolecular chemistry, and molecular machines. This topic collection covers all manuscripts about drug delivery systems.

Dr. Carmine Coluccini
Dr. Paolo Coghi
Dr. Xingxing Fan
Topic Editors

Keywords

  • drug delivery
  • drug release
  • drug targeting
  • prodrug
  • drug coordination

Participating Journals

Journal Name Impact Factor CiteScore Launched Year First Decision (median) APC
Macromol
macromol
- 5.2 2021 20.4 Days CHF 1000 Submit
Molecules
molecules
4.2 7.4 1996 15.1 Days CHF 2700 Submit
Nanomaterials
nanomaterials
4.4 8.5 2010 13.8 Days CHF 2900 Submit
Pharmaceutics
pharmaceutics
4.9 7.9 2009 14.9 Days CHF 2900 Submit
Polymers
polymers
4.7 8.0 2009 14.5 Days CHF 2700 Submit

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Published Papers (3 papers)

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18 pages, 2148 KiB  
Article
Nebivolol Polymeric Nanoparticles-Loaded In Situ Gel for Effective Treatment of Glaucoma: Optimization, Physicochemical Characterization, and Pharmacokinetic and Pharmacodynamic Evaluation
by Pradeep Singh Rawat, Punna Rao Ravi, Mohammed Shareef Khan, Radhika Rajiv Mahajan and Łukasz Szeleszczuk
Nanomaterials 2024, 14(16), 1347; https://doi.org/10.3390/nano14161347 - 14 Aug 2024
Viewed by 741
Abstract
Nebivolol hydrochloride (NEB), a 3rd-generation beta-blocker, was recently explored in managing open-angle glaucoma due to its mechanism of action involving nitric oxide release for the vasodilation. To overcome the issue of low ocular bioavailability and the systemic side effects associated with conventional ocular [...] Read more.
Nebivolol hydrochloride (NEB), a 3rd-generation beta-blocker, was recently explored in managing open-angle glaucoma due to its mechanism of action involving nitric oxide release for the vasodilation. To overcome the issue of low ocular bioavailability and the systemic side effects associated with conventional ocular formulation (aqueous suspension), we designed and optimized polycaprolactone polymeric nanoparticles (NEB-PNPs) by applying design of experiments (DoE). The particle size and drug loading of the optimized NEB-PNPs were 270.9 ± 6.3 nm and 28.8 ± 2.4%, respectively. The optimized NEB-PNPs were suspended in a dual-sensitive in situ gel prepared using a mixture of P407 + P188 (as a thermo-sensitive polymer) and κCRG (as an ion-sensitive polymer), reported previously by our group. The NEB-PNPs-loaded in situ gel (NEB-PNPs-ISG) formulation was characterized for its rheological behavior, physical and chemical stability, in vitro drug release, and in vivo efficacy. The NEB-PNPs-loaded in situ gel, in ocular pharmacokinetic studies, achieved higher aqueous humor exposure (AUC0–t = 329.2 ng × h/mL) and for longer duration (mean residence time = 9.7 h) than compared to the aqueous suspension of plain NEB (AUC0–t = 189 ng × h/mL and mean residence time = 6.1 h) reported from our previous work. The pharmacokinetic performance of NEB-PNPs-loaded in situ gel translated into a pharmacodynamic response with 5-fold increase in the overall percent reduction in intraocular pressure by the formulation compared to the aqueous suspension of plain NEB reported from our previous work. Further, the mean response time of NEB-PNPs-loaded in situ gel (12.4 ± 0.6 h) was three times higher than aqueous suspension of plain NEB (4.06 ± 0.3 h). Full article
(This article belongs to the Topic Advances in Controlled Release and Targeting of Drugs)
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19 pages, 13325 KiB  
Article
Dual-Functionalized Mesoporous Silica Nanoparticles for Celecoxib Delivery: Amine Grafting and Imidazolyl PEI Gatekeepers for Enhanced Loading and Controlled Release with Reduced Toxicity
by Diky Mudhakir, Ebrahim Sadaqa, Zuliar Permana, Jihan Eldia Mumtazah, Normalita Faraz Zefrina, Jovinka Natalie Xeliem, Latifa Fawzia Hanum and Neng Fisheri Kurniati
Molecules 2024, 29(15), 3546; https://doi.org/10.3390/molecules29153546 - 27 Jul 2024
Cited by 1 | Viewed by 1320
Abstract
The development of targeted drug delivery systems has been a pivotal area in nanomedicine, addressing challenges like low drug loading capacity, uncontrolled release, and systemic toxicity. This study aims to develop and evaluate dual-functionalized mesoporous silica nanoparticles (MSN) for targeted delivery of celecoxib, [...] Read more.
The development of targeted drug delivery systems has been a pivotal area in nanomedicine, addressing challenges like low drug loading capacity, uncontrolled release, and systemic toxicity. This study aims to develop and evaluate dual-functionalized mesoporous silica nanoparticles (MSN) for targeted delivery of celecoxib, enhancing drug loading, achieving controlled release, and reducing systemic toxicity through amine grafting and imidazolyl polyethyleneimine (PEI) gatekeepers. MSN were synthesized using the sol–gel method and functionalized with (3-aminopropyl) triethoxysilane (APTES) to create amine-grafted MSN (MSN-NH2). Celecoxib was loaded into MSN-NH2, followed by conjugation of imidazole-functionalized PEI (IP) gatekeepers synthesized via carbodiimide coupling. Characterization was conducted using Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR). Drug loading capacity, entrapment efficiency, and in vitro drug release at pH 5.5 and 7.4 were evaluated. Cytotoxicity was assessed using the MTT assay on RAW 264.7 macrophages. The synthesized IP was confirmed by FTIR and 1H-NMR. Amine-grafted MSN demonstrated a celecoxib loading capacity of 12.91 ± 2.02%, 2.1 times higher than non-functionalized MSN. In vitro release studies showed pH-responsive behavior with significantly higher celecoxib release from MSN-NH2-celecoxib-IP at pH 5.5 compared to pH 7.4, achieving a 33% increase in release rate within 2 h. Cytotoxicity tests indicated significantly higher cell viability for IP-treated cells compared to PEI-treated cells, confirming reduced toxicity. The dual-functionalization of MSN with amine grafting and imidazolyl PEI gatekeepers enhances celecoxib loading and provides controlled pH-responsive drug release while reducing systemic toxicity. These findings highlight the potential of this advanced drug delivery system for targeted anti-inflammatory and anticancer therapies. Full article
(This article belongs to the Topic Advances in Controlled Release and Targeting of Drugs)
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15 pages, 3171 KiB  
Article
Encapsulation of Gemcitabine on Porphyrin Aluminum Metal-Organic Framework by Mechano-Chemistry, Delayed Drug Release and Cytotoxicity to Pancreatic Cancer PANC-1 Cells
by Sheriff Umar and Alexander Samokhvalov
Molecules 2024, 29(13), 3189; https://doi.org/10.3390/molecules29133189 - 4 Jul 2024
Viewed by 1089
Abstract
Gemcitabine is a widely used antimetabolite drug of pyrimidine structure, which can exist as a free-base molecular form (Gem). The encapsulated forms of medicinal drugs are of interest for delayed and local drug release. We utilized, for the first time, a novel approach [...] Read more.
Gemcitabine is a widely used antimetabolite drug of pyrimidine structure, which can exist as a free-base molecular form (Gem). The encapsulated forms of medicinal drugs are of interest for delayed and local drug release. We utilized, for the first time, a novel approach of mechano-chemistry by liquid-assisted grinding (LAG) to encapsulate Gem on a “matrix” of porphyrin aluminum metal-organic framework Al-MOF-TCPPH2 (compound 2). The chemical bonding of Gem to compound 2 was studied by ATR-FTIR spectroscopy and powder XRD. The interaction involves the C=O group of Gem molecules, which indicates the formation of the encapsulation complex in the obtained composite. Further, the delayed release of Gem from the composite was studied to phosphate buffered saline (PBS) at 37 °C using an automated drug dissolution apparatus equipped with an autosampler. The concentration of the released drug was determined by HPLC-UV analysis. The composite shows delayed release of Gem due to the bonded form and constant concentration thereafter, while pure Gem shows quick dissolution in less than 45 min. Delayed release of Gem drug from the composite follows the kinetic pseudo-first-order rate law. Further, for the first time, the mechanism of delayed release of Gem was assessed by the variable stirring speed of drug release media, and kinetic rate constant k was found to decrease when stirring speed is decreased (diffusion control). Finally, the prolonged time scale of toxicity of Gem to pancreatic cancer PANC-1 cells was studied by continuous measurements of proliferation (growth) for 6 days, using the xCELLigence real-time cell analyzer (RTCA), for the composite vs. pure drug, and their differences indicate delayed drug release. Aluminum metal-organic frameworks are new and promising materials for the encapsulation of gemcitabine and related small-molecule antimetabolites for controlled delayed drug release and potential use in drug-eluting implants. Full article
(This article belongs to the Topic Advances in Controlled Release and Targeting of Drugs)
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