Route and Type of Formulation Administered Influences the Absorption and Disposition of Vitamin B12 Levels in Serum

Abstract

The administration of biological compounds that optimize health benefits is an ever-evolving therapeutic goal. Pharmaceutical and other adjunctive biological compounds have been administered via many different routes in order to produce a systemic pharmacological effect. The article summarizes the findings from an Australian comparative study in adults administered vitamin B12 through different oral delivery platforms. A total of 16 subjects (9 males, 7 females) voluntarily partook in a comparative clinical study of five different vitamin B12 formulations across a six-month period, completing 474 person-hours of cumulative contribution, that was equivalent to an n = 60 participation. A nanoparticle delivered vitamin B12 through a NanoCelle platform was observed to be significantly (p < 0.05) better absorbed than all other dose equivalent platforms (i.e., tablets, emulsions, or liposomes) from baseline to 1, 3, and 6 h of the study period. The nanoparticle platform delivered vitamin B12 demonstrated an enhanced and significant absorption profile as exemplified by rapid systemic detection (i.e., 1 h from baseline) when administered to the oro-buccal mucosa with no reports of any adverse events of toxicity. The nanoparticle formulation of methylcobalamin (1000 µg/dose in 0.3 mL volume) showed bioequivalence only with a chewable-dissolvable tablet that administered a five times higher dose of methylcobalamin (5000 µg) per tablet. This study has demonstrated that an active metabolite embedded in a functional biomaterial (NanoCelle) may constitute a drug delivery method that can better access the circulatory system.

The Plasma Bioavailability of Coenzyme Q10 Absorbed from the Gut and the Oral Mucosa

“…We have previously reported on the absorption and blood levels achieved with orally administered vitamin B 12 formulations [25]. In that study, we investigated a nanotechnology-based micelle formulation, developed to capture the idea of exploiting the delivery of organic molecules at the nanometre scale via the oro-buccal mucosa [25]. Oro-buccal delivered formulations, such as that achieved with vitamin B 12 , demonstrated a more enhanced bioavailability than capsules, tablets, or a liposome formulation.…”

“…Nanotechnology-based delivery systems present platforms that could allow for the safe and efficacious delivery of poorly intestinally absorbed molecules, such as CoQ 10 . We have previously documented the safety, tolerability, and efficacious delivery of a vitamin complex in a micelle nanoparticle delivery system [25], and as such, provide further knowledge to progress the basic research efforts to a nanoparticle CoQ 10 formulation.…”

Current Nanocarrier Strategies Improve Vitamin B12 Pharmacokinetics, Ameliorate Patients’ Lives, and Reduce Costs

“…Indeed, lipid-based nanoparticles have been used to deliver lipophilic active substance via the facial lymphatics and in turn into the systemic circulation [58,89]. In a recent study, the authors have compared different oral preparations including nanocarriers to administer VitB12 in healthy people [90]. In particular, they observed the level of VitB12 in the plasma after six hours of the administration of 1000 mg of VitB12 given in four different buccal preparations including two oral spray formulations consisting of methylcobalamin embedded in liposomes (approximately 100 nm) and methylcobalamin encompassed in 20 nm nanoparticles (NanoCelle) made up of a hydrophobic core and an outer hydrophilic shell [90].…”

Methylcobalamine (Vitamin B12): Water Soluble Vitamin with Various Pharmacological Aspect

“…4 Vitamin B12 is a water-soluble vitamin that plays a crucial role in the proper functioning of the brain and nervous system, blood production, and stress and fatigue control. 5,6 • Types of vitamin B12…”