Administration of Micronized Caffeine Using a Novel Oral Delivery Film Results in Rapid Absorption and Electroencephalogram Suppression

Abstract

Route of administration is well-known to impact factors ranging from absorption and distribution, up through the subjective effects of active ingredients. Different routes of administration confer specific advantages, such as more rapid absorption resulting from intravenous injection, or increased convenience with oral administration, but a combination of both rapid and convenient delivery is highly desirable. QuickStrip™ was designed as a rapidly dissolving thin film matrix that contains active ingredients, which may be promising for rapid and convenient delivery via the oral mucosa. To assess the delivery of QuickStrip™, we administered the well-characterized active ingredient caffeine to mice and compared QuickStrip™ to standard oral gavage delivery at an equivalent dose of 20 mg kg-1. Using HPLC assessment of serum concentrations of caffeine, we found that QuickStrip™ delivery resulted in higher serum levels of caffeine at 1, 10, and 30 min following administration compared to gavage. QuickStrip™ also produced greater bioavailability compared to gavage, as demonstrated by area under the curve analysis. Caffeine delivered by QuickStrip™ produced robust behavioral activation of locomotion, consistent with gavage caffeine. Electroencephalographic (EEG) assessment of central nervous system effects demonstrated that both gavage and QuickStrip™ caffeine produced suppression of delta and theta, consistent with prior literature on the effects of caffeine. In addition, QuickStrip™ produced a more rapid onset of EEG suppression, supporting the more rapid absorption demonstrated in the serum studies. Collectively, these studies suggest that QuickStrip™ may provide a balance between convenience and rapid onset, offering new options for delivery of therapeutics.

Effect of caffeine in chocolate (Theobroma cacao) on the alveolar bone mineral density in guinea pigs (Cavia cobaya) with orthodontic tooth movement

“…In addition, the route or method of administration can also affect the amount of active concentration of caffeine on the body's physiological response. 25 The oral administration of gavage tends to have a slow onset of therapeutic effect, causing the caffeine potential to decrease due to metabolic processes in the gastrointestinal tract and liver.…”

Behavioral arrest and a characteristic slow waveform are hallmark responses to selective 5-HT2A receptor activation

“…Electroencephalography (EEG) and electromyography (EMG) electrodes were implanted under isoflurane anesthesia. Two channels of EEG were recorded bilaterally from the frontal cortex, with ground supplied by placement of an electrode in the caudal parietal area 66 , 67 . Following implantation, mice were divided randomly into 25I-NBOH or 25I-NBOH with nicotine pretreatment (n = 6) groups.…”

“…EEG data before administration provided baseline, allowing the same animals to be used as their own control. After a minimum of 7 days of postoperative recovery, EEG activity was recorded at a sampling rate of 1000 Hz using the Pinnacle system for mouse during the first four hours of the dark phase of the 24 h cycle 66 , 67 . Mice were first acclimatized to the recording chamber and preamplifier for 60 min, then injected with 0.5% DMSO in PBS vehicle before recording at least 60 min of baseline.…”

“…Mice were first acclimatized to the recording chamber and preamplifier for 60 min, then injected with 0.5% DMSO in PBS vehicle before recording at least 60 min of baseline. During baseline recordings, sleep was suppressed or interrupted by introduction of novel objects as necessary following procedures from our prior studies 66 , 67 . After at least 60 min of baseline, mice were administered 25I-NBOH via intraperitoneal injection.…”

Preparation, Characterization and Studies of Physicochemical and Biological Properties of Drugs Coating Lactose in Fluidized Beds

“…The activation conditions of samples have been chosen based on the advantages of transmucosal (buccal and sublingual) delivery: the rate of action associated with high vascularization of mucosal zones, the possibility of reducing the therapeutic dosage, no need to drink water, the absence of destruction outside of gastrointestinal digestive enzymes with efficiency, simplicity and cost-effectiveness of production [50,51].…”