Abstract
Insomnia is becoming increasingly prevalent in the world general population. Therapies used by patients include over-the-counter therapies, herbal and dietary supplements, and pharmacological or nonpharmacological treatments. Among these, zolpidem is a pharmacological treatment popularly used for insomnia. Zolpidem is well tolerated and especially efficacious for initiation of sleep, and therefore is effective for the treatment of sleep-onset insomnia. The purpose of the present study was to design and evaluate zolpidem nanoparticle-impregnated buccal films to prolong the duration of its action. Zolpidem nanospheres were prepared by double emulsion solvent evaporation and then loaded into buccoadhesive films (Z1-Z4) comprised of different concentrations of HPMC K100, Eudragit® RL 100, and carbopol 974P. The prepared films were characterized for physicomechanical properties, mucoadhesion, percent hydration, in vitro drug release, ex vivo permeation, and in vivo studies. In vitro drug release was found to depend upon film composition. Ex vivo studies showed that film Z4 had the highest flux. In vivo studies revealed that administration of zolpidem nanosphere-impregnated film enhanced absorption of the drug (p < 0.0001), with a higher peak plasma concentration (52.54 ± 8.22 ng/mL) and area under the curve from time 0 to α (236.00 ± 39.51 ng.h/mL) than oral administration. The increase in time taken to reach the maximum drug concentration (1.5 h) further signifies the potential of these films to provide prolonged drug release. Given these promising results, we concluded that these buccal films could be an alternative route for effective zolpidem delivery.
Highlights
Insomnia is becoming increasingly rampant, affecting from 10% to around 60% of the general population.[1]
We propose an alternative drug delivery route involving a buccoadhesive film impregnated with zolpidem nanospheres that can provide a rapid onset of action together with prolonged release from poly(lactic-co-glycolic acid) [PLGA] nanospheres
A number of buccal films impregnated with nanospheres have been developed and shown to enhance the therapeutic efficacy of drugs, improve pharmacokinetic profiles, and modulate drug release.[24,25]
Summary
Insomnia is becoming increasingly rampant, affecting from 10% to around 60% of the general population.[1]. Pharmacological treatments include the use of hypnotics. First-generation hypnotics (barbiturates, carbamates, chloral hydrate, and methaqualone) typically exert a prolonged hypnosedative effect, which impacts patient work performance the following day. Benzodiazepine hypnotics were introduced in the 1970s and were a major breakthrough in the treatment of insomnia. Compared to first-generation hypnotics, benzodiazepine hypnotics show improved safety in terms of tolerance and withdrawal effects. Side effects, such as hangover, dependency, and rebound insomnia, can occur with declining use.[8] benzodiazepines still fall short of being ideal compounds for promoting physiological sleep
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