RETRACTED ARTICLE: Preparation and characterization of novel lipid nanocapsules of ropivacaine for transdermal delivery

Abstract

Ropivacaine, a novel long-acting local anesthetic, has been proved to own superior advantage. However, the application form used in clinic, ropivacaine hydrochloride (Naropin Injection), which should be administed intravenously, is causing poor patient convenience. The purpose of this study was to formulate ropivacaine (RPV) in lipid nanocapsules (LNCs) and character the potential of LNCs in delivering RPV transdermally to exploit novel external preparation. The RPV-LNCs were successfully prepared by phase inversion technique and the formulation was characterized in terms of size, zeta potential, ex vivo permeation study, and pharmacodynamics. The prepared RPV-LNCs displayed a typical core-shell structure with a narrow size distribution of 62.1 ± 1.7 nm and drug loading of 1.35 ± 0.20%. The results of differential scanning calorimetry (DSC) analysis and X-ray diffraction showed that RPV was in amorphous crystalline state when encapsulated into LNCs. Furthermore, the results of ex vivo permeation study displayed that RPV-LNCs had an improved permeability (349.0 ± 11.5 μg cm(-2) versus 161.0 ± 1.3 μg cm(-2)) compared with free RPV. The results of histopathology study showed that interaction between LNCs and skin could break the close conjugation of corneocyte layers. In the mice writhing test, RPV-LNCs exhibited obvious analgesic effect by both prolonging pain latency and reducing the writhing response with an inhibition rate of 91.3% compared to the control group. In conclusion, RPV-LNCs could be a promising delivery system to encapsulate RPV and deliver RPV for transdermal administration.

Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

“…All kinds of SLN and NLC suspensions prepared above were centrifuged at 10,000 rpm for 10 min and the supernatant was discarded. 14 , 25 , 26 The pellet was washed with Milli-Q water for three times. Mannitol (5.0%, w/v) was added as a cryoprotectant for the freeze-drying process.…”

A novel local anesthetic system: transcriptional transactivator peptide-decorated nanocarriers for skin delivery of ropivacaine

“…Whereas, various clinical studies indicated that RVC was rapidly cleared from the injection site and showed short efficacy of the severity of pain (approximately 2 h postoperatively) 8. Moreover, intravenous administration brings poor patient convenience and other toxicities such as arrhythmia 9,10. These clinical results have prompted that it was critical to the development of appropriate delivery systems and different administration routes that circumvent the aforementioned problem.…”

Lipid nanoparticles loading triptolide for transdermal delivery: mechanisms of penetration enhancement and transport properties

“…The results of HE studies indicated that the TPL-NPs could permeate into skin by changing SC structure. Both the interactions between mixed surfactants (Tween 80 and Transcutol HP) and skin and lipid exchange between lecithin and SC could increase the skin intercellular space and loosen SC dense structure [ 37 ]. Besides, TPL-NPs could inhibit or prevent evaporation, which could improve skin moisture and hydration [ 38 , 39 ].…”