Lidocaine and Cyclodextrin Complexes as a Bio-Textile Patch for Fast-Releasing Topical Administration of Lidocaine

Bio-textiles are primarily engineered for specific biomedical end-uses like textile-based drug-delivery carriers for appropriated <i>in-vivo</i> target sites while maintaining somatic harmony. The use of nanotechnology for fabricating such bio-textiles via electrospinning gained importance because of controllable nanoscale diameters, the encapsulation amount of active agents, and overall efficacy in targeted delivery overcoming first-pass metabolism barriers. Fine-tuning such parameters positively affects the morphology interface, imparts enhanced physiochemical properties, and facilitates bio-nano-interface construction. Responsive polymeric base materials as encapsulation agents for electrospun nanofibers for active agents like medicaments are preferred for their biocompatibility and homeostasis during interaction with bio-compounds. The large surface area and highly porous structure of the nanoparticles allow easier disintegration upon subjection to proximal physiological fluids. The protein corona expedites the stable transition of the nanoparticles to the target delivery site via endocytosis or direct penetration. The amorphized state of the active agent within the nanofibrous matrix allows easier adsorption into target organs. Apart from polymeric bases, cyclodextrins are a safe choice for nanofiber matrices to confine active agents via inclusion complexation (IC) within the hydrophobic truncated cone for drug delivery systems by amorphization of the crystalline active agents and enhancing its solubility, bioavailability, and stability. Cyclodextrins are more water soluble than polymers and become a better choice as an encapsulation agent because solubilizing polymers need toxic solvents sometimes. Cyclodextrin help in the fast or slow, or controlled release of the encased active agents leading to drug delivery in a similar fashion as the polymeric nanofibers. Cyclodextrin and active agent inclusion complexes can be electrospun into nanofibers in the form of strips or onto textile substrates to form bio-textiles. In this study, Lidocaine (Lid), a crystalline and poorly water-soluble amino-amide drug, was encapsulated within Hydroxypropylated Beta Cyclodextrin (HPβCyD) nanofiber matrices to enhance its topical bioavailability and solubility. Aqueous solutions of Lid/HPβCyD-IC in different molar ratios were electrospun into nanofibrous (NFs) strips and checked for their physiochemical properties to ascertain IC formation and understand the efficacy of encapsulation and amorphization of Lid in HPβCyD nano matrix through 1H-NMR, FTIR, XRD, DSC, and TGA. The Lid/HPβCyD-IC NFs were deposited on a non-woven cotton patch to create a bio-textile patch for topical administration. The <i>in-vitro </i>release performance was examined, and the findings corroborated the fast-release corollary.