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Pharmaceutics
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Controlled Delivery Formulations (Volume II)
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Controlled Delivery Formulations (Volume II)

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (20 December 2021) | Viewed by 18747

Special Issue Editor

Prof. Dr. Marta González-Álvarez

E-Mail Website
Guest Editor
Department of Engineering and Pharmaceutical Technology, Faculty of Pharmacy, Miguel Hernandez University, 03550 Alicante, Spain
Interests: dissolutión; controlrelease; disintegration; drug development
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Controlled release formulations are designed to release drug molecules at a specific release rate and at specific sites to maximize therapeutic effects and improve a patient’s compliance.

There are different types of classifications for different controlled release formulations that take into account several factors such as extended release, delayed time, or the strategic release process based on the physiological characteristics in the different administration routes.

Advanced controlled release systems allow for different administrative pathways. Most of these are designed for the oral, parenteral, and transdermal routes, but the controlled release dosage forms of the oral mucosa, the eye, the implantation under the skin, and the nasal route have been developed.

This Special Issue has the aim of highlighting current progress in controlled delivery formulations.

Prof. Dr. Marta González-Álvarez
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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

  • controlled release
  • nanoparticles
  • microparticles
  • hydrogels
  • dendrimers
  • liposomes
  • adminsitration routes

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Related Special Issue

Published Papers (4 papers)

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Research

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21 pages, 3060 KiB  
Article
Development of Extended-Release Mini-Tablets Containing Metoprolol Supported by Design of Experiments and Physiologically Based Biopharmaceutics Modeling
by Michele Georges Issa, Natalia Vieira de Souza, Bruna Wenyi Chuang Jou, Marcelo Dutra Duque and Humberto Gomes Ferraz
Pharmaceutics 2022, 14(5), 892; https://doi.org/10.3390/pharmaceutics14050892 - 19 Apr 2022
Cited by 5 | Viewed by 4131
Abstract
The development of extended-release dosage forms with adequate drug release is a challenge for pharmaceutical companies, mainly when the drug presents high solubility, as in Biopharmaceutics Classification System (BCS) class I. This study aimed to develop extended-release mini-tablets containing metoprolol succinate (MS), while [...] Read more.
The development of extended-release dosage forms with adequate drug release is a challenge for pharmaceutical companies, mainly when the drug presents high solubility, as in Biopharmaceutics Classification System (BCS) class I. This study aimed to develop extended-release mini-tablets containing metoprolol succinate (MS), while integrating design of experiments (DOE) and physiologically based biopharmaceutics modeling (PBBM), to predict its absorption and to run virtual bioequivalence (VBE) studies in both fasted and fed states. Core mini-tablet formulations (F1, F2, and F3) were prepared by direct compression and coated using nine coating formulations planned using DOE, while varying the percentages of the controlled-release and the pore-forming polymers. The coated mini-tablets were submitted to a dissolution test; additional formulations were prepared that were optimized by simulating the dissolution profiles, and the best one was submitted to VBE studies using GastroPlus® software. An optimized formulation (FO) containing a mixture of immediate and extended-release mini-tablets showed to be bioequivalent to the reference drug product containing MS when running VBE studies in both fasted and fed states. The integration of DOE and PBBM showed to be an interesting approach in the development of extended-release mini-tablet formulation containing MS, and can be used to rationalize the development of dosage forms. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations (Volume II))
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17 pages, 6800 KiB  
Article
Customisable Tablet Printing: The Development of Multimaterial Hot Melt Inkjet 3D Printing to Produce Complex and Personalised Dosage Forms
by Anna Lion, Ricky D. Wildman, Morgan R. Alexander and Clive J. Roberts
Pharmaceutics 2021, 13(10), 1679; https://doi.org/10.3390/pharmaceutics13101679 - 14 Oct 2021
Cited by 17 | Viewed by 4114
Abstract
One of the most striking characteristics of 3D printing is its capability to produce multi-material objects with complex geometry. In pharmaceutics this translates to the possibility of dosage forms with multi-drug loading, tailored dosing and release. We have developed a novel dual material [...] Read more.
One of the most striking characteristics of 3D printing is its capability to produce multi-material objects with complex geometry. In pharmaceutics this translates to the possibility of dosage forms with multi-drug loading, tailored dosing and release. We have developed a novel dual material hot-melt inkjet 3D printing system which allows for precisely controlled multi-material solvent free inkjet printing. This reduces the need for time-consuming exchanges of printable inks and expensive post processing steps. With this printer, we show the potential for design of printed dosage forms for tailored drug release, including single and multi-material complex 3D patterns with defined localised drug loading where a drug-free ink is used as a release-retarding barrier. For this, we used Compritol HD5 ATO (matrix material) and Fenofibrate (model drug) to prepare both drug-free and drug-loaded inks with drug concentrations varying between 5% and 30% (w/w). The printed constructs demonstrated the required physical properties and displayed immediate, extended, delayed and pulsatile drug release depending on drug localisation inside of the printed formulations. For the first time, this paper demonstrates that a commonly used pharmaceutical lipid, Compritol HD5 ATO, can be printed via hot-melt inkjet printing as single ink material, or in combination with a drug, without the need for additional solvents. Concurrently, this paper demonstrates the capabilities of dual material hot-melt inkjet 3D printing system to produce multi-material personalised solid dosage forms. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations (Volume II))
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16 pages, 2987 KiB  
Article
Selection and Incorporation of siRNA Carrying Non-Viral Vector for Sustained Delivery from Gellan Gum Hydrogels
by Anastasios Nalbadis, Marie-Luise Trutschel, Henrike Lucas, Jana Luetzkendorf, Annette Meister and Karsten Mäder
Pharmaceutics 2021, 13(10), 1546; https://doi.org/10.3390/pharmaceutics13101546 - 23 Sep 2021
Cited by 3 | Viewed by 2417
Abstract
The local controlled release of siRNA is an attractive and rational strategy to enhance and extend the effectiveness of gene therapy. Since naked and unmodified siRNA has a limited cell uptake and knockdown efficiency, the complexation of siRNA with non-viral carriers is often [...] Read more.
The local controlled release of siRNA is an attractive and rational strategy to enhance and extend the effectiveness of gene therapy. Since naked and unmodified siRNA has a limited cell uptake and knockdown efficiency, the complexation of siRNA with non-viral carriers is often necessary for the delivery of bioactive RNA. We evaluated the performance of three different non-viral siRNA carriers, including DOTAP lipoplexes (DL), chitosan polyplexes (CP), and solid lipid complexes (SLC). The physicochemical properties of the siRNA-nanocarriers were characterized by dynamic light scattering and gel electrophoresis. After in vitro characterization, the carrier with the most appropriate properties was found to be the DL suspension, which was subsequently loaded into a gellan gum hydrogel matrix and examined for its drug load, stability, and homogeneity. The hydrogels microstructure was investigated by rheology to assess the impact of the rheological properties on the release of the siRNA nanocarriers. A controlled release of complexed siRNA over 60 days in vitro was observed. By comparing the results from fluorescence imaging with data received from HPLC measurements, fluorescence imaging was found to be an appropriate tool to measure the release of siRNA complexes. Finally, the bioactivity of the siRNA released from hydrogel was tested and compared to free DL for its ability to knockdown the GFP expression in a DLD1 colon cancer cell model. The results indicate controlled release properties and activity of the released siRNA. In conclusion, the developed formulation is a promising system to provide local controlled release of siRNA over several weeks. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations (Volume II))
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Review

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36 pages, 2742 KiB  
Review
Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications
by Napoleon-Nikolaos Vrettos, Clive J. Roberts and Zheying Zhu
Pharmaceutics 2021, 13(10), 1591; https://doi.org/10.3390/pharmaceutics13101591 - 30 Sep 2021
Cited by 52 | Viewed by 7389
Abstract
There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage [...] Read more.
There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage form in the upper gastrointestinal tract (GIT) that can be sufficient to ensure complete solubilisation of the drugs in the stomach fluids, followed by subsequent absorption in the stomach or proximal small intestine. This can be beneficial for drugs that have an “absorption window” or are absorbed to a different extent in various segments of the GIT. Therefore, gastroretentive technologies in tandem with controlled-release strategies could enhance both the therapeutic efficacy of many drugs and improve patient compliance through a reduction in dosing frequency. The paper reviews different gastroretentive drug delivery technologies and controlled-release strategies that can be combined and summarises examples of formulations currently in clinical development and commercially available gastroretentive controlled-release products. The different parameters that need to be considered and monitored during formulation development for these pharmaceutical applications are highlighted. Full article
(This article belongs to the Special Issue Controlled Delivery Formulations (Volume II))
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