title: Doxycycline hyclate-loaded bleached shellac in situ forming microparticle for intraperiodontal pocket local delivery.
abstract: Bleached shellac (BS) is a water-insoluble polyester resin made up of sesquiterpenoid acids esterified with hydroxy aliphatic acids. In this study, BS dissolved in N-methyl pyrrolidone (NMP), dimethyl sulfoxide (DMSO) and 2-pyrrolidone was used as the internal phase of oil in oil emulsion using olive oil emulsified with glyceryl monostearate (GMS) as the external phase of in situ forming microparticles (ISM). Doxycycline hyclate (DH)-loaded BS ISMs were tested for emulsion stability, viscosity, rheology, transformation into microparticles, syringeability, drug release, surface topography, in vitro degradation and antimicrobial activities against Staphylococcus aureus, Streptococcus mutans and Porphyromonas gingivalis. All emulsions exhibited pseudoplastic flow and notably low syringeability force. Slower transformation from emulsion into microparticles of ISM prepared with 2-pyrrolidone was owing to slower solvent exchange of this solvent which promoted less porous structure of obtained BS matrix microparticles. The system containing 2-pyrrolidone exhibited a higher degradability than that prepared with DMSO. Developed DH-loaded BS ISMs exhibited a sustainable drug release for 47days with Fickian diffusion and effectively inhibited P. gingivalis, S. mutans and S. aureus. Therefore a DH-loaded BS ISM using olive oil containing GMS as the external phase and 2-pyrrolidone as a solvent was a suitable formulation for periodontitis treatment.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand. Electronic address: thawatchaienator@gmail.com.
authors.forename: Thawatchai
authors.initials: T
authors.lastname: Phaechamud
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand. Electronic address: chanyaboonsub_n@silpakorn.edu.
authors.forename: Nuttapong
authors.initials: N
authors.lastname: Chanyaboonsub
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand. Electronic address: inaeokark@gmail.com.
authors.forename: Orn
authors.initials: O
authors.lastname: Setthajindalert
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D004318:Doxycycline / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004355:Drug Stability; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry; D000069463:Olive Oil / Q000737:chemistry; D010316:Particle Size; D010514:Periodontal Pocket / Q000188:drug therapy / Q000378:metabolism; D016966:Porphyromonas gingivalis / Q000187:drug effects / Q000254:growth & development; D011760:Pyrrolidinones / Q000737:chemistry; D012116:Resins, Plant / Q000737:chemistry*; D012212:Rheology; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D013295:Streptococcus mutans / Q000187:drug effects / Q000254:growth & development; D013499:Surface Properties; D014783:Viscosity
chemical_list: D000900:Anti-Bacterial Agents; D004655:Emulsions; D005989:Glycerides; D000069463:Olive Oil; D011760:Pyrrolidinones; D012116:Resins, Plant; C048159:glyceryl monostearate; C003934:shellac; C038678:N-methylpyrrolidone; C028537:2-pyrrolidone; D004318:Doxycycline; D004121:Dimethyl Sulfoxide
keywords: Bleached shellac; Doxycycline hyclate; In situ forming microparticle; Intraperiodontal pocket; Local delivery