Journal of Applied Pharmaceutical Science (JAPS)
Permanent URI for this collection
Editor: Dr. Khalid Akhter Ansari
ISSN: 2231-3354; (Print)
Frequency: 12 issues a year
Language: Englishh
An Official Publication of Open Science Publishers
Open Access Peer-reviewed journal
Web site: https://www.japsonline.com/
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Item The nanocrystalline cellulose from Ananas comosus leaf wastes: An overview to extraction, purification, and applications as curcumin drug delivery system(Open Science Publishers LLP, 2024-12) Sumaiyah, S; Hasibuan, PAZ; Syahputra, H; Lubis, MF.Currently, antibacterial materials are attracting considerable attention across various fields. In this study, curcumin (Cur) was prepared with nanocrystal cellulose (NCC) into the polyvinyl alcohol (PVA) matrix to improve the functional properties of a pure Cur-NCC-PVA film. The NCC was obtained from Ananas comosus leaves and characterized by Fourier transform infrared (FTIR), scanning electron microscope (SEM), X-ray diffraction (XRD), and particle size analysis. The variations of Cur concentrations (50, 75, and 100 ?g) were added to prepare Cur-NCC-PVA films. The release kinetics of Cur from the films was determined using a spectrophotometer and the release kinetic model was obtained using Korsmeyer-Peppas kinetic model. The antibacterial activity of Cur-NCC-PVA films was established using the diffusion method. The results of NCC characteristics showed satisfactory significance. The FTIR showed a functional group of chemical composition that confirmed the removal of non-cellulosic constituents. XRD confirmed the crystallinity index of NCC of 75.89%. Meanwhile, the particle size of NCC of 268.45 nm. The development of Cur-NCC- PVA films showed a uniform yellow color. The release of curcumin in all films was increased depending on the time following the zero-order kinetic reaction. The non-Fickian kinetics demonstrated the mechanism of Cur release from the film. The Cur-NCC-PVA films in Cur concentration of 100 ?g were confirmed to have the highest antibacterial activity and significantly different between 50 and 75 ?g Cur-NCC-PVA films against Bacillus subtilis, Streptococcus spp., and Escherichia coli. The Cur-NCC-PVA films described the potential activity for topical formulation in skin disease treatment.Item Chemometric analysis of GC-MS chemical profiles and biological activities of three citrus essential oils in Indonesia(Open Science Publishers LLP, 2024-12) Einstivina, Nuryandani; Erliana, Novitasari; Muhammad, Fatih Abdurrahman; Nurul, Habibie; Ardiba, Rakhmi Sefrienda; Dedy, Kurnianto; Jasmadi, Jasmadi; Yusuf, Andriana.Citrus species essential oils (EOs) are significant sources of bioactive compounds and demonstrate diverse therapeutic effects. However, limited documentation exists regarding the phytochemicals associated with their biological activities. This study aims to assess the antioxidant activity, plant inhibitory properties, and brine shrimp cytotoxic effects of EOs derived from three Citrus species: C. sinensis, C. limon, and C. hystrix. Utilizing chemometric analysis and gas chromatography-mass spectrometry (GC-MS) fingerprints, the volatile components contributing to antioxidant activity were elucidated. The peels of the Citrus samples were hydro-distillated to obtain EOs, and subsequently subjected to antioxidant, plant inhibitory, and brine shrimp cytotoxic assays. The results indicated that C. limon EO exhibited the highest antioxidant activity, while C. hystrix and C. sinensis EOs demonstrated pronounced inhibitory effects against Artemia salina and Lactuca sativa, respectively. GC-MS analysis facilitated the identification of key compounds in each EO. Principal component analysis and hierarchical cluster analysis effectively categorized Citrus EOs based on their antioxidant properties, highlighting the proximity of C. limon and C. sinensis. Among the identified compounds, D-limonene, ?-terpineol, caryophyllene, (+)-3-carene, ?-pinene, (-)-spathulenol, trans-p-mentha-1(7),8-dien-2-ol, and trans-verbenol were the most discriminating compounds affected the antioxidant activity of C.limon and C. sinensis EOs.Item Development of levofloxacin glycosylated mesoporous silica nanoparticles for urinary tract infections(Open Science Publishers LLP, 2024-12) Mukhopadhyay, S; Narayan, R; Gadag, S; Shenoy, PA; Garg, S; Ashwini, T; Nayak, UY.Nanoparticle drug delivery for infectious disease has paved the way for effective treatment; mesoporous silica nanoparticles (MSNs) with versatile design options, tunable pore size, high surface area, and adequate pore volume have garnered widespread interest. The current study deals with the synthesis of MSNs loaded with levofloxacin (LVF), followed by glycosylation to enhance the uptake by bacterial cells. The MSNs were prepared by modifying Stober’s process. The amino-modified MSNs were glycosylated using D-Glucuronic acid by EDAC-NHS coupling chemistry. The LVF -loaded glycosylated MSNs (GLY-MSN) were characterized for various parameters and in vitro antimicrobial efficacy study. The surface functionalized MSNs had a particle size of 673.6 ± 60.81nm and were found to be spherical from the SEM images. The drug loading capacity for plain MSNs and GLY-MSN was found to be 10.41% ± 0.81% and 11.43% ± 0.93%, respectively. The LVF release from GLY-MSN was found to be 21.02% ± 3.38% whereas that from plain MSN was 7.50% ± 1.31% at the end of 48 hours. The minimum inhibitory concentration of LVF-GLY-MSN on Escherichia coli was found to be lesser than that for LVF and LVF-MSN. Hence, the synthesized GLY-MSN may be an effective drug delivery system for the treatment of drug-resistant bacterial infections.Item Availability, prices, and affordability of essential medicines in Asia: A systematic review(Open Science Publishers LLP, 2024-10) Amin, MQ; Kristina, SA; Satibi, S.Essential medicines are vital for healthcare, but nearly one-third of the global population faces challenges accessing them. World Health Organization (WHO) and Health Action International (HAI) collaborated on a manual with standardized methods for measuring drug availability, prices, and affordability to assist governments in formulating effective policies. A systematic review was conducted to analyze the availability, pricing, and affordability of essential medicines across several Asian countries. A comprehensive search was conducted across databases (Scopus, PubMed, and Google Scholar). The review targeted studies that employed WHO-HAI methods. Articles predating 2018 and those not published in English were excluded, resulting in seven articles and subsequently presented descriptively. The availability in the public sector is generally lower than in the private sector. Moreover, the overall availability in public and private sectors falls below the targets set by the WHO global action plan. Private-sector medicine prices were consistently higher than in the public sector. Affordability analysis showed that branded drugs were less accessible compared to generic drugs, with a majority of medications requiring more than one day’s income (1.1–5.2) for individuals to afford. The comprehensive assessment highlights the need for ongoing efforts by authorities to regulate and improve the availability, pricing, and affordability of essential medicines to ensure universal accessibility.Item Angelica keiskei leaves extract attenuates psychosocial stress in overcrowding-subjected rats(Open Science Publishers LLP, 2024-12) Siswanto, FM.Angelica keiskei is currently used as a popular functional food with various beneficial effects, including antioxidant, anti-obesity, anti-tumor, anti-diabetic, and anti-bacterial. A recent in vitro study reported that A. keiskei inhibits monoamine oxidases (MAOs), suggesting the antidepressant property of A. keiskei. However, in vivo studies on laboratory animals subjected to psychosocial stress have not been conducted. In this study, the effects of an A. keiskei leaf extract (AKE) on rats undergoing chronic social overcrowding stress were explored. Six-month-old male and female Wistar rats were housed in groups of three in 12 × 12 × 18 cm cages (overcrowding) for 28 days. Both male and female rats were divided into two groups (N = 10); the control group received oral distilled water, while the other group (treatment group) received 20 mg/kgBW/day of AKE supplementation. The results showed that AKE-treated rats exhibited lower anxiety- and depressive-related behaviors than that of control-stressed rats. AKE significantly decreased corticosterone and increased testosterone and estrogen levels in stressed rats. Additionally, brain tissue malondialdehyde and TNF-alpha levels were reduced, while brain neurotransmitter 5-hydroxytryptamine and antioxidant superoxide dismutase levels were elevated by the AKE. These findings suggest, for the first time, that AKE could alleviate overcrowding stress-induced behavioral, neuroendocrine, antioxidant, and inflammatory dysfunctions. AKE extract could potentially be used as an agonist to reduce stress and depression.Item Flux dynamics of C-5 amino acid precursors in fed-batch cultures of Streptomyces clavuligerus during clavulanic acid biosynthesis(Open Science Publishers LLP, 2024-10) Gómez-Gaona, LM; Ramírez-Malule, H; Gómez-Ríos, D.Clavulanic acid (CA) is a well-known ?-lactamase inhibitor that is mainly obtained from submerged cultures of Streptomyces clavuligerus. Dynamic genome-scale in silico studies were performed to gain insights into the intracellular metabolic fluxes of C-5 precursors during the cultivation of wild-type S. clavuligerus in batch and fed-batch operation. A preliminary literature screening was conducted for media selection and determination of culture conditions for further cultivation in a 5-L bioreactor. Simulations provided insights into the metabolism of C-5 precursors in CA biosynthesis. In addition, carbon utilization for CA biosynthesis was assessed in terms of the ratio of total carbon used in CA biosynthesis to the total carbon influx in batch and feed media. Based on simulation results, we proposed a modification of the glycerol-sucrose-proline-glutamate medium for fed-batch cultivation to improve the carbon utilization for CA biosynthesis. The proposed fed-batch scenario achieved higher specific CA concentration at lower biomass production, indicating better carbon utilization for its synthesis. The dynamic in silico fluxes suggests that metabolic fluxes in this scenario would be stable, favoring a longer stage of continued antibiotic secretion.Item Patient and healthcare professional perspective on challenges in lipid profile management in dyslipidemia patients: Two separate cross-sectional surveys(Open Science Publishers LLP, 2024-12) Bhandari, R; Ganachari, MS.Dyslipidemia is one of the major causes of cardiovascular ailments. Despite the fact patients with dyslipidemia continue to increase due to dependent on patient-related factors. To comprehensively explore patients’ knowledge, attitudes, and practices related to dyslipidemia, while also identifying challenges in lipid profile management among healthcare professionals. Two separate cross-sectional studies were conducted for 6 months (July–December 2021) in a tertiary care teaching hospital. The questionnaire (tool) for both surveys was prepared after a thorough review of the literature and then validated by a group of healthcare professionals. Eligible participants were enrolled after taking written informed consent. The current findings suggest poor knowledge, attitude, and practice of patients toward dyslipidemia and its management. Only 23.76% of healthcare professionals have attended seminars or continuing medical education on the management of dyslipidemia in the past year. It is surprising that only 37.62% of healthcare professionals surveyed know about the Lipid Association of India expert consensus statement on the management of dyslipidemia in Indians. Patient forgetfulness (66.37%) followed by the low education level of the patient (59.41%), side effects of the treatment (41.58%), high cost of the drugs (40.59%), and are the common reasons for noncompliance to the dyslipidemia therapy as reported by healthcare professionals. Patient-related factors contribute to major challenges in the management of dyslipidemia. The lack of awareness among healthcare professionals regarding dyslipidemia guidelines is attributed to the diversity in available guidelines and the limited applicability of Western-centric recommendations to Asian populations.Item Suppression of adipogenesis and stimulation of lipolysis by oxyresveratrol and heartwood extract from Artocarpus lacucha in adipocyte culture(Open Science Publishers LLP, 2024-10) Trisat, K; Limpeanchob, N.Obesity is associated with an increased risk of various non-communicable diseases such as type 2 diabetes, cardiovascular disease, respiratory problems, and certain cancers. The availability of safe therapeutic compounds for treating obesity is limited, emphasizing the importance of investigating natural remedies as alternatives. Oxyresveratrol, a bioactive compound, has shown promise for the anti-obesity effect. Thus, the present study investigated anti-adipogenesis and lipolysis-inducing activities of oxyresveratrol and oxyresveratrol-enriched extract from Artocarpus lacucha so-called Puag-Haad in culture adipocytes. Treatment of 3T3-L1 adipocytes with these compounds for specific time periods covering differentiation (D0-3), lipogenesis (D3-10), or adipogenesis (D0-10). The intracellular lipid accumulation was determined by Oil Red O-staining and the glycerol release from mature adipocytes was measured and referred to as lipolysis. The result showed that oxyresveratrol and Puag-Haad dose- dependently inhibited lipid accumulation. Suppression during the differentiation period of adipocytes played a critical role in such inhibitory activity. These compounds also effectively induced lipolysis but by different pathways. Puag- Haad-mediated lipolysis depended on ?-adrenergic receptors whereas these receptors did not influence the activity of oxyresveratrol. These findings suggest that oxyresveratrol and Puag-Haad hold promise as anti-obesity agents by preventing lipid accumulation in the adipocytes and inducing lipolysis thereby reducing fat mass in adipose tissue.Item Emulsifier ratio and shock treatment effect on the characteristics of eucalyptus–peppermint oil-based mouthwash nanoemulsion(Open Science Publishers LLP, 2024-12) Winarti, C; Hamaisa, A; Lesmayati, S; Misgiyarta, M; Gusmaini, G.Eucalyptus oil, the main active ingredient in eucalyptol, is usually used in health products, but studies using eucalyptus oil in the form of nanoemulsions combined with peppermint oil have not been widely conducted. This study examined the influence of emulsifier ratios on nanoemulsion formulations of mouthwashes containing eucalyptus and peppermint oil. The ratios of emulsifiers (Tween 80 and PEG 400) used are 5:0, 4:1, 3:2; 2:3, 1:4, and 0:5. The parameters observed were particle size, turbidity, pH, refractive index (RI), stability, and inhibition against Staphylococcus aureus bacteria. The results showed that the best ratio of Tween and PEG provided a higher clarity value with a smaller particle size. Stability measurements revealed no separation of the resulting emulsion, and the physical properties changed only slightly when exposed to low and high temperatures. The pH of the emulsion for all formulas ranged from 5.61 to 5.91. The findings of the inhibitory test against S. aureus revealed that eucalyptus oil treatment generally showed no inhibition except for F5 (1:4) and F6 (0:5) treatment. The best treatment based on physicochemical characteristics is the ratio of Tween:PEG = 3:2.Item Flavonoid compound of red fruit papua and its derivatives against sars-cov-2 mpro: An in silico approach(Open Science Publishers LLP, 2024-12) Ananto, AD; Pranowo, HD; Haryadi, W; Prasetyo, N.In the past years, the world has experienced a profound impact due to the abrupt appearance of a new virus (COVID- 19), presenting a significant threat to human health. Currently, there exists no widely established treatment for COVID-19 that proves consistently effective, but many studies have implemented drug repurposing and the use of herbal medicines. The potential of antiviral compounds from natural products can be predicted through in silico approach. This study aimed to determine and design flavonoid compounds from red fruits and their derivatives that have the potential to suppress the SARS-CoV-2 Mpro, ensuring a stable molecular framework and adhering to a standard pharmacokinetic profile. The study started with molecular docking using a lead compound followed by Molecular dynamics (MD) simulation up to 100 ns and pharmacokinetic prediction. The analysis of docking outcomes reveals that among flavonoid compounds, quercetin 3’-glucoside exhibits the most favorable binding energy value. Furthermore, the identification of hydrogen bonds with amino acid residues Asn142 and Cys145 provides additional rationale for selecting this compound as a pivotal candidate in the design of novel derivatives. The molecular docking procedure and subsequent MD simulations were conducted utilizing the Yasara-structure software. Furthermore, the evaluation of the pharmacokinetic profile was performed utilizing pkCSM ADMET to gain insights into the compound’s absorption, distribution, metabolism, excretion, and toxicity characteristics. According to the docking outcomes, among the 225 newly designed compounds, the ligand with code SR133 demonstrated the most favorable binding energy of ?8.0950 Kcal/mol, surpassing the reference compound. Subsequent MD simulation analysis indicates that this ligand demonstrates good stability. The presence of hydrogen bonds in the active site of SARS- CoV-2Mpro involving the main amino acid residues Asn142 and Cys145 further clarifies that this new compound has excellent inhibitory potential. The pharmacokinetic prediction of SR133 shows that this compound has a good pharmacokinetic profile and is worth proposing as a new drug candidate.Item Study of Gnetum gnemon metabolites as potential anti-breast and prostate cancer by metabolomic and molecular docking(Open Science Publishers LLP, 2024-12) Auli, WN; Husniati, H; Suprahman, NY; Fauziyya, R; Sarmoko, S; Ashari, A; Nainggolan, IM; Tachrim, ZP; Lotulung, PDN; Wulandari, R; Adyani, MN; Sari, BR; Gustiantini, NN; Fasya, GA.Breast and prostate cancers are significant health concerns worldwide, demanding novel and effective therapeutic approaches. This study explores the potential of Gnetum gnemon seed metabolites as anticancers agent through metabolomic profiling and molecular docking analysis. Six metabolites from G. gnemon seed were identified, which met Lipinski’s rule of five criteria, suggesting their drug-like properties. A panel of 10 molecular target proteins, including PTGS1, PTGS2, ESR1, SIRT1, SIRT3, SIRT5, AKT1, JAK2, BRAF, and NOS3, relevant to breast and prostate cancer pathways, were selected for molecular docking simulations. The binding interactions and free binding energy assessments identified gnetol and gnetin C as the most promising metabolites, showing strong interactions with multiple target proteins. Gnetol exhibited potential in targeting ESR1 and SIRT5, suggesting a mechanism for breast cancer inhibition. On the other hand, gnetin C emerged as a potent allosteric inhibitor of AKT1, potentially impacting breast and prostate cancer pathways. These findings highlight G. gnemon metabolites, particularly gnetol and gnetin C, as potential candidates for further preclinical and clinical studies as anti-breast and prostate cancer agents.Item Novel bioanalytical LC-MS/MS method for determination of metoprolol in human plasma(Open Science Publishers LLP, 2024-12) Atmakuri, LR; Peeriga, R; Begum, S; Gaddamedi, N; Vallamkonda, B; Baratam, A.Our study describes a novel, fast, and accurate method for estimating metoprolol (MET) in human blood plasma using LC-MS/MS technique. To prepare the samples, we used MET d7 as an internal standard (ISTD) and isolated MET from plasma using a special LLE technique. Following evaporation and reconstitution, the samples were injected into a specific chromatography column. Using a technique called single reaction monitoring; we were able to detect MET and the ISTD without interference from other blood plasma components. MET produced a unique signal and the ISTD produced a slightly different but related signal. Our analysis showed a reliable relationship between the amount of MET and the signal strength (correlation coefficient ? 0.9956). This relationship held true across a range of MET concentrations. Additionally, tests confirmed that MET remained stable in blood plasma under various conditions, including room temperature storage, injector storage, freeze-thaw cycles, and long-term freezing. This newly developed method adheres to validation guidelines set by the USFDA. It can be effectively used to measure MET levels in blood plasma for both routine testing and pharmacokinetic studies.Item Effect of treadmill exercise on the liver, kidney health, and serum IL-10 levels in high-fat diet-induced obese male Wistar rats(Open Science Publishers LLP, 2024-12) Sheik, SM; Mallya, HM; Manel, DN; Pai, KSR; Iyer, VLR; Suryakanth, VB; Shenoy, RP.This study investigated the impact of treadmill exercise on liver and kidney health in obese rats induced by a high-fat diet (HFD), alongside serum IL-10 levels. Rats were divided into normal control, HFD, HFD with atorvastatin, and HFD with exercise groups. Obesity was induced over 11 months via the HFD, while the exercise group underwent treadmill training three times per week for 90 days. Parameters measured included body weight, lipid profile, liver and kidney function tests, rat interleukine-10, and histopathology of the liver and kidney. Significant increases in body weight, lipid profile, and liver and kidney function tests, alongside decreased IL-10 levels, were observed in the HFD groups, indicating obesity-associated complications. After 90 days of exercise, significant reductions in body weight and lipid profile, alongside improved liver and kidney functions were noted, accompanied by increased IL-10 expression. The exercise group exhibited occasional liver micro vesicular fat droplets but an otherwise healthy liver and kidney appearance. Treadmill exercise demonstrated beneficial effects on liver and kidney health in male obese rats with HFD-induced obesity, primarily through the amelioration of IL-10 levels.Item Cognitive decline in type II diabetes mellitus among post-menopausal women: A cross-sectional study in South India(Open Science Publishers LLP, 2024-12) Dhivya, K; Sarumathy, S; Manigandan, G.This study was contemplated to ascertain the occurrence of cognitive impairment and explore the relationship between cognition and diabetes mellitus type 2 (T2DM) in post-menopausal women. The present cross- sectional study was conducted in the community setting in and around Anaicut Panchayat, Vellore, over 6 months (July 2023 to Dec 2023). Post-menopausal women with T2DM in the age group of above 35 years were included. The Montreal Cognitive Assessment (MoCA) scale was utilized to evaluate the cognitive function. Glycated hemoglobin (HbA1c) was also measured. The acquired data were analyzed using IBM Statistical Package for the Social Sciences (SPSS) software version 23. The inclusion criteria were met by 188 subjects. The diabetic women who were involved in the study have an average age of 57 years. The current study population evinced a mean MoCA score of 20.91 ± 3.99 and a mean HbA1c level of 9.27 ± 2.45 suggesting a strong link between cognitive dysfunction and hyperglycemia. 67% of the study subjects exhibited mild cognitive impairment (MCI). A noticeable inverse relationship was found between MoCA score and duration of T2DM (r = ?0.744) as well as between MoCA score and HbA1c (r = ?0.769). This study suggested that the duration of T2DM and the level of HbA1c have an antithetical influence on cognitive function. Due to the higher prevalence exists for MCI in diabetic patients, it is recommended that healthcare professionals should assess cognitive function in diabetic patients in their routine clinical practice to prevent the progression of dementia.Item Role of alpha-7 nicotinic acetylcholine receptor down-regulation in cyclic nucleotide reduction in memory-related brain regions of Alzheimer’s rats(Open Science Publishers LLP, 2024-12) Singh, S; Agrawal, N; Goyal, A.In this study, we investigated the effect of the downregulation of ?7 nicotinic acetylcholine receptors (?7nAChRs) by Streptozotocin (STZ) on the level of cyclic nucleotides. Three groups of six rats each—Control, Sham (received an Intracerebroventricular injection of artificial cerebrospinal fluid, and STZ were formed. Except for the control group, all rats were anesthetized with 45 mg/kg of pentobarbitone. The STZ was administered intracerebroventricularly at a dose of 3 mg/kg to STZ group rats on Day 1 as well as Day 3 of an experimental period of 18 days. By using the Morris Water Maze (MWM) along with the Y-maze test, behavioral parameters were assessed, and biochemical analysis was assessed within the hippocampus, prefrontal cortex as well as amygdala of the rat brain. Statistical analysis was performed using repeated measures with one-way and two-way analysis of variance. Bonferroni and Student Newman–Keuls post hoc test was used to determine significance between experimental groups, with a significance threshold of p < 0.05. STZ administration resulted in a notable decline in the cognitive function of rats, as evidenced by longer transfer latency, reduced duration spent, and decreased overall distance covered within the designated quadrant (in percentage) in the MWM assessment. Moreover, STZ lowered the spontaneous change in behavior observed in the rodents during the Y-maze evaluation and decreased Cyclic Adenosine Monophosphate and Cyclic Guanosine Monophosphate (cyclic nucleotides) concentrations within the HIP, PFC, and Amygdale of rat brain regions. Conclusion: The ?7nAChR downregulation may form a basis that could serve as a foundation for cognitive impairments alongside reduced cyclic nucleotides’ concentration in specific areas of the rat brain. Thus, cyclic nucleotides could be a probable target to stimulate the ?7nAChR mediated mechanism in STZ-mediated conditions.Item The trend of publication about Lumbricus rubellus for periodontitis treatment in the Scopus database: A bibliometric analysis(Open Science Publishers LLP, 2024-10) Andayasari, L; Dwiastuti, SAP; Dharmawati, IGAA; Suiraoka, IP; Bekti, HS; Swastini, IGAAP; Nurhayati; Susianti, N; Nurlinawati, I; Suratri, MAL; Hendarwan, H; Yustiantara, PS; Setyawan, EI.Periodontitis presents as a sustained deterioration of the periodontium, ultimately resulting in tooth loss. Lumbricus rubellus, a taxonomically recognized species commonly called the earthworm, is a significant component of natural constituents. This extraordinary organism exhibits intrinsic characteristics that confer antibacterial and anti-inflammatory capabilities. Nevertheless, it is essential to acknowledge that only a restricted subset of these pharmaceutical compounds has undergone meticulous scrutiny through clinical trials despite the potential effectiveness of L. rubellus in the treatment of periodontitis. The present investigation utilizes the Scopus database to conduct a bibliometric examination of the antioxidant characteristics of diverse strains of L. rubellus. This evaluation is performed through the utilization of the RStudio and VOSviewer applications. Consequently, 55 papers were encompassed within the ultimate bibliometric dataset. Moscow State University is widely acknowledged as a highly productive academic institution with significant global contributions. Mihara H is extensively acknowledged as the author with the highest level of productivity. The scholarly publication by Mihara et al. in 1991 significantly impacted the respective scientific discipline. These results provide insights to stimulate pharmaceutical research collaborations and reveal open issues about L. rubellus in the context of periodontitis therapy.Item In silico design of sitagliptin bioisosteres as new inhibitors of Mpro SARS-CoV-2(Open Science Publishers LLP, 2024-12) Abad-Giron, A; Asmad-Cruz, L; Cordova-Muñoz, AM; Gamarra-Sanchez, CD; Silva-Correa, CR; Villarreal-La Torre, VE.Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the virus that caused the last major pandemic and has led to multiple efforts being carried out around the world to investigate molecules such as specific chemotherapy drugs against this virus, such as the drug Sitagliptin, which inhibits Mpro, a protease of the virus, by acting on a highly conservative substrate recognition pocket in different coronaviruses. The study aims to develop new compounds under bioisosteric replacement techniques and obtain new SARS-Cov-2 Mpro inhibitors that are more effective than Sitagliptin. For this, 50 bioisosteric derivatives of Sitagliptin were designed, and the pharmacodynamic, pharmacokinetic, and physicochemical properties were analyzed. First, the physicochemical properties of oral absorption were analyzed according to the principles of Lipinski and Veber. The molecular docking was carried out between the protease Mpro (Protein Data Bank Code 7BB2) and the 26 bioisosteres that had the best oral absorption, with the bioisosteres modified in 2,4,5-trifluorophenyl being those that presented a lower affinity energy than that of Sitagliptin. In addition, molecules with pyrrole-pyrazole or similar groups have better pharmacokinetic properties. It is concluded that the pyrrole-pyrazole carboxamide derivative molecule has better energy affinity and ligand efficiency than the other bioisosteres; additionally, it has adequate pharmacokinetic properties, so it would be the best candidate to continue in in vitro or in vivo studies.Item RP-HPLC method for quantification of cefotaxime sodium by using design of experiment, a green analytical approach: Analytical method development, validation, and application(Open Science Publishers LLP, 2024-12) Nair, A; Chandrashekhar, HR; Nayak, UY.The current work integrates design of experiment (DoE) techniques for developing, validating, and quantifying Cefotaxime sodium through RP-HPLC. Four independent factors were considered: flow rate, mobile phase ratio, oven temperature, and injection volume. A full factorial design was applied to optimize the parameters and determine the significant variables. Using the DoE approach, a more environmentally friendly separation and quantification were achieved with the help of the Venusil XBP. C8 column (5 um × 4.6 × 250 mm), a flow rate of 0.8 ml/minute, and a mobile phase ratio consisting of a binary combination of A:B (15:65). The organic phase (A) consisted of acetonitrile, while the aqueous phase (B) consisted of ammonium acetate, and the pH was adjusted to 6.1 with the aid of glacial acetic acid. The injection volume was set at 20 ?l, and the elution was performed at a wavelength of 235 nm using a UV detector. The method was validated according to International Conference on Harmonisation guidelines, and it successfully determined the amount of Cefotaxime in Cefotaxime-loaded nanosponges. Tools such as Analytical Greenness metric (AGREE), “National Environmental Method Index” (NEMI), and “Green Analytical Procedure Index” (GAPI) were used to assess the greenness of the proposed method, along with a comparison of the proposed method with other reported HPLC methods. The proposed method proved to be eco-friendly, with better qualitative and quantitative results, as well as greener NEMI and GAPI quadrants. It also achieved a higher AGREE score (0.68) than the reported method (0.44).Item Novel nano-cubosomal chlorhexidine for endodontic irrigation: Development, characterization, and performance evaluation against E. faecalis and streptococcal biofilms in human extracted teeth(Open Science Publishers LLP, 2024-12) Mukthamath, SU; Raychaudhuri, R; Ballal, M; Pentapati, KC; Shirur, KS; Mutalik, S.Disinfection of the root canal system is one of the most complicated procedures and involves the use of a variety of equipment and techniques, irrigation regimens, and intracanal medications. “Cubosomes” (CUs) are among the few nanocarriers that are currently being explored for active drug delivery systems. A novel cubosomal chlorhexidine (CHX) for root canal irrigation was developed, and its release profile and antimicrobial efficacy against Enterococcus faecalis and streptococcal biofilms were evaluated. CUs were characterized for shape, particle size, polydispersity index, zeta potential, and drug entrapment. Drug release was determined using the dialysis method. Microbial analysis of live and dead bacteria was performed via confocal laser scanning microscopy (CLSM). The average particle size, polydispersity index, and zeta potential of the CHX CUs were 157 nm, 0.4, and 19 mV, respectively. The drug entrapment efficiency was approximately 47%. Drug release studies revealed that the cubosomal formulation released approximately 77% of the drug at the end of 6 hours, and complete release was detected at 24 hours. Confirmation of biofilm formation by CLSM and the percentage (%) survival of biofilm cells revealed that the Cubosomal formulation more effectively inhibited biofilm formation even after 48 hours. Both colony-forming unit and CLSM tests revealed that cubosomal CHX showed improved antimicrobial efficacy. The novel cubosomal CHX delivery system for endodontic irrigation was proven to be successful, as it improved the release of CHX, in turn improving its antimicrobial efficacy compared to that of regular CHX solution.Item Economic evaluation of fixed-dose drug combinations: A systematic review(Open Science Publishers LLP, 2024-12) Phung, TL; Ong, DT; Ngo, NTN; Pham, TT; Nguyen, HT; Duong, KNC; Dang, MTN; Alcusky, MJ; Amante, DJ; Nguyen, HL.This study aimed to review the quality of published evidence on the cost-effectiveness of fixed-dose drug combinations (FDCs), summarize key methodologic assumptions, and make recommendations for future economic evaluations of FDCs. The search was conducted on four databases, namely Medline, Embase, Web of Science, and the International Network of Agencies for Health Technology Assessment. Studies were selected if they assessed the cost-effectiveness of FDCs compared to one or more single active ingredient dosage forms or placebo. The Consolidated Health Economic Evaluation Reporting Standards 2022 checklist was utilized for evaluating the quality of studies. The study protocol was registered in PROSPERO (CRD42021295388). A total of 39 studies were eligible for inclusion in the review. While most of the studies (n = 29) reported that FDCs are cost-effective, the comparator in the economic evaluations was not justified explicitly in most studies (n = 34). Modeling that examined cost-effectiveness did not incorporate medication adherence (n = 22), failing to consider a key advantage of FDCs. The majority of studies investigating FDCs reported that they were cost-effective interventions. However, further economic evaluations based on long-term clinical trials with larger populations are necessary. Also, future economic studies should incorporate superior treatment adherence with FDC into the model structure.