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Deciphering immune dynamics in atherosclerosis: Inflammatory mediators as biomarkers and therapeutic target
No full textBackground: Atherosclerosis, one of the main causes of cardiovascular disease, is driven by complex interactions between lipid metabolism and immune mechanisms in the vascular system. Regulatory molecules, particularly protein fragments derived from cytokines, chemokines and other immune-related proteins, play a central role in modulating inflammation and immune responses in atherosclerotic plaques. Results: Recent advances in peptidomics have revealed the dual role of immune system-derived peptides as indicators and effectors of atherosclerotic cardiovascular disease (ASCVD). Certain subsets of immune cells, such as pro-inflammatory monocytes and regulatory T cells, contribute to this peptide-mediated regulation. New findings suggest that these peptides may serve as diagnostic biomarkers and therapeutic targets in atherosclerosis. Conclusion: This review highlights the translational relevance of immune-mediated peptides in ASCVD and emphasizes their diagnostic and therapeutic potential. By integrating peptidomics with immunology research, a new framework for understanding and targeting inflammation in atherosclerosis is proposed, opening new avenues for precision medicine in cardiovascular care
ZoomLab®-assisted powder processability evaluation for directly-compressible formulation development
No full textDue to high need for comprehensive understanding of material properties
relevant for direct compression, different expert systems have emerged,
including the ZoomLab® assistant. The aim of this work was to evaluate the
applicability of this platform in powder processability assessment and
formulation development, intended for direct compression, using caffeine
as a model drug. Thorough powder characterization was performed and
experimentally obtained results were implemented in the ZoomLab®
platform. Powder blends containing either CombiLac®, MicroceLac® 100 or
FlowLac® 90 exhibited high processability scores and were used in further
analysis. The powder blends investigated exhibited fair to good flowability
(Carr index 1 MPa) and relatively short
disintegration time (<10 min). Experimentally obtained powder blend
characteristics highly correlated with powder processability evaluation
provided within the ZoomLab® platform. These results indicate that
ZoomLab® platform represents a valuable complementary tool, which may
accelerate pharmaceutical development
Sustainable Analysis of Diclofenac Salts: A Chemometric Approach to Mixed-Mode Liquid Chromatography With Charged Aerosol Detection
No full textActive pharmaceutical ingredients (APIs) are often used in salt form because of enhanced bioavailability. This study aims to propose a new environmentally friendly method for the analysis of raw diclofenac substance, achieving simultaneous analysis of diclofenac and its counterions (Na+ and K+), utilizing mixed-mode liquid chromatography (MMLC) and charged aerosol detector (CAD). To optimize the critical method characteristic—the mobile phase composition—a 32 full factorial design of experiments and multiobjective decision making using Derringer's desirability function were employed. Two optimized methods with acceptable run times and satisfactory peak separation were developed. The methods compared the use of acetonitrile (ACN) and acetone (ACE) in terms of method sustainability. The mobile phase composition in the first method (MMLC–ACN) was 40% ACN and 60% ammonium acetate buffer (48.00 mM, pH 4.82), whereas in the second, improved method (MMLC–ACE), it was 50% ACE and 50% ammonium acetate buffer (40.00 mM, pH 4.62). The eco-friendliness of the developed methods was assessed using the GAPI, the Analytical GREEnness (AGREE) score, and the Greenness Index. The method with ACE as the mobile phase modifier demonstrated a better environmental profile, achieving an AGREE score of 0.69, compared to the ACN-based method, which scored 0.60. Method performance characteristics of the MMLC–ACE method used for the quantitative analysis of diclofenac salt raw materials were evaluated according to ICH Q2(R2) guidelines: precision—repeatability (RSD from 1.07% to 2.41% and recovery >97%), selectivity between critical peak pair (αNa/K > 1) and obtained linear response within concentration range of 50%–150% (r > 0.99)
Implementacija vakcinacije u apotekama protiv humanog papiloma virusa: Pregled literature
No full textIn most EU countries, pharmacists as community-based health care professionals (HCPs)
can provide education and vaccination services, which can enhance convenience and accessibility
for patients. This is especially important in areas where vaccine-coverage rates (VCRs) are
suboptimal and in underserved areas where access to HCPs may be limited.
The aim of this review is to describe the impact and feasibility of human papillomavirus
(HPV)-related pharmacy-based vaccination (PBV) programs. The findings indicate that
expanding access to vaccinations through pharmacies has the potential to improve immunization
rates, particularly in underserved or hard-to-reach populations. Pharmacists’ roles as advocates,
educators, and vaccine providers can address barriers, improve awareness, and promote
vaccination uptake. Collaboration with other HCPs is essential for enabling a comprehensive
approach to HPV vaccination promotion.
In conclusion, PBV programs have the potential to serve as an effective strategy for
improving immunization rates in both rural and urban areas. The integration of pharmacies,
through multi-disciplinary approach into HPV immunization programs can expand access, spread
awareness, provide education, clarify concerns, increase convenience, and reach underserved
populations. However, careful planning, training, and collaboration with other HCPs such as
physicians and nurses, are necessary to overcome challenges and ensure the safe and efficient
delivery of vaccines through pharmacies.U većini zemalja EU, farmaceuti kao zdravstveni radnici u zajednici mogu pružati
obrazovne i vakcinalne usluge, što može poboljšati pogodnost i dostupnost za pacijente. Ovo je
posebno važno u oblastima gde su stope vakcinacije (VCR) suboptimalne i u nedovoljno
opskrbljenim područjima gde je pristup zdravstvenim radnicima (HCP) ograničen. Cilj ovog
pregleda je da opiše uticaj i izvodljivost programa vakcinacije vezanih za humani papiloma virus
(HPV) koji se sprovode u apotekama. Nalazi ukazuju na to da širenje pristupa vakcinama putem
apoteka ima potencijal da poboljša stope imunizacije, posebno u nedovoljno opskrbljenim ili
teško dostupnim populacijama. Uloge farmaceuta kao pobornika, edukatora i pružalaca usluge
vakcinacije mogu prevazići prepreke, poboljšati svest i podstaći prihvatanje vakcina. Saradnja sa
drugim zdravstvenim radnicima je ključna za omogućavanje sveobuhvatnog pristupa promociji
HPV vakcinacije. Zaključak je da programi vakcinacije u apotekama imaju potencijal da budu
efikasna strategija za poboljšanje stopa imunizacije u ruralnim i urbanim oblastima. Integracija
apoteka, kroz multidisciplinarni pristup u programe imunizacije protiv HPV-a, može proširiti
pristup, povećati svest, pružiti obrazovanje, razjasniti zabrinutosti, povećati pogodnost i dostići
nedovoljno opskrbljene populacije. Međutim, pažljivo planiranje, obuka i saradnja sa drugim
zdravstvenim radnicima kao što su lekari i medicinske sestre su neophodni da se prevaziđu izazovi
i obezbedi sigurna i efikasna isporuka vakcina putem apoteka
Green fluidized bed granulation: investigation of the influence of water content and povidone grade
No full textThe pharmaceutical industry has recently been identified as one of the main contributors to climate change [1]. In recent years, pharmaceutical companies have been working hard to reduce their environmental footprint, but the changes are still negligible in relation to the use of carbon-intensive traditional manufacturing technologies. It is well known that wet granulation, which is the most commonly used method in tablet production, contributes significantly to greenhouse gas emissions. Green fluidized bed granulation (GFBG) has recently been introduced as an environmentally friendly alternative to wet granulation, characterized by the absence of a drying phase [2]. The aim of the present study was to investigate the influence of the water content and the type of povidone (PVP) used as a binder on the flowability and tableting properties of granulates prepared by GFBG
Rational design of SIRT2 inhibitors: Integrating 3D-QSAR, molecular docking and machine learning techniques
No full textSIRT2 influences processes such as apoptosis, DNA repair, and the cell cycle, making it an attractive
target for therapeutic intervention in cancer treatment. Although potent inhibitors have been developed, the
main challenge remains the design of highly selective SIRT2 inhibitors, especially due to the structural
similarity of the NAD+ binding site across other members of the sirtuin family. Currently, derivatives of 5
((3-amidobenzyl)oxy)nicotinamides stand out as some of the most selective and effective SIRT2 inhibitors,
paving the way for further research toward the development of new therapeutically relevant molecules. [1]
In this study, we developed a 3D-Quantitative Structure-Activity Relationship (3D-QSAR) model based
on a dataset of 86 nicotinamide-based SIRT2 inhibitors complemented by GRIND-derived pharmacophore
models. [2] External validation confirmed the reliability of the 3D-QSAR model in predicting SIRT2
inhibition within the defined range of application. [3] The model interpretation enabled the design of novel
SIRT2 inhibitors. Furthermore, based on molecular docking results for the SIRT1–3 isoforms, we developed
two classification machine learning models to predict the selectivity of inhibitors for the SIRT1/2 and SIRT2/3
isoforms, which was confirmed by external validation. The integration of 3D-QSAR, selectivity modeling
and ADMET predictions facilitated the identification of promising selective SIRT2 inhibitors (Figure 1).
These in silico identified inhibitors will be synthesized and tested in vitro to confirm their efficacy and
selectivity and pave the way for novel SIRT2-targeted therapies for cancer and neurodegenerative diseases.33rd Annual GP2A Medicinal Chemistry Conference, XIVth Paul Ehrlich MedChem Euro-PhD Network Meeting &
COST Action OneHealthdrugs, Abstract Book
Nantes Université – France, 11th – 13th June 202
Towards direct transformation of nanoemulsions into nanoemulsion gels: traditional vs. new-generation gelling agents
No full textThe aim of this study is to investigate the possibility of direct gellation of fragile
carriers, such as low-energy nanoemulsions with traditional and new-generation gelling agents. Carbomer 980 and xanthan gum were used in this study as represenatives of traditionally used gelling agents in hydrophilic gels, while polyacrylate-crosspolymer 6 was selected as a novel gelling agent. Nanoemulsions with ibuprofen as the model active were first prepared via the phase inversion emulsification (EPI) method and then directly transformed to nanoemulsion gels with the addition of 1% of a selected gelling agent
Low-energy nanoemulsions with citrus essential oils: formulation development and antioxidant activity
No full textThe main goal of this study was to develop stable low energy nanoemulsions with 6 different citrus essential oils as potential actives in cosmetic (nano)formulations
and to evaluate their antioxidant activity
Exploring the world of the oil-water interface – low energy nanoemulsions with ibuprofen
No full textThis study investigates the nature of the oil-water interface of low-energy nanoemulsions with ibuprofen. ..
Analysis of non-cholesterol sterols and fatty acids in patients with graves’ orbitopathy: insights into lipid metabolism in relation to the clinical phenotype of disease
No full textPurpose: Graves’ orbitopathy (GO) is a complex inflammatory disease of the orbit. A potential link between cholesterol metabolism and the occurrence of GO is possible, but still unexplored. This study aims to investigate patients’ lipid status, fatty acid content, and cholesterol homeostasis markers, all in relation to the clinical phenotype of GO. Methods: This cross-sectional study enrolled 89 consecutive patients with GO of varying degrees of activity and severity. Conventional lipid parameters were measured using routine biochemical methods. Concentrations of cholesterol synthesis and cholesterol absorption markers were analyzed by a GC-FID method. The percentage composition of individual fatty acids was determined by GC-FID. Total concentration of thyrotropin-receptor antibodies was measured by a binding immunoassay (Roche Diagnostics), while their stimulating activity (TSAb) was quantified using a cell-based bioassay (Quidelortho). Results: HDL-C concentration was significantly lower in patients with an active GO compared to an inactive form of GO (p = 0.032). The ApoB/ApoA1 ratio was significantly higher in a more severe GO (p = 0.029). Also, a positive correlation between LDL-C and TSAb levels (ρ = 0.255, p = 0.019) was observed. Lathosterol concentration significantly increased in more severe GO cases (p = 0.045). Moreover, the level of cholesterol synthesis-to-absorption index (CSI/CAI) positively correlated with CAS score (ρ = 0.232, p = 0.048). Palmitic acid was significantly associated with active GO (p = 0.012). The levels of desmosterol, lathosterol, CSI/CAI, and oleic acid were significantly associated with TSAb levels. Conclusions: Alterations in patients’ lipid profile and the cholesterol homeostasis were associated with a worse clinical phenotype of GO