Abstract
In many instances, one or more components of a pharmaceutical or cosmetic formulation is an oil. The aims of this study were two-fold. First, to examine the potential of preferential uptake of one oily vehicle component over another into a model barrier membrane (silicone) from blended vehicles (comprising two from the common excipients isohexadecane (IHD), hexadecane (HD), isopropyl myristate (IPM), oleic acid (OA) and liquid paraffin). Second, to study the effect of membrane-vehicle interactions on the diffusion of model permeants (caffeine (CF), methyl paraben (MP) and butyl paraben (BP)) from blended vehicles. Selective sorption and partition of some oils (especially IHD and IPM) at the expense of other oils (such as OA) was demonstrated to take place. For example, the membrane composition of IHD was enriched compared to a donor solution of IHD-OA: 41%, 63% and 82% IHD, compared to donor solution composition of 25%, 50% and 75% IHD, respectively. Pre-soaking the membrane in IHD, HD or LP, rather than phosphate buffer, enhanced the flux of MP through the membrane by 2.6, 1.7 and 1.3 times, respectively. The preferential sorption of individual oil components from mixtures altered the barrier properties of silicone membrane, and enhanced the permeation of CF, MP and BP, which are typically co-formulated in topical products.
Highlights
The passage of compounds through a biological membrane after topical application is divided into four main stages
Artificial membranes are often used during the development of a formulation to aid in the process of selecting a vehicle and excipients or alternatively as a quality control tool [17]
There are potentially a large number of bi-component mixtures that can be generated from the oils used in the current study, and the oils are frequently present as mixed blends in pharmaceutical and cosmetic products
Summary
The passage of compounds through a biological membrane after topical application is divided into four main stages. If a vehicle component interacts with the membrane in some way, it may alter the membrane’s physicochemical properties This in turn is likely to lead to the changed permeation of a co-formulated compound through the modified membrane in comparison to the original, unmodified membrane (e.g., if the compound is delivered using a non-interacting vehicle). This could be as a consequence of inducing change in the partition of the compound into the vehicle-containing membrane or by a direct effect on the barrier properties of the membrane, resulting in the modulation of drug transport [2]. In some cases, the delivery and penetration of the vehicle to the membrane can be as important as that of the drug itself
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