Calixto Giovana Maria Fioramonti, Muniz Bruno Vilela, Castro Simone R, de Araujo Jaiza Samara Macena, de Souza Amorim Klinger, Ribeiro Lígia N M, Ferreira Luiz Eduardo Nunes, de Araújo Daniele Ribeiro, de Paula Eneida, Franz-Montan Michelle
Department of Biosciences, Piracicaba Dental School, University of Campinas-UNICAMP, Piracicaba 13414-903, Brazil.
Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas 13083-872, Brazil.
Pharmaceutics. 2021 Oct 21;13(11):1760. doi: 10.3390/pharmaceutics13111760.
Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTC) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTC slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry.
近期有报道称,通过鼻腔喷雾给予丁卡因(TTC)和羟甲唑啉可实现上颌牙的无针局部麻醉,且不会引起疼痛、恐惧和压力。这项工作旨在评估负载TTC的混合系统是否能降低细胞毒性、促进持续渗透,并提高TTC对上颌牙的麻醉效果,从而在牙科手术中实现安全、有效、无痛且持久的镇痛。基于包裹在纳米结构脂质载体(NLC)中的4% TTC并掺入泊洛沙姆407热可逆水凝胶的混合系统(TTC),展现出适用于鼻腔局部应用的理想流变学、力学和粘膜粘附特性。与对照制剂相比,使用TTC减缓了麻醉剂在体外透过鼻黏膜的渗透速度,维持了对神经母细胞瘤细胞的细胞毒性,并使镇痛持续时间增加了两倍,这是通过对小鼠进行甩尾试验观察到的。此处获得的结果为未来对含有负载TTC的NLC的热可逆混合水凝胶进行临床评估开辟了前景,旨在开发一种用于牙科的有效、局部、鼻内、无针麻醉方法。