Current Issue : January - March Volume : 2021 Issue Number : 1 Articles : 5 Articles
Theobjective of the current study was to introduce “Polylactic co-GlycolicAcid- (PLGA-) Coated CeramicMicroparticles” as an innovative drug delivery system, loaded with a new combination of triple antibiotics (penicillin G, metronidazole, and ciprofloxacin (PMC)) for use in endodontic treatments. Ceramic microparticles were made from β-tricalcium phosphate and hydroxyapatite and examined by “Scanning Electronic Microscope (SEM).” Then, fixed amounts of the selected antibiotics were added to a prepared PLGA solution and stirred thoroughly. Next, the prepared ceramic microparticles were dispersed completely in the drugs solution. The deposited “PMC-loaded PLGA-coated ceramic microspheres (PPCMs)” were dried and incubated in phosphate buffer saline (PBS) for 21 days. The drug release from PPCMs was quantified by a UV spectrophotometer. The antimicrobial activity of PPCMs was investigated using the “Agar Plate Diffusion Test (ADT),” “Minimum Inhibitory Concentration (MIC),” and “Minimum Bactericidal Concentration (MBC)” against Enterococcus faecalis (E. faecalis) and Aggregatibacter actinomycetemcomitans (A.a). The cell viability test (MTT) was conducted for cytotoxicity against human gingival fibroblasts. SEM micrographs of PPCMs showed spherical-like ceramic microparticles with smooth surfaces. Crystal-like antibiotic particles (chunks) were also found on PPCMs. Initial burst of antibiotics (31 μg/mL, 160 μg/mL, and 18 μg/ mL for ciprofloxacin, metronidazole, and penicillin G, respectively, in the first 4 days) followed by gradual and sustained release was observed within a period of 21 days. PPCMs demonstrated pH close to normal physiological environment and antibacterial activity against E. faecalis and A.a in the first 2 days.MTTshowed cell viability of more than 70%for PPCMs after 24 h and 72 h of exposure. In conclusion, PPCMs demonstrated satisfactory release of antibiotics, antibacterial activity against the selected microorganisms, and biocompatibility. Thus, PPCMs may be used to deliver modified triple antibiotics to the root canal system for use in endodontic applications....
The purpose of this study was to improve the bioavailability of carbamazepine (CBZ), a poorly water-soluble antiepileptic drug, via modified-release amorphous solid dispersions (mr-ASD) by a thin film freezing (TFF) process. Three types of CBZ-mr-ASD with immediate-, delayed-, and controlled-release properties were successfully prepared withHPMCE3 (hydrophilic), L100-55 (enteric), and cellulose acetate (CA, lipophilic), defined as CBZ-ir-ASD, CBZ-dr-ASD, and CBZ-cr-ASD, respectively. A dry granulation method was used to prepare CBZ-mr-ASD capsule formulations. Various characterization techniques were applied to evaluate the physicochemical properties of CBZ-mr-ASD and the related capsules. The drug remained in an amorphous state when encapsulated within CBZ-mr-ASD, and the capsule formulation progress did not affect the performance of the dispersions. In dissolution tests, the preparations and the corresponding dosage forms similarly showed typical immediate-, delayed-, and controlled-release properties depending on the solubility of the polymers. Moreover, single-dose 24 h pharmacokinetic studies in rats indicated that CBZ-mr-ASD significantly enhanced the oral absorption of CBZ compared to that of crude CBZ. Increased oral absorption of CBZ was observed, especially in the CBZ-dr-ASD formulation, which showed a better pharmacokinetic profile than that of crude CBZ with 2.63- and 3.17-fold improved bioavailability of the drug and its main active metabolite carbamazepine 10,11-epoxide (CBZ-E)....
In the present study we investigated the protective role of intranasal rosuvastatin liquid crystalline nanoparticles (Ros-LCNPs) against pentylenetetrazole (PTZ) induced seizures, increasing current electroshock (ICES) induced seizures, and PTZ-induced status epilepticus. From the dose titration study, it was evident that intranasal rosuvastatin (ROS), at lower dose, was more effective than oral and intraperitoneal ROS. The Ros-LCNPs equivalent to 5 mg/kg ROS were developed by hydrotrope method using glyceryl monooleate (GMO) as lipid phase. The high resolution TEM revealed that the formed Ros-LCNPs were cubic shaped and multivesicular with mean size of 219.15 ± 8.14 nm. The Ros-LCNPs showed entrapment efficiency of 70.30 ± 1.84% and release was found to be biphasic following Korsmeyer–Peppas kinetics. Intranasal Ros-LCNPs (5 mg/kg) showed significant increase in latency to PTZ-induced seizures and ICES seizure threshold compared to control and intranasal ROS solution. Additionally, intranasal Ros-LCNPs provided effective protection against PTZ-induced status epilepticus. No impairment in cognitive functions was observed following intranasal Ros-LCNPs. The results suggested that Ros-LCNPs could be an effective and promising therapeutics for the epilepsy management....
In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility....
Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity....
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