Pharmaceutical Areas Research Articles

Investigation of Trends in the Research on Transferrin Receptor-Mediated Drug Delivery via a Bibliometric and Thematic Analysis.

This study systematically reviews and characterizes the existing literature on transferrin/transferrin receptor-mediated drug delivery. Transferrin is an iron-binding protein. It can be used as a ligand to deliver various proteins, genes, ions, and drugs to the target site via transferrin receptors for therapeutic or diagnostic purposes via transferrin receptors. This study is based on a cross-sectional bibliometric analysis of 583 papers limited to the subject areas of pharmacology, toxicology, and pharmaceutics as extracted from the Scopus database in mid-September 2022. The data were analyzed, and we carried out a performance analysis and science mapping. There was a significant increase in research from 2018 onward. The countries that contributed the most were the USA and China, and most of the existing research was found to be from single-country publications. Research studies on transferrin/transferrin receptor-mediated drug delivery focus on drug delivery across the blood-brain barrier in the form of nanoparticles. The thematic analysis revealed four themes: transferrin/transferrin receptor-mediated drug delivery to the brain, cancer cells, gene therapy, nanoparticles, and liposomes as drug delivery systems. This study is relevant to academics, practitioners, and decision makers interested in targeted and site-specific drug delivery.

Advanced Studies on Drug Delivery Systems: Characterization and Their Impact on Pharmaceutical and Medicinal Areas

This work shows some advanced studies in model pharmaceutical formulations that help to develop guidelines for the rational design of controlled release systems [...]

MALDI-TOF MS database expansion for identification of Bacillus and related genera isolated from a pharmaceutical facility

Bacillus and related genera are among the main bacterial groups isolated from pharmaceutical production areas. The identification of Bacillus species and related genera by classical methods is particularly difficult, due to similarities between closely related species. The Matrix-Assisted Laser Desorption Ionization-Time of Flight Mass Spectrometry (MALDI-TOF MS) is one of the most promising techniques for chemotaxonomic characterization of microorganisms, being an alternative to genotypic methods. This study aimed to identify Bacillus strains and related genera isolated from immunobiological production areas by phylogenetic analysis of housekeeping genes and expand the database associated with MALDI-TOF MS to improve their identification. In a previous study, 97 aerobic endospore-forming bacteria isolated from a pharmaceutical facility were analyzed by MALDI-TOF MS and 16S rRNA gene full-length sequencing. All strains were identified as Bacillus and related genera by the latest methodology. Among the 97 strains, 22 were unidentified and 2 strains were misidentified by MALDI-TOF MS. In the present study, these 24 strains were subjected to 16S rRNA gene phylogenetic analysis. Strains not identified at species level by this methodology were submitted to rpoB gene phylogenetic analysis. After identifying the strains, 19 of the 24 strains were incubated for 24, 48, and 72 h on Tryptic Soy Agar and Sheep Blood Agar and subjected to analysis by MALDI-TOF MS. A SuperSpectrum for each strain was created and entered into the equipment database. Finally, the 24 strains were again submitted to proteomic analysis by MALDI-TOF MS, and, at this time, all were correctly identified. The genotypic identification of in-house isolated strains and the introduction of these spectra in MALDI-TOF MS, in order to obtain a customized database, proved to be an extremely effective tool in the identification of Bacillus and related genera from pharmaceutical industry origin.

Overview of Bioactive Fungal Secondary Metabolites: Cytotoxic and Antimicrobial Compounds.

Microorganisms are known as important sources of natural compounds that have been studied and applied for different purposes in distinct areas. Specifically, in the pharmaceutical area, fungi have been explored mainly as sources of antibiotics, antiviral, anti-inflammatory, enzyme inhibitors, hypercholesteremic, antineoplastic/antitumor, immunomodulators, and immunosuppressants agents. However, historically, the high demand for new antimicrobial and antitumor agents has not been sufficiently attended by the drug discovery process, highlighting the relevance of intensifying studies to reach sustainable employment of the huge world biodiversity, including the microorganisms. Therefore, this review describes the main approaches and tools applied in the search for bioactive secondary metabolites, as well as presents several examples of compounds produced by different fungi species with proven pharmacological effects and additional examples of fungal cytotoxic and antimicrobial molecules. The review does not cover all fungal secondary metabolites already described; however, it presents some reports that can be useful at any phase of the drug discovery process, mainly for pharmaceutical applications.

Current Applications and Benefits of Polymeric Nanocarriers for the Management of Skin Disorders.

Preparations for topical application are highly important for therapeutic and cosmetic use since the skin has an extensive and accessible application area. Among the many advantages, this route avoids the systemic effects of the substances and, therefore, fewer adverse reactions are observed. However, the skin is an organ with a remarkable barrier effect, which can compromise the administration of pharmacologically / cosmetologically active molecules. Thus, the skin permeability of substances is a challenge that is only achieved through the preparation of formulations capable of overcoming that same barrier. Nanotechnology was introduced in the pharmaceutical and cosmetic areas to enable the development of systems for the delivery of substances and the optimization of already existing formulations. Among the several benefits and advantages of nanotechnology for topical application is the increased penetration of the drug in the skin, the improvement of the stability of the active, decrease in the active substances (reducing the possible toxic effects and allergic reactions caused by the high concentration of these compounds), and even the intensification of the drug action. This manuscript reviews the topical delivery technologies based on polymeric nanocarriers (PNC) as nanoparticles (NP) and nanogels (NG) and their benefits for better efficacy in most common cutaneous disorders. It starts with skin properties, the aspects for the penetration of active ingredients in the skin and cutaneous penetration challenges, followed by a summary of strategies for skin penetration/permeation of drugs. Then, the focus of the current research was to review NPs and NGs explored for skin disorders management published during the last years.

Chitosan on the surface of nanoparticles for enhanced drug delivery: A comprehensive review.

The ability of chitosan (CTS) to promote mucoadhesion, trigger positive/negative surface interactions, and open tight junctions has inspired researchers to coat lipid-based and polymeric-based nanoparticles with CTS in an attempt to reach new heights in the delivery of drugs and nutraceuticals across different routes. This article discusses literature relevant to the pharmaceutical and biomedical area published in the last 10years on nanoparticles overlaid with CTS. Herein, we addressed the technical aspects of the coating procedure by adding CTS solution to nanoparticles that have already been produced or during the production phase. Besides, we reviewed the applications of CTS coated nanoparticles as drug delivery systems in the oral and non-oral routes of administrations. Special attention was paid to the physicochemical and biological benefits of the CTS coating, such as improving physicochemical stability, enhancing cell and tissue interactions, controlled drug release, and augmentation of active substance bioavailability and efficacy. Moreover, this review projects the current standing and future prospects of the delivery system. The future calls for more investigations on therapeutic proteins, genes and vaccines as potential cargos. Extensive studies on the merits of integrating CTS with hydropolymer-synthesized nanoparticles and using longer-chain and chemically-modified variants of CTS are also warranted.

Exploring Entrepreneurial Intentions among Vietnamese Students in Hanoi University of Pharmacy: A Multifactorial Analysis

Published on: October 2022Journal of Young Pharmacists, 2022; 14(4):425-429Original Article | doi:10.5530/jyp.2022.14.86 Authors:Do Xuan Thang*, Nguyen Le Hang, Le Quynh Anh, Nguyen Thanh BinhDepartment of Pharmaceutical Management and Pharmacoeconomics, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Hanoi, VIETNAM. Abstract:Background: Promoting entrepreneurship has proved itself as an essence of pharmaceutical education and the development of business activities in the pharmaceutical area. However, factors affecting the entrepreneurial intentions (EI) of pharmaceutical students are very diverse, and highly dependent on local entrepreneurial environment. This study aimed at determining factors affecting on EI of students at Hanoi University of Pharmacy (HUP), Vietnam. Materials and Methods: This cross-sectional study was conducted with 1227 students of HUP in 2019. Factor analysis (EFA) and multivariate regression analysis were employed to identify factors, as well as the intensity of each factor influencing the EI of the students. The reliability of the questionnaire was tested using Cronbach’s alpha (0.728 to 0.910). Results: The findings indicated that there are four main factors influencing students’ EI explaining 57.9% of the total outcome. These factors include perceived desirability, perceived feasibility, propensity to act, and entrepreneurship education. Perceived desirability was considered as the highest impact on the learner motivation according to the regression results (beta=0.533, p<0.05). Conclusion: Based on the results obtained, the current study identified some key issues that Hanoi University of Pharmacy needs to consider for offering appropriate interventional solutions such as improving entrepreneurial courses as well as creating an entrepreneurial ecosystem to support entrepreneurial intentions of pharmacy students in Vietnam.Keywords: Entrepreneurial Intentions, Entrepreneurship education, Pharmacy education, Exploratory factor Analysis, Hanoi University of Pharmacy.

Preparation and chemical study on metallic bonding with antibiotics in nanometer form to raise the therapeutic efficiency: structural characterizations of Cu(II), Co(II) and Ni(II) 6-aminopenicillinic acid complexes

&#x0D; ABSTRACT. The medical and pharmaceutical areas are interested in the production of metal-biomolecule complexes because to their strong biological activity against bacteria, fungus, and cancers. The purpose of this paper was to synthesise of three coloured transition metal complexes of copper(II), cobalt(II), and nickel(II) with a 6-aminopenicillinic drug ligand (6-apen). The analyses of elemental analysis (carbon, hydrogen, and nitrogen), molar conductivity, magnetic susceptibility, infrared (FTIR), and electronic (UV-Vis) spectroscopy provided a thorough characterization of the solid complexes. The low molar conductance values of the produced solid complexes suggested that they were not electrolytic. The 6-apen drug ligand has more than one site of coordination as carboxylic group, β-lactam nitrogen, nitrogen of –NH2 group, oxygen of carbonyl β-lactam group and sulfur of the five–member ring. The microanalytical, spectroscopic and thermogravimetric analyses indicated a 1:2 (Metal : Ligand) stoichiometry of all complexes. The 6-apen ligand acts as a bidentate ligand that the coordination site occurs through the oxygen of deprotonated carboxylic group and β-lactam nitrogen. The thermogravimetric analysis confirmed the absence of crystalline water molecules outside the coordination sphere. The anticancer availability of the 6-apen free drug was checked against of 2Q7K receptor prostate cancer using a molecular docking calculation.&#x0D; &#x0D; KEY WORDS: 6-Aminopenicillinic, Coordination, Metals ions, FTIR, Molecular docking&#x0D; Bull. Chem. Soc. Ethiop. 2023, 37(1), 91-100. &#x0D; DOI: https://dx.doi.org/10.4314/bcse.v37i1.8

Lignins and their potential for use as biopolymers in pharmaceutical engineering - a review

Nature offers a diverse set of renewable biopolymers, among them the variety of natural polyphenols, whose structural diversity provides opportunities for further manipulation like the generation of chemicals and novel functional materials. These land‑based renewable biomaterials exhibit also a wide range of heterogeneous intrinsic reactivities and activities that render them ideal starting oligomeric and polymeric materials for the generation of multifunctional supramolecular structures as well as the development of high value-added materials.&#x0D; Lignins in particular display a variety of common physico‑chemical features that can be of enormous interest with respect to their eventual use in the pharmaceutical area. These natural polyphenols possess some interesting pharmaceutical properties such as antioxidant, anti‑inflammatory, antibacterial and eventually antiviral activities. In addition, based on their chemical features, i.e., oligomers and/or polymers of monolignol C9-building blocks. lignins can be exploited in the pharmaceutical sector mainly as material for generation of matrices and carriers for drug delivery. The present work attempts a review of the state of the art in lignin use in pharmaceutical applications.&#x0D; &#x0D; Keywords&#x0D; biopolymers, lignins, microcapsules, nanoparticles, renewable resources

Conformity assessment of medicines containing antibiotics – A multivariate assessment

Pharmaceutical products must meet quality requirements to ensure the efficacy and safety of pharmacological treatment. Non-compliance of medicines can cause economic losses and compromise the patient's health. In this work, the risks of false compliance/non-compliance decisions for parenteral antibiotics (cephalothin, ciprofloxacin and metronidazole) were evaluated on the basis of analytical results, measurement uncertainties and specification limits. Physicochemical and biological quality assays were performed according to pharmacopeial procedures. Measurement uncertainties were determined using the bottom-up approach or the probability of false-positive/false-negative results. The risks of false compliance/non-compliance decisions were estimated using the frequentist approach and Monte Carlo simulations. Guard-bands were determined through a validated spreadsheet for calculating univariate and multivariate acceptance limits. All risk values (particular risks and total risk, consumer's or producer's risk) were below the maximum permissible risk value. The univariate and multivariate guard-bands defined more restrictive specification values, reducing the risks of false compliance/non-compliance decisions. One antibiotic presented unsatisfactory results regarding the drug content and was classified as out of specification product. The application of risk management tools in the pharmaceutical area contributes to improving the quality and safety of products and supports decision-making.

Advances in mass spectrometry imaging for toxicological analysis and safety evaluation of pharmaceuticals.

Safety issues caused by pharmaceuticals have frequently occurred worldwide, posing a tremendous threat to human health. As an essential part of drug development, the toxicological analysis and safety evaluation is of great significance. In addition, the risk of pharmaceuticals accumulation in the environment and the monitoring of the toxicity from natural medicines have also received ongoing concerns. Due to a lack of spatial distribution information provided by common analytical methods, analyses that provide spatial dimensions could serve as complementary safety evaluation methods for better prediction and evaluation of drug toxicity. With advances in technical solutions and software algorithms, mass spectrometry imaging (MSI) has received increasing attention as a popular analytical tool that enables the simultaneous implementation of qualitative, quantitative, and localization without complex sample pretreatment and labeling steps. In recent years, MSI has become more attractive, powerful, and sensitive and has been applied in several scientific fields that can meet the safety assessment requirements. This review aims to cover a detailed summary of the various MSI technologies utilized in the biomedical and pharmaceutical area, including technical principles, advantages, current status, and future trends. Representative applications and developments in the safety-related issues of different pharmaceuticals and natural medicines are also described to provide a reference for pharmaceutical research, improve rational clinical medicine use, and ensure public safety.

Extraction-HPLC Green Methodology for Determination of Phenolic Compounds from Fruits by using Brij-58 Surfactant.

A green, simple and cost-effective, validated high-performance liquid chromatographic (HPLC) with UV detector has been developed an analytical method for the simultaneous determination of the most significant phenolic compounds viz. Gallic acid (GA), Quercetin (QC) and Ferulic acid (FA). The detection limit of GA, QC, FA was 0.303, 0.168, 0.0976μg/mL and quantitation limit was 0.918, 0.051, 0.295μg/mL, respectively. All parameters of planned validated method were carried out as per the ICH guidelines. This analytical method was applied to determine the phenolic compounds in fruits cultivated in India. Phenolic compounds in fruits extract were quantified using regression equations. This method can be scaled up to determine the alkaloids from several medicinal and poisonous plants samples in pharmaceutical, forensics and industrial areas.

Synthesis of polybutylene succinate via Lipase-Catalyzed Transesterification: Enzyme Stability, reuse and PBS properties in bulk polycondensations

Environmental problems involving the inappropriate disposal of non-biodegradable polymers and the production of petrochemical monomers have stimulated the interest in the development of renewable and biodegradable polymers. Among those, polybutylene succinate (PBS) has been highlighted, as it is a biodegradable polyester, synthesized from monomers that can be originated from fermentation processes. Moreover, regarding the application of biocompatible and non-toxic polymers in pharmaceutical and biomedical areas, enzymes can be considered an interesting alternative when compared to metallic catalysts. Therefore, this work aimed to investigate the lipase-catalyzed bulk polycondensation of diethyl succinate and 1,4-butanediol and to evaluate the molar mass distribution of the PBS produced. The recovery of the biocatalyst for application in reuse cycles was also performed. Preliminary tests indicated an enzyme concentration of 10% by mass (regarding the monomers) and a synthesis temperature of 90 °C as the best-operating conditions, in terms of weight of collected by-product (related to the conversion of the functional groups) and the molar masses (Mw: 4,000 g.mol−1), in reactions that lasted 90 min. These conditions were used in the subsequent recycling tests of the biocatalyst. The reuse of Novozym 435 allowed for 6 cycles, with good catalytic activity in the first 4 cycles. Moreover, the loss of enzyme activity in the last cycles was recovered through enzyme partial replacement (addition of 25% of fresh enzyme to 75% of used one). The promising results of enzymatic polycondensations performed in bulk aim to contribute to the development of not only more environmentally friendly polymers but also the use of greener reaction conditions.

Spatial Distribution and Assessment of the Human Health Risks of Heavy Metals in a Retired Pharmaceutical Industrial Area, Southwest China.

Heavy metals pollution in pharmaceutical industries received increasing attention. A total of 94 soil samples were collected in this study. Results showed the mean contents of Hg, Cd, As, Pb, Ni and Cu were 0.21, 0.26, 9.59, 55.06, 51.52 and 50.81mg·kg-1, respectively. The spatial distribution of metals in topsoil largely attributed to the pharmaceutical production process. The distribution of Hg and As were related to the production of medical absorbent cotton. While Ni was related to the fuel supply of Ni-rich coal. Cr, Cu and Pb mainly distributed in the process which they were used as catalysts. The vertical migration of metals was complex in soil. To a great extent, it was related to the texture of the soil and the properties of metals in this filed. The total non-cancer and cancer human health risk were within the limits of USEPA (10-6 a-1). This demonstrated the health risks of individual's exposure to heavy metals in this factory was acceptable.

Immunomodulatory activity of mannosylglycerate and two unnatural mannosyl‐oligosaccharides obtained from microbial fermentation on RAW264.7 macrophages

AbstractMannosyl compounds have been widely used in nutrition, fodder, and vaccine adjuvant industries. In our previous study, the engineered strains for the biosynthesis of three mannosyl compounds including β‐1,2‐mannobiose (M2‐β‐1,2), β‐1,2‐mannotriose (M3‐β‐1,2), and mannosylglycerate (MG) have been developed. However, their biological activities have not been reported. Here, those three compounds were successfully purified after fermentation of the engineered strains, and their potential immunomodulatory activities on RAW264.7 macrophages were investigated with commercialized β‐1,4‐mannotriose (M3‐β‐1,4) as control. Our results showed that M3‐β‐1,2 and MG promoted the viability and phagocytic function of RAW264.7. Meanwhile, the cytokine TNF‐α and interleukin‐6 (IL‐6) level of RAW264.7 macrophages were significantly enhanced upon the stimulation of M3‐β‐1,2 and MG compared with M3‐β‐1,4. Moreover, MG significantly stimulated macrophages to secrete IL‐10 compared with other mannan oligosaccharides. Finally, this study proved that the immunomodulatory activity of M3‐β‐1,2 and MG on RAW 264.7 cells was mainly through mitogen‐activated protein kinases and myeloid differentiation protein 88 (MyD88)‐dependent signaling pathways. All these findings suggested that M3‐β‐1,2 and MG exhibited immunomodulatory activities in the innate and adaptive immune systems, thus facilitating the application potential in developing of mannosyl compounds as an immunomodulator available for food and pharmaceutical area.

Polycaprolactone triol-based polyurethane film conjugated ibuprofen to sustained release: Synthesis, physicochemical, cytotoxic, and release studies

Polyurethanes are among the most ubiquitous materials in the biomedical and pharmaceutical areas. Thus, in this study, polycaprolactone-triol-based polyurethane conjugated ibuprofen (coded as PU-ibu) was synthesized by a two-step condensation method and characterized according to composition, morphological, thermal, and mechanical. In addition to wettability, hemocompatibility, cytotoxicity, and in vitro release. In addition to wettability, hemocompatibility, cytotoxicity, and in vitro release. The synthesized PU film had a smoother surface and superior mechanical properties compared to PU-ibu film.Moreover, PU was capable of swelling in PBS while PU-ibu film exhibited a surprising “de-swelling” behavior. Additionally, PU-ibu film not only had adequate wettability, excellent hemocompatibility, and sustained delivery capability but also greatly enhanced the proliferation of fibroblast cells. Therefore, the PU-ibu film provides a potential novel system for sustained drug delivery.

Predicting Throughput and Melt Temperature in Pharmaceutical Hot Melt Extrusion.

Even though hot melt extrusion (HME) is a commonly applied process in the pharmaceutical area, determination of the optimal process parameters is demanding. The goal of this study was to find a rational approach for predetermining suitable extrusion parameters, with a focus on material temperature and throughput. A two-step optimization procedure, called scale-independent optimization strategy (SIOS), was applied and developed further, including the use of an autogenic extrusion mode. Three different polymers (Plasdone S-630, Soluplus, and Eudragit EPO) were considered, and different optimal process parameters were assessed. The maximum barrel load was dependent on the polymers’ bulk density and the extruder size. The melt temperature was influenced by the screw speed and the rheological behavior of the polymer. The melt viscosity depended mainly on the screw speed and was self-adjusted in the autogenic extrusion. A new approach, called SIOS 2.0, was suggested for calculating the extrusion process parameters (screw speed, melt temperature and throughput) based on the material data and a few extrusion experiments.

Priority procedures for medicaments: a demonstrated tool to expedite the examination of relevant patents to public health

The delay in analyzing patent requests from the pharmaceutical area in Brazil and some vagueness in Brazil's Intellectual Property Law lead to a longer validity of many medicine patents, inhibiting generic drugs from being available in Brazil. Therefore, this investigation aims at: a) analyzing the effectiveness of priority procedures in patent processes requested by the Ministry of Health (Ministério da Saúde, MS) as a tool to make analyses faster; and b) assessing any synergy in the co-operation of MS, the National Institute of Industrial Property and the National Health Surveillance Agency, which decreased the necessary time to finish the analysis in both institutions.

Effect of Ionic Liquids in the Elaboration of Nanofibers of Cellulose Bagasse from Agave tequilana Weber var. azul by Electrospinning Technique.

The objective of this paper was to report the effect of ionic liquids (ILs) in the elaboration of nanofibers of cellulose bagasse from Agave tequilana Weber var. azul by the electrospinning method. The ILs used were 1-butyl-3-methylimidazolium chloride (BMIMCl), and DMSO was added as co-solvent. To observe the effect of ILs, this solvent was compared with the organic solvent TriFluorAcetic acid (TFA). The nanofibers were characterized by transmission electron microscopy (TEM), X-ray, Fourier transform-infrared using attenuated total reflection (FTIR-ATR) spectroscopy, and thermogravimetric analysis (TGA). TEM showed different diameters (ranging from 35 to 76 nm) of cellulose nanofibers with ILs (CN ILs). According to X-ray diffraction, a notable decrease of the crystalline structure of cellulose treated with ILs was observed, while FTIR-ATR showed two bands that exhibit the physical interaction between cellulose nanofibers and ILs. TGA revealed that CN ILs exhibit enhanced thermal properties due to low or null cellulose crystallinity. CN ILs showed better characteristics in all analyses than nanofibers elaborated with TFA organic solvent. Therefore, CN ILs provide new alternatives for cellulose bagasse. Due to their small particle size, CN ILs could have several applications, including in food, pharmaceutical, textile, and material areas, among others.

Titanium(IV) oxide nanoparticles functionalized with various meso-porphyrins for efficient photocatalytic degradation of ibuprofen in UV and visible light

Hybrid materials based on nanometric size bare anatase titanium(IV) oxide and meso-functionalized porphyrins were obtained and subsequently characterized in terms of surface morphology with SEM, HR-TEM, nanoparticle size with NTA, crystallinity with XRD and chemical composition with UV-DRS, ATR-FTIR, TGA and Raman spectroscopy. Prepared nanoparticles were studied in photocatalytic degradation of ibuprofen which is an example of an emerging contaminant from the area of pharmaceuticals. During photocatalytic tests, the materials were irradiated with four different wavelengths from UV and visible light ranges. Photocatalytic activity of hybrid materials was compared with bare titanium(IV) oxide and, in the case of said materials, the activity was dependent on the peripheral substituents of porphyrins with different anchoring groups and the wavelengths used for irradiation. For the UV light range tests, hybrid materials showed similar or higher photoactivity in photodegradation of ibuprofen (average 83% and 87% reduction of initial ibuprofen concentration) when compared to bare titanium(IV) oxide (86% reduction). The hybrid materials showed adequate photoactivity (29% and 43% reduction) in the ibuprofen photodegradation study under visible light, unlike bare titanium(IV) oxide (zero activity). Acute toxicities of hybrid materials were studied using Microtox.