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A Nanocarrier Skin-Targeted Drug Delivery System using an Ascorbic Acid Derivative

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Abstract

Purpose

As trisodium L-ascorbyl 2-phosphate 6-palmitate (APPS), an ascorbic acid derivative, is an amphiphilic substance, it forms micelles in aqueous solutions. Micelles are used as drug carriers and can emulsify drugs that are poorly soluble in water, such as nadifloxacin (NDFX). The purpose of this study was to prepare nanocarriers using APPS to carry NDFX into Yucatan micropig skin.

Methods

After synthesis of the NDFX nanoparticles by using the hydration method, physical evaluations were carried out that included assessments of particle size and zeta potential, encapsulation efficiency, particle structure by transmission electron microscopy, 31P–NMR spectra, and particle stability. Functional evaluations of the nanoparticles included 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays, skin penetration tests, and fluorescence microscopy observations.

Results

The encapsulation efficiency of NDFX in the nanoparticles was approximately 75%. With added magnesium chloride, the nanoparticles remained stably dispersed in aqueous solution for at least 14 days at 25°C under protection from light. In addition, the nanoparticle formulation improved the skin permeability of NDFX.

Conclusion

APPS-derived nanoparticles were shown to be useful as skin-targeting nanocarriers.

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Scheme 1

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Abbreviations

APPS:

Trisodium L-ascorbyl 2-phosphate 6-palmitate

DDSs:

Drug delivery systems

DLS:

Dynamic light scattering

DPPH:

2,2-diphenyl-1-picrylhydrazyl

DSPE-PEG 2000:

Distearoyl phosphatidylethanolamine-polyethylene glycol 2000

EE%:

Encapsulation efficiency rate

HPLC:

High-performance liquid chromatography

IC50 :

50% inhibitory concentration

IPM:

Isopropyl myristate

NDFX:

Nadifloxacin

PEG:

Polyethylene glycol

TEM:

Transmission electron microscopy

YMP:

Yucatan micropig

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Authors and Affiliations

  1. Laboratory of Drug Safety Management, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado-shi, Saitama, 3500295, Japan

    Yutaka Inoue, Mitsue Hibino, Isamu Murata & Ikuo Kanamoto

Authors
  1. Yutaka Inoue
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  2. Mitsue Hibino
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  3. Isamu Murata
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  4. Ikuo Kanamoto
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Correspondence to Yutaka Inoue.

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Inoue, Y., Hibino, M., Murata, I. et al. A Nanocarrier Skin-Targeted Drug Delivery System using an Ascorbic Acid Derivative. Pharm Res 35, 1 (2018). https://doi.org/10.1007/s11095-017-2311-3

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  • DOI: https://doi.org/10.1007/s11095-017-2311-3

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