Ars Pharmaceutica (Internet)

Hybrid Intelligence Applied to Professional Pharmaceutical Healthcare Services: Enhancing Human Intelligence with Advanced Technologies

Pedro Amariles, Jaime Alejandro Hincapié — Wed, 19 Mar 2025 00:00:00 +0000

Foeniculum vulgare Miller for the treatment of symptoms associated with the menopause

Hilaria M. García-Bienes, Candelaria C. Sánchez-Mateo — Wed, 19 Mar 2025 00:00:00 +0000

Introduction: Several studies have shown that preparations of fennel (Foeniculum vulgare Miller) may be useful in relieving symptoms associated with the menopause. The aim of this paper is to review published articles on the efficacy and safety of fennel in the treatment of menopausal symptoms.

Method: Articles published from January 2011 to July 2024 were searched in the University of La Laguna (ULL) search engine, “PuntoQ”. Randomised and controlled clinical trials (with placebo or other drugs) with the keywords in the abstract, text or title, both in English and Spanish, were selected.

Results: Eleven articles that met the inclusion criteria were identified. We found that fennel preparations, especially its essential oil, may be useful in reducing the frequency and intensity of menopausal symptoms, mainly vegetative symptoms (hot flushes and night sweats) and psychological symptoms. In addition, improvements in hormone levels (increased levels of estradiol), quality of life, sexual function and symptoms of vaginal atrophy have been observed. No significant adverse effects were observed at the doses administered.

Conclusions: Fennel preparations (especially its essential oil) have been shown to be effective and well tolerated in the treatment of menopausal symptoms. However, due to the limitations of the trials reviewed, more high-quality clinical research is needed to confirm these findings.

Identification and characterization of adverse events associated with Cannabis use: A comprehensive review

Valeria Silva-Rivera, Valentina Lopera, Pedro Amariles — Wed, 19 Mar 2025 00:00:00 +0000

Introduction: Available structured information about adverse events related to cannabis can contribute to appropriate use medical cannabis.

Objective: Summarize and characterize the adverse events related to cannabis use.

Method: Comprehensive review regarding to adverse events associated to cannabis use in PubMed. Mesh terms (“Cannabis” and “Drug-Related Side Effects and Adverse Reactions”) were employed, focusing on human studies published in English or Spanish with full-text access, up to November 1, 2024. Two researchers reviewed the identified articles and reached a consensus on their inclusion. Additionally, relevant references from these articles were considered.

Results: A total of 47 adverse events associated to cannabis use were identified, mainly affecting the central nervous and cardiovascular systems, especially mental disorders, somnolence, and gastrointestinal conditions. No fatal adverse events were identified related to cannabis.

Conclusions: The use of cannabis is associated to adverse events, particularly in the central nervous and cardiovascular systems. More studies are needed to identify and characterize adverse events associated to cannabis.

Curcumin and its derivatives as potential antiviral candidates against monkeypox (mpox): a review of computational studies

Wed, 19 Mar 2025 00:00:00 +0000

Introduction: Monkeypox (mpox) is an infectious disease caused by the mpox virus that is of global health concern because the outbreak, as of May 2023, has affected more than 80,000 people in hundreds of countries. Currently, there is no specific treatment, including antivirals, for mpox patients. Exploration of active compounds for mpox continues, one of which is curcumin and its derivatives. Curcumin is a polyphenol compound predominantly found in turmeric which has been documented to have antiviral effects. Therefore, this study aims to explore studies investigating the potential of curcumin and its derivatives as antiviral candidates in targeting mpox.

Method: Literature published from inception to 2024 in ScienceDirect, PubMed, Scopus, and Google Scholar was searched. Keywords used in this search included curcuma, curcumin, tetrahydrocurcumin, demethoxycurcumin, bisdemethoxycurcumin, turmeric, monkeypox, and mpox.

Results: The literature search results found five computational studies involving the compound curcumin and its derivatives, including tetrahydroxycurcumin and demethoxycurcumin. All studies showed that curcumin and its derivatives have better binding affinity with mpox proteins compared to control of several antivirals. Curcumin and its derivatives have strong potential in inhibiting mpox virus replication and modulating the immune system.

Conclusions: This review concludes that curcumin and its derivatives have potential as antiviral candidates for mpox. However, related studies remain limited and confined to computational studies. Further preclinical experimental and clinical studies are needed to confirm their effectiveness and mechanisms of action.

Gradual dose reduction versus abrupt deprescription of antipsychotic in patients with dementia: A systematic review

Alex Oyarzo Cuevas, Eva Martin-Ruiz, Antonio Olry de Labry Lima — Wed, 19 Mar 2025 00:00:00 +0000

Objective: To synthesize the available evidence on antipsychotic gradual dose reduction or abrupt deprescription in the older people population with dementia.

Methods: A systematic review of intervention studies. PubMed, Embase, Web of Science-Core Collection, Cochrane Library, Scopus, MEDLINE(Ovid), and PsycINFO databases were consulted. Articles were eligible for inclusion if they were intervention studies (randomized or quasi-experimental trials) evaluating the effectiveness of dose reduction or complete withdrawal antipsychotic deprescribing strategies in people with dementia. The screening process, data extraction, data analysis and bias risk assessment were performed by two independent reviewers and any discrepancies were triangulated with a third reviewer.

Results: Eight clinical trials were ultimately included in the systematic review, two of which were quasi experimental. Over 60% of participants came from nursing or care homes. There is evidence of several strategies for deprescribing antipsychotics. Five studies used an abrupt withdrawal schedule and three studies used a gradual dose reduction. Deprescription through abrupt and gradual withdrawal schedules showed no significant differences in the management of behavioral symptoms, although abrupt withdrawals showed significantly higher rates of relapse and/or adverse events.

Conclusion: Deprescribing antipsychotics is feasible in those people with dementia, and it is associated with benefits in terms of survival, and with potential improved outcomes in the management and relapse of behavioral and psychological symptoms of dementia. It seems reasonable that tapering off antipsychotic medication should be assessed after 12 weeks of treatment or when behavioural symptoms are under control.

Application of 3D printing technology for the pharmaceutical formulation of flavonoids

Ivo Heyerdahl-Viau — Wed, 19 Mar 2025 00:00:00 +0000

Introduction: 3D printing is an advanced technology that can be used to formulate pharmaceutical compounds with low solubility, such as flavonoids—plant-derived compounds to which various pharmacological effects have been attributed. This review describes studies in which this technology has been applied to formulate flavonoids into different pharmaceutical forms.

Methodology: A bibliographic review was conducted by searching databases such as Google Scholar and PubMed search engine up to January 2025, using the keywords “3D printing,” “flavonoids,” and “formulation.” Original articles published in English were selected.

Results: Five articles were found. In these studies, the flavonoids puerarin, catechin, apigenin, and quercetin were formulated. Puerarin, a flavonoid with cardiovascular effects, was used in gastric floating tablets that extended its stomach retention time and improved its release compared to conventional tablets. For catechin and apigenin (flavonoids with antioxidant and anticancer properties, respectively), oral mucoadhesive films were designed, allowing rapid local absorption for the treatment of oral ulcers and leukoplakia, respectively. Quercetin, known for its antimicrobial activity against Mycobacterium tuberculosis, was formulated into dermal patches that achieved sustained drug release for 70 hours in in vitro studies and maintained stable plasma levels for up to 18 days in animal models.

Conclusion: 3D printing has been successfully used to formulate flavonoids into different pharmaceutical forms, significantly improving their biopharmaceutical properties. However, this is basic research, therefore, it is important to conduct formal preclinical trials to benefit real patients, including veterinary patients.

Solubility Enhancement of Brexpiprazole for Schizophrenia using HPβ Cyclodextrin Ternary Complexation

Neha Chauhan, Amit Patel, Ravish Patel — Wed, 19 Mar 2025 00:00:00 +0000

Introduction: The present study focuses on the solubility and dissolution rate enhancement of Brexpiprazole with Hydroxy Propyl β-cyclodextrin and succinic acid as a solubiliser for schizophrenia.

Materials & Method: Brexpiprazole was obtained as a gift sample from CTX Life sciences, Sachin, Surat. Hydroxypropyl beta cyclodextrin was gifted by Good Health Pvt. Ltd Sachin, Surat. Binary and ternary complexes were prepared using three different methods and characterized using the fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and invitro dissolution studies.

Results: It was observed that among different ratios of drug and polymer used, 1:5 ratio of drug and polymer for binary complex was found to be the optimized and solvent evaporation method gave the best results. The ternary complex was then prepared using this ratio in different concentration of succinic acid (0.25, 0.5 and 1 % w/w) and optimum concentration of succinic acid as a solubiliser was of 1 %. The drug release was found to be maximum 92 % as compared to binary complex. The fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction results confirmed the formation of stable complex.

Conclusions: It was concluded that ternary complex had maximum drug release of 92% at the end of 60 minutes resulting in solubility and dissolution rate enhancement.

Formulation, Development, and Evaluation of Flubiprofen Sustained Release Tablets Using a Quality-by-Design Approach

Wed, 19 Mar 2025 00:00:00 +0000

Introduction: Flurbiprofen acts by blocking the cyclooxygenase (COX) enzymes in your body from carrying out their normal function. The study made flubiprofen tablets that last a long time by directly compressing them with carbopol, HPMC K100M, and HPMC K4M polymers. An anti-inflammatory non-steroid is flubiprofen.

Method: The research formulates and develops sustained-release flubiprofen tablets by direct compression with carbopol, HPMC K100M, and HPMC K4M polymers. The highest flubiprofen concentration in ethanol, according to pre-formulation tests, was 215 nm.

Results: The compressibility tablet was tested for thickness, diameter, medication content, and friability. Every exam was good. The compressibility index, bulk density, angle of repose, and tapped density showed good results for the tablet mix. In-vitro release tests were performed utilizing a USP device type II at 50 RPM, 0.1 N HCl in the dissolving media for two hours, and phosphate buffer pH 6.8 for six hours at 37 +0.5°C. A UV-visible spectrophotometer with a 215 nm setting assessed drug release at different periods. This formulation research indicated 99.25 % drug release from F2.

Conclusions: One benefit of the sustained release dosage form is that it allows a medication to be administered gradually over an extended period in order to keep the blood level of concentration constant. This may improve patient compliance and increase drug output.

Evaluation of the Probiotic Potential of Bacillus velezensis SNR14-4 Strain from Nile Tilapia Gills Using Genomic and In Vitro Approach

Wed, 19 Mar 2025 00:00:00 +0000

Introduction: The current investigation assessed a novel strain of Bacillus velezensis SNR14-4, isolated from the gills of Nile tilapia intending to consider it as a promising probiotic contender.

Methods: Initially, an extensive analysis of the genome of the particular isolate was carried out employing bioinformatics tools to anticipate its characteristics and potential probiotic attributes. The total genome of SNR14-4, recognized as B. velezensis via 16S rRNA and whole-genome sequencing and phylogenetic analysis, is composed of a singular circular chromosome with a genome size of 4.1 Mb, a total length of 4183910 bp, and an average guanine-cytosine (GC) content of 46.52 %. Valuable insights were acquired utilizing AntiSMASH to detect secondary metabolite biosynthetic gene clusters, and functional gene annotation relevant to probiotic traits was accomplished by utilizing RASTtk and PROKKA. The absence of virulence elements, ascertained via genomic analysis, facilitated a targeted in vitro exploration.

Results: SNR14-4 displayed notable probiotic characteristics and exhibited antimicrobial efficacy against common fish pathogens. HR-LCMS QTOF analysis of the microbial extract unveiled several potent antimicrobial compounds synthesized by the strain.

Conclusions: B. velezensis SNR14-4 showcases promise as a probiotic candidate, either as a single point of source or as a part of probiotic consortia made of similar strains.

Topical Ethosomal Formulation of Alpha Arbutin: Dermatokinetic Study and In-vitro Evaluation

Wed, 19 Mar 2025 00:00:00 +0000

Introduction: Melasma is a skin disorder characterized by increase in melanin production causes patient inconvenience. Alpha-arbutin blocks epidermal melanin biosynthesis by inhibiting enzymatic oxidation of Tyrosine. Alpha-arbutin is hydrophilic and poorly permeates through stratum corneaum. Ethosomes enhance permeability of drugs into deeper layers and extend the release. The main goal of this study was to prepare ethosomal gel containing alpha-arbutin to enhance permeation to skin.

Method: Ethosomes gel of alpha arbutin were prepared by cold method using soy lecithin, ethanol, and propylene glycol (PG) and evaluated for in vitro drug diffusion, vesicle size, entrapment efficiency and dermatokinetic study.

Results: The entrapment efficiency and drug diffusion of the prepared ethosomal gel containing alpha arbutin were found to be 94.99 % and 106.63 %, respectively. The vesicle size, polydispersity index, and zeta potential of the ethosomes formulated with 20 % w/w ethanol and 4 % w/w soy lecithin were recorded as 138.1 nm, 0.406, and -48 mV, respectively. The in vitro diffusion study illustrated burst release, with 97.56 ± 0.68 % drug released at 90 minutes. At the end of 8 hours, approximately 47.85% of the drug had diffused from the ethosomal gel. The dermatokinetic study demonstrated that the retention time of the drug in the dermis and epidermis was significantly higher in the ethosomal gel compared to the marketed cream.

Conclusions: Alpha arbutin was successfully formulated as an ethosomal suspension and converted into a gel. Due to the higher concentration of ethanol, drug permeation into the dermis and epidermis was significantly improved. Dermatokinetic studies demonstrated better retention of the drug in the dermis and epidermis layers compared to the marketed formulation.

Antibiotic resistant bacteria in surface waters of the pampeana region, Argentina

Wed, 19 Mar 2025 00:00:00 +0000

Introduction:Antibiotics are widely used in human and veterinary medicine for the therapeutic treatment of infectious diseases. They can reach the aquatic environment after being used in animal husbandry as growth promoters and for therapeutic purposes. In this work, the presence of antibiotic-resistant bacteria in the natural canal system that connects a feedlot in the Pampa Ondulada with the Arroyo Burgos, in the Province of Buenos Aires, was evaluated.

Method: The prevalence of Gram-negative bacilli resistant to veterinary and human antibiotics was determined. The antibiotic sensitivity of selected Gram-negative bacteria was evaluated by the disk diffusion method. Bacterial isolates resistant to ceftazidime or cefotaxime were designated as suspected ESBL producers. Potential ESBL-producing isolates were confirmed by the disk diffusion method with clavulanic acid.

Results: Among the isolated strains we find: Escherichia coli, Enterobacter cloacae, Pseudomonas fluorescens, Cedecea davisae and Pseudomonas oryzihabitans. In the resistance profile we can observe high resistance to third-generation cephalosporins for clinical use such as ceftazidime and cefotaxime. According to phenotypic assays, 60% of ceftazidime-resistant strains are ESBL producers.

Conclusions: Diffuse contamination with bacteria resistant to beta-lactam antibiotics for both veterinary and clinical use could be determined. These results represent a problem for public health.