Rapidly dissolving bilayer microneedle arrays – A minimally invasive transdermal drug delivery system for vitamin B12

Abstract

Vitamin B12 plays an essential role in one-carbon metabolism in the human body. A deficiency in this vitamin can lead to severe haematopoietic and neuropsychiatric disorders and is currently treated by oral or parenteral administration of exogenous vitamin. Unfortunately, the absorption of orally taken vitamin B12 is low and highly variable, while injections can cause pain and anxiety. Thus, an efficient alternative drug delivery system for overcoming these shortcomings is highly desirable. Novel polymeric microneedle (MN) arrays have the potential for minimally invasive transdermal treatment of vitamin B12 deficiency. Bilayer dissolving MN arrays (19 x 19 needles, 600 µm height) containing 135 µg vitamin B12 were cast using two different aqueous polymer blends. MN arrays showed sufficient mechanical strength for skin insertion, dissolved rapidly and delivered 72.92% of their drug load in vitro over 5 h. Ultimately, the potential of delivering a therapeutically relevant dose of vitamin B12 transdermally was demonstrated in vivo in Sprague-Dawley rats by comparison to subcutaneous injections. Maximum plasma levels of 0.37 µg/mL occurred 30 min post-MN application, highlighting the ability of fabricated MN arrays to rapidly deliver vitamin B12 transdermally.

Microneedle-Based Delivery: An Overview of Current Applications and Trends

“…The maximum plasma concentration (Cmax) of vitamin B12 after MNA application was 0.37 ± 0.04 μg/mL, while the subcutaneous administration provided a Cmax of 1.30 ± 0.25 μg/mL. No drug was detectable after 24 h in the animals treated with the subcutaneous injection, while the vitamin could be detected in animals treated with MNA after 30 h, proving that MNA provided an extended release [ 145 ].…”

Spun Biotextiles in Tissue Engineering and Biomolecules Delivery Systems

“…The absence of several types of vitamins in the human body can lead to severe health problems ranging from megaloblastic anemia to Parkinson's disease [225,226]. In an attempt to improve transdermal delivery of Vitamin B12, Vitamin E and Vitamin A and surpassing more effectively the skin barrier, Madhaiyan et al [219] and Taepaiboon et al [227] explored alternative routes based on nanofibrous constructs made of PCL and cellulose acetate, respectively.…”

“…In an attempt to improve transdermal delivery of Vitamin B12, Vitamin E and Vitamin A and surpassing more effectively the skin barrier, Madhaiyan et al [219] and Taepaiboon et al [227] explored alternative routes based on nanofibrous constructs made of PCL and cellulose acetate, respectively. Vitamin B12 (cobalamin) is a water-soluble vitamin necessary for red blood cell formation, neurological function and DNA synthesis and is naturally present in some foods [226]. In turn, Vitamin E and Vitamin A acid are lipid-soluble substances that prevent skin disorders and have antioxidant properties [227].…”

Novel Design Approaches in the Fabrication of Polymeric Microarray Patches via Micromoulding

“…Thus, pain or bleeding do not occur. Increasing evidence is displayed in the literature of the great promise of MAPs to enhance the transdermal delivery of both low-and high-molecular-weight therapeutic agents [5][6][7][8][9][10][11][12][13][14]. Research has focused on different types of MAPs made from a wide range of materials.…”