Current Issue : January-March Volume : 2024 Issue Number : 1 Articles : 5 Articles
In this present formulation study, vinpocetine-loaded nano-spray-dried polymeric micelles were developed via nano-spray-drying. Three different mucoadhesive excipients were applied in the studies, namely chitosan, hyaluronic acid and hydroxypropyl methylcellulose. In all cases, the formulations had a proper particle size and drug content after drying with spherical morphology and amorphous structure. After rapid dissolution in water, the polymeric micelles had a particle size around 100–130 nm, in monodisperse size distribution. The high encapsulation efficiency (>80%) and high solubilization (approx. 300-fold increase in thermodynamic solubility) contributed to rapid drug release (>80% in the first 15 min) and fast passive diffusion at simulated nasal conditions. The formulated prototype preparations fulfilled the demands of a low-viscosity, moderately mucoadhesive nasal drug delivery system, which may be capable of increasing the overall bioavailability of drugs administered via the auspicious nasal drug delivery route....
Amorphous solid dispersions (ASDs) enable formulations to improve the solubility of poorly soluble active pharmaceutical ingredients (APIs). The amorphous state is reached through the disruption of the crystalline lattice of an API resulting in an increased apparent solubility with faster disintegration. Nevertheless, this form is characterized by a high-energy state which is prone to re-crystallization. To ensure a stable ASD, excipients, e.g., polymers that form a matrix in which an API is dispersed, are used. The applicable polymer range is usually linked to their solubility in the respective solvent, therefore limiting the use of hydrophilic polymers. In this work, we show the applicability of the hydrophilic polymer, polyvinyl alcohol (PVA), in spray-dried solid dispersions. Using a three-fluid nozzle approach, this polymer can be used to generate ASDs with a targeted dissolution profile that is characterized by a prominent spring and desired parachute effect showing both supersaturation and crystallization inhibition. For this purpose, the polymer was tested in formulations containing the weakly basic drug, ketoconazole, and the acidic drug, indomethacin, both classified as Biopharmaceutics Classification System (BSC) class II drugs, as well as the weakly basic drug ritonavir classified as BCS IV. Furthermore, ritonavir was used to show the enhanced drug-loading capacity of PVA derived from the advantageous viscosity profile that makes the polymer an interesting candidate for spray drying applications....
α–Mangostin, which is a natural xanthone compound, inhibits the metastasis and survival of various cancer cell types. However, its therapeutic effectiveness is limited by low water solubility and very poor absorption. There are several studies that developed the drug delivery system for α–mangostin, but they are still a remaining challenge. Drug delivery techniques are severely hampered by the breakdown of nanoparticles inside endosomes. The abrasive chemical environment in these compartments causes both the nanoparticles and the encapsulated α–mangostin to degrade throughout the course of the voyage. Intracellular defenses against external materials refer to this collective mechanism. A pH-responsive liposome named PAsp(DET-Cit)–Toc, made of lipids and a charge-conversion polymer (CCP), has been created for the targeted transport of α–mangostin in order to avoid this deteriorative outcome. The average hydrodynamic size of CCP–liposome particles is 98.59 ± 5.1 nm with a PDI of 0.098 ± 0.02 and a negative zeta potential of 22.31 ± 2.4 mV. TEM showed the shape of the spherical CCP–liposomes. α–Mangostin is successfully captured inside CCP– liposome and the loading yield reached the highest encapsulation efficiency of 83% with 150 μg/mL of α–mangostin. In the acidic condition of pH 5.0, an initial burst of α–mangostin reached 50% after 6 h in buffer solution. CCP–liposomes could escape from endosomes even after 3 h, and almost 80% of CCP–liposomes escaped after 24 h. The cell ability of α–mangostin-loaded-CCP–liposome incubated in buffer solutions of 5.0 decreased significantly and was close to free α–mangostin. Our data proved that α–mangostin-loaded CCP–liposome delivered more effectively α–mangostin into cells and prevented the degradation of α–mangostin inside cells, especially endosomal degradation....
Nausea and vomiting are symptoms associated with a lot of diseases and oral tablets may be unprofitable for patients especially those suffering from nausea and vomiting. Therefore, this study aimed to formulate a new meclizine and pyridoxine combination formula for chewable tablets and provide rapid drug absorption and decrease motion sickness. The new chewable formulation has been prepared to provide fast action, is more acceptable, and could be used for all age categories. Seven trials haves been carried out to prepare to find the suitable one where formula 7 of the chewable gum preparation exhibited good taste and hardness, while the gelatin formulation give an accepted formula after four trials with better taste and good acceptance. The prepared formulations give a dissolution profile of meclizine (95.53–102.8%) and pyridoxine (99.25 ± 115%) and assay (98 + 0.05–99.3 ± 0.8%) for meclizine and (97 ± 0.9–100.0 ± 0.08%) for the pyridoxine in three prepared formulations of chewable tablets. Followed by the evaluation, the formulation and testing them on human volunteers are carried out to confirm their effect to ensure acceptance and fast actions. The finding is promising for preparing a new route of administration of meclizine and pyridoxine combination to be used in the market....
Spray freeze-drying has emerged as a valid alternative to traditional spray drying to produce therapeutic dry microparticles. In particular, the spherical shape and high porosity of spray freeze-dried microparticles make them suitable for pulmonary drug delivery through dry powder inhalers. However, an appropriate particle size and fine particle fraction are required to guarantee lung deposition. This study used ultrasonic spray freeze-drying to generate dry microparticles composed of mannitol either alone or added with the bronchodilator salbutamol sulphate. The influence of the solid concentration and the feed flow rate on the particle size, morphology, surface area, porosity, and crystallinity was investigated. Growing particle size was observed, increasing the concentration and feed flow rate. Similarly, the addition of the drug led to a larger particle size and surface area. The in vitro simulation of drug deposition highlighted the dependence of the aerodynamic properties on the solid concentration and feed flow rate. Due to the lower density and particle geometric size, the highest fine particle fraction (26%) and smallest mass median aerodynamic diameter (4.4 μm) were reached at the lowest solid concentration and feed flow rate....
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