Development of Spray-Dried Micelles, Liposomes, and Solid Lipid Nanoparticles for Enhanced Stability.

Micelles, liposomes, and solid lipid nanoparticles (SLNs) are promising drug delivery vehicles; however, poor aqueous stability requires post-processing drying methods for maintaining long-term stability. The objective of this study was to compare the potential of lipid-based micelles, liposomes, and SLNs for producing stable re-dispersible spray-dried powders with trehalose or a combination of trehalose and L-leucine. This study provides novel insights into the implementation of spray drying as a technique to enhance long-term stability for these lipid-based nanocarriers.

Development and preclinical testing of a naloxone prodrug depot for extended protection against opioid overdose.

The opioid crisis, driven by synthetic opioids like fentanyl, demands innovative solutions. The opioid antidote naloxone has a short action ( ~ 1 hour), requiring repeated doses. To address this, we present a new and simple naloxone prodrug delivery system repurposing a hydrophilic derivative of acoramidis, a potent transthyretin ligand.

Green Synthesis of Zinc Oxide Nanoparticles from Flower Extract Coated with Chitosan for Potential Healing Effects on Diabetic Wounds by Inhibiting TNF-α and IL-6/IL-1β Signaling Pathways.

Background: Diabetes Mellitus is a multisystem chronic pandemic, wound inflammation, and healing are still major issues for diabetic patients who may suffer from ulcers, gangrene, and other wounds from uncontrolled chronic hyperglycemia. contain bioactive compounds such as flavonoids and phenolics that support wound healing via antioxidant, anti-inflammatory, and antibacterial properties. Our study aimed to develop a combination of eco-friendly formulations of green synthesis of ZnO-NPs by extract and further incorporate them into 2% chitosan (CS) gel.

Revolutionizing Psoriasis Topical Treatment: Enhanced Efficacy Through Ceramide/Phospholipid Composite Cerosomes Co-Delivery of Cyclosporine and Dithranol: In-Vitro, Ex-Vivo, and in-Vivo Studies.

Purpose: Improving the treatment of psoriasis is a serious challenge today. Psoriasis is an immune-mediated skin condition affecting 125 million people worldwide. It is commonly treated with cyclosporine-A (CsA) and dithranol (DTH).

An empirical predictive model for determining the aqueous solubility of BCS class IV drugs in amorphous solid dispersions.

Context: Determining solubility of drugs is laborious and time-consuming process that may not yield meaningful results. Amorphous solid dispersion (ASD) is a widely used solubility enhancement technique. Predictive models could streamline this process and accelerate the development of oral drugs with improved aqueous solubilities.

Evaluation of ceftriaxone pharmacokinetics in hospitalized Egyptian pediatric patients.

This study aimed to evaluate ceftriaxone pharmacokinetics that affects the achievement of targets in the treatment of critically ill children (meningitis, pneumonia, urinary tract infection, peritonitis, and infective endocarditis( who were admitted to Zagazig University Pediatric hospital in Egypt to monitor for the drug adverse effects.Blood samples were obtained from 24 hospitalized pediatric patients (ages ranging from 2.5 months to 12 years) after administering the calculated dose of ceftriaxone via intravenous bolus route.

The deleterious effect of xylene-induced ear edema in rats: Protective role of dexketoprofen trometamol transdermal invasomes via inhibiting the oxidative stress/NF-κB/COX-2 pathway.

Pain and inflammation could have a negative impact on a patient's quality of life and performance, causing them to sleep less. Dexketoprofen trometamol (DKT) is a water-soluble, nonselective NSAIDs. Because DKT is quickly eliminated in the urine after oral delivery, its efficacy is limited and must be taken repeatedly throughout the day.

A comparative study on micelles, liposomes and solid lipid nanoparticles for paclitaxel delivery.

The purpose of this work was to compare the in vitro and in vivo characteristics of LDV-targeted lipid-based micelles, liposomes and solid lipid nanoparticles (SLN) to provide further insights into their therapeutic potential for clinical development. Micelles, liposomes and SLN were prepared using LDV peptide amphiphiles and palmitic acid-derived lipids using solvent evaporation, thin-film hydration and microfluidic mixing respectively. Nanocarriers were characterized for their physicochemical properties, paclitaxel loading efficiency, in vitro release behavior, stability in biological media as well as in vivo antitumor efficacy in melanoma xenograft model.

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, , , and studies evaluation.

Loratadine (LORA), is a topical antihistamine utilized in the treatment of ocular symptoms of COVID-19. The study aimed to develop a Loratadine Nanostructured Lipid Carriers Ocugel (LORA-NLCs Ocugel), enhance its solubility, trans-corneal penetrability, and bioavailability. full-factorial design was established with 2 trials to investigate the impact of several variables upon NLCs properties.

Role of physicochemical properties of some grades of hydroxypropyl methylcellulose on in vitro mucoadhesion.

Relationships between physicochemical properties of hydroxypropyl methylcellulose (HPMC) compacts and their in vitro mucoadhesive performances were investigated in this study. Some commercial grades of HPMC (K3, E3, E5, E50, K4M, E4M and K15M) were prepared into compacts, and their surface hydrophilicity and hydration behavior were characterized. The in vitro mucoadhesive performance was determined by the tensile strength between the compacts and different regions of mucosal membrane (buccal, sublingual, stomach, and intestine).

Formulation, Characterization and Comparative Pharmacokinetic Study of Bupropion Floating Raft System as a Promising Approach for Treating Depression.

The aim of this study was to formulate, evaluate, and compare satiety-enhancing floating raft system (FRS) of bupropion as gastroretentive drug delivery systems (GRDDS) using in-situ gelling pectin and alginate. Bupropion was considered as a good candidate for such systems due to high water solubility that requires frequent dosing. Pectin and alginate could prolong satiety sensation augmenting weight loss of bupropion.

Design and preparation of nanostructures based on Krafft point of nonionic amphiphiles for delivery of poorly water-soluble compounds.

Micellar solubilization can effectively dissolve low water-soluble compounds in aqueous environment, however, the micellar systems are not able to withstand dilution and maintain solubilization of poorly water-soluble drugs below critical micelle concentration. To overcome the drawbacks of conventional micellar solubilization, nonionic polyoxyethylated surfactants with Krafft points at or higher than body temperature were chosen to create novel micelle-based nanostructures as a delivery vehicle for poorly water-soluble compounds. A technique "thermo-spray process" was developed for the preparation of the nanostructures-containing formulation, in which the drug-containing micelle solution was first prepared and maintained at the elevated temperature above the Krafft point of the surfactant, then spray dried to solidify the obtained micelle-like nanostructure at room temperature.

Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers.

Purpose: Bupropion is an antidepressant drug that facilitates weight loss. It is a highly water-soluble drug that needs multiple dosing, so it is considered a potential candidate for oral controlled-release dosage form. The aim of this research was to formulate and evaluate satiety-inducing swellable floating bupropion tablets by direct compression targeting depression associated with eating disorders.

Development, Implementation and Assessment of a Comprehensive Strategic Plan in a School of Pharmacy.

To develop, implement and assess a strategic plan and its process within a school of pharmacy. The process for developing the strategic plan included five phases: designing and scanning by a planning committee; divergent thinking with input from key internal and external stakeholders who shared their vision for the school; convergent planning in which faculty members helped to prioritize the clusters, goals, and metrics that had been identified; refining ideas into strategies; and assessment, during which metrics were aligned with assessment plans and data were collected and analyzed. The completed strategic plan had five broad strategies, 20 specific goals, and 90 associated metrics.

Effect of Lipophilicity and Drug Ionization on Permeation Across Porcine Sublingual Mucosa.

Sublingual route is one of the oldest alternative routes studied for the administration of drugs. However, the effect of physical-chemical properties on drug permeation via this route has not been systemically investigated. The objective of this study was to determine the effect of two key physicochemical properties, lipophilicity and ionization, on the transport of drugs across porcine sublingual mucosa.

Expression of P-glycoprotein and CYP3A4 along the porcine oral-gastrointestinal tract: implications on oral mucosal drug delivery.

Objectives: To characterize the expression of Pgp and CYP3A4 along the oral-gastrointestinal (GI) tract for understanding the potential roles of CY3A4 and Pgp in oral mucosal drug delivery.

Design: Porcine buccal mucosa, sublingual mucosa, esophagus and jejunum, ileum and colon tissues were used for studying the mRNA and protein expression of CYP3A4 and Pgp. mRNA and protein were determined using real-time quantitative polymerase chain reaction (PCR) and western blot, respectively.

In silico model of drug permeability across sublingual mucosa.

The objective of this work was to develop an in silico model to predict the sublingual permeability of a drug based on physicochemical descriptors of a molecule. Fourteen model drugs with diverse physicochemical properties were selected for this study. Molecular volume, molecular weight, logP, logD (pH 6.

Predictive models for drugs exhibiting negative food effects based on their biopharmaceutical characteristics.

Context: A drug is defined to exhibit food effects if its pharmacokinetic parameter, area under the curve (AUC₀₋∞) is different when co-administered with food in comparison with its administration on a fasted stomach. Food effects of drugs administered in immediate release dosage forms were classified as positive, negative, and no food effects.

Objective: In this study, predictive models for negative food effects of drugs that are stable in the gastrointestinal tract and do not complex with Ca²⁺ are reported.

Interactions of topiramate with polyethylene glycol 8000 in solid state with formation of new polymorph.

Topiramate [2,3:4,5-bis-O-(1-methylethylidene) β-D-fructo-pyranose sulfamate] was found to form a new polymorphic form in the presence of polyethylene glycol 8000 (PEG). Comparative study of the solid state interactions of PEG and structural topiramate analogue lacking sulfamate group (Diacetone D-fructose) indicated that the sulfamate moiety was essential for the formation of the new polymorph. The drug-polymer interactions were investigated using differential s canning calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and hot stage microscopy.

Relative bioavailability of chlorothiazide from mucoadhesive compacts in pigs.

The relative bioavailability of chlorothiazide from mucoadhesive polymeric compacts is compared to commercial oral suspension in pigs. A single-dose randomized study was conducted in 12 healthy pigs that are 9-10 weeks old. After overnight fasting, pigs were divided into two groups of six animals.

Estimation of the theoretical pore sizes of the porcine oral mucosa for permeation of hydrophilic permeants.

The oral mucosa is an attractive alternative site for the delivery of macromolecules. However, hydrophilic macromolecules are generally not well absorbed through the oral mucosa because of their hydrophilicity and size. The transport of these molecules across the oral mucosa may occur via the aqueous route.

Investigation of some factors contributing to negative food effects.

A drug is defined as exhibiting negative food effects, if the co-administration of food statistically decreases its area under the curve, AUC, when compared with its administration on a fasted stomach. In this study, the role of biopharmaceutical factors that contribute to negative food effects was studied using furosemide, nadolol, tacrine and atenolol (as model compounds exhibiting negative food effects), and prednisolone, hydrochlorothiazide and ibuprofen (as model compounds that do not show any food effects). The physiological pH of the upper intestinal tract is lower, at pH 5, in the postprandial state when compared with the preprandial state, pH 6.

In silico prediction of drug permeability across buccal mucosa.

Purpose: To develop and validate a computational model capable of predicting buccal permeability based on various structural and physicochemical descriptors.

Methods: Apparent permeability coefficients (K(p)) of 15 different drugs across porcine buccal mucosa were determined. Multiple linear regression (MLR) and maximum likelihood estimations (MLE) were used to develop the model based on a training set of 15 drugs with permeability as the response variable and the various descriptors as the predictor variables.

Effect of thermodynamic activities of the unionized and ionized species on drug flux across buccal mucosa.

The objective of this work was to delineate the contribution of thermodynamic activities of ionized and unionized species on buccal drug permeation. The flux and permeability of a model acidic (nimesulide) and basic (bupivacaine) drug were determined across porcine buccal mucosa at different pH conditions. Thermodynamic activities of ionized and unionized drug species were expressed as degree of saturation (DS) and also calculated using a modified Debye-Hückel equation.