Natural resin-based solvent exchange induced in-situ forming gel for vancomycin HCl delivery to periodontal pocket

Khaing, Ei Mon; Intaraphairot, Torsak; Chuenbarn, Tiraniti; Chantadee, Takron; Phaechamud, Thawatchai

doi:10.1016/j.matpr.2021.03.622

Cited by 9 publications

(8 citation statements)

References 48 publications

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“…The steeper drug release observed in the initial phase may be attributed to drug release through the gel state before a slower release through the more solid-like matrix in the later phase of the release profile. A similar release pattern has been reported for doxycycline hyclate and vancomycin HCl released from natural-resinbased ISGs [14,49]. The process of drug release should be irreversible delivery because the transformed Nc mass could not dissolve in the release medium.…”

Section: In Vitro Drug Release Studysupporting

confidence: 72%

Moxifloxacin HCl-Incorporated Aqueous-Induced Nitrocellulose-Based In Situ Gel for Periodontal Pocket Delivery

Senarat,

Rojviriya,

Sarunyakasitrin

et al. 2023

Gels

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A drug delivery system based on an aqueous-induced in situ forming gel (ISG) consists of solubilizing the drug within an organic solution of a polymer using a biocompatible organic solvent. Upon contact with an aqueous medium, the solvent diffuses out and the polymer, designed to be insoluble in water, solidifies and transforms into gel. Nitrocellulose (Nc), an aqueous insoluble nitrated ester of cellulose, should be a promising polymer for an ISG using water induction of its solution to gel state via phase inversion. The aim of this investigation was to develop and evaluate a moxifloxacin HCl (Mx)-incorporated aqueous-induced Nc-based ISG for periodontitis treatment. The effects of different solvents (N-methyl pyrrolidone (NMP), DMSO, 2-pyrrolidone (Py), and glycerol formal (Gf)) on the physicochemical and bioactivity properties of the ISGs were investigated. The viscosity and injection force of the ISGs varied depending on the solvent used, with Gf resulting in higher values of 4631.41 ± 52.81 cPs and 4.34 ± 0.42 N, respectively. All ISGs exhibited Newtonian flow and transformed into a gel state upon exposure to the aqueous phase. The Nc formulations in DMSO showed lower water tolerance (12.50 ± 0.72%). The developed ISGs were easily injectable and demonstrated water sensitivity of less than 15.44 ± 0.89%, forming a gel upon contact with aqueous phase. The transformed Nc gel effectively prolonged Mx release over two weeks via Fickian diffusion, with reduced initial burst release. Different solvent types influenced the sponge-like 3D structure of the dried Nc ISGs and affected mass loss during drug release. Incorporating Nc reduced both solvent and drug diffusion, resulting in a significantly narrower zone of bacterial growth inhibition (p < 0.05). The Mx-incorporated Nc-based ISGs exhibited efficient antibacterial activity against four strains of Staphylococcus aureu and against periodontitis pathogens including Aggregatibacter actinomycetemcomitans and Porphyromonas gingivalis. This study suggests that the developed Mx-incorporated Nc-based ISGs using DMSO and NMP as the solvents are the most promising formulations. They exhibited a low viscosity, ease of injection, and rapid transformation into a gel upon aqueous induction, and they enabled localized and prolonged drug release with effective antibacterial properties. Additionally, this study represents the first reported instance of utilizing Nc as the polymer for ISG. Further clinical experiments are necessary to evaluate the safety of this ISG formulation.

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Section: In Vitro Drug Release Studysupporting

confidence: 72%

Moxifloxacin HCl-Incorporated Aqueous-Induced Nitrocellulose-Based In Situ Gel for Periodontal Pocket Delivery

Senarat,

Rojviriya,

Sarunyakasitrin

et al. 2023

Gels

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“…The small pore formation could be observed at the surface of the CO-added formulations at 60 min. The phase inversion of the rosin ISG promoted the formation of a gel outer layer at the initial stage, and the polymer interior slowly transformed into the stable matrix over time [ 44 ]. The inclusion of CO 2.5% to 10% (IM-RC2.5-IMRC10) delayed the formation of an opaque gel surface.…”

Section: Resultsmentioning

confidence: 99%

“…Rosin also has film-forming properties as well as anticancer and antimicrobial activities [ 37 , 38 , 39 , 40 ]. It has been used as a matrix-forming agent in various drug delivery systems, such as microparticles, and nanoparticles for controlled drug delivery [ 41 , 42 , 43 , 44 ]. The rosin-based ISG system with adding lime peel oil could modulate rosin gel formation, drug release and inhibition zone of antimicrobial activities [ 45 ].…”

Section: Introductionmentioning

confidence: 99%

Imatinib Mesylate-Loaded Rosin/Cinnamon Oil-Based In Situ Forming Gel against Colorectal Cancer Cells

Khaing

Intaraphairot

Mahadlek

et al. 2022

Gels

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Localized delivery systems have been typically designed to enhance drug concentration at a target site and minimize systemic drug toxicity. A rosin/cinnamon oil (CO) in situ forming gel (ISG) was developed for the sustainable delivery of imatinib mesylate (IM) against colorectal cancer cells. CO has been claimed to express a potent anticancer effect against various cancer cells, as well as a synergistic effect with IM on colorectal cancer cells; however, poor aqueous solubility limits its application. The effect of rosin with the adding CO was assessed on physicochemical properties and in vitro drug release from developed IM-loaded rosin/CO-based ISG. Moreover, in vitro cytotoxicity tests were conducted against two colorectal cancer cells. All formulations exhibited Newtonian flow behavior with viscosity less than 266.9 cP with easier injectability. The adding of CO decreased the hardness and increased the adhesive force of the obtained rosin gel. The gel formation increased over time under microscopic observation. CO-added ISG had a particle-like gel appearance, and it promoted a higher release of IM over a period of 28 days. All tested ISG formulations revealed cytotoxicity against HCT-116 and HT-29 cell lines at different incubation times. Thus, CO-loaded rosin-based ISG can act as a potentially sustainable IM delivery system for chemotherapy against colorectal cancer cells.

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“…The aqueous insoluble property of rosin makes it suitable for preparing a solvent exchange-induced in situ forming gel. It was previously reported that rosin in some organic solvents could transform from a solution into insoluble matter in an aqueous environment [ 17 ]. However, no additives were applied to the rosin-based in situ forming gel, and the effect of additives on the formulation qualities has not yet been determined.…”

Section: Introductionmentioning

confidence: 99%

Lime Peel Oil–Incorporated Rosin-Based Antimicrobial In Situ Forming Gel

Khaing

Mahadlek

Okonogi

et al. 2022

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Localized intra-periodontal pocket drug delivery using an injectable in situ forming gel is an effective periodontitis treatment. The aqueous insoluble property of rosin is suitable for preparing a solvent exchange-induced in situ forming gel. This study aims to investigate the role of incorporating lime peel oil (LO) on the physicochemical properties of injectable in situ forming gels based on rosin loaded with 5% w/w doxycycline hyclate (DH) in dimethyl sulfoxide (DMSO) and N-methyl pyrrolidone (NMP). Their gel formation, viscosity, injectability, mechanical properties, wettability, drug release, and antimicrobial activities were evaluated. The presence of LO slowed gel formation due to the loose precipitate formation of gel with a high LO content. The viscosity and injectability were slightly increased with higher LO content for the DH-loaded rosin-based in situ forming gel. The addition of 10% LO lowered gel hardness with higher adhesion. LO incorporation promoted a higher drug release pattern than the no oil-added formulation over 10 days and the gel formation rate related to burst drug release. The drug release kinetics followed the non-Fickian diffusion mechanism for oil-added formulations. LO exhibited high antimicrobial activity against Porphyromonas gingivalis and Staphylococcus aureus. The DH-loaded rosin in situ forming gel with an addition of LO (0, 2.5, 5, and 10% w/w) inhibited all tested microorganisms. Adding 10% LO to rosin-based in situ forming gel improved the antimicrobial activities, especially for the P. gingivalis and S. aureus. As a result, the study demonstrates the possibility of using an LO amount of less than 10% loading into a rosin-based in situ forming gel for efficient periodontitis treatment.

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Natural resin-based solvent exchange induced in-situ forming gel for vancomycin HCl delivery to periodontal pocket

Cited by 9 publications

References 48 publications

Moxifloxacin HCl-Incorporated Aqueous-Induced Nitrocellulose-Based In Situ Gel for Periodontal Pocket Delivery

Moxifloxacin HCl-Incorporated Aqueous-Induced Nitrocellulose-Based In Situ Gel for Periodontal Pocket Delivery

Imatinib Mesylate-Loaded Rosin/Cinnamon Oil-Based In Situ Forming Gel against Colorectal Cancer Cells

Lime Peel Oil–Incorporated Rosin-Based Antimicrobial In Situ Forming Gel

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