Design of Liposomal Lidocaine/Cannabidiol Fixed Combinations for Local Neuropathic Pain Treatment
The administration of drug fixed combinations by nanocarriers is a new attractive approach since it can allow improvements in both the skin penetration of cargo compounds and their synergistic effects. The cutaneous administration of lidocaine (LD) and118金宝搏app (CBD) combination can be useful for the local treatment of neuropathic pain. In fact, these drugs might exert a complementary effect on pain acting on sodium and calcium channels. In this study, the feasibility to deliver this combination in the deeper layers of the skin using deformable liposomes was studied. Based on a study of the drug affinity forlipidDSC执行的组件，118金宝搏app was loaded in the lipid bilayer for limiting the leakage, while LD was loaded in the inner core by a pH gradient method (G-liposomes) or after previous encapsulation in micelle (DiMiL). The effect of the presence of补间80还评估了脂质体膜。Dimil增加了皮肤渗透和CBD和LD真皮的保留，相对于G-脂质体（R24dermis: 11.52 ± 2.4 against 4.51 ± 0.8 µg/cm2for CBD; 19.6 ± 2.9 against 3.2 ± 0.1 µg/cm2for LD). Moreover, both DiMiL and G-liposomes were more efficient than control formulations carrying free drugs in improving drug skin permeation. Interestingly, in the presence of a drug exerting a fluidizing effect such as CBD, the removal of Tween 80 from the composition led to an improved control of drug release and a higher extent of drug retention in the dermis layer.
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材料s
Soy-phosphatidylcholine (S 100) and 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) were kindly provided by脂肪(瑞士Steinhausen);Kolliphor HS 15（K-HS15）由BASF(Cesano Maderno, Italy); LD base was obtained from A.C.E.F. S.p.A. (Fiorenzuola d’Arda, Italy) andTween®80从克罗达（法国巧克力）；PEG 400and ascorbic acid were purchased from VWR (VWR Prolabo Chemicals, Leuven, Belgium), whereas ammonium molybdate, sodium dihydrogen phosphate, and analytical-grade solvents were obtained from默克Life Science (Milan, Italy); CBD was kindly gifted by Indena S.p.A. (Milano, Italy). Versatis® (LD Plaster) was from Grunenthal (Aachen, Germany). Finally, sodium hydroxide and orthophosphoric acid were obtained from Carlo Erba (Milan, Italy).
Franzè，S。；安吉洛（L. Angelo）；Casiraghi，A。;Minghetti，P。;Cilurzo，F。脂质体利多卡因/大麻二酚固定组合的设计，用于局部神经性疼痛治疗。药物2022,14, 1915. https://doi.org/10.3390/pharmaceutics14091915
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