A Novel Binary Supercooled Liquid Formulation for Transdermal Drug Delivery

Abstract

The aim of this study was to prepare binary supercooled liquid (SCL) by intermolecular interaction and apply this formulation to transdermal drug delivery. Ketoprofen (KET) and ethenzamide (ETH) were selected as binary SCL component. Thermal analysis of physical mixtures of KET and ETH showed decreases in melting points and glass transition below room temperature, thereby indicating formation of KET-ETH SCL. Intermolecular interactions between KET and ETH in the SCL were evaluated from Fourier transform (FT)-IR spectra. KET-ETH SCL maintained SCL state at 25°C with silica gel over 31 d and at 40°C/89% relative humidity (RH) over 7 d. KET SCL and KET-ETH SCL showed similar permeability of KET for hairless mice skin, which was twofold higher than that of KET aqueous suspension. Our findings suggest that the SCL state could enhance the skin permeation of drugs and the binary SCL formed by intermolecular interaction could also improve the stability of the SCL. The binary SCL system could become a new drug form for transdermal drug delivery.

Solubility Determination and Thermodynamic Correlation of 2-Ethoxybenzamide in 12 Pure Solvents from 288.15 to 328.15 K

“…The onset point of the endothermic melting peak is determined to be 402.95 ± 0.28 K (expanded uncertainty for a 0.95 level of confidence). This value is in good agreement with the previously reported ones in the literature. , However, compared with the melting point reported in ref, there is a deviation between the two values. The possible reasons are that the raw materials of 2-ethoxybenzamide are different, and the operating conditions of DSC are different.…”

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

“…Different from polymer-based ASD, a co-amorphous system possesses lower volume/mass of dosage with superior physical stability [ 6 , 15 ]. Furthermore, drug combinations are also intended to form co-amorphous systems in order to enhance solubility/dissolution of poorly soluble drugs, and also achieve potential combination therapy [ 16 ], such as ketoprofen-ethenzamide [ 17 ] and famotidine and ibuprofen [ 18 ].…”

Self-gelation involved in the transformation of resveratrol and piperine from a co-amorphous system into a co-crystal system

“…Different from polymer-based ASDs, co-amorphous drug delivery systems show superior physical stability with lower volume/mass of dosage. 13,14 Furthermore, drug combinations are also designed to form co-amorphous systems in order to not only increase drug solubility/dissolution but also obtain the advantage of combination therapy, 15 such as ketoprofenethenzamide 16 and famotidine-ibuprofen. 17 Similarly, the preparation of co-crystal systems is also a promising crystalengineering strategy for enhancing the solubility/dissolution and stability of pharmaceuticals as well as implementing potential combined applications.…”