In Situ Gel for Sustained 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 2023) | Viewed by 3343

Special Issue Editors


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Guest Editor
Programme of Pharmaceutical Engineering, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
Interests: in situ forming gels; applications of materials in pharmaceutical technology; phase inversion in situ gel; drug delivery systems; mechanistic of in situ gel formation

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Guest Editor
Department of Pharmaceutical Sciences, Chiang Mai University, Chiang Mai 50200, Thailand
Interests: solvent exchange-induced in situ gel; mechanistic of in situ gel formation; in situ forming matrices; dynamic modelling; applications of materials in pharmaceutical technology; controlled drug delivery systems

Special Issue Information

Dear Colleagues,

In situ gel systems have grown in importance as an appealing sustained drug delivery systems owing to their less complicated fabrication with an interesting approach based on the presence of gelling agents to modulate/localize the release of drug or biomedical compounds and provide the efficient bioactivities. These drug delivery systems improve patient compliance and comfort due to their special characteristic feature of ‘Sol to Gel’ transition. In situ gelling systems are the formulations in solution form before entering into the body, but they allow for the change to gel form under various physiological conditions. The sol to gel transition depends on various stimuli including temperature, change in pH, solvent exchange, UV radiation, and the presence of specific molecules or ions. Various natural/synthetic resins and polymers and other materials act as the crucial ingredient in situ gel forming systems. In situ gel systems can potentially be applied or administrated for oral, ocular, transdermal, buccal, intra-peritoneal, parenteral, injectable, rectal and vaginal routes.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following fields:

  • Synthesis, blend, composite, and interpenetrating polymer network modifications of material for in situ gel systems.
  • Physicochemical and bioactivities characteristics of in situ gel.
  • Mechanistic of in situ gel formation and new experiment for characterization of in situ gel.
  • Kinetic or mechanism of drug or active compound release from in situ forming gel.
  • Applications of in situ gel for oral, ocular, transdermal, buccal, intra-peritoneal, parenteral, injectable, rectal and vaginal routes and related areas such as biomedical use.
  • Stability, safety, clinical studies and efficacy of in situ gel.

Dr. Thawatchai Phaechamud
Dr. Takron Chantadee
Guest Editors

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Keywords

  • in situ gel
  • in situ depot
  • in situ implant
  • in situ forming matrices
  • pH responsive hydrogels
  • thermosensitive gel
  • self-forming polymeric depot
  • ion-induced gelation
  • sustained biomedical active compound delivery
  • controlled drug release
  • phase inversion in situ gel
  • mechanistic of in situ gel formation

Published Papers (2 papers)

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Research

24 pages, 3937 KiB  
Article
Development of an Antiviral Ion-Activated In Situ Gel Containing 18β-Glycyrrhetinic Acid: A Promising Alternative against Respiratory Syncytial Virus
by Burcu Özkan, Ebru Altuntaş, Ümmühan Ünlü, Hasan Hüseyin Doğan, Yıldız Özsoy and Rabia Çakır Koç
Pharmaceutics 2023, 15(8), 2055; https://doi.org/10.3390/pharmaceutics15082055 - 31 Jul 2023
Cited by 1 | Viewed by 1217
Abstract
The human respiratory syncytial virus (hRSV) is a major cause of serious lower respiratory infections and poses a considerable risk to public health globally. Only a few treatments are currently used to treat RSV infections, and there is no RSV vaccination. Therefore, the [...] Read more.
The human respiratory syncytial virus (hRSV) is a major cause of serious lower respiratory infections and poses a considerable risk to public health globally. Only a few treatments are currently used to treat RSV infections, and there is no RSV vaccination. Therefore, the need for clinically applicable, affordable, and safe RSV prevention and treatment solutions is urgent. In this study, an ion-activated in situ gelling formulation containing the broad-spectrum antiviral 18β-glycyrrhetinic acid (GA) was developed for its antiviral effect on RSV. In this context, pH, mechanical characteristics, ex vivo mucoadhesive strength, in vitro drug release pattern, sprayability, drug content, and stability were all examined. Rheological characteristics were also tested using in vitro gelation capacity and rheological synergism tests. Finally, the cytotoxic and antiviral activities of the optimized in situ gelling formulation on RSV cultured in the human laryngeal epidermoid carcinoma (HEp-2) cell line were evaluated. In conclusion, the optimized formulation prepared with a combination of 0.5% w/w gellan gum and 0.5% w/w sodium carboxymethylcellulose demonstrated good gelation capacity and sprayability (weight deviation between the first day of the experiment (T0) and the last day of the experiment (T14) was 0.34%), desired rheological synergism (mucoadhesive force (Fb): 9.53 Pa), mechanical characteristics (adhesiveness: 0.300 ± 0.05 mJ), ex vivo bioadhesion force (19.67 ± 1.90 g), drug content uniformity (RSD%: 0.494), and sustained drug release over a period of 6 h (24.56% ± 0.49). The optimized formulation demonstrated strong anti-hRSV activity (simultaneous half maximal effective concentration (EC50) = 0.05 µg/mL; selectivity index (SI) = 306; pre-infection EC50 = 0.154 µg/mL; SI = 100), which was significantly higher than that of ribavirin (EC50 = 4.189 µg/mL; SI = 28) used as a positive control against hRSV, according to the results of the antiviral activity test. In conclusion, this study showed that nasal in situ gelling spray can prevent viral infection and replication by directly inhibiting viral entry or modulating viral replication. Full article
(This article belongs to the Special Issue In Situ Gel for Sustained Drug Delivery)
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20 pages, 3253 KiB  
Article
Levofloxacin HCl-Incorporated Zein-Based Solvent Removal Phase Inversion In Situ Forming Gel for Periodontitis Treatment
by Setthapong Senarat, Catleya Rojviriya, Napaphol Puyathorn, Nutdanai Lertsuphotvanit and Thawatchai Phaechamud
Pharmaceutics 2023, 15(4), 1199; https://doi.org/10.3390/pharmaceutics15041199 - 10 Apr 2023
Cited by 4 | Viewed by 1715
Abstract
Zein is composed of nonpolar amino acids and is a water-insoluble protein used as the matrix-forming agent of localized in situ forming gel (ISG). Therefore, this study prepared solvent removal phase inversion zein-based ISG formulations to load levofloxacin HCl (Lv) for periodontitis treatment [...] Read more.
Zein is composed of nonpolar amino acids and is a water-insoluble protein used as the matrix-forming agent of localized in situ forming gel (ISG). Therefore, this study prepared solvent removal phase inversion zein-based ISG formulations to load levofloxacin HCl (Lv) for periodontitis treatment using dimethyl sulfoxide (DMSO) and glycerol formal (GF) as the solvents. Their physicochemical properties were determined, including viscosity, injectability, gel formation, and drug release. The topography of dried remnants after drug release was revealed using a scanning electron microscope and X-ray computed microtomography (μCT) to investigate their 3D structure and % porosity. The antimicrobial activities were tested against Staphylococcus aureus (ATCC 6538), Escherichia coli ATCC 8739, Candida albicans ATCC 10231, and Porphyromonas gingivalis ATCC 33277 with agar cup diffusion. Increasing zein concentration or using GF as the solvent notably enhanced the apparent viscosity and injection force of the zein ISG. However, its gel formation slowed due to the dense zein matrix barrier’s solvent exchange: the higher loaded zein or utilization of GF as an ISG solvent prolonged Lv release. The SEM and μCT images revealed the scaffold of dried ISG in that their % porosity corresponded with their phase transformation and drug release behavior. In addition, the sustainability of drug diffusion promoted a smaller antimicrobial inhibition clear zone. Drug release from all formulations was attained with minimum inhibitory concentrations against pathogen microbes and exhibited a controlled release over 7 days. Lv-loaded 20% zein ISG using GF as a solvent exhibited appropriate viscosity, Newtonian flow, acceptable gel formation and injectability, and prolonged Lv release over 7 days with efficient antimicrobial activities against various test microbes; thus, it is the potential ISG formulation for periodontitis treatment. Consequently, the Lv-loaded solvent removal zein-based ISGs proposed in this investigation offer promising potential as an efficacious drug delivery system for periodontitis treatment by local injection. Full article
(This article belongs to the Special Issue In Situ Gel for Sustained Drug Delivery)
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