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Objective: The aim of this study was to develop a novel W/O microemulsion for a natural extract of Wen-Luo-Tong (WLT) containing mainly icariin, hydroxysafflor yellow A (HSYA) and gallic acid to be applied to skin as a potential treatment for peripheral neuropathy.

Methods: The oil phase was selected on the basis of affinity with the surfactant and co-surfactant. Pseudo-ternary diagrams were constructed to optimize microemulsions and finally stability studies were performed on the selected formulations. Droplet sizes were analyzed by using a zetasizer and were found to be within the desired range. Selected microemulsions with acceptable viscosities, containing 5%, 8% and 10% of water extract solution, were used for in vitro skin penetration studies using Franz diffusion cells and excised rat skin. New LC-MS/MS and UPLC-Q-TOF/MS methods were employed for quantitative and qualitative analysis.

Results: The optimized formulation (ME-4) consisting of 10% (w/w) water extract solution, 60% isopropyl myristate, 30%(w/w) Smix: Propylene glycol (5:2) significantly increased the cumulative permeated amounts of HSYA, icariin and gallic acid compared with the water extract solution controls.

Conclusion: This novel formulation also increased the number of components penetrating rat skin. Ten components were detected in the Franz cell receptor solution using a UPLC-Q-TOF/MS system after the application of formulation ME-4 for 24h on the skin in vitro. However, only one component was detected after applying the control. Therefore, the microemulsion ME-4 was selected for future in vivo pharmacodynamic studies.

Titel:	Transdermal Delivery of Compounds with Different Lipophilicity and Molecular Weight from W/O Microemulsions Analyzed by UPLC-QTOF/ MS and LC-MS/MS.
Autor/in / Beteiligte Person:	Lin, H ; Michniak-Kohn, B ; Xia, Z ; Xu, L ; Kang, Q ; Chen, C ; Ma, S ; Wu, Q
Zeitschrift:	Current drug delivery, Jg. 15 (2018), Heft 7, S. 1009
Veröffentlichung:	Saif Zone, Sharjah, U.A.E. ; San Francisco, CA : Bentham Science Publishers, c2004-, 2018
Medientyp:	academicJournal
ISSN:	1875-5704 (electronic)
DOI:	10.2174/1567201815666171221125411
Schlagwort:	Administration, Cutaneous Animals Chalcone administration & dosage Chalcone analogs & derivatives Chalcone chemistry Chalcone pharmacokinetics Chromatography, High Pressure Liquid Flavonoids administration & dosage Flavonoids chemistry Flavonoids pharmacokinetics Gallic Acid administration & dosage Gallic Acid chemistry Gallic Acid pharmacokinetics Male Molecular Weight Myristates administration & dosage Myristates chemistry Myristates pharmacokinetics Permeability Propylene Glycol administration & dosage Propylene Glycol chemistry Propylene Glycol pharmacokinetics Quinones administration & dosage Quinones chemistry Quinones pharmacokinetics Rats, Sprague-Dawley Skin metabolism Surface-Active Agents administration & dosage Surface-Active Agents chemistry Surface-Active Agents pharmacokinetics Tandem Mass Spectrometry Emulsions administration & dosage Emulsions chemistry Emulsions pharmacokinetics Skin Absorption
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article Language: English [Curr Drug Deliv] 2018; Vol. 15 (7), pp. 1009-1019. MeSH Terms: Emulsions* / administration & dosage ; Emulsions* / chemistry ; Emulsions* / pharmacokinetics ; Skin Absorption* ; Administration, Cutaneous ; Animals ; Chalcone / administration & dosage ; Chalcone / analogs & derivatives ; Chalcone / chemistry ; Chalcone / pharmacokinetics ; Chromatography, High Pressure Liquid ; Flavonoids / administration & dosage ; Flavonoids / chemistry ; Flavonoids / pharmacokinetics ; Gallic Acid / administration & dosage ; Gallic Acid / chemistry ; Gallic Acid / pharmacokinetics ; Male ; Molecular Weight ; Myristates / administration & dosage ; Myristates / chemistry ; Myristates / pharmacokinetics ; Permeability ; Propylene Glycol / administration & dosage ; Propylene Glycol / chemistry ; Propylene Glycol / pharmacokinetics ; Quinones / administration & dosage ; Quinones / chemistry ; Quinones / pharmacokinetics ; Rats, Sprague-Dawley ; Skin / metabolism ; Surface-Active Agents / administration & dosage ; Surface-Active Agents / chemistry ; Surface-Active Agents / pharmacokinetics ; Tandem Mass Spectrometry Contributed Indexing: Keywords: LC-MS/MS; Microemulsion; UPLC-Q-TOF/MS; gallic acid; hydroxysafflor yellow A; icariin; transdermal delivery. Substance Nomenclature: 0 (Emulsions) ; 0 (Flavonoids) ; 0 (Myristates) ; 0 (Quinones) ; 0 (Surface-Active Agents) ; 0RE8K4LNJS (isopropyl myristate) ; 146087-19-6 (hydroxysafflor yellow A) ; 5S5A2Q39HX (Chalcone) ; 632XD903SP (Gallic Acid) ; 6DC9Q167V3 (Propylene Glycol) ; VNM47R2QSQ (icariin) Entry Date(s): Date Created: 20171223 Date Completed: 20181024 Latest Revision: 20181024 Update Code: 20240513

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Transdermal Delivery of Compounds with Different Lipophilicity and Molecular Weight from W/O Microemulsions Analyzed by UPLC-QTOF/ MS and LC-MS/MS.