Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment.
Eudragit RS (ERS), a quaternary polyacrylate positively charged polymer, exhibits a very low permeability and swells in aqueous media independently of pH without dissolving. Owing to its high solubility in N-methyl pyrrolidone (NMP), it was interesting to apply as polymer matrix for solvent-exchanged in situ forming gel. The aim of this research was to prepare in situ forming gels from ERS to deliver the antimicrobial agents (doxycycline hyclate, metronidazole, and benzoyl peroxide) for periodontitis treatment. They were evaluated for viscosity and rheology, gel formation, syringeability, drug release, and antimicrobial activities. The solvent exchange between NMP and an external aqueous simulated gingival crevicular fluid stimulated the dissolved ERS transforming into the opaque rigid gel. Antimicrobial agent loaded ERS systems exhibited Newtonian flow with acceptable syringeability. The higher-loaded ERS promoted the more prolongation of drug release because of the retardation of water diffusion into the precipitated matrix. Antimicrobial activities against Staphylococcus aureus, Escherichia coli, Candida albicans, Streptococcus mutans, and Porphyromonas gingivalis depended on type of drugs and test microorganisms. Doxycycline hyclate loaded ERS systems showed these activities greater than the others; however, all of them could inhibit all test microorganisms. Thus, the solvent exchange-induced in situ forming gels comprising ERS-antimicrobial drugs exhibited potential use as localized delivery systems for periodontitis treatment.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand. thawatchaienator@gmail.com.
Thawatchai
T
Phaechamud
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand.
Takron
T
Jantadee
Pharmaceutical Intelligence Unit Prachote Plengwittaya, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand.
Jongjan
J
Mahadlek
Department of Biopharmacy, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand.
Purin
P
Charoensuksai
Faculty of Pharmaceutical Sciences and Medical Products Innovations from Polymers in Clinical Use Research Unit, Prince of Songkla University, Songkhla, 90112, Thailand.
Wiwat
W
Pichayakorn
D000180:Acrylic Resins / Q000737:chemistry*; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D004058:Diffusion; D065546:Drug Liberation / Q000235:genetics; D005782:Gels / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests / Q000379:methods; D010518:Periodontitis / Q000188:drug therapy* / Q000382:microbiology; D011108:Polymers / Q000737:chemistry; D011760:Pyrrolidinones / Q000737:chemistry; D012212:Rheology; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D014783:Viscosity; D014867:Water / Q000494:pharmacology
D000180:Acrylic Resins; D000890:Anti-Infective Agents; D005782:Gels; D011108:Polymers; D011760:Pyrrolidinones; D012997:Solvents; D014867:Water; C050528:Eudragit RS; C038678:N-methylpyrrolidone
Eudragit RS; antimicrobial; in situ forming gel; periodontitis treatment; solvent exchange