Preparation of paeonol nanoemulsion and investigation of vascular endothelial cells uptake

WANG Sibu; CHEN Ying; DING Yang; XIAO Ting; LIU Wen; SHEN Xiangchun; TAO Ling; LUO Xinghong

doi:10.11665/j.issn.1000-5048.20220607

Journal of China Pharmaceutical University > 2022 > 53(6): 690-697. > DOI: 10.11665/j.issn.1000-5048.20220607

WANG Sibu, CHEN Ying, DING Yang, XIAO Ting, LIU Wen, SHEN Xiangchun, TAO Ling, LUO Xinghong. Preparation of paeonol nanoemulsion and investigation of vascular endothelial cells uptake[J]. Journal of China Pharmaceutical University, 2022, 53(6): 690-697. DOI: 10.11665/j.issn.1000-5048.20220607

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Preparation of paeonol nanoemulsion and investigation of vascular endothelial cells uptake

1.
School of Pharmacy, Guizhou Engineering Center for Efficient Utilization of Natural Drug Resources (Guiyang Joint Key Laboratory of Efficient Utilization of Natural Drug Resources), Guizhou Medical University, Guizhou 550025
2.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009
3.
State Key Laboratory of Translational Medicine and Innovative Drug, Jiangsu Simcere Pharmaceutical Co., Ltd., Nanjing 210042, China

Funds: This study was supported by Guizhou High-level Innovative Talents Project (Guizhou Science and Technology [2015] No.4029); and the Pharmacy International Science and Technology Cooperation Base of Guizhou Medical University (Guizhou Technology Platform Talent [2017] 5802)

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Received Date: May 06, 2022
Revised Date: December 15, 2022

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Abstract

Abstract

In order to improve the poor solubility and low bioavailability of paeonol (Pae), paeonol-nanoemulsion (Pae-NE) was prepared, and its effect on uptake of human umbilical vein endothelial cells (HUVECs) was investigated.Pae-NE was prepared by phase inversion composition (PIC), the formulation of Pae-NE was optimized by single factor method and central composite design-response surface method (CCD), and the pharmaceutical properties were further characterized.Moreover, MTT was applied to evaluate the toxicity of Pae-NE on HUVECs, and the cellular uptake efficiency of Pae-NE was detected by fluorescence microscopy and flow cytometry.The results showed that the optimal formulation of Pae-NE was 20 mg of Pae, 55.1 mg of LCT, 144.9 mg of MCT, 600 mg of HS15, and 200 mg of 1,2 propylene glycol.The Pae-NE appearance was a light blue emulsion, and the average particle size is (25.69 ± 0.03) nm, with PDI of 0.182 ± 0.09, Zeta potential of -(4.01 ± 0.30) mV and good stability.The drug loading of Pae-NE was (1.967 ± 0.28) mg/mL and encapsulation rate of (99.36 ± 0.1)%.Pae-NE performed no significant effect on HUVECs growth in the Pae concentration range of 10^-1-10^-3μg/mL.Moreover, NE as a drug delivery carrier significantly enhanced the uptake efficiency of Pae on HUVECs.In conclusion, Pae-NE preparation method was simple and stable, and promotes HUVECs uptake efficiency of Pae, suggesting that NE was a better dosage form reference for the lipid-soluble drug of Pae.
- paeonol,
- nanoemulsion,
- preparation,
- human umbilical vein endothelial cells,
- cell uptake

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Preparation of paeonol nanoemulsion and investigation of vascular endothelial cells uptake

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