Development of a novel solid lipid nanoparticles-loaded dual-reverse thermosensitive nanomicelle for intramuscular administration with sustained release and reduced toxicity

Title
Development of a novel solid lipid nanoparticles-loaded dual-reverse thermosensitive nanomicelle for intramuscular administration with sustained release and reduced toxicity
Author(s)
용철순Fakhar ud Din[Fakhar ud Din]Rehmana Rashid[Rehmana Rashid]Omer Mustapha[Omer Mustapha]김동욱[김동욱]박종혁[박종혁]구세광[구세광]오유경[오유경]윤유석[윤유석]김종오최한곤[최한곤]
Keywords
DRUG-DELIVERY SYSTEM; SKELETAL-MUSCLE; HYDROGEL; STABILITY; BIOAVAILABILITY; MICROSPHERES; DISSOLUTION; FORMULATION; MICE; GEL
Issue Date
201505
Publisher
ROYAL SOC CHEMISTRY
Citation
RSC ADVANCES, v.5, no.54, pp.43687 - 43694
Abstract
To develop a novel solid lipid nanoparticles (SLNs)-loaded dual-reverse thermosensitive nanomicelle (DRTN) for intramuscular administration of flurbiprofen with sustained release and reduced toxicity, the DRTN was prepared with flurbiprofen-loaded SLNs, poloxamer 407 (P 407), poloxamer 188 (P 188) and water. Its rheological characterization, release, stability, pharmacokinetics and morphology were evaluated after intramuscular administration to rats. These SLNs were solid at 25 degrees C and transformed into liquid form at physiological temperature due to their melting point of about 32 degrees C. Furthermore, the DRTN retained a liquid state at 25 degrees C and gelled inside the body owing to its gelation temperature of about 34.7 degrees C, leading to an opposite reversible property of the SLNs. When compared to the hydrogel, it significantly decreased the drug release and exhibited a reduced initial fast release. It sustained a high plasma concentration for 60 h, which was significantly higher when compared to the suspension, indicating enhanced bioavailability. However, it showed a lower plasma concentration, AUC, and C-max values than that found for the hydrogel, suggesting the retarded release and decreased side effects of the drug. Unlike the hydrogel, it induced no injury to rat muscle as a result of no direct contact of the drug. It was stable for four months. Therefore, this novel DRTN system could be a strong candidate for the intramuscular administration of flurbiprofen.
URI
http://hdl.handle.net/YU.REPOSITORY/32292http://dx.doi.org/10.1039/c5ra05656j
ISSN
2046-2069
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약학대학 > 약학부 > Articles
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