An in vitro aerosolization efficiency comparison of generic and branded salbutamol metered dose inhalers

Background: Due to the high rate of pulmonary diseases, respiratory drug delivery systems have been attracted excessive attention for the past decades. Because of limitations and growing drug bill, physicians are encouraged to prescribe generically whenever possible. The purpose of this study was to evaluate whether there was any significant difference in aerosolization performance between a reference brand Salbutamol (A) Metered Dose Inhalers (MDIs) and two generic products (B and C). Methods: The aerosolization performance of MDIs was evaluated by calculating aerosolization indexes including fine particle fraction (FPF), fine particle dose (FPD), geometric standard deviation (GSD) and mass median aerodynamic diameters (MMAD) by using the next generation impactor. Results: Although aerosolization indexes of MDI A were superior than the Iranian brands, but the differences were not statistically significant. Conclusion: These results verified that generic MDIs deliver similar quantities of Salbutamol to the reference brand and aerosolization performance parameters of generic Salbutamol MDIs did not differ significantly from the reference brand

Development and characterization of nanostructured pharmacosomal mesophases: An innovative delivery system for bioactive peptides

Purpose: To potentially enhance the bioavailability and extend the bioactivity effectiveness of Isoleucine-Proline-Proline (IPP, an antihypertensive bioactive peptide of dairy origin), a novel Lyotropic Liquid Crystalline Pharmacosomal Nanoparticle (LLCPNP) was synthesized, and its physicochemical and technological characteristics were studied. Methods: LLCPNPs precursors were developed using IPP and soy phosphatidylcholine via complex formation. Polarized light microscopy, small angle X-ray scattering, differential scanning calorimetry, dynamic light scattering and Fourier transform infrared spectroscopy were employed to characterize the physicochemical properties of the nanoparticles. The in-vitro release and its related mechanisms were also studied. Results: Fourier transform infrared spectroscopy confirmed the complexation between the components of LLCPNPs. Phase behavior evaluation by polarized light microscope showed the characteristic birefringent texture. These findings along with those of small angle X-ray scattering and differential scanning calorimetry proved the formation of lamellar LLCPNPs. These particles represented nanometric size (<100 nm), high incorporation efficiency (93.72%) and proper physicochemical stability during long-term storage. In-vitro studies demonstrated a sustained release behavior fitted to non-Fickian diffusion and Higuchi kinetic models. Conclusion: The present study results emphasized that LLCPNPs could be proposed as an unrivaled carrier to promote the bioavailability, stability and shelf-life of nutraceutical and biopharmaceutical formulations containing bioactive peptides

Effect of different concentrations of specific inhibitor of matrix metalloproteinases on the shear bond strength of self-adhesive resin cements to dentin

Considering the probability of chemical and enzymatic reactions between matrix metalloproteinases (MMPs) in the dentin structure and their specific inhibitors, the aim of the present study was to evaluate the effect of different concentrations of specific inhibitor of MMPs (galardin) on the shear bond strength of self-adhesive resin cements to dentin. Forty-eight sound human premolars were mounted in self-cured acrylic resin after removal of the enamel on the buccal and lingual surfaces. The dentin surfaces achieved were polished and prepared with 600-grit silicon carbide paper. The samples were divided into 3 groups (n=16) based on the concentration of galardin used (with no galardin, galardin at a high concentration and galardin at a low concentration). In addition, 96 composite resin blocks, measuring 3 mm in height and diameter, were prepared. The composite resin blocks were bonded to the buccal and lingual surface dentin with Rely-X Unicem (RXC) and Speed CEM (SPC) self-adhesive resin cements, respectively, according to manufacturers? instructions. After 24 hours of storage in distilled water at 37°C, the shear bond strength values were determined in MPa and fracture modes were evaluated under a stereomicroscope. Data were analyzed with two-way ANOVA and post-hoc Bonferroni test (?=0.05). The shear bond strength of galardin at high concentration was significantly higher than that in the control group and galardin at a low concentrations (P<0.001). In addition, galardin at a low concentration exhibited higher shear bond strength compared to the control group (P=0.005). Furthermore, higher shear bond strength values were reported with the use of RXC compared to SPC (P<0.001). Irrigation with galardin increased the shear bond strength of self-adhesive resin cements to dentin and this increase had a direct relationship with the concentration of galardin in the solution

Physicochemical and Aerosolization Assessment of Inhalable Spray Dried Fluconazole Powder

Background: Respiratory fungal diseases therapy is still facing challenges as a result of increasing autoimmune disorders, cancers, and immunosuppressive medication usage. Fluconazole is a wide spectrum antifungal agent and is still used successfully in the treatment of opportunistic infections in combination with other antifungal agents. Since, the treatment of respiratory fungal diseases requires prolonged hospitalization; it may increase the chances of other opportunistic infections. Considering the reported drug resistance and adverse effects of systemic administration, it appears that localized pulmonary antifungal therapy may be a suitable alternative route. According to the reported suitable inhalation properties of spray dried powders; spray drying technique was used to prepare fluconazole powders. Methods: Different spray drying parameters such as inlet temperature, pump rate, aspiration%, solvent type, as well as fluconazole concentration were evaluated for powder production. The optimized formulations were characterized using scanning electron microscopy (SEM), x-ray diffraction (XRD), differential scanning calorimetry (DSC) and aerodynamic parameters. Results: All selected formulations showed a smooth surface with similar mass median aerodynamic diameter (MMAD) in a respiratory acceptable range. While optimized powder showed a lower geometric standard deviation (GSD) of 1.5 with higher fine particle fraction (FPF) of 26% and almost complete deposition recovery of 97%. Conclusion: Based on in vitro characterization results, it appears that spray drying is an appropriate and cost-effective technique for the production of inhalable fluconazole powder. It is characterized by a narrower size distribution and delivers a higher dose which may be more cost effective for mass production

Phytosome and Liposome: The Beneficial Encapsulation Systems in Drug Delivery and Food Application

Due to poor solubility in lipids, many of bioactive components (Nutraceutical materials) show less bioactivity than optimal state in water solution. Phytosomes improve absorption and bioavailability of biomaterials. Liposomes, spherical shaped nanocarriers, were discovered in the 1960s by bangham. Due to their composition, variability and structural properties, liposomes and phytosomes are extremely versatile, leading to a large number of applications including pharmaceutical, cosmetics and food industrial fields. They are advanced forms of herbal formulations containing the bioactive phytoconstituents of herb extracts such as flavonoids, glycosides and terpenoids, which have good ability to transit from a hydrophilic environment into the lipid friendly environment of the outer cell membrane. They have better bioavailability and actions than the conventional herbal extracts containing dosage. Phytosome technology has increasing effect on the bioavailability of herbal extracts including ginkgo biloba, grape seed, green tea, milk thistle, ginseng, etc., and can be developed for various therapeutic uses or dietary supplements. Liposomes are composed of bilayer membranes, which are made of lipid molecules. They form when phospholipids are dispersed in aqueous media and exposed to high shear rates by using micro-fluidization or colloid mill. The mechanism for formation of liposomes is mainly the hydrophilic-hydrophobic interactions between phospholipids and water molecules. Here, we attempt to review the features of phytosomes and liposomes as well as their preparation methods and capacity in food and drug applications. Generally, it is believed that phytosomes and liposomes are suitable delivery systems for nutraceuticals, and can be widely used in food industry

Stomach-Specific Drug Delivery of Clarithromycin Using aSemi Interpenetrating Polymeric Network Hydrogel Made ofMontmorillonite and Chitosan: Synthesis, Characterization and InVitro Drug Release Study

Purpose: In this study, we aimed to prepare an extended drug delivery formulation ofclarithromycin (CAM) based on a semi-interpenetrating polymer network (semi-IPN) hydrogel.Methods: Synthesis of semi-IPN hydrogel nanocomposite made of chitosan (CS), acrylicacid (AA), acrylamide (AAm), polyvinylpyrrolidone (PVP), and montmorillonite (MMT) wasperformed by free radical graft copolymerization method. Swelling kinetic studies were done inacidic buffer solutions of hydrochloric acid (pH = 1.2), acetate (pH = 4), and also distilled water.Also, the effects of MMT on the swelling kinetic, thermal stability, and mechanical strengthof the hydrogels were evaluated. Moreover, in vitro release behavior of CAM and its releasekinetics from hydrogels were studied in a hydrochloric acid buffer solution.Results: Fourier transform infrared spectroscopy (FTIR) results revealed that synthesis of semi-IPN superabsorbent nanocomposite and CAM incorporation into hydrogel was performed,successfully. Introducing MMT into hydrogel network not only improved its thermal stabilitybut also increased mechanical strength of the final hydrogel product. Also, in comparisonwith neat hydrogel (1270 g/g), hydrogel nanocomposite containing 13 wt% MMT exhibitedgreater equilibrium swelling capacity (1568 g/g) with lower swelling rate. In vitro drug releaseexperiments showed that CS-g-poly(AA-co-AAm)/PVP/MMT/CAM formulation possesses asustained release character over extended period of time compared with CS-g-poly(AA-co-AAm)/PVP/CAM formulation.Conclusion: In the presence of MMT, the effective life time of drug is prolonged, demonstrating asustained release property. The reason is that interlinked porous channels within superabsorbentnanocomposite network hinder penetration of aqueous solutions into hydrogel and subsequentlycause a slower drug release