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  • Preparation and evaluation of submicron-carriers for naringenin topical application.

Preparation and evaluation of submicron-carriers for naringenin topical application.

International journal of pharmaceutics (2015-01-24)
Ming-Jun Tsai, Yaw-Bin Huang, Jhih-Wun Fang, Yaw-Syan Fu, Pao-Chu Wu
ABSTRACT

Submicron emulsion system is one kind of submicron-carrier that can ensure close contact and increase the amount of drug transport into the skin. In the present study, naringenin was loaded into a submicron emulsion system for topical applications. The enhancement effect of drug permeability through skin, stability, and skin irritation of naringenin-loaded submicron emulsions were evaluated. The results showed that the transdermal amount and deposition amount in skin of naringenin from submicron emulsion formulations were significantly increased when compared to the control group of saturated aqueous solution of naringenin. The drug-loaded submicron emulsions showed thermodynamic stability after centrifugation and cooling-heating cycle tests. The level of drug was more than 98% after 3 months of storage at 25°C and 40°C. In skin irritation test, the result also demonstrated that naringenin-loaded submicron emulsion had less skin irritation, indicating that the formulation can possibly be developed for topical application.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Naringenin, natural (US), 98%
Sigma-Aldrich
Acetic acid-12C2, 99.9 atom % 12C
Sigma-Aldrich
Isopropyl myristate, 98%
Sigma-Aldrich
Triethylamine, ≥99.5%
Supelco
(±)-Naringenin, analytical standard
Sigma-Aldrich
Acetic acid, ≥99.5%, FCC, FG
Sigma-Aldrich
Acetic acid, natural, ≥99.5%, FG
Sigma-Aldrich
Isopropyl myristate, ≥98%
Sigma-Aldrich
Methanol solution, NMR reference standard, 4% in methanol-d4 (99.8 atom % D), NMR tube size 3 mm × 8 in.
Sigma-Aldrich
Triethylamine, ≥99%
Sigma-Aldrich
Isopropyl myristate, ≥90% (GC)
Sigma-Aldrich
(±)-Naringenin, ≥95%
Sigma-Aldrich
Triethylamine, for amino acid analysis, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, BioUltra, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, for protein sequence analysis, ampule, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, puriss. p.a., ≥99.5% (GC)
Supelco
Triethylamine, analytical standard
Sigma-Aldrich
Methanol solution, contains 0.50 % (v/v) triethylamine
Sigma-Aldrich
Isopropyl myristate, Vetec, reagent grade, 98%
Supelco
Isopropyl myristate, Pharmaceutical Secondary Standard; Certified Reference Material
USP
Isopropyl myristate, United States Pharmacopeia (USP) Reference Standard
Supelco
Residual Solvent - Acetonitrile, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Hesperetin, analytical standard
Sigma-Aldrich
Acetic acid, for luminescence, BioUltra, ≥99.5% (GC)
Supelco
Acetic acid, analytical standard
Supelco
Acetonitrile, analytical standard
Supelco
Methanol, analytical standard
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Acetonitrile, anhydrous, 99.8%
Sigma-Aldrich
Hesperetin, ≥95%