Development of meloxicam potassium-containing co-spray-dried inhalation powder with sodium stearate

Abstract

Pulmonary drug delivery (PDD) has potential for both local and systemic therapy. Our research group is focus- ing on the development of dry powder inhalation (DPI) systems for PDD due to their beneficial properties. Although there is not yet a marketed inhalation product for non-steroidal anti-inflammatory drugs (NSAIDs), their therapeutic use in sev- eral lung diseases is well established and successful DPI developments have been performed with them. Sodium stearate (NaSt) is a promising excipient for DPI development, but its role in NSAIDs has not yet been investigated. Thus, the aim was to study DPI samples produced by co-spray-drying, applying meloxicam potassium (MXP) as an NSAID drug, and different concentrations (0-2 w/w%) of NaSt. Physicochemical investigations, in vitro lung deposition, and in vitro drug release measurements were performed. It can be stated that co-spray-drying of MXP with NaSt resulted in remarkable morphological differences by increasing the concentration of NaSt, which had a positive effect on cohesive work. Further- more, applying of NaSt accelerates the dissolution in simulated lung fluid (SLF). NaSt as excipient has a future for the formulation of the DPI systems because there are in the development focus the attaintment of the higher FPF values and improvement of dissolution in SLF.

Development of novel formulated ciprofloxacin hydrochloride containing dry powder inhalation system

“…Mechanical dry coating of classical large carriers is also possible with fine carrier particles, which are also called "secondary carriers". The average size of these particles is smaller compared to that of the classic large carriers, but their optimal diameter for DPI systems has not yet been agreed upon, with some studies suggesting a particle size of around 5-8 µm as an ideal range [46].…”

“…There is still a wide range of in vitro (and in vivo) lung deposition results of marketed and published DPI formulations, not to mention inhalers and patients as influencing factors. The manufacturing of DPI formulations has a lot of potentials, as the number of active ingredients, excipients, preparation methods, and parameters used is huge [46,47]. Basically, 2 main groups of formulations are distinguished in the literature for DPIs: traditional carrier-based and carrier-free composites.…”

“…On the other hand, besides α-lactose monohydrate, which is currently the most dominant carrier for commercialized carrier-based DPIs, other carrier candidates have come to the fore due to their favorable properties and test results e.g. mannitol, glucose monohydrate, sorbitol, etc [46]. In addition, a number of developments have in recent years been made in the field of surface treatment of carrier particles, which are summarized in Figure 3.…”

“…reduced roughness) by coating with fluidization (e.g. α-lactose monohydrate carrier hydroxypropyl methylcellulose (HPMC), distilled water, and lactose-containing coating fluid), which has been reported to lead to enhanced in vitro lung deposition results [46]. Besides the wet surface modification methods described so far, the fourth option is the mechanical dry coating of the carrier particles, which is also aimed at improving lung deposition results.…”

“…The powder mixtures were prepared according to the rules of powder blending before Turbula mixing. The surface modification of the carrier (IH70) was completed by using 2.0 w/w% of MgSt relative to the final formulations [84,[111][112][113] -Table 8.with Turbula blending for 4 h [114].…”