Fundamental investigation of a novel drug delivery system, a transdermal delivery system with jet injection

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Abstract

A new drug delivery system simultaneously using jet injection and a transdermal delivery system was proposed. After pretreatment of hairless rat skin by a jet injector containing physiological saline without any drug to make a pore in the skin, aqueous solution containing gentamycin sulfate, nicardipine hydrochloride or theophylline was applied on the pore. Absorption clearance (volume flow rate) through the skin (the product of permeability coefficient and application area) was almost the same (0.4 μl/h) with any type of drug and regardless of properties and concentrations. Plasma concentration of gentamycin when the distance between the injector and skin surface was 5 mm was twice that when there was no space between the two. It was found by morphological observation that injection from 5 mm away made a larger pore in the stratum corneum (about 0.3 mm2) and a clear saline reservoir in the viable epidermis and dermis. Mathematical analysis showed that this larger pore greatly increased the skin delivery (absorption) rate, whereas the saline reservoir increased it little. This high delivery rate continued for over 1 week with theophylline.

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    Citation Excerpt :

    Various mechanical, electrical, and chemical approaches have been used in the past to breach the SC barrier. While chemical penetration enhancers (Williams and Barry, 2004) interact directly with lipid bilayers, extracting and/or fluidizing lipids in the SC, many physical methods such as jet injectors (Inoue et al., 1996) and microneedles (McAllister et al., 2003) employ mechanical perturbation of the SC for injecting molecules of interest into the skin. Electrical methods such as iontophoresis (Meyer et al., 1988) employ voltage gradients for solute migration or electroporation (Prausnitz et al., 1993), which involves high-voltage pulses for shorter time periods to open up pathways in the SC.

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