Formulation and In Vivo Pain Assessment of a Novel Niosomal Lidocaine and Prilocaine in an Emulsion Gel (Emulgel) of Semisolid Palm Oil Base for Topical Drug Delivery

一种新型利多卡因和丙胺卡因脂质体乳胶凝胶(乳胶凝胶)的制备及其体内疼痛评估,该乳胶凝胶以半固体棕榈油为基质,用于局部给药。

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Abstract

This study aimed to formulate semisolid niosomal encapsulated lidocaine and prilocaine using the patented palm oil base Hamin-C(®) for further characterization and in vivo pain assessment. Seven formulations were initially studied with various chemical compositions. A thin-layer film hydration method was used to produce niosome using a mixture of surfactant (Span(®) 40 or Span(®) 60) and cholesterol (CHOL) at a 1:1 ratio, with/without a charge-inducing agent (diacetyl phosphate) (DCP) and with/without labrasol(®). Niosome F1 formulation had been identified as the highest %EE achieved, at 53.74 and 55.63% for prilocaine and lidocaine, respectively. Furthermore, NIO-HAMIN F1 emulgel indicated the best formulation with higher permeability of prilocaine and lidocaine compared to the rest of the formulations. The reformulation of optimization of NIO-HAMIN F1 emulgel using a cold process to NIO-HAMIN F1-C emulgel to improve the viscosity resulted in higher diffusion of prilocaine and lidocaine by 5.71 and 33.38%, respectively. In vivo pain perception studies by verbal rating score (VRS) and visual analogue score (VAS) on healthy subjects show a comparable local anesthetic effect between NIO-HAMIN F1-C emulgel and EMLA(®) cream.

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