Micronized Zaleplon Delivery via Orodispersible Film and Orodispersible Tablets

Abstract

The following research study focuses on improving the solubility of zaleplon (BCS class II drug) via micronization technique in order to enhance its oral delivery in orodispersible formulations. Zaleplon along with a surfactant solution was micronized by ultrasonication. The micronization process reduced the particle size of the crystalline drug about six-fold from its original size of 155.5 μm. The micronized zalepon dispersion was lyophilized to allow for a change in the state of matter (to a powder). The superior dissolution parameters (Q, Q, IDR, MDR, MDT, DE, and RDR) of zaleplon in microcrystalline form over the original crystalline form in in vitro dissolution studies had unraveled that micronization technique is an efficient tool in enhancing drug solubility. The micronized zaleplon solid dispersion (after lyophilization) was loaded into orodispersible tablet (ODT) and orodispersible film (ODF) formulations. The positive quality of ODT with adequate hardness and smooth texture was attributing to the presence of Pearlitol Flash® as a ready to use ODT platform. On the other hand, the ODF loaded with micronized zaleplon and prepared with Lycoat® RS 720 (as a film former) ensured adequate tensile strength. The disintegration time of ODT and ODF was 30 ± 5 and 35 ± 5 s, respectively. Thus, the orodispersible formulations containing micronized zaleplon have a strong potential for rapid disintegration following superior absorption in solution state through oral cavity into the blood stream, envisaging better oral delivery.

Enhancement of zaleplon oral bioavailability using optimized self-nano emulsifying drug delivery systems and its effect on sleep quality among a sample of psychiatric patients

“…Dissolution of CF12 was studied compared to control Zal capsules using USP dissolution apparatus type II (paddles) rotating at 75 rpm (Manda et al., 2018). The dissolution was performed in 300 ml of HCl (pH1.2) at 37 ± 0.5 °C.…”

“…Different strategies have been adopted by formulators to improve the bioavailability of Zaleplon. Solid dispersions, oro-dispersible films, inclusion complexes using cyclodextrin and micro-/nanoemulsions are examples for these strategies (Waghmare et al., 2008; Abd-Elrasheed et al., 2018; Manda et al., 2018). Nano-scale technologies/carriers have been utilized for improving solubility of hydrophobic drugs and hence their therapeutic performance.…”

Oromucosal films: from patient centricity to production by printing techniques

“…ethanol to improve the solubility of diazepam [46]) or the addition of solubility enhancers [47], the use of organic acids to influence pH-dependent solubility [48], the use of mesoporous silica nanoparticles as a carrier for poorly water-soluble drugs (e.g. prednisolone) [49], and micronization of the API to reduce its particle size [50]. Particle size reduction is an often used method to improve the solubility of poorly watersoluble APIs [51][52][53][54][55][56].…”

The potential of ODFs as carriers for drugs/vaccines against COVID-19

“…ODFs are excellent and attractive carriers for delivery of various over the counter (OTC) or prescription drugs [17], herbal extracts [18][19][20][21], vaccines [22], probiotics [23], and vitamins [24]. Drugs are either directly introduced [25][26][27][28] in the formulation of ODFs or size reduced and converted to solid dispersions [29] or nanoparticles [30,31] or solid lipid microparticles [32] or micronized and surface modified using silica [33] which not only help in enhancing the amount of drug that could be loaded on to ODFs but also help in enhancing the release rate and, bioavailability of the drug. At present, ODFs are used as an excellent carrier system for delivering various therapeutically active agents.…”