Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Pharmaceutics

Cristina Quílez¹  Diego Velasco¹  JoséL. Jorcano¹  Carmen Alvarez-Lorenzo²  Clara López-Iglesias²  CarlosA. García-González²  Joana Barros³  FernandoJ. Monteiro³ 

[1] Department of Bioengineering and Aerospace Engineering, Universidad Carlos III de Madrid (UC3M), 28911 Leganés (Madrid), Spain;Department of Pharmacology, Pharmacy and Pharmaceutical Technology, I+D Farma group (GI-1645), Faculty of Pharmacy, Agrupación Estratégica de Materiales (AeMAT) and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain;Instituto de Investigação e Inovação em Saúde da Universidade do Porto (i3S), Instituto de Engenharia Biomédica (INEB), Faculdade de Engenharia (FEUP), Universidade do Porto, 4200-135 Porto, Portugal;

关键词: SLMPs;    drug delivery;    lidocaine HCl;    3D-bioprinting;    PGSS technique;    wound healing;   

DOI  :  10.3390/pharmaceutics12090870

来源: DOAJ

【 摘 要 】

The delivery of bioactive agents using active wound dressings for the management of pain and infections offers improved performances in the treatment of wound complications. In this work, solid lipid microparticles (SLMPs) loaded with lidocaine hydrochloride (LID) were processed and the formulation was evaluated regarding its ability to deliver the drug at the wound site and through the skin barrier. The SLMPs of glyceryl monostearate (GMS) were prepared with different LID contents (0, 1, 2, 4, and 10 wt.%) using the solvent-free and one-step PGSS (Particles from Gas-Saturated Solutions) technique. PGSS exploits the use of supercritical CO₂ (scCO₂) as a plasticizer for lipids and as pressurizing agent for the atomization of particles. The SLMPs were characterized in terms of shape, size, and morphology (SEM), physicochemical properties (ATR-IR, XRD), and drug content and release behavior. An in vitro test for the evaluation of the influence of the wound environment on the LID release rate from SLMPs was studied using different bioengineered human skin substitutes obtained by 3D-bioprinting. Finally, the antimicrobial activity of the SLMPs was evaluated against three relevant bacteria in wound infections (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). SLMPs processed with 10 wt.% of LID showed a remarkable performance to provide effective doses for pain relief and preventive infection effects.

【 授权许可】

Unknown