Synthesis, spectroscopic, thermal properties, in vitro release, and stability studies of ibuprofen-loaded microspheres c
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Synthesis, spectroscopic, thermal properties, in vitro release, and stability studies of ibuprofen‑loaded microspheres cross‑linked with hexachlorocyclotriphosphazene/ octachlorocyclotetraphosphazene Gülsel Yurtdaş‑Kırımlıoğlu, et al. [full author details at the end of the article] Received: 16 June 2020 / Revised: 27 August 2020 / Accepted: 13 October 2020 © Springer-Verlag GmbH Germany, part of Springer Nature 2020
Abstract Ibuprofen (IBU) is a non-steroidal anti-inflammatory drug (NSAID) with antiinflammatory, analgesic, and antipyretic properties used to treat rheumatoid arthritis, osteoarthritis, and mild to moderate pain. However, it has extremely low aqueous solubility, rapid biotransformation with a half-life of nearly 2 h and poor tissue absorption resulting in poor bioavailability. One of the most important strategies for avoiding NSAID-related toxicity is modified release polymeric systems. Crosslinked polyphosphazene microspheres are attractive systems in drug delivery, as they are biocompatible and biodegradable. In the current work, novel cross-linked inorganic hybrid polyphosphazene microspheres were synthesized by self-assembly precipitation polymerization between hexachlorocyclotriphosphazene (trimer)/ octachlorocyclotetraphosphazene (tetramer) as a cross-linker and 4,7-dihydroxyisoflavone (4.7 DHF) as a monomer. The structure of synthesized microspheres was identified several techniques in detail. IBU was successfully incorporated into the trimeric and tetrameric polyphosphazene microspheres. Particle size, zeta potential, drug loading, morphology, thermal, FT-IR, and XRD analyses, and IBU quantification using UPLC method were carried out to evaluate the microspheres. Considering the higher drug loading values and smaller particle size, trimer-based microspheres (4.7 DHF-TRI-IBU) were selected for further studies. In vitro release studies from 4.7 DHF-TRI-IBU demonstrated modified release pattern which followed zero-order kinetic model. Characteristics of 4.7 DHF-TRI-IBU were found to remain stable at 4 °C ± 1 °C, 25 °C ± 1 °C and 40 °C ± 1 °C during the storage period of 3 months. In vitro characterization analyses showed that spherical, micron-sized 4.7 DHF-TRIIBU microspheres with prolonged release pattern has the potential of enhancing analgesic and anti-inflammatory activity. Keywords Ibuprofen · Polyphosphazene · Microspheres · Release kinetics · Hexachlorocyclotriphosphazene · Octachlorocyclotetraphosphazene
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Polymer Bulletin
Introduction Phosphazenes are inorganic–organic hybrid macromolecules based on repetitive − P= N− units with amine or hydroxyl-derived organic side groups and generally observed as cyclic compounds and polymers with a linear or branched structure. They are grouped as linear, cyclic, and polyphosphazenes in three categories. Chlorine atoms attached to phosphorus atoms in the structure of hexachlorocyclotriphosphazene (HCCP) (trimer) and octachlorocyclotetraphosphazene (tetramer) (OCCP) form phosphazenes as a result of substitution reactions
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