INCLUSION AND CHARACTERIZATION OF KETOPROFEN INTO DIFFERENT MESOPOROUS SILICA NANOPARTICLES USING THREE LOADING METHODS

Objective: The objective of the present study was to encapsulate ketoprofen into MCM-41, SBA-15 and uncalcined SBA-15 (unc SBA-15) using different loading methods. Investigate the effect of using different loading methods, and the effect of pore sizes on the loading capacity of mesoporous silica. Finally, determine if any changes in the mesoporous structure occurred after KP loading. Methods: Ketoprofen (KP) with about 1.5 nm molecular size was selected for encapsulation into three mesoporous silica nanoparticles (MSN). These MSN particles were selected to cover a wide range of pore diameters: MCM-41 (3.4 nm), SBA-15 (6.2 nm) and uncalcined SBA-15 (7.0 nm). Loading of KP was done by three loading methods namely rotavapor, soaking, and immersion method. The loading capacity was examined via solvent extraction. Characterization of the loaded mesoporous silica nanoparticles was done by high resolution transmission electron microscopy (HRTEM), small angle X-ray diffraction (SAXRD), nitrogen adsorption/desorption isotherms, differential scanning calorimetry (DSC), and Fourier transform infrared (FT-IR) spectroscopy. Results: KP was successfully encapsulated into MCM-41, SBA-15 and uncalcined SBA-15 without affecting the mesoporous structure. The loading process was done using three different loading methods. Rotavapor loading method yielded higher loading capacities compared to soaking and immersion method. Another important factor that affected the amount of loaded KP into MSN particles were the Pore sizes of the host particles. MCM-41, which had the smallest pore size, had the least amount of loaded drug. On the other hand, uncalcined SBA-15, which had the largest pore size, had the highest amount of loaded KP. Conclusion: This study is a promising issue for the incorporation of KP into different mesoporous silica nanoparticles

Formulation and in-vitro evaluation of fast dissolving tablets containing a poorly soluble antipsychotic drug

The aim of the present study was to formulate olanzapine fast dissolving tablets (FDT). Olanzapine is a poorly water soluble drug that undergoes first pass metabolism in liver resulted in low oral bioavailability. The water solubility is enhanced by formation of co-amorphous dispersion by solvent evaporation under vacuum method using a polycarboxylic acid (ascorbic acid) as a coformer in two different molar ratios (1:1 and 1:2). The prepared systems were evaluated using differential scanning calorimeter (DSC), Fourier Transform Infra-Red analysis (FTIR), X-ray powder diffraction (XRPD), Scanning electron microscopy (SEM) and saturated solubility. The co-amorphous dispersion system in a molar ratio 1:2 is higher in solubility than 1:1, so it was selected for incorporation into FDT formulation. Compatability study between olanzapine and different tablet excipients including DSC and FTIR showed that the drug is compatible with the selected tablet excipients. Direct compression method was used in FDT formulations using different types and concentrations of superdisintegrants. FDTs were evaluated for weight variation, hardness, friability, wetting time, drug content uniformity, invitro disintegration time and invitro dissolution study. All the prepared FDTs were complied with the compendia standards. F3 and F8 showed lower disintegration time and higher percent of drug dissolved, so they were selected for stability study. After storage for 3 months at 30ºC at 65% relative humidity, both formulations were physically stable regarding color and integrity and had only minor increases in disintegration time, drug content and friability after three months’ storage. The results indicate that olanzapine FDT tablets may serve as a successful strategy for enhancing the bioavailability of olanzapine

DEVELOPMENT AND IN VITRO EVALUATION OF MUCOADHESIVE BILAYER BUCCAL TABLETS OF CARVEDILOL

Objectives: Carvedilol (CVD) is a nonselective β-adrenergic blocker that suffers from low absolute bioavailability (25-35%) due to first-pass metabolism. CVD-loaded buccal tablets were developed as a promising approach to overcome this limitation.Methods: The bilayers tablets were prepared by the direct compression technique. CVD-containing layer was based on one of four high molecular weight polymers; hydroxy propyl methylcellulose K15M (HPMC), Polyethylene oxide WSR N-750 (PEO), chitosan (CH) and Eudragit® RS-100 (EUD). An occlusive backing of ethylcellulose 20 (Ethocel®) was adopted as a second layer. The tablets were characterized for weight variation, thickness, friability % and drug content. Further studies were conducted to evaluate their swelling indices, surface pH, in vitro adhesion retention periods and in vitro drug release profiles.Results: The prepared tablets followed the compendial requirements for thickness, friability %, drug content and weight variation. The surface pH of all tablets ranged from 6.43 to 7.44 while their adhesion retention periods varied from 3.12 to 4.24 h. The best achieved system (PEO-based matrix; F4) displayed a reasonable adhesion retention period and a promising sustained drug release profile, over at least 8 hours, following non-fickian diffusion kinetics. This could indicate the contribution of swelling and erosion mechanisms for drug release.Conclusions: The current work succeeded in developing and evaluation of promising mucoadhesive CVD matrices suitable for buccal administration. Further pharmacokinetic and clinical studies are suggested to confirm the ability of the best achieved system to avoid the first pass metabolism of CVD and improve patient compliance.Â

Enhanced dissolution of meloxicam from orodispersible tablets prepared by different methods

The objective of this study was formulation, development and evaluation of meloxicam orodispersible tablets. ODTs were prepared by two methods including sublimation technique where different subliming agents like camphor, menthol and thymol were used with Ac-Di-Sol as a superdisintegrant. Each subliming agent was used in three different concentrations (5, 10 and 15% w/w). Tablets were first prepared and later exposed to vacuum. Meloxicam ODTs were also prepared by freeze-drying an aqueous dispersion of meloxicam containing a matrix former, a sugar alcohol, and a collapse protectant. In addition, different disintegration accelerators were tested (each in 1% w/v) including PVP K25, PVP K90, PEG 6000, PEG 4000, PEG 400, tween 80 and tween 20. The prepared ODTs from two methods were evaluated for weight variation, thickness, drug content, friability, hardness, wetting time, in vitro disintegration time and in vitro dissolution study. The best formulation was subjected to stability testing for 3 months at temperatures 40 °C and 75% relative humidity and at 60 °C. All formulations showed disintegration time ranging from 1 to 46 s. All the prepared formulae complied with the pharmacopoeial requirements of the drug contents. T17 gave the best in vitro disintegration and dissolution results. ODT formula T17 has shown no appreciable changes with respect to physical characters, meloxicam content and dissolution profiles when stored at elevated temperatures. In conclusion the results of this work suggest that orodispersible tablets of meloxicam with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by employing freeze drying and sublimation methods

Partial splenic artery embolization in portal hypertension patients with hypersplenism: Two interval-spaced sessions’ technique

AbstractPurposeTo evaluate the ability of interval spaced sessions of transcatheter partial splenic artery embolization (PSE) to avoid the potential post procedure major complications, in portal hypertension patients with hypersplenism.Material and methodsThe study included 50 patients (39 male and 11 females). All patients had liver cirrhosis and portal hypertension with hypersplenism and hyperactive bone marrow. All patients underwent PSE in two sessions separated at least by 1month interval. Immediate, short and intermediate term follow-up for 1year were done.ResultsWe had no post procedure mortality. None of the patients developed septic shock, splenic abscess or needed emergency surgery. Ten of our patients developed subcapsular collections which were treated conservatively. All of our patients showed significant increase in the thrombocyte count after the first session which becomes remarkable after the second session and remained at appropriate levels during the follow up period.ConclusionPSE using two (interval-spaced) sessions with careful pre- and post procedure medications and care; is really effective non surgical minimally invasive procedure in avoiding the potential post procedure complications while achieving remarkable hematologic response on controlling hypersplenism in cirrhotic patients with portal hypertension

Experimental Investigation to Improve the Energy Efficiency of Solar PV Panels Using Hydrophobic SiO2 Nanomaterial

This research aims to experimentally improve the overall efficiency of solar photovoltaic (PV) panels by coating them with hydrophobic SiO2 nanomaterial. Also, an accurate mathematical model was used to estimate the parameters of the PV panel, which is a non-linear optimization problem. Based on the experimental data and using the particle swarm optimization (PSO) algorithm, the optimal five parameters of a single diode model of a PV panel were determined in this study. This experimental work was conducted and carried out in the Renewable Energy Laboratory of Assiut University, Egypt. A comparative analysis was completed for three identical solar PV panels; the first panel was coated with hydrophobic SiO2 nanomaterial, so it was considered to be a self-cleaning panel; the second panel was uncoated and cleaned manually on a daily basis; and the third panel was kept dusty all the time through the experimental investigation, and was used as a reference. Experimentally, the output power of the PV panels was monitored for each panel in this study. Also, the anti-static and anti-reflection effects of coating solar PV panels with hydrophobic SiO2 nanomaterial were investigated experimentally. According to the obtained experimental results, it was found that the use of SiO2 coating for PV panels results in the better performance of the PV panels. The overall efficiency of the coated panel increased by 15% and 5%, compared to the dusty panel and the uncoated panel which was manually cleaned daily, respectively

Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo, bio-distribution and in vivo pharmacokinetic studies

Being one of the highly effective drugs in treatment of Alzheimer’s disease, Rivastigmine brain targeting is highly demandable, therefore liposomal dispersion of Rivastigmine was prepared containing 2 mol% PEG-DSPE added to Lecithin, Didecyldimethyl ammonium bromide (DDAB), Tween 80 in 1:0.02:0.25 molar ratio. A major challenge during the preparation of liposomes is maintaining a stable formulation, therefore the aim of our study was to increase liposomal stability by addition of DDAB to give an electrostatic stability and PEG-DSPE to increase stability by steric hindrance, yielding what we called an electrosteric stealth (ESS) liposomes. A medium nano-sized liposome (478 ± 4.94 nm) with a nearly neutral zeta potential (ZP, −8 ± 0.2 mV) and an entrapment efficiency percentage of 48 ± 6.22 was prepared. Stability studies showed no major alteration after three months storage period concerning particle size, polydispersity index, ZP, entrapment efficiency and in vitro release study confirming the successful formation of a stable liposomes. No histopathological alteration was recorded for ESS liposomes of the sheep nasal mucosa. While ESS liposomes showed higher % of drug permeating through the sheep nasal mucosa (48.6%) than the drug solution (28.7%). On completing the in vivo pharmacokinetic studies of 36 rabbits showed 424.2% relative bioavailability of the mean plasma levels of the formula ESS compared to that of RHT intranasal solution and 486% relative bioavailability of the mean brain levels

Magnetic resonance imaging features of post-COVID-19 regional and invasive sino-nasal mucormycosis

Abstract Background Sino-nasal mucormycosis is an opportunistic, invasive fungal disease which has shown a rising trend in the setting of COVID-19. The objective of this study is to document and analyze demographic data, clinical presentation and MR imaging spectra for early detection and management of post-COVID-19 sino-nasal mucormycosis. Results Sixty-two cases of sino-nasal mucormycosis were enrolled in this study; their mean age was 50.65 ± 8.25 years, with significant female predominance. Nine patients (14.5%) had active COVID-19 and 53 (85.5%) were recent COVID-19 cases. Sixty patients have not received COVID-19 vaccine. The mean duration from the initial COVID-19 laboratory confirmation to the detection of sino-nasal mucormycosis was 25.7 +/− 4.6 days. Thirty-five patients (56.5%) were kept in the hospital for COVID management and 4 of them received intensive care unit (ICU) treatment. Twenty-seven patients (43.5%) were treated in home isolation. Corticosteroids were administered in 48 cases (77.4%). Twenty-nine patients (46.8%) had been given oxygen for an average time of 11.2 ± 4.15 days. Diabetes was found in 56 cases (90.3%). The most common clinical symptoms were headache, seen in 52 patients (83.87%). The ethmoid sinus was the most common paranasal sinus involved in our study, seen in 47 cases (75.81%). In 36 cases (58%), multiple sinuses were involved. MRI staging according to the extent of regional involvement. Stage 1 seen in 2 cases (3.23%), stage 2 in 13 cases (20.97%), stage 3 in 35 cases (56.45%) and stage 4 in 12 cases (19.35%). Conclusions MRI shows a spectrum of findings in sino-nasal mucormycosis. Imaging plays a major role in staging and assessing the extent of involvement and complications. In light of this, mortality and morbidity can be dramatically decreased with adequate evaluation and therapy