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Thermo-responsive Polyurethane Organogel for Norfloxacin Delivery

Abstract

To overcome the constraints presented by the conventional hydrogel-based skin patch, including poor transdermal penetration activity and reluctant release of the encapsulated lipophilic drugs, a facile organogel constitute of amphiphilic hexamethylene diisocyanate (HDI)-based polyurethanes (PUs) was developed in 1,3-propanediol, the amphiphilic components of poly (ethylene glycol) (PEG) and HDI allows for formulation of distinctive segregated domains PEG and HDI based on inter- and intra-molecular interaction between HDI segments. Of note, convenient cooling down process allows for formulation of stable and homogenous organogel. In addition, functional host 2,6-dimethyl-β-cyclodextrin (CD) group as drug reservoir was included in PEG-HDI-CD aiming for encapsulation of the pharmaceutical compound (norfloxacin), characterized by its gel to sol state transition in the range of 24~36 °C, consequently conducing to minimal drug release profile at 4 °C but accelerated rate of drug release at physiological temperature, this is particular important for industrial applications. The in vitro drug release and transdermal experimental results showed that the organogel as a drug carrier was capable of releasing the drug efficiently, improving the transdermal delivery, and exhibited bactericidal activity over 80% in vivo. Moreover, the introduced CD moieties could increase the solubility of lipophilic drugs and the dissociation rate in biological milieu, which appeared to benefit for promoted drug release rate and transdermal efficiency as compared to CD-free organogel.

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Publication details

The article was received on 27 Oct 2017, accepted on 24 Nov 2017 and first published on 27 Nov 2017


Article type: Paper
DOI: 10.1039/C7PY01803G
Citation: Polym. Chem., 2017, Accepted Manuscript
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    Thermo-responsive Polyurethane Organogel for Norfloxacin Delivery

    D. Liu, Q. Chen, Y. Long, J. Ma and H. Gao, Polym. Chem., 2017, Accepted Manuscript , DOI: 10.1039/C7PY01803G

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