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Citrem-phosphatidylcholine nano-self-assemblies: Solubilization of bupivacaine and its role in triggering colloidal transition from vesicles to cubosomes and hexosomes

DOI: 10.1039/C9CP01878F DOI Help

Authors: Rama Prajapati (University of Copenhagen) , Susan Weng Larsen (University of Copenhagen) , Anan Yaghmur (University of Copenhagen)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Physical Chemistry Chemical Physics

State: Published (Approved)
Published: June 2019

Abstract: Improvement of pain management strategies after arthroscopic surgery by multimodal analgesia may include the use of long-acting amide local anesthetics. Among these anesthetics, the low molecular weight local anesthetic agent bupivacaine (BUP) is attractive for use in postoperative pain management. However, it has relatively a short duration of action and imposes higher risk of systemic toxicity at relatively large bolus doses. Bupivacaine encapsulation in lipid-based delivery systems is an attractive strategy for prolonging its local anaesthetic effect and reducing the associated undesirable systemic side effects. Here, we discuss the potential development of liquid crystalline nanocarriers by using a binary lipid mixture of citrem and soy phosphatidylcholine (SPC) at different weight ratios. The produced safe-by-design family of citrem/SPC nanoparticles are attractive for use in the development of nanocarriers owing to the previously reported hemocompatibility. BUP encapsulation efficiency (EE), depending on the lipid composition , was in the range of 65-77%. In this study, nanoparticle tracking analysis (NTA) and synchrotron small-angle X-ray scattering (SAXS) were employed to gain insight into the effect of BUP solubilization and lipid composition on the size and structural characteristics of the produced citrem/SPC nanodispersions. BUP loading led to a slight change in the mean sizes (diameters) and size distributions of citrem/SPC nanoparticles. However, we found that BUP accommodation into the nanoparticles’ self-assembled interiors, triggers in BUP concentration- and lipid composition-dependent manners significant structural alterations that involve vesicles-cubosomes and vesicles-hexosomes transitions. The structural tunability of citrem/SPC nanoparticles and the implications for a potential use for intra-articular BUP delivery are discussed.

Subject Areas: Biology and Bio-materials, Chemistry, Medicine


Instruments: I22-Small angle scattering & Diffraction