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Formulation of Aucklandiae Radix Extract-Loaded Nanoemulsions and Its Characterization and Evaluations In Vitro and In Vivo

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Abstract

This study aimed to screen, design, and evaluate an optimal nanoemulsion formulation for Aucklandiae Radix extraction (ARE). A simple lattice design (SLD) method was used to determine the preparation process of Aucklandiae Radix extract-nanoemulsions (ARE-NEs). After optimization, the average particle size of ARE-NEs was 14.1 ± 1.1 nm, polydispersity index was 0.2376, and pH was 6.92. In vitro penetration tests verified that the permeability ratios of costunolide (CE), dehydrocostus lactone (DE), and ARE-NEs were approximately 6.33 times and 8.20 times higher, respectively, than those of the control group. The results of the pharmacokinetic study indicated that after topical administration, the content of the index components of ARE-NEs increased in vivo, with a longer release time and higher bioavailability in vivo than in vitro. The index components were CE and DE, respectively. In addition, a skin irritation test was conducted on normal and skin-damaged rabbits, aided by HE staining and scanning electron microscopy, to reveal the transdermal mechanism of ARE-NEs and proved that NEs are safe for topical application. ARE-NEs energetically developed the properties of skin and penetration through the transdermal route, which were secure when applied via the transdermal delivery system .

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Data Availability

The datasets generated during and/or analyzed during the current study are available from the corresponding author on reasonable request.

Abbreviations

ARE:

Aucklandiae Radix extraction

ARE-NEs:

Aucklandiae Radix extract nanoemulsions

ARE-Y:

Aucklandiae Radix extract yield

AUC:

Area under the plasma concentration–time curve

CE:

Costunolide

CEARE-Y:

CE in extract yield

Cmax:

Maximum plasma concentration

DE:

Dehydrocostus lactone

DEARE-Y:

DE in extract yield

EE:

Encapsulation efficiency

GTCC:

Glyceryl octyl decanoate

HPLC:

High-performance liquid chromatography

IPM:

Isopropyl myristate

IPP:

Isopropyl palmitate

LLWL 1349:

Labrafac Lipophile WL 1349

NEs:

Nanoemulsions

O/W NEs:

Oil-in-water nanoemulsions

OA:

Oleic acid

PBS:

Phosphate buffer

PDI:

Polydispersity index

PG:

1,2-Propanediol

PG:

1,2-Propanediol

SC:

Stratum corneum

SEM:

Scanning electron microscope

SLD:

Simplex lattice design

T1/2:

Drug half-life

TDDS:

Transdermal drug delivery system

Transcutol P:

Diethylene glycol monoethyl ether

Tween 20:

Polysorbate 20

Tween 80:

Polysorbate 80

UPLC-Xevo-TQ-S:

Ultra-high-performance liquid chromatography-mass spectrometry

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Funding

This work was supported by the basic research project of Logistics University of Chinese People’s Armed Police Force and National Natural Science Foundation of China Youth Fund Project (No. 81503467).

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Author notes

  1. Meng Zhang and Huimin Li contributed equally to this work.

Authors and Affiliations

  1. Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, People’s Republic of China

    Meng Zhang, Xinrui Wang, Jingze Zhang & Dailin Liu

  2. Tianjin Modern Innovation Chinese Medicine Technology Co., Ltd, Tianjin, 300380, People’s Republic of China

    Meng Zhang, Xinrui Wang, Lifei Luo, Jingze Zhang & Dailin Liu

  3. Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, 100850, People’s Republic of China

    Huimin Li

  4. Department of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin, 300309, People’s Republic of China

    Li Zhang & Jingyang Li

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  1. Meng Zhang
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Contributions

M.Z. and H.M.L—investigation, data curation, and writing (original draft preparation).

Conceptualization: L.Z, J.Z.Z.; methodology: L.Z., J.Y.L, H.M.L., J.Z.Z.; formal analysis and investigation: M.Z., H.M.L., X.R.W., L.F.L.; writing (original draft preparation): M.Z.; writing (review and editing): M.Z., J.Z.Z., D.L.L.; resources: L.Z., J.Z.Z., J.Y.L., D.L.L.; supervision: J.Z.Z., D.L.L.

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Correspondence to Dailin Liu.

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Zhang, M., Li, H., Zhang, L. et al. Formulation of Aucklandiae Radix Extract-Loaded Nanoemulsions and Its Characterization and Evaluations In Vitro and In Vivo. Appl Biochem Biotechnol 195, 3156–3179 (2023). https://doi.org/10.1007/s12010-022-04232-9

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