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. 2022 Dec;29(1):263-269.
doi: 10.1080/10717544.2021.2023695.

Combination anesthetic therapy: co-delivery of ropivacaine and meloxicam using transcriptional transactivator peptide modified nanostructured lipid carriers in vitro and in vivo

Shu Yuan  1 , Jun Chen  1 , Shuo Feng  2 , Min Li  1 , Yingui Sun  1 , Yuzhen Liu  2
Affiliations

Combination anesthetic therapy: co-delivery of ropivacaine and meloxicam using transcriptional transactivator peptide modified nanostructured lipid carriers in vitro and in vivo

Shu Yuan et al. Drug Deliv. 2022 Dec.

Abstract

Combination therapy combining two drugs in one modified drug delivery system is used to achieve synergistic analgesic effect, and bring effective control of pain management, especially postoperative pain management. In the present study, a combination of drug delivery technologies was utilized. Transcriptional transactivator (TAT) peptide modified, transdermal nanocarriers were designed to co-deliver ropivacaine (RVC) and meloxicam (MLX) and anticipated to achieve longer analgesic effect and lower side effect. TAT modified nanostructured lipid carriers (TAT-NLCs) were used to co-deliver RVC and MLX. RVC and MLX co-loaded TAT-NLCs (TAT-NLCs-RVC/MLX) were evaluated through in vitro skin permeation and in vivo treatment studies. NLCs-RVC/MLX showed uniform and spherical morphology, with a size of 133.4 ± 4.6 nm and a zeta potential of 20.6 ± 1.8 mV. The results illustrated the anesthetic pain relief ability of the present constructed system was significantly improved by the TAT modification through the enhanced skin permeation efficiency and the co-delivery of MLX along with RVC that improved pain management by reducing inflammation at the injured area. This study provides an efficient and facile method for preparing TAT-NLCs-RVC/MLX as a promising system to achieve synergistic analgesic effect.

Keywords: Combination anesthetic; co-delivery; meloxicam; nanostructured lipid carriers; ropivacaine.

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Conflict of interest statement

No potential conflict of interest was reported by the author(s).

Figures

Figure 1.
Figure 1.
Scheme graph and morphology of TAT-NLCs-RVC/MLX.
Figure 2.
Figure 2.
In vitro cytotoxicity of drugs loaded NLCs and free drugs evaluated by the L929 cells viability. Data presented as means ± SD (n = 3). *p<.05.
Figure 3.
Figure 3.
In vitro skin permeation efficiency of RVC (A) and MLX (B) from NLCs and free drugs compared using the Franz diffusion cells with the skin of rats. Data presented as means ± SD (n = 3). *p<.05.
Figure 4.
Figure 4.
In vivo skin permeation profiles of RVC (A) and MLX (B) from NLCs and free drugs evaluated on the abdominal site of SD rats. Data presented as means ± SD (n = 3). *p<.05.
Figure 5.
Figure 5.
In vivo anesthetic pain relief effects of drugs loaded NLCs and free drugs. Data presented as means ± SD (n = 3). *p<.05.
See this image and copyright information in PMC

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