Optimisation of Cosolvent Concentration for Topical Drug Delivery III – Influence of Lipophilic Vehicles on Ibuprofen Permeation

Abstract

Previously, we have reported the effects of water, ethanol, propylene glycol and various binary and ternary mixtures of these solvents on the permeation of ibuprofen in model membranes and in skin. The present study investigates the influence of lipophilic vehicles on the transport of ibuprofen in silicone membrane and in human skin. The permeation of ibuprofen was measured from mineral oil (MO), Miglyol® 812 (MG) and binary mixtures of MO and MG. The solubility of ibuprofen was 5-fold higher in MG than in MO, however, the permeation of ibuprofen from the pure vehicles and combinations of both was comparable in silicone membrane. Additionally, there were no significant differences in skin permeation for MO and MG vehicles. When the permeation of various hydrophilic and lipophilic vehicles is considered, a trend between flux values for the model membrane and skin is evident (r² = 0.71). The findings suggest that silicone membrane may provide information on qualitative trends in skin permeation for vehicles of diverse solubility and partition characteristics.

In vitro skin models as a tool in optimization of drug formulation

“…Dias et al (2007) conducted a study on a wide selection of vehicles (mineral oil, isopropyl myristate, oleic acid, decanol, octanol, butanol, ethanol, propylene glycol, glycerin and water as well as their mixtures) on the permeation of caffeine, salicylic acid and benzoic acid. For example, the effect of both hydrophilic and lipophilic vehicles (water, ethanol, propylene glycol, mineral oil, Miglyol 812) on the penetration of ibuprofen has been studied (Watkinson et al, 2009a;Watkinson et al, 2009b;Watkinson et al, 2011). The studies on the molecular mechanism of interaction between different vehicles (ethanol, isopropyl myristate, dimethyl isosorbide, PEG 200 and PEG 400 and Transcutol P ® ) with the model membranes, through the thermodynamic and kinetic analyses of the uptake, membrane partitioning and transport studies of a model compound, have also been conducted (Oliveira et al, 2010;Oliveira et al, 2011;Oliveira et al, 2012).…”

Oral transmucosal delivery of naratriptan

“…The cumulative amount of drug permeated per unit area of buccal mucosa (µg/cm 2 ) was plotted against the collection time (min) using Excel 2010 (Microsoft, USA) as reported previously. The slope of this graph at the steady state was considered as the flux (Jss) and the extrapolated x-axis intercept as the lag time (tlag) as reported by Watkinson et al (2010). The cumulative amount/area (Qn) at time (n) was determined and the permeability coefficient (kp) was calculated from Jss as reported in our previous publication (Sattar et al, 2015).…”

Basiscreme DAC: Characteristics and possibility of use for compounding drugs in pharmacy

“…Poznato je da promene u sastavu podloge u preparatima različitih proizvođača sa istom lekovitom supstancom, u istoj koncentraciji, uslovljavaju razlike u ishodima lokalne dermatološke terapije. Rezultati brojnih istraživanja pokazuju da izbor pomoćnih supstanci utiče na sudbinu lekovite supstance u koži (2)(3)(4). Ovo predstavlja svojevrstan problem, budući da nije moguće formirati sistem za međusobno poređenje dermatoloških preparata, prema jačini dejstva.…”