Abstract
Vitamin B12 deficiency, which may result in anemia and nerve damage if left untreated, is currently treated by administration of cyanocobalamin via oral or intramuscular routes. However, these routes are associated with absorption and compliance issues which have prompted us to investigate skin as an alternative site of administration. Delivery through skin, however, is restricted to small and moderately lipophilic molecules due to the outermost barrier, the stratum corneum (SC). In this study, we have investigated the effect of different enhancement techniques, chemical enhancers (ethanol, oleic acid, propylene glycol), iontophoresis (anodal iontophoresis) and microneedles (soluble maltose microneedles), which may overcome this barrier and improve cyanocobalamin delivery. Studies with different chemical enhancer formulations indicated that ethanol and oleic acid decreased the lag time while propylene glycol based formulations increased the lag time. The formulation with ethanol (50%), oleic acid (10%) and propylene glycol (40%) showed the maximum improvement in delivery. Iontophoresis and microneedle treatments resulted in enhanced permeation levels compared to passive controls. These enhancement approaches can be explored further to develop alternative treatment regimens.
Highlights
Vitamin B12 is essential for the development of red blood cells, body growth, and maintenance of the nervous system [1]
We have evaluated the permeation profiles of cyanocobalamin, in vitro, to study the effects of chemical enhancers, iontophoresis and microneedles on its transdermal delivery
To check the effect of chemical and physical enhancement techniques on delivery of cyanocobalamin, the donor concentration was selected as 10 mg/mL
Summary
Vitamin B12 is essential for the development of red blood cells, body growth, and maintenance of the nervous system [1]. Application of transdermal delivery to a wider range of drugs is limited due to the outermost barrier of skin, the stratum corneum. Various approaches have been undertaken to enhance the delivery of drugs through skin These strategies include passive/active chemical and physical permeation enhancement techniques to bypass the stratum corneum barrier. Chemical penetration enhancements (CPEs) are present in a large number of transdermal, dermatological, and cosmetic products to aid dermal absorption of curatives and anesthetics. They provide several advantages such as design flexibility with formulation chemistry, patch application over a large area (>10 cm2) and the absence of external physical delivery mechanisms. To characterize the effects of chemical enhancement on the stratum corneum
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