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Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics

Acta Pharmaceutica Sinica B 2022年第2期12卷 621-636页

作者： Carlos Bendicho-Lavilla iria seoane-viano Francisco J.OteroEspinar Asteria Luzardo-Alvarez Department of Pharmacology Pharmacy and Pharmaceutical TechnologyFaculty of PharmacyUniversity of Santiago de Compostela(USC)Santiago de Compostela 15782Spain Paraquasil Group Health Research Institute of Santiago de Compostela(IDIS)Santiago de Compostela 15706Spain Department of Pharmacology Pharmacy and Pharmaceutical TechnologySchool of SciencesCampus de LugoUniversity of Santiago de CompostelaLugo 27002Spain

Diabetes mellitus is a major health problem with increasing prevalence at a global *** discovery of insulin in the early 1900 s represented a major breakthrough in diabetes management,with further milestones being subsequently achieved with the identification of glucagon-like peptide-1(GLP-1)and the introduction of GLP-1 receptor agonists(GLP-1 RAs)in clinical ***,the subcutaneous delivery of biotherapeutics is a well-established route of administration generally preferred over the intravenous route due to better patient compliance and prolonged drug ***,current subcutaneous formulations of GLP-1 RAs present pharmacokinetic problems that lead to adverse reactions and treatment *** this review,we discuss the current challenges of subcutaneous administration of peptide-based therapeutics and provide an overview of the formulations available for the different routes of administration with improved bioavailability and reduced frequency of administration.

关键词： Type 2 diabetes mellitus Glucagon-like peptide-1 receptor agonists Exenatide Subcutaneous administration Amylin mimetics Drug delivery systems Biotherapeutics Peptide delivery Controlled-release formulations Microparticles Nanoparticles

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3D printed tacrolimus suppositories for the treatment of ulcerative colitis

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Asian Journal of Pharmaceutical Sciences 2021年第1期16卷 110-119页

作者： iria seoane-viano Jun Jie Ong Asteria Luzardo-Alvarez Miguel Gonzalez-Barcia Abdul W.Basit Francisco J.Otero-Espinar Alvaro Goyanes Department of Pharmacology Pharmacy and Pharmaceutical TechnologyFaculty of PharmacyUniversity of Santiago de CompostelaSantiago de Compostela 15782Spain Department of Pharmaceutics UCL School of PharmacyUniversity College LondonLondon WC1N 1AXUK Pharmacy Department University Clinical Hospital Santiago de Compostela(SERGAS)(CHUS)Santiago de Compostela 15706Spain FabRx Ltd. AshfordKent TN240RWUK Departamento de Farmacologia Farmacia y Tecnologia FarmaceuticaI+D Farma Group(GI-1645)Universidade de Santiago de CompostelaSantiago de Compostela 15782Spain

Ulcerative colitis is a global health problem,affecting millions of individuals *** an inflammatory condition localised in the large intestine,rectal delivery of immunosuppressive therapies such as tacrolimus is a promising strategy to maximise drug concentration at the site of action whilst minimising systemic side ***,for the first time,self-supporting 3D-printed tacrolimus suppositories were prepared without the aid of moulds using a pharmaceutical semi-solid extrusion(SSE)3D *** suppositories were printed vertically in three different sizes using combinations of two lipid pharmaceutical excipients(Gelucire 44/14 or Gelucire 48/16)and coconut *** both suppository formulations had the appropriate viscosity characteristics for printing,the Gel 44 formulation required less energy and force for extrusion compared to the Gel 48 *** Gel 44 disintegrated more rapidly but released tacrolimus more slowly than the Gel 48 *** the tacrolimus release profiles were significantly different,both suppository systems released more than 80% drug within 120 *** and XRD analysis was inconclusive in determining the solid-state properties of the drug in the *** summary,this article reports on the fabrication of 3D printed selfsupporting suppositories to deliver personalised doses of a narrow therapeutic index drug,with potential benefits for patients with ulcerative colitis.

关键词： 3D printed drug products Semi-solid extrusion 3D printing Inflammatory bowel disease Suppository drug delivery Pressure assisted syringe M3dimaker

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