Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment

Phaechamud, Thawatchai; Jantadee, Takron; Mahadlek, Jongjan; Charoensuksai, Purin; Pichayakorn, Wiwat

doi:10.1208/s12249-016-0534-y

Cited by 22 publications

(14 citation statements)

References 61 publications

(70 reference statements)

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“…The addition of clove oil, clotrimazole, and more borneol increased the viscosity of the systems because the decrease in solvent content led to an increased solutes concentration and environmental viscosity. Nonetheless, all of them exhibited a prominently low viscosity (<8 cPs) compared with typical polymer-based ISG because of the low density, small size, and unsophisticated structure of borneol loaded in NMP [35][36][37][38]. These obtained viscosity data also corresponded with the previous report that the viscosity of vancomycin HCl-loaded borneol-based ISG using DMSO as a solvent for periodontal pocket delivery was noticeably lower than 20 cPs [23].…”

Section: Viscosity and Rheological Behaviorsupporting

confidence: 86%

Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy

Lertsuphotvanit

Tuntarawongsa

Jitrangsri

et al. 2023

Gels

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Oral candidiasis encompasses fungal infections of the tongue and other oral mucosal sites with fungal overgrowth and its invasion of superficial oral tissues. Borneol was assessed in this research as the matrix-forming agent of clotrimazole-loaded in situ forming gel (ISG) comprising clove oil as the co-active agent and N-methyl pyrrolidone (NMP) as a solvent. Their physicochemical properties, including pH, density, viscosity, surface tension, contact angle, water tolerance, gel formation, and drug release/permeation, were determined. Their antimicrobial activities were tested using agar cup diffusion. The pH values of clotrimazole-loaded borneol-based ISGs were in the range of 5.59–6.61, which are close to the pH of 6.8 of saliva. Increasing the borneol content in the formulation slightly decreased the density, surface tension, water tolerance, and spray angle but increased the viscosity and gel formation. The borneol matrix formation from NMP removal promoted a significantly (p < 0.05) higher contact angle of the borneol-loaded ISGs on agarose gel and porcine buccal mucosa than those of all borneol-free solutions. Clotrimazole-loaded ISG containing 40% borneol demonstrated appropriate physicochemical properties and rapid gel formation at microscopic and macroscopic levels. In addition, it prolonged drug release with a maximum flux of 370 µg·cm−2 at 2 days. The borneol matrix generated from this ISG obsentively controlled the drug penetration through the porcine buccal membrane. Most clotrimazole amounts still remained in formulation at the donor part and then the buccal membrane and receiving medium, repectively. Therefore, the borneol matrix extended the drug release and penetration through the buccal membrane efficiently. Some accumulated clotrimazole in tissue should exhibit its potential antifugal activity against microbes invading the host tissue. The other predominant drug release into the saliva of the oral cavity should influence the pathogen of oropharyngeal candidiasis. Clotrimazole-loaded ISG demonstrated efficacious inhibition of growth against S. aureus, E. coli, C. albicans, C. krusei, C. Lusitaniae, and C. tropicalis. Consequently, the clotrimazole-loaded ISG exhibited great potential as a drug delivery system for oropharyngeal candidiasis treatment by localized spraying.

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Section: Viscosity and Rheological Behaviorsupporting

confidence: 86%

Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy

Lertsuphotvanit

Tuntarawongsa

Jitrangsri

et al. 2023

Gels

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“…Nevertheless, all the rosin ISGs minimized the burst-IM release effect, and a more sustainable drug release could be attained up to 28 days. Typically, the drug release from the ISG system containing low concentrated polymer is faster than that of a high concentration [ 28 , 65 ]. Increasing the polymer concentration decreases the drug diffusion in the release medium during the solidification process by increasing the mass of the matrix as a barrier to drug diffusion [ 26 ].…”

Section: Resultsmentioning

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 injectability was determined using a texture analyser in compression mode (TA.XT plus, Stable Micro Systems, UK) to gauge the ease of administering the prepared ISG via injection by needle, as previously described by 23 . The resin ISG was inserted into a 1 ml syringe with a 27-gauge needle that was clamped to a stainless stand.…”

Section: Injectability Testmentioning

confidence: 99%

Natural-resin in-situ-forming gels: Physicochemical characteristics and bioactivities

Khaing¹,

Intaraphairot²,

Santimaleeworagu³

et al. 2021

Pharm Sci Asia

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An injectable in situ-forming gel (ISG) is a promising approach as a drug delivery system. In this study, natural resins including aloe, benzoin and propolis dissolved in N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO) were investigated as ISG systems for their ability to form matrices in phosphate buffer. Regarding their functions as ISG, their pH values, viscosities, flow behaviours, surface tensions and injectabilities were tested. Benzoin and propolis exhibited greater matrix formation than aloe, owing to their higher resin contents. Benzoin and propolis in DMSO formed matrices with a faster solvent exchange rate compared with those in NMP. The former had a higher viscosity than the latter, but both of them exhibited similar densities and surface tensions. The 35% and 40% w/w benzoin in DMSO exhibited dominant matrix formations with acceptable injectability via syringe. The 35% w/w benzoin and propolis ISG in DMSO efficiently inhibited the growth of Staphylococcus aureus strains, and the propolis ISG also exhibited a clear inhibition zone against Porphyromonas gingivalis, whereas aloe did not. From the cell viability assay, propolis exhibited a higher toxicity against HCT116 colon cancer cells (IC50=95 µg/ml) compared with benzoin (IC50=400 µg/ml), whereas the resin from aloe showed no toxic effect on this cell. Due to their rapid insoluble matrix formation after contacting aqueous fluid as well as their antibacterial and cytotoxic activities against colon cancer cell, the 35% w/w benzoin and propolis in DMSO have the potential for use as a matrix former for ISGs.

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Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment

Cited by 22 publications

References 61 publications

Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy

Clotrimazole-Loaded Borneol-Based In Situ Forming Gel as Oral Sprays for Oropharyngeal Candidiasis Therapy

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

Natural-resin in-situ-forming gels: Physicochemical characteristics and bioactivities

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