Preparation and Characterization of Universal Liquid Proliposomes Encapsulating Water-soluble Efficacious Substances.

This study aims to enhance the oral bioavailability of Nadolol (NDL), a β-blocker used in the management of hypertension, by incorporating it into a liposome-based delivery system. To improve the formulation's stability, mucoadhesion, and permeability, chitosan coating was applied. Liposomes were prepared via the ethanol injection method using soy phosphatidylcholine and diacetyl phosphate. Chitosan coating was applied by adding chitosan solution (1% v/v acetic acid) at different chitosan-to-lipid ratios (0.1-0.4 w/w). The optimal formulation was selected based on particle size, PDI, and zeta potential. Characterization included encapsulation efficiency, drug loading, enzymatic stability, drug release, and Caco-2-based cytotoxicity and permeability assays. The particle size and polydispersity index of the optimized formulations, L1-NDL, L2-NDL, L1C-NDL, and L2C-NDL, were measured as 27.02 ± 0.18 nm, 24.55 ± 0.22 nm, 160.10 ± 3.17 nm, 161.00 ± 2.30 nm, 0.39 ± 0.01, 0.37 ± 0.01, 0.19 ± 0.01, and 0.18 ± 0.02. Encapsulation efficiencies of 56.01 ± 3.70% and 43.87 ± 1.24% were recorded for L1C-NDL and L2C-NDL, respectively, while drug loading capacities were 61.47 ± 2.03% and 67.80 ± 0.74%, respectively. In an enzymatic degradation study, it was found that chitosan coating increased the stability of liposomes in the gastric media. The in vitro release was higher at both pH 1.2 and 6.8. Caco-2 assays confirmed >95% cell viability and enhanced permeability in the apical-tobasolateral direction. In the permeability study, chitosan-coated liposomal formulations demonstrated enhanced transport in the apical-to-basolateral direction, indicating improved intestinal permeability. Chitosan-coated liposomes improved NDL's stability and permeability, showing promise as an effective oral delivery system.

Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation

Vanillin as a natural cross-linking agent in chitosan-based films: Optimizing formulation by response surface methodology

In vitro and in vivo evaluation of isoxsuprine loaded invasomes for efficient treatment of diabetes‐accelerated atherosclerosis

β-site amyloid precursor protein cleaving enzyme (BACE1) represents a key target for Alzheimer’s disease (AD) therapy because it is essential for producing the toxic amyloid β (Aβ) peptide that plays a crucial role in the disease’s development. BACE1 inhibitors are a promising approach to reducing Aβ levels in the brain and preventing AD progression. However, systemic delivery of such inhibitors to the brain demonstrates limited efficacy because of the presence of the blood-brain barrier (BBB). Nose-to-brain (NtB) delivery has the potential to overcome this obstacle. Liposomal drug delivery systems offer several advantages over traditional methods for delivering drugs and nucleic acids from the nose to the brain. The current study aims to prepare, characterize, and evaluate in vitro liposomal forms of donepezil, memantine, BACE-1 siRNA, and their combination for possible treatment of AD via NtB delivery. All the liposomal formulations were prepared using the rotary evaporation method. Their cellular internalization, cytotoxicity, and the suppression of beta-amyloid plaque and other pro-inflammatory cytokine expressions were studied. The Calu-3 Transwell model was used as an in vitro system for mimicking the anatomical and physiological conditions of the nasal epithelium and studying the suitability of the proposed formulations for possible NtB delivery. The investigation results show that liposomes provided the effective intracellular delivery of therapeutics, the potential to overcome tight junctions in BBB, reduced beta-amyloid plaque accumulation and pro-inflammatory cytokine expression, supporting the therapeutic potential of our approach.Graphical

The absorption behavior of cyclosporin A lecithin vesicles in rat intestinal tissue

Efficient preparation of liquid photonic crystals and their application in bionic structural coloration of textiles

Zero order delivery of itraconazole via polymeric micelles incorporated in situ ocular gel for the management of fungal keratitis

Morphology control and crystal structure and properties analysis of FOX-7/HMX composite crystals prepared by rotary evaporation method

Microscopic observation is necessary for the treatment of bone tissue microloss. To observe the process of bone tissue maturation is an essential research content in the field of orthopaedics. In many cases, people have to distinguish between new bone and mature bone, sometimes involving software calculation, and conventional HE staining obviously cannot fully meet the requirements. The quality of imaging directly affects the therapeutic effect of medical staff. In order to prove the effect of laser scanning confocal microscope (LSCM) on the observation of bone tissue micro damage, a piece of pig iliac bone and a piece of human femoral head were selected. The two kinds of bone tissue were divided into three small pieces respectively, and then stained with calcein green and alizarin red, or added with 5 ml of 1000 ml/L ethanol, and then placed under the LSCM and fluorescein Scanning under light microscope. This article uses silk fibroin as the raw material to prepare high-strength bilayer membranes using rotary evaporation method. Through relevant performance experiments, the results show that the mechanical properties of the double-layer silk fibroin film are about 12.48 MPa, and the tensile strength at break is about 13.66%. With the addition of hydroxyapatite, the mechanical properties of the silk fibroin film are improved. The addition of VEGF has little effect on the mechanical properties, and the addition of growth factor has little effect on the tensile strength of the material. The double-layer silk fibroin membrane was degraded in protease for 2 weeks, with a mass loss of about 19.3%. There was almost no degradation phenomenon in PBS solution; The release of VEGF from the double-layer silk fibroin membrane was about 17.3% after 2 weeks, with a relatively fast release rate in the early stage, and then the rate slowed down. The total release of VEGF decreased compared to the pure SF/VEGF membrane. Through the analysis of the scanning image, it is found that the image signal-to-noise ratio of alizarin red stained human femoral head is 6.956 higher than that of fluorescence microscope. In terms of image error rate, fluorescence microscope is 4.228 higher than laser scanning confocal microscope. The edge definition of laser scanning confocal microscope was 22.17 higher than that of fluorescence microscope, and the image clarity of stained bone tissue was higher than that of bone tissue only added ethanol. Therefore, the imaging effect of bone tissue staining is better, and the image generated by LSCM is higher than that generated by fluorescence microscope.

IntroductionChemotherapy, the first approach in breast cancer management, is limited owing to systemic toxicity and drug resistance. For instance, 5-fluorouracil in recommended doses cause severe side effects, highlighting the urgent necessity of finding more effective and safer combinations. Hence, this study aims to develop biocompatible natural-based nanocarriers for the co-delivery of loratadine, an antihistaminic drug along with 5-fluorouracil in order to enhance the anticancer efficacy while reducing the required dose of 5-fluorouracil.MethodsIn silico virtual screening was performed to examine the probable molecular interactions between loratadine or 5-fluorouracil, individually with two different polymers, chitosan and zein, to determine the most suitable carrier system. Zein exhibited superior binding affinity compared to chitosan. Nanoparticle optimization was conducted using a Box-Behnken design with zein, tannic acid, and either loratadine or 5-fluorouracil concentration as independent variables. The optimized formulations were characterized by dynamic light scattering, entrapment efficiency, morphology, in-vitro release, followed by cytotoxicity, apoptosis, and cell-cycle analyses in MCF-7 cells.ResultsThe optimal formulation consisted of zein (50 mg), tannic acid (131.93 mg), and loratadine or 5-fluorouracil (5 mg). The optimized formulation of Loratadine loaded nanoparticles (NPs) showed a particle size of 197 nm, polydispersity index (PDI) of 0.153, zeta potential of –21.78 mV, and entrapment efficiency of 61.33%. Furthermore, the optimized 5-fluorouracil loaded nanoparticles exhibited a particle size of 231 nm, 0.170 for PDI, zeta potential of –24.01 mV, and EE of 74.91% for entrapment efficiency. The sustained drug release profile exhibited a controlled pattern over 24–48 h. Flow cytometry results showed that the mixed nanoparticles exhibited potent cytotoxicity equivalent to 5-fluorouracil loaded nanoparticles alone despite containing only half the 5-fluorouracil dose, confirming a potential synergistic effect.ConclusionThese findings confirmed the potential of drug-loaded nanoparticles as promising drug delivery systems for breast cancer management.

A systematic approach for synthesis of optimal polymer films for radioactive decontamination and waste reduction

Metoprolol tartrate serves as a primary treatment option for hypertension, along with angina and heart failure, because it belongs to the β-blocker class of drugs. Researchers have developed Oral Disintegrating Tablets (ODT) to avoid patient non-compliance and dysphagia, especially for elderly and pediatric patients. The unique form of ODT enables patients to administer medications easily and achieve better therapeutic outcomes. A research study developed metoprolol tartrate ODT supported by three superdisintegrant agents, which included Croscarmellose Sodium (CCS), Sodium Starch Glycolate (SSG), and Crospovidone (CP), with the main purpose of enhancing drug release and disintegration performance. A direct compression method is used to formulate ODT to evaluate different superdisintegrant ratios and their influence on tablet characteristics alongside disintegration durations. The pre-compression studies of this powder blend measured bulk density and tapped density, together with compressibility index an angle of repose and Hausner’s ratio to evaluate proper flowability and compressibility characteristics. Fourier Transform Infrared Spectroscopy (FTIR) analysis proved that metoprolol tartrate showed no chemical reactions with the superdisintegrants while demonstrating their ability to work together successfully. Post-compression studies examined weight variation, hardness, friability, drug content uniformity, wetting time, and in vitro disintegration time, together with dissolution efficiency. The in vitro disintegration study confirmed that tablets dissolved rapidly within seconds and exhibited efficient drug substance release. The most optimal formulation, F5, has shown 99.8% of the drug release within 8 minutes, thus considered as the best formulation for metoprolol therapeutic delivery. The optimised formulation demonstrates an effective solution for conventional solid dosage forms by achieving consistent drug delivery for cardiovascular disease management. Major Findings: The study successfully developed an Oral Disintegrating Tablet (ODT) of Metoprolol Tartrate using three key superdisintegrants: Croscarmellose Sodium, Sodium Starch Glycolate, and Crospovidone. These agents played a vital role in enhancing tablet disintegration and accelerating drug release. The optimized formulation (F5) showed excellent flow properties, uniformity, and rapid disintegration, releasing 99.8% of the drug within just 8 minutes. This formulation offers a patient-friendly solution, particularly beneficial for elderly and pediatric patients with swallowing difficulties, and supports improved adherence in cardiovascular therapy.

The poor solubility of itraconazole (ITZ) has limited its efficacy in the treatment of vaginal candidiasis. Accordingly, the improvement of ITZ solubility using a solid dispersion technique was important to enhance its antifungal activity. Besides, as the purpose of this research was to develop local-targeting formulations, bioadhesive-thermosensitive in situ vaginal gel combined with the gel-flake system was found to be the most suitable choice. To obtain optimum solubility, entrapment efficiency, and drug-loading capacity, optimization of solid dispersion (SD) and gel-flake formulations of ITZ was performed using a composite central design. The results showed that the optimized formulation of SD-ITZ was able to significantly enhance its solubility in both water and simulated vaginal fluid to reach the values of 4.211 ± 0.23 and 4.291 ± 0.21 mg/mL, respectively. Additionally, the optimized formulation of SD-ITZ gel flakes possessed desirable entrapment efficiency and drug-loading capacity. The in situ vaginal gel containing SD-ITZ gel flakes was prepared using PF-127 and PF-68, as the gelling agents, with the addition of hydroxypropyl methylcellulose (HPMC) as the mucoadhesive polymer. It was found that the obtained in situ vaginal gel provided desirable physicochemical properties and was able to retain an amount of more than 4 mg of ITZ in the vaginal tissue after 8 h. Importantly, according to the in vivo antifungal activity using infection animal models, the incorporation of the solid dispersion technique and gel-flake system in the formulation of the bioadhesive-thermosensitive in situ vaginal gel led to the most significant decrease of the growth of Candida albicans reaching <1 log colony-forming units (CFU)/mL or equivalent to <10% of the total colony after 14 days, indicating the improvement of ITZ antifungal activity compared to other treated groups. Therefore, these studies confirmed a great potential to enhance the efficacy of ITZ in treating vaginal candidiasis. Following these findings, several further experiments need to be performed to ensure acceptability and usability before the research reaches the clinical stage.

The aim of this work is to investigate the influence of the ethanol content of adducts on the catalytic behavior of related Ziegler-Natta (ZN) catalysts in propylene homo- and copolymerizations (with 1-hexene comonomer) in terms of activity, isotacticity, H2 response, and comonomer incorporation. For this purpose, three MgCl2.nEtOH adducts with n values of 0.7, 1.2, and 2.8 were synthesized and used in the synthesis of related ZN catalysts. The catalysts were thoroughly characterized using XRD, BET, SEM, EDX, N2 adsorption-desorption, and DFT techniques. Additionally, the microstructure of the synthesized (co)polymers was distinguished via DSC, SSA, and TREF techniques. Their activity was found to enhance with the adduct's ethanol content in both homo- and copolymerization experiments, and the increase was more pronounced in homopolymerization reactions in the absence of H2. Furthermore, the catalyst with the highest ethanol content provided a copolymer with a lower isotacticity index, a shorter meso sequence length, and a more uniform distribution of comonomer within the chains. These results were attributed to the higher total surface area and Ti content of the corresponding catalyst, as well as its lower average pore diameter, a larger proportion of large pores compared to the other two catalysts, and its spherical open bud morphology. It affirms the importance of catalyst/support ethanol-content control during the preparation process. Then, molecular simulation was employed to shed light on the iso-specificity of the polypropylene produced via synthesized catalysts.