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Pharmaceutics
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New Technology for Prolonged Drug Release, 2nd Edition
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New Technology for Prolonged Drug Release, 2nd Edition

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 (20 October 2024) | Viewed by 14361

Special Issue Editors

Dr. Marta Szekalska

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Guest Editor
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15222 Białystok, Poland
Interests: spray drying; alginates; natural polymers; microparticles; drug dosage formulations
Special Issues, Collections and Topics in MDPI journals
Dr. Katarzyna Sosnowska

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15222 Białystok, Poland
Interests: modification of delivery systems; semisolid forms; pharmaceutical analysis; drug dosage formulations
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Prolonged drug delivery systems have become the standard in drug formulation development. The most important benefits of such dosage forms include a longer duration of action, decreasing frequency of drug administration to improve patient compliance, and lower plasma concentration, which may reduce the risk of adverse effects and decrease fluctuation in plasma concentration. All these advantages promote the achievement of higher therapeutic efficacy. Innovative technologies are applicable for the increased performance of both existing and new pharmaceutical active compounds. A sustained release profile of drug substances is obtained using various technologies. One of these is the process of applying natural and synthetic polymers, which play an important role in the preparation of gelling matrixes or coating dosage forms. Another technique used to obtain a prolonged delivery system involves microencapsulation, formulating micro- or nanoparticulate systems.

This Special Issue will be a collection of full article papers and review papers focusing on recent progress in new drug delivery technologies, allowing for a sustained release profile of active substances.

Dr. Marta Szekalska
Dr. Katarzyna Sosnowska
Guest Editors

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

  • prolonged drug delivery
  • sustained release
  • formulation and dosage form development
  • polymers for extended release
  • micro/nanoparticulate system
  • modification of active substances

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Published Papers (7 papers)

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Research

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20 pages, 3601 KiB  
Article
Formulation, Characterisation, and Biocompatibility Assessment of Rifampicin-Loaded Poly(d,l-lactide-co-glycolide) Composites for Local Treatment of Orthopaedic and Wound Infections
by Mitali Singhal, Colin C. Seaton, Alexander Surtees and Maria G. Katsikogianni
Pharmaceutics 2024, 16(11), 1467; https://doi.org/10.3390/pharmaceutics16111467 - 18 Nov 2024
Cited by 1 | Viewed by 1934
Abstract
Background/Objectives: The escalating challenge of antimicrobial resistance (AMR) necessitates the development of targeted antibiotic delivery platforms, minimising systemic administration. Polymer-based drug delivery emerges as a promising solution, ensuring sustained release and prolonged efficacy of bioactive compounds, ensuring long-term efficacy. Methods: This study focuses [...] Read more.
Background/Objectives: The escalating challenge of antimicrobial resistance (AMR) necessitates the development of targeted antibiotic delivery platforms, minimising systemic administration. Polymer-based drug delivery emerges as a promising solution, ensuring sustained release and prolonged efficacy of bioactive compounds, ensuring long-term efficacy. Methods: This study focuses on encapsulating rifampicin (RIF), a key antibiotic for orthopaedic and wound-related infections, within Poly(d,l-lactide-co-glycolide) (PLGA), a biodegradable polymer, through solvent casting, to formulate a PLGA-RIF composite membrane. Comprehensive characterisation, employing Fourier-transformed infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), thermal analysis and X-ray Diffraction (XRD), confirmed the integrity of both the starting and produced materials. UV-Vis spectroscopy revealed a controlled drug release profile over 21 days in various media, with the chosen media influencing the drug release, notably the tryptic soya broth (TSB) caused the highest release. The quantitative assessment of the antimicrobial efficacy of the developed PLGA-RIF composite was conducted by measuring the size of the inhibition zones against both Gram-negative and Gram-positive bacteria. Results: The results confirmed the composite’s potential as a robust antibacterial biomaterial, demonstrating a rapid and effective antibacterial response. Cytocompatibility tests incorporated human fibroblast and osteoblast-like cell lines and demonstrated that the RIF:PLGA (1:8) formulation maintained eukaryotic cell viability, indicating the composite’s potential for targeted medical applications in combating bacterial infections with minimal systemic impact. Conclusions: This study presents the significance of investigating drug release within appropriate and relevant physiological media. A key novelty of this work therefore lies in the exploration of drug release dynamics across different media, allowing for a comprehensive understanding of how varying physiological conditions may influence drug release and its effect on biological responses. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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11 pages, 798 KiB  
Article
Comparative Pharmacokinetics of Sustained-Release versus Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study
by Shefali Thanawala, R. Abiraamasundari and Rajat Shah
Pharmaceutics 2024, 16(10), 1248; https://doi.org/10.3390/pharmaceutics16101248 - 25 Sep 2024
Viewed by 3053
Abstract
Background: Exogenous melatonin, a nutraceutical for maintaining a healthy sleep–wake cycle and managing sleep disorders, requires large, repeated doses due to its low bioavailability and short half-life. This necessitates the development of a sustained-release formulation with a longer half-life and sustained plasma concentration. [...] Read more.
Background: Exogenous melatonin, a nutraceutical for maintaining a healthy sleep–wake cycle and managing sleep disorders, requires large, repeated doses due to its low bioavailability and short half-life. This necessitates the development of a sustained-release formulation with a longer half-life and sustained plasma concentration. Therefore, exogenous novel 5 mg sustained-release melatonin capsules (Melatonin-SR, test product) were formulated. Methods: This open-label cross-over study compared the pharmacokinetics (maximum concentration [Cmax], time to reach Cmax [Tmax], area under the curve [AUC], and elimination half-life [t1/2]) and the safety of Melatonin-SR with 5 mg immediate-release melatonin capsules (Melatonin-IR, reference product) after single-dose oral administration in healthy fasting adults. Results: Sixteen participants (aged 18–45 years) were randomized (1:1) to receive either Melatonin-SR or Melatonin-IR in two periods with a 7-day washout period. Melatonin-SR reported a lower Cmax (11,446.87 pg/mL) compared to Melatonin-IR (22,786.30 pg/mL). The mean Tmax of Melatonin-SR and Melatonin-IR was 1.26 h and 0.87 h, respectively. The mean t1/2 of Melatonin-SR (5.10 h) was prolonged by five-fold compared to Melatonin-IR (1.01 h). One adverse event (vomiting) was reported following the administration of the Melatonin-IR. Conclusions: Melatonin-SR resulted in higher and sustained plasma melatonin concentrations for an extended period and was well-tolerated. Hence, Melatonin-SR may be a promising nutraceutical for maintaining healthy sleep. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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15 pages, 4688 KiB  
Article
Development of Gastroretentive Floating Combination Tablets Containing Amoxicillin Trihydrate 500 mg and Levofloxacin 125 mg for Eradicating Resistant Helicobacter pylori
by Da Hun Kim, Sa-Won Lee, Jun Hak Lee, Jin Woo Park, Sung Mo Park, Han-Joo Maeng, Tae-Sung Koo and Kwan Hyung Cho
Pharmaceutics 2024, 16(10), 1242; https://doi.org/10.3390/pharmaceutics16101242 - 24 Sep 2024
Cited by 1 | Viewed by 1482
Abstract
Background/Objectives: The aim of this work was to prepare and characterize gastroretentive floating combination tablets (GRCTs) containing 500 mg of amoxicillin trihydrate (AMX) and 125 mg of levofloxacin (LVX) that provide sustained drug release and stability at gastric pH levels for the eradication [...] Read more.
Background/Objectives: The aim of this work was to prepare and characterize gastroretentive floating combination tablets (GRCTs) containing 500 mg of amoxicillin trihydrate (AMX) and 125 mg of levofloxacin (LVX) that provide sustained drug release and stability at gastric pH levels for the eradication of resistant Helicobacter pylori. Method: GRCTs were prepared with low-density excipients and hydrophilic swellable polymers, including hydroxypropyl methylcellulose (HPMC) of various viscosities, polyethylene oxide (PEO), and carboxymethylcellulose (CMC), by the direct compression method. The prepared GRCTs were investigated and optimized in terms of pH stability, tablet hardness, floating lag time and total floating time, drug release rate, gel strength. Results: AMX and LVX in GRCT were stable at the HP eradication target pH above 4.0. The effervescent GRCT composition (AMX/LVX/HPMC [4000 cP]/CMC/microcrystalline cellulose/citric acid/sodium bicarbonate/calcium silicate/silicon dioxide/magnesium stearate = 500/125/50/50/125/40/60/30/10/10, w/w) yielded acceptable hardness (>6 kp), reduced floating lag time (<5 s), a long floating duration (>12 h), and sustained release rates of AMX and LVX (>90% until 12 h). This optimized GRCT had a gel strength of 107.33 ± 10.69 g and pH > 4.0, which maintained the tablets’ shape and AMX stability for 12 h. Conclusions: Collectively, the formulated effervescent GRCTs combining AMX and LVX represented a promising candidate dosage form for eradicating resistant H. pylori. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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12 pages, 7272 KiB  
Article
Core-Shell Microspheres Prepared Using Coaxial Electrostatic Spray for Local Chemotherapy of Solid Tumors
by Xiaowei Zhang, Rundong Zhu, Xingzhi Wang, Hao Wang, Zushun Xu, Yongan Wang, Dongqin Quan and Liao Shen
Pharmaceutics 2024, 16(1), 45; https://doi.org/10.3390/pharmaceutics16010045 - 28 Dec 2023
Cited by 8 | Viewed by 1776
Abstract
Local chemotherapy is an alternative therapeutic strategy that involves direct delivery of drugs to the tumor site. This approach avoids adverse reactions caused by the systemic distribution of drugs and enhances the tumor-suppressing effect by concentrating the drugs at the tumor site. Drug-loaded [...] Read more.
Local chemotherapy is an alternative therapeutic strategy that involves direct delivery of drugs to the tumor site. This approach avoids adverse reactions caused by the systemic distribution of drugs and enhances the tumor-suppressing effect by concentrating the drugs at the tumor site. Drug-loaded microspheres are injectable sustained-release drug carriers that are highly suitable for local chemotherapy. However, a complex preparation process is one of the main technical difficulties limiting the development of microsphere formulations. In this study, core-shell structured microspheres loaded with paclitaxel (PTX; with a core-shell structure, calcium alginate outer layer, and a poly (lactic acid-co-glycolic acid) copolymer inner layer, denoted as PTX-CA/PLGA-MS) were prepared using coaxial electrostatic spray technology and evaluated in vitro and in vivo. PTX-CA/PLGA-MS exhibited a two-stage drug release profile and enhanced anti-tumor effect in animal tumor models. Importantly, the preparation method reported in this study is simple and reduces the amount of organic solvent(s) used substantially. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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30 pages, 7651 KiB  
Article
Mucoadhesive Alginate/Pectin Films Crosslinked by Calcium Carbonate as Carriers of a Model Antifungal Drug—Posaconazole
by Marta Szekalska, Anna Czajkowska-Kośnik, Bartosz Maciejewski, Iwona Misztalewska-Turkowicz, Agnieszka Zofia Wilczewska, Jurga Bernatoniene and Katarzyna Winnicka
Pharmaceutics 2023, 15(10), 2415; https://doi.org/10.3390/pharmaceutics15102415 - 3 Oct 2023
Cited by 8 | Viewed by 2341
Abstract
The mucosal membrane of the oral cavity, due to its unique structure and availability, constitutes an appropriate site for the delivery of drugs, both with local and systemic effects. Mucoadhesive buccal films are drug dosage forms that due to their convenience of application, [...] Read more.
The mucosal membrane of the oral cavity, due to its unique structure and availability, constitutes an appropriate site for the delivery of drugs, both with local and systemic effects. Mucoadhesive buccal films are drug dosage forms that due to their convenience of application, flexibility and size, are characterized by patients’ compliance. Sodium alginate and pectin are natural polymers from the polysaccharides group, with mucoadhesive properties, that are widely applied to obtain buccal films. However, their hydrophilic nature and poor water resistance limit their application in sustained drug release formulations. Hence, the aim of this investigation was to design alginate/pectin buccal films by a one-step crosslinking technique—with the application of calcium carbonate. This technique was applied to prepare crosslinked alginate and alginate/pectin mucoadhesive films with a model antifungal drug—posaconazole. The obtained formulations were evaluated for the impact of crosslinking and pectin’s presence on their pharmaceutical, mucoadhesive, mechanical and physicochemical properties. Additionally, the antifungal activity of the prepared films against Candida spp. was evaluated. It was shown that pectin’s presence in the formulations improved flexibility, mucoadhesion and antifungal activity. The crosslinking process reduced mucoadhesiveness and antifungal activity but significantly enhanced the mechanical properties and stability and enabled prolonged drug release. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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Review

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20 pages, 3414 KiB  
Review
Oral Bioavailability Enhancement of Anti-Cancer Drugs Through Lipid Polymer Hybrid Nanoparticles
by Saud Almawash
Pharmaceutics 2025, 17(3), 381; https://doi.org/10.3390/pharmaceutics17030381 - 17 Mar 2025
Viewed by 830
Abstract
Cancer is considered as the second leading cause of death worldwide. Chemotherapy, radiotherapy, immunotherapy, and targeted drug delivery are the main treatment options for treating cancers. Chemotherapy drugs are either available for oral or parenteral use. Oral chemotherapy, also known as chemotherapy at [...] Read more.
Cancer is considered as the second leading cause of death worldwide. Chemotherapy, radiotherapy, immunotherapy, and targeted drug delivery are the main treatment options for treating cancers. Chemotherapy drugs are either available for oral or parenteral use. Oral chemotherapy, also known as chemotherapy at home, is more likely to improve patient compliance and convenience. Oral anti-cancer drugs have bioavailability issues associated with lower aqueous solubility, first-pass metabolism, poor intestinal permeability and drug absorption, and degradation of the drug throughout its journey in the gastrointestinal tract. A highly developed carrier system known as lipid polymer hybrid nanoparticles (LPHNs) has been introduced. These nanocarriers enhance drug stability, solubility, and absorption, and reduce first-pass metabolism. Consequently, this will have a positive impact on oral bioavailability enhancement. This article provides an in-depth analysis of LPHNs as a novel drug delivery system for anti-cancer agents. It discusses an overview of the limited bioavailability of anti-cancer drugs, their reasons and consequences, LPHNs based anti-cancer drug delivery, conventional and modern preparation methods as well as their drug loading and entrapment efficiencies. In addition, this article also gives an insight into the mechanistic approach to oral bioavailability enhancement, potential applications in anti-cancer drug delivery, limitations, and future prospects of LPHNs in anti-cancer drug delivery. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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19 pages, 932 KiB  
Review
Polycystic Ovary Syndrome and the Potential for Nanomaterial-Based Drug Delivery in Therapy of This Disease
by Mingqin Shi, Xinyao Li, Liwei Xing, Zhenmin Li, Sitong Zhou, Zihui Wang, Xuelian Zou, Yuqing She, Rong Zhao and Dongdong Qin
Pharmaceutics 2024, 16(12), 1556; https://doi.org/10.3390/pharmaceutics16121556 - 4 Dec 2024
Viewed by 2004
Abstract
Polycystic ovary syndrome (PCOS) is the predominant endocrine disorder among women of reproductive age and represents the leading cause of anovulatory infertility, which imposes a considerable health and economic burden. Currently, medications used to treat PCOS can lead to certain adverse reactions, such [...] Read more.
Polycystic ovary syndrome (PCOS) is the predominant endocrine disorder among women of reproductive age and represents the leading cause of anovulatory infertility, which imposes a considerable health and economic burden. Currently, medications used to treat PCOS can lead to certain adverse reactions, such as affecting fertility and increasing the risk of venous thrombosis. Drug delivery systems utilizing nanomaterials, characterized by prolonged half-life, precision-targeted delivery, enhanced bioavailability, and reduced toxicity, are currently being employed in the management of PCOS. This innovative approach is gaining traction as a favored strategy for augmenting the therapeutic efficacy of medications. Consequently, this paper discusses the roles of nanoparticles, nanocarriers, and targeted ligands within nanomaterial-based drug delivery systems, aiming to identify optimal methodologies for treating PCOS using nanomaterials. Additionally, prospective research avenues concerning nanomaterial-based delivery systems in the context of PCOS, as well as the implications of existing insights on the advancement of novel therapies for PCOS, are highlighted. Full article
(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)
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