title: Biodegradable salicylate-based poly(anhydride-ester) microspheres for controlled insulin delivery.
abstract: Salicylate-based poly(anhydride-esters) (PAEs) chemically incorporate salicylic acid (SA) into the polymer backbone, which is then delivered in a controlled manner upon polymer hydrolysis. In this work, a salicylate-based PAE is a carrier to encapsulate and deliver insulin. Polymer microspheres were formulated using a water/oil/water double-emulsion solvent evaporation technique. The microspheres obtained had a smooth surface, high protein encapsulation efficiency, and relatively low emulsifier content. Insulin was released in vitro for 15 days, with no signs of aggregation or unfolding of the secondary structure. The released insulin also retained bioactivity in vitro. Concurrently, SA was released from the microspheres with polymer degradation and anti-inflammatory activity was observed. Based upon these results, the formulated microspheres enable simultaneous delivery of insulin and SA, both retaining bioactivity following processing.
authors.affiliation: Department of Chemistry and Chemical Biology, Rutgers University, Piscataway, New Jersey, 08854.
authors.forename: Roberto
authors.initials: R
authors.lastname: Delgado-Rivera
authors.forename: Roselin
authors.initials: R
authors.lastname: Rosario-Meléndez
authors.forename: Weiling
authors.initials: W
authors.lastname: Yu
authors.forename: Kathryn E
authors.initials: KE
authors.lastname: Uhrich
mesh_terms: D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry*; D002460:Cell Line; D003692:Delayed-Action Preparations; D004952:Esters / Q000737:chemistry*; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000494:pharmacology; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D063347:Native Polyacrylamide Gel Electrophoresis; D010766:Phosphorylation / Q000187:drug effects; D049388:Polyanhydrides / Q000737:chemistry*; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D051381:Rats; D012459:Salicylates / Q000737:chemistry*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D004952:Esters; D007328:Insulin; D049388:Polyanhydrides; D012459:Salicylates; D014409:Tumor Necrosis Factor-alpha; D051057:Proto-Oncogene Proteins c-akt
keywords: controlled release; insulin; microspheres; poly(anhydride-esters); salicylic acid
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