bluuebunny/crossref_metadata_2025 huggingface dataset:
DATING THE MAP OF RUSSIA AND RECORDS OF THE LANDS LOCATED ON THE LEFT BANK OF THE RIVER
Authors:   Institute of History, Archaeology and Ethnology of the Far-Eastern People Russia Academy of Sciences Far-Eastern Branch, Vradiy Sergey
Published: March 2024

Two rare sources, the Map of Russia (《俄國輿地圖》) and the Records of the Lands Located on the Left Bank of the River (《江左輿地記》), are of considerable interest to those who study the 19th century history of border interactions between Russia, Korea, and China, or the history of the Korean community in the Primorskiy region of Russia. These rare documents assumed to be one of the first attempts to represent 19th century Russia by Koreans. It appeared at a time when the Korean royal court, trying to get rid of China’ centuries-old trusteeship, to limit Japan’s colonial aspirations, and to find an alternative for the encroachments from Western countries, began to strengthen its relations with Russia. The author discusses the manuscripts authorship, the probable time of its writing, while using newly found materials from archives of Japan Ministry of Foreign Affairs, Academia Sinica (Taiwan), and evaluates the significance of the said documents.
POPULARITY OF STANISLAVSKY IN CHINA
Authors:   Nanjing University, Dong Xiao
Published: March 2024

Konstantin Sergeevich Stanislavsky is the most influential theater director of the Soviet era in the first half of the 20th century. The system he created, which is based on the “art of experiencing”, had a profound impact on the performing arts of the 20th century. Since it was introduced into China in the 1940s, it has played a very important role in the development of contemporary Chinese drama performance art in the 1950–1960 years. In the 1960–1970, Stanislavsky was criticized in China. Since the late 1970s, although Stanislavsky has been vindicated in China, his importance has correspondingly weakened with the popularity of Brecht. It can be said that the encounter of Stanislavsky in China is a typical example, reflecting acceptance and interpretation of Russian Soviet literature and art in China. To some extent, this tendency obscures the real value of Russian Soviet literature and art. It is a problem worthy of reflection.
ON HISTORY OF TRUTHFUL BIOGRAPHY — THE FIRST ANTHOLOGY OF TRANSLATIONS OF MODERN CHINESE PROSE INTO RUSSIAN LANGUAGE
Authors:   St. Petersburg State University, Rodionov Alexey
Published: March 2024

The paper involves archival materials, scientific literature and the information system of the Beijing Lu Xun Museum to examine the history of the preparation and circumstances of the publication of the first collection of translations of modern Chinese prose into Russian — Truthful Biography. Novellas and Stories of Modern China published by the Molodaya gvardiya Publishing House in 1929. The author concludes that the publication of the collection Truthful Biography was a logical result of the attention of the Soviet Union to the China engulfed by the revolution. Shortcomings in the translation of literary texts reflect not only the insufficient level of Chinese language proficiency among some translators, but also the lack of traditions and norms of translation of modern Chinese literature in the Soviet Union in the late 1920s. Nevertheless, the collection Truthful Biography. Novellas and Stories of Modern China can be considered a starting point in the translation of modern Chinese literature into Russian and the beginning of the involvement of specialists in modern China in the Soviet Union in the study of Chinese literature. en_GB
LOVE STANZAS IN SOGI’S POEM
Authors:   Far Eastern Federal University, Breslavets Tatiana , Vinokurova Tatiana ,   Far Eastern Federal University
Published: March 2024

The article is devoted to the peculiarities of the work of Iyo Soga, the author of “connected stanzas” (renga). The ways of presenting love lyrics in the poem Sogi dokugin nanihito hyakuin (One hundred stanzas of the poet Sogi, 1499) are highlighted. The issues of the influence of the previous classical literature on the poet’s work, the specifics of intra-literary continuity in the history of medieval Japanese verse are discussed. The implicit meanings of love stanzas are revealed. Precedent texts with which the stanzas of the poem establish associative links are found. Intertextuality acts as the meaning-forming beginning of renga poetry.
NINETEENTH CENTURY SIAMESE LITERATURE AT THE DAWN OF WESTERNIZATION
Authors:   University of Hamburg, Dressler Jan R.
Published: March 2024

Until the introduction of printing technology during the 19th century, Siamese literature was disseminated and passed on in manuscript form only. Unfavorable climatic conditions, various adverse historical events and a lack of institutions responsible for the preservation of literary manuscripts hamper modern-day scholarly efforts to reconstruct Siamese literary history. In order to broaden the evidential basis available to scholars of pre-modern Siamese literature, qualitative as well as quantitative data were drawn from inventory lists of two manuscript collections, which hitherto had been in the possession of Prince-Patriarch Phra Paramanuchit Chinorot (1790–1853) and Prince Rakronnaret (1791–1848). Despite these records’ limited number and scope, they offer valuable insights into the size and composition of two private libraries, access to ancient and contemporary literary texts, as well as into the tastes of a highly educated mid-19th-century elite readership.
Buddhist Approach to International Relations
Authors: Galdino Neto José Francelino , Gadelha Davi
Published: March 2024

Resenha.
Safety Issues of Herb-Warfarin Interactions
Authors: Hazra Subhajit , Singh Preet Amol , Bajwa Neha
Published: March 2024

Warfarin is a popular anticoagulant with high global demand. However, studies have underlined serious
safety issues when warfarin is consumed concomitantly with herbs or its formulations. This review
aimed to highlight the mechanisms behind herb-warfarin interactions while laying special emphasis on its PKPD
interactions and evidence on Herb-Warfarin Interaction (HWI) with regards to three different scenarios,
such as when warfarin is consumed with herbs, taken as foods or prescribed as medicine, or when used in special
situations. A targeted literature methodology involving different scientific databases was adopted for acquiring
information on the subject of HWIs. Results of the present study revealed some of the fatal consequences
of HWI, including post-operative bleeding, thrombosis, subarachnoid hemorrhage, and subdural hematomas
occurring as a result of interactions between warfarin and herbs or commonly associated food products
from Hypericum perforatum, Zingiber officinale, Vaccinium oxycoccos, Citrus paradisi, and Punica
granatum. In terms of PK-PD parameters, herbs, such as Coptis chinensis Franch. and Phellodendron
amurense Rupr., were found to compete with warfarin for binding with plasma proteins, leading to an increase
in free warfarin levels in the bloodstream, resulting in its augmented antithrombic effect. Besides, HWIs were
also found to decrease International Normalised Ratio (INR) levels following the consumption of Persea americana
or avocado. Therefore, there is an urgent need for an up-to-date interaction database to educate patients
and healthcare providers on these interactions, besides promoting the adoption of novel technologies, such as
natural language processing, by healthcare professionals to guide them in making informed decisions to avoid
HWIs.
Ginsenoside Rb1 Inhibits the Proliferation of Lung Cancer Cells by Inducing the
Mitochondrial-mediated Apoptosis Pathway
Authors: Feng Lin , Liu Xinze , Sun Kaijing , Sun Ying , Wu Wei , Chen Changbao , Jin Xin , Wan Xilin
Published: March 2024

Background:

Lung cancer is one of the more common malignant tumors posing a great threat to human
life, and it is very urgent to find safe and effective therapeutic drugs. The antitumor effect of ginsenosides has
been reported to be a treatment with a strong effect and a high safety profile.

Objective:

This paper aimed to investigate the inhibitory effect of ginsenoside Rb1 on 95D and NCI-H460 lung
cancer cells and its pathway to promote apoptosis.

Methods:

We performed the CCK-8 assay, fluorescence staining assay, flow cytometry, scratch healing assay, and
Transwell assay to detect the effects of different concentrations of ginsenoside Rb1 on the antitumor activity of
95D and NCI-H460 cells and Western Blot detected the mechanism of antitumor effect.

Results:

Ginsenoside Rb1 treatment significantly increased the inhibition and apoptosis rates of 95D and NCIH460
cells and inhibited the cell cycle transition from S phase to G2/M. Rb1 induces apoptosis by altering the
levels of P53, Bax, Cyto-c, Caspase-8, Caspase-3, Cleaved Caspase-3, Bcl-2, MMP-2, and MMP-9 proteins and
activating the external apoptotic pathway.

Conclusion:

Ginsenoside Rb1 inhibits proliferation and migration and induces apoptosis of 95D and NCI-H460
lung cancer cells by regulating the mitochondrial apoptotic pathway to achieve antitumor activity.
The Effect of SnO2 and Rh on Pt Nanowire Catalysts for Ethanol Oxidation
Authors: Valerio Neto Edmundo , Almeida Caio , Eguiluz Katlin , Salazar-Banda Giancarlo
Published: March 2024

In this study, we synthesized Pt-Rh nanowires (NWs) through chemical reduction of metallic precursors using formic acid at room temperature, excluding the use of surfactants, templates, or stabilizing agents. These NWs were supported on two substrates: carbon (Vulcan XC-72R) and carbon modified with tin oxide (SnO2) via the sol-gel method (10 wt.% SnO2). We explored the electroactivity of Pt/SnO2/C, Pt-Rh/C, Pt-Rh/SnO2(commercial)/C (commercial SnO2), and Pt-Rh/SnO2/C NWs toward electrochemical oxidation of ethanol in acidic media using various techniques, including CO-stripping, cyclic voltammetry, derivative voltammetry, chronoamperometry, and steady-state polarization curves. Physical characterization involved X-ray diffraction and transmission electron microscopy. The synthesized NWs exhibit higher ethanol oxidation activity than the commercial Pt/C (Johnson Matthey™) catalyst. Rh atoms are hypothesized to enhance complete ethanol oxidation, while the NW morphology improves ethanol adsorption at the catalyst surface for subsequent oxidation. Additionally, the choice of support material plays a significant role in influencing the catalytic activity. The superior catalytic activity of Pt-Rh/SnO2/C NWs may be attributed to the facile dissociation of the C-C bond, low CO adsorption (electronic effect due to Rh presence), and the bifunctional mechanism facilitated by the oxophilic nature of the SnO2 support.
Calculated Human Leucocyte Antigens Evolutionary Divergence (cHED)
Authors: Lima Bruno A
Published: March 2024

Human Leucocyte Antigens (HLA) constitute a highly polymorphic set of genes pivotal to the immune response. The HLA heterozygous advantage hypothesis assumes that heterozygous individuals at the HLA level have a wider range of peptides for T cell recognition than homozygous individuals. Consequently, they possess an enhanced capacity to trigger a targeted immune reaction. The divergent allele advantage hypothesis is an extension of heterozygous advantage, considering the excessive sequence divergence between alleles of the same HLA locus. The HLA Evolutionary Divergence (HED) score has been proposed to quantify this divergence between alleles of the same HLA locus. Presented here is the calculated HED (cHED), an open-source web application designed for the computation of HED scores about the 5 classical HLA genes (HLA-A, -B, -C, -DRB1, and -DQB1) when delineated at two-field resolution.
Tendencias de investigación de probióticos utilizados en animales monogástricos
Authors: Morales Castañeda Alexis
Published: March 2024

El análisis de redes por temáticas afines, permitió identificar una red compuesta por Universiti Putra Malaysia, Islamic Azad University, Zhejiang University y Kangwon National University, siendo el principal contenido de sus investigaciones, los temas de suplementación de aditivos alimenticios de Bacillus subtilis y su efecto en el crecimiento, la utilización de bacteriófagos y la eficacia de probióticos multimicrobiales comerciales en presentaciones liquidas y sólidas para reducir infecciones intestinales.
Identifying Existing Guidelines, Frameworks, Checklists, and Recommendations for Implementing Patient-Reported Outcome Measures: Protocol for a Scoping Review
Authors: Jayasinghe Randi Thisakya , Ahern Susannah , Maharaj Ashika D , Romero Lorena , Ruseckaite Rasa
Published: March 2024

Background

Implementing patient-reported outcome measures (PROMs) to measure and evaluate health outcomes is increasing worldwide. Along with this emerging trend, it is important to identify which guidelines, frameworks, checklists, and recommendations exist, and if and how they have been used in implementing PROMs, especially in clinical quality registries (CQRs).

Objective

This review aims to identify existing publications, as well as publications that discuss the application of actual guidelines, frameworks, checklists, and recommendations on PROMs’ implementation for various purposes such as clinical trials, clinical practice, and CQRs. In addition, the identified publications will be used to guide the development of a new guideline for PROMs’ implementation in CQRs, which is the aim of the broader project.

Methods

A literature search of the databases MEDLINE, Embase, CINAHL, PsycINFO, and Cochrane Central Register of Controlled Trials will be conducted since the inception of the databases, in addition to using Google Scholar and gray literature to identify literature for the scoping review. Predefined inclusion and exclusion criteria will be used for all phases of screening. Existing publications of guidelines, frameworks, checklists, recommendations, and publications discussing the application of those methodologies for implementing PROMs in clinical trials, clinical practice, and CQRs will be included in the final review. Data relating to bibliographic information, aim, the purpose of PROMs use (clinical trial, practice, or registries), name of guideline, framework, checklist and recommendations, the rationale for development, and their purpose and implications will be extracted. Additionally, for publications of actual methodologies, aspects or domains of PROMs’ implementation will be extracted. A narrative synthesis of included publications will be conducted.

Results

The electronic database searches were completed in March 2024. Title and abstract screening, full-text screening, and data extraction will be completed in May 2024. The review is expected to be completed by the end of August 2024.

Conclusions

The findings of this scoping review will provide evidence on any existing methodologies and tools for PROMs’ implementation in clinical trials, clinical practice, and CQRs. It is anticipated that the publications will help us guide the development of a new guideline for PROMs’ implementation in CQRs.

Trial Registration

PROSPERO CRD42022366085; https://tinyurl.com/bdesk98x

International Registered Report Identifier (IRRID)

DERR1-10.2196/52572
Measuring Physical Functioning Using Wearable Sensors in Parkinson Disease and Chronic Obstructive Pulmonary Disease (the Accuracy of Digital Assessment of Performance Trial Study): Protocol for a Prospective Observational Study
Authors: de Graaf Debbie , de Vries Nienke M , van de Zande Tessa , Schimmel Janneke J P , Shin Sooyoon , Kowahl Nathan , Barman Poulami , Kapur Ritu , Marks Jr William J , van 't Hul Alex , Bloem Bastiaan R
Published: March 2024

Background

Physical capacity and physical activity are important aspects of physical functioning and quality of life in people with a chronic disease such as Parkinson disease (PD) or chronic obstructive pulmonary disease (COPD). Both physical capacity and physical activity are currently measured in the clinic using standardized questionnaires and tests, such as the 6-minute walk test (6MWT) and the Timed Up and Go test (TUG). However, relying only on in-clinic tests is suboptimal since they offer limited information on how a person functions in daily life and how functioning fluctuates throughout the day. Wearable sensor technology may offer a solution that enables us to better understand true physical functioning in daily life.

Objective

We aim to study whether device-assisted versions of 6MWT and TUG, such that the tests can be performed independently at home using a smartwatch, is a valid and reliable way to measure the performance compared to a supervised, in-clinic test.

Methods

This is a decentralized, prospective, observational study including 100 people with PD and 100 with COPD. The inclusion criteria are broad: age ≥18 years, able to walk independently, and no co-occurrence of PD and COPD. Participants are followed for 15 weeks with 4 in-clinic visits, once every 5 weeks. Outcomes include several walking tests, cognitive tests, and disease-specific questionnaires accompanied by data collection using wearable devices (the Verily Study Watch and Modus StepWatch). Additionally, during the last 10 weeks of this study, participants will follow an aerobic exercise training program aiming to increase physical capacity, creating the opportunity to study the responsiveness of the remote 6MWT.

Results

In total, 89 people with PD and 65 people with COPD were included in this study. Data analysis will start in April 2024.

Conclusions

The results of this study will provide information on the measurement properties of the device-assisted 6MWT and TUG in the clinic and at home. When reliable and valid, this can contribute to a better understanding of a person’s physical capacity in real life, which makes it possible to personalize treatment options.

Trial Registration

ClinicalTrials.gov NCT05756075; https://clinicaltrials.gov/study/NCT05756075

International Registered Report Identifier (IRRID)

DERR1-10.2196/55452
User Perceptions of Wearability of Knitted Sensor Garments for Long-Term Monitoring of Breathing Health: Thematic Analysis of Focus Groups and a Questionnaire Survey (Preprint)
Authors: Fobelets Kristel , Mohanty Nikita , Thielemans Mara , Thielemans Lieze , Lake-Thompson Gillian , Liu Meijing , Jopling Kate , Yang Kai
Published: March 2024

BACKGROUND

Long-term unobtrusive monitoring of breathing patterns can potentially give a more realistic insight into the respiratory health of people with asthma or chronic obstructive pulmonary disease than brief tests performed in medical environments. However, it is uncertain whether users would be willing to wear these sensor garments long term.

OBJECTIVE

Our objective was to explore whether users would wear ordinary looking knitted garments with unobtrusive knitted-in breathing sensors long term to monitor their lung health and under what conditions.

METHODS

Multiple knitted breathing sensor garments, developed and fabricated by the research team, were presented during a demonstration. Participants were encouraged to touch and feel the garments and ask questions. This was followed by two semistructured, independently led focus groups with a total of 16 adults, of whom 4 had asthma. The focus group conversations were recorded and transcribed. Thematic analysis was carried out by three independent researchers in 3 phases consisting of familiarization with the data, independent coding, and overarching theme definition. Participants also completed a web-based questionnaire to probe opinion about wearability and functionality of the garments. Quantitative analysis of the sensors’ performance was mapped to participants’ garment preference to support the feasibility of the technology for long-term wear.

RESULTS

Key points extracted from the qualitative data were (1) garments are more likely to be worn if medically prescribed, (2) a cotton vest worn as underwear was preferred, and (3) a breathing crisis warning system was seen as a promising application. The qualitative analysis showed a preference for a loose-fitting garment style with short sleeves (13/16 participants), 11 out of 16 would also wear snug fitting garments and none of the participants would wear tight-fitting garments over a long period of time. In total, 10 out of 16 participants would wear the snug fitting knitted garment for the whole day and 13 out of 16 would be happy to wear it only during the night if not too hot. The sensitivity demands on the knitted wearable sensors can be aligned with most users’ garment preferences (snug fit).

CONCLUSIONS

There is an overall positive opinion about wearing a knitted sensor garment over a long period of time for monitoring respiratory health. The knit cannot be tight but a snugly fitted vest as underwear in a breathable material is acceptable for most participants. These requirements can be fulfilled with the proposed garments. Participants with asthma supported using it as a sensor garment connected to an asthma attack alert system.
HISTOMORPHOLOGICAL STUDY OF TRANSURETHRAL RESECTION OF PROSTATE SPECIMENS
Authors: SUPARNA V SUVERNAKAR  , DEEPAK SADHU  , NITISH P INGOLE
Published: March 2024

Objectives: (The objectives of the study are as follows: 1) To study various histomorphological patterns of transurethral resection of prostate specimens. (2) To classify malignant lesions with Gleason’s grading and to do Prostate-specific antigen (PSA) level and immunohistochemistry as required.
Methods: It was a cross-sectional study conducted from January 2022 to June 2023 in a tertiary care hospital. Fifty-seven patients study who underwent transurethral resection of the prostate (TURP) surgery with hypertrophied prostate during the study period were included in the study on the basis of a predefined inclusion and exclusion criteria. Demographic characteristics of all the cases were analyzed. Clinical features, presenting complaints, histopathological findings, and the final diagnosis were studied. For statistical purposes, p value < 0.05 was taken as statistically significant.
Results: The majority of the participants were in the age group of 60–69 years (42.11%) followed by people in the age group of 70–79 years (35.09%). Benign disease of prostrate was common than the malignant disease. BHP was the most common disease encountered and was seen in 37 (64.91%) cases. Among 37 patients with BHP, 70.27% (26) patients had increased PSA levels. Among 10 patients of BHP with CP 8 (80%) patients had increased levels of PSA. Serum PSA levels were increased in all the cases of malignancy, Adenocarcinoma prostate and PIN.
Conclusion: In patients undergoing TURP modified Gleason scoring patterns and prognostic grade grouping should be done in conjunction for assessing prognosis and management. Immunohistochemistry and molecular genetic analysis are valuable adjuncts to the diagnosis in these cases.
AZITHROMYCIN AND OSELTAMIVIR QUANTIFICATION METHOD DEVELOPED AND VALIDATED USING LIQUID CHROMATOGRAPHY-TANDEM MASS SPECTROMETRY IN DRIED BLOOD SPOT
Authors: RAHMANIA TESIA AISYAH , HARAHAP YAHDIANA , SANDY KURNIA
Published: March 2024

Objective: The development and use of bio-sampling techniques for the analysis of COVID-19 drugs oseltamivir and azithromycin using the Dried Blood Spot technique simultaneously using LC-MS/MS aims to obtain optimal conditions and validated analytical methods using LC-MS/MS according to Food and Drug Administration 2018 recommendations.
Methods: Azithromycin and oseltamivir analyses were performed using LC-MS/MS with C18 Acquity® Bridged Ethylene Hybrid (BEH) column 1.7 m, 100 x 2.1 mm. The matrix sample used is Dried Blood Spot (DBS) with azithromycin and Oseltamivir as the raw material and acyclovir as the internal standard. Optimum analytical conditions were obtained on a gradient mobile phase using 0.1% formic acid-methanol solution with a flow rate of 0.2 ml/minute. The quantification of the analysis was carried out using triple quadrupole mass spectrometry with positive electrospray ionization (ESI) mode.
Results: The calibration curve ranged from 0.5 to 160 g/ml, and the Lower Limit of Quantification (LLOQ) achieved was 25.31 and 25.37 ng/ml. Sensitivity, selectivity, linearity, precision, carry-over, accuracy, stability, and recovery were found to be within the suitable limits and fully validated by the guidelines from the Food and Drug Administration 2018.
Conclusion: The method developed successfully passed all of the FDA's 2018 full validation guidelines, with the LLOQ achieved for azithromycin and Oseltamivir was 25.31 and 25.37 ng/ml.
FORMULATION AND EVALUATION OF MODIFIED PULSATILE CAPSULE FOR CHRONOPHARMACOTHERAPY OF RHEUMATOID ARTHRITIC PAIN
Authors: JYOTHIRMAYI PASAM , BHARATHI ARIGELA , SEKHARA REDDY D. RAMA
Published: March 2024

Objective: The objective of the present study was to design and evaluate pulsincap system for chrono pharmacotherapy of rheumatoid arthritis that combines advantages of both immediate and sustained release technology with the suitable delay of drug release.
Methods: Pulsatile drug delivery system based on pulsincap® technology was designed using mucoadhesive microspheres and Tramadol bilayer tablet plugs. The drug-excipient interaction was carried out by FTIR. Hardness, thickness, lag time, and swelling index all play a role in optimizing tablet plugs. The microspheres were examined for parameters such as particle size, surface morphology, encapsulation efficiency, swelling index, % mucoadhesion, and in vitro dissolution.
Results: In modified pulsincaps, bilayer tablet plug shows drug release within 40 min and hydrogel plugs shows good swelling index and suitable lag time. In microspheres formulations, MF9 is the most suitable among them as it shows better drug content, particle size, surface morphology, in vitro drug release, and release kinetics. The drug is released right away, followed by the dissolution of the enteric coating at pH 6.8, followed by a suitable delay of 6 hours, and then the maximum amount of drug release is 99.62% at the end of 10th h.
Conclusion: The pulsatile delivery system developed with HPMCK4M and tamarindus gum as plugging material showed a satisfactory lag period when compared to Tamarindus gum alone. Drug release can be achieved from treated gelatin capsule and hydrogel plug for a prolonged period by MF9 formulation.
MODIFYING FRACTION EXTRACTED FROM SESEWANUA (CLERODENDRUM FRAGRANS WILD) LEAVES IN SNEDDS PREPARATIONS: CHARACTERIZATION AND BIOAVAILABILITY TEST
Authors: SAPIUN ZULFIAYU , IMRAN ARLAN K. , ASWAD AHMAD , USMAN NUR MOHAMAD , YSRAFIL YSRAFIL , PANIGORO NUR’AINUN , UTINA NURRAHMATIA , ALIWU IKSANDI
Published: March 2024

Objective: This study aimed to determine the effect of compound modification using acyl chloride derivatives on n-hexane: ethyl acetate fraction of sesewanua leaves, focusing on the characteristics and pharmacokinetics profile in Self-Nano-emulsifying Drug Delivery System (SNEDDS) preparations.
Methods: A quasi-experimental method was used with six SNEDDS formulas, namely F0 (without active substance), F1 (acetyl chloride fraction), F2 (propanoyl chloride fraction), F3 (butyryl chloride fraction), and F4 (pentanoyl chloride fraction) and F5 (piperine compound). The fractions were subjected to characterization tests, including particle size, polydispersity index, and zeta potential as well as determination of pharmacokinetics profile using the modified crane and Wilson method.
Results: The results showed that the characterization tests of particle size using Particle Size Analyzer (PSA) for F0-F5 on gastric fluid included 15.8, 17,367, 20,367, 15.8, 28.233, and 21.533 nm. The polydispersity index values were 0.211, 0.438, 0.311, 0.383, 0.394, and 0.397, while the Zeta Potential values were-22,267,-22.2,-23.5,-24,033,-22,967, and-21.6 mV, respectively. The pharmacokinetics profile of AUC0-∞ was as follows: F0 0 μg, F1 492.83, F2 492.83, F3 245.98, F4 492.94, and F5 843.38 μg. Fraction five (F5) as a control had a higher AUC0-∞ value than compared to the fractions modified with acyl chloride derivatives. The T1/2 elimination values were F0 0 h, F1 22.5 h, F2 10.811 h, F3 35.54 h, F4 231.01 h, and F5 15.469 h.
Conclusion: Based on the results, the addition of acetyl, propanoyl, butyryl, and penthanoyl chloride affected Particle Size Characterization Analysis and pharmacokinetics profile of SNEDDS preparation of n-hexane: ethyl acetate fraction. Structural modification showed the ability to alter the bioavailability of the active ingredient according to the desired therapeutic goal.
APPROACH TO OPTIMIZE THE SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM FOR AZILSARTAN MEDOXOMIL USING BOX BEHNKEN DESIGN AND DESIRABILITY FUNCTION
Authors: KUMARI P. V. KAMALA , LIKHITHA G. , HUSSAIN MUSTAQ SHEIK JAKIR
Published: March 2024

Objective: Develop and optimize a novel self-micro emulsifying drug delivery system (SMEDDS) for enhancing the water solubility of Azilsartan (AZL) by employing the Box-Behnken design and the desirability function.
Methods: The formulation of AZL-SMEDDS consists of clove oil (oil component), Tween 20 (surfactant), propylene glycol (co-surfactant) as the independent variables and the active drug. Using a 3-level Design, the impact of independent variables on the formulation was examined. These variables' specified ranges are 20-40 mg, 50-80 mg, and 5-30 mg for X1, X2 and X3 respectively. Particle size (Y1), PDI (Y2), and dissolution % (Y3) were the response variables investigated in this study.
Results: The results indicated that the optimal values for Clove oil (X1), Tween 20 (X2), and Propylene glycol (X3) were determined to be 28.69, 76.45, and 24.93 (mg), respectively. Based on these optimized conditions, the predicted data points for the response variables Particle Size (Y1), Polydispersity (Y2), and dissolution % (Y3) were determined to be 59.85 nm, 0.729 and 55.406%, respectively.
Conclusion: The empirical results obtained from the optimized formulation exhibited a strong correlation with the predicted values. The optimized AZL-SMEDDS formulation demonstrated a rapid rate of drug solubility and greater bioavailability than AZL powder.
FORMULATION AND EVALUATION OF SUSTAINED-RELEASE FLOATING MATRIX TABLETS OF VALGANCICLOVIR HYDROCHLORIDE
Authors: G. YASHAVANTH , GOUDANAVAR PRAKASH , T. MALLAMMA , FATTEPUR SANTHOSH
Published: March 2024

Objective: The present study aimed to formulate and evaluate the formulated sustained-release floating matrix tablets of valganciclovir hydrochloride to produce a stable and bioavailable dosage form.
Methods: The tablets were prepared using hydrophilic and hydrophobic polymers such as ethyl cellulose, Hydroxy-propyl methylcellulose (HPMC), and Povidone. The formulations were subjected to evaluation characteristics such as drug content, hardness, friability, floating lag time, total floating time, and In vitro drug dissolution studies.
Results: The formulation composition and method of manufacturing are novel for this particular active moiety and robustness was assessed using a central composite design. All the formulation trials exhibited more than 90% of drug release in 12 h duration, with a floating lag time of more than 11 h, and drug content was found more than 90% across the batches. The hardness and friability profiles were found to be uniform across the batches. The preliminary evaluation confirms the received drug is pure and FTIR results show that the drug and excipients are compatible. The hardness and friability profiles were found consistent across the batches. All the formulation trials of central composite design have shown more than 90% of drug release in 12 h duration, with a floating lag time of more than 11 h, and drug content was found more than 90% across the batches.
Conclusion: The formulated valganciclovir hydrochloride sustained release floating matrix tablets showed an increased GRT with a sustained release for 12 h, thereby allowing a better window for absorption and consequently improving the drug's therapeutic effect.
EFFECT OF PEGYLATED POLYPROPYLENE IMINE DENDRITIC ARCHITECTURE ON PHARMACOKINETICS OF PYRAZINAMIDE ON RABBITS
Authors: BALASUBRAMANIAN ARUL , BALASUBRAMANIAN VALLI MANALAN , RAMALINGAM KOTHAI
Published: March 2024

Objective: This study sought to investigate the impact of pegylated polypropylene imine dendrimer-loaded pyrazinamide on drug delivery and assess this novel formulation's pharmacokinetic parameters.
Methods: Various concentrations of pyrazinamide-loaded dendrimers were formulated in four distinct batches, with the most promising formulation selected for administration to New Zealand rabbits. Plasma concentrations of the drug were subsequently compared to those of the pure drug. Pharmacokinetic parameters, including maximum plasma concentration (Cmax), time to reach Cmax (tmax), the area under the curve (AUC), the area under the first moment curve (AUMC), elimination rate constant (λz), biological half-life (t1/2), and mean residence time (MRT), were meticulously determined.
Results: The plasma drug concentration Vs time profile illustrated a sustained release pattern for the pyrazinamide drug-loaded dendrimer formulation compared to the pure drug. While a minor alteration was observed in peak plasma concentration, a notable divergence was noted in all other pharmacokinetic parameters. The AUC demonstrated a fourfold increase for pyrazinamide drug-loaded dendrimers, rising from 8657.94±295.10 to 34663.89±702.89 (ng/ml/h), and the mean residence time nearly doubled when compared to the pure drug.
Conclusion: Pyrazinamide drug-loaded dendrimers exhibit significant potential for enhancing drug release compared to the pure drug. This novel formulation promises a substantial and sustained drug release profile, holding promise for improving therapeutic outcomes and patient compliance in the treatment of relevant conditions.
EPLERENONE FLOATING MICROSPHERES: RADIOGRAPHIC AND PHARMACOKINETIC STUDIES IN RABBITS
Authors: BOORUGU RAMBABU , G.V. RADHA
Published: March 2024

Objective: The objective of the present investigation was to evaluate gastro-retentive performance and pharmacokinetic parameters of Eplerenone-optimized floating microspheres compared with formulated floating tablets.
Methods: Microsphere contains antihypertensive drug Eplerenone as a core material encapsulated with the polymeric membrane for sustained drug release were prepared by solvent diffusion-evaporation technique. The prepared microspheres were evaluated for qualitative and quantitative parameters. The optimized formulation showed favorable in vitro floating and drug release profile. The gamma scintigraphy of the formulation was carried out in rabbit in order to determine the floating ability of the final formulation with barium sulfate. Prolonged gastric residence time of over 12 h was achieved in all the animals. Eplerenone-loaded optimized formulation was orally administered to rabbit and blood samples were used to determine pharmacokinetic parameter by using WinNonlin software 3.0 version.
Results: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the Floating tablet showed improved parameters of Cmax; similarly, time to reach peak plasma concentration (t-max) for Eplerenone Floating microspheres was 4 times increased against Floating tablet formulation. The area under the curve (AUC) for formulated floating tablet was found to be 9.69 µg/ml, whereas for floating microspheres it was 16.28 µg/ml, for formulated floated tablet absorption rate constant Ka was 1.61 h, elimination rate constant was 0.112 h and elimination half-life 6.2 h. The comparison of these data undoubtedly shows that the Cmax was not much valid, but AUC was increased to about 1.68 times in case of floating microspheres, absorption rate constant was found to be decrease 3.22 times when related to the floating microspheres, whereas Ke was found to be decrease 2.11 times when equated to floating microspheres, elimination half-life was increased by almost about two times.
Conclusion: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the floating tablets showed enhanced parameters of the formulated due to floating nature of the present designed formulation.
EXPLORATION OF ANTI-MELANOMA POTENTIAL OF PHYTOCHEMICALS FROM NYCTANTHES ARBORTRISTIS THROUGH COMPUTATIONAL STUDIES
Authors: BANERJEE SHARMISTHA , BHARKATIYA MEENAKSHI , PRAKASH RAO SURADA , BAGHEL ISHITA , BAGHEL MADHURI
Published: March 2024

Objective: The goal of the current research is to identify the dominant phytochemical from the plantNyctanthesarbor-tristis Linn. and to investigate their binding affinities against the proteins BRaf Kinase mutant (3OG7) and Hsp90 Chaperone (2VCJ) that causesmelanoma.
Methods: In this work, Schrodinger software was utilized to investigate the anti-cancer potential of phytochemicals Nyctanthesarbor-tristis against specific target proteins, namely BRaf Kinase mutant (3OG7) and Hsp90 Chaperone (2VCJ) Inhibitors.
Results: Based on the outcome of the docking investigation, phytochemicals that exhibited highest binding affinity to the specified protein targets were subjected to induced fit docking and MM-GBSA computations using the Schrodinger Maestro version 2021.2 in prime module. According to the analysis, the compounds with the highest binding affinities for 2VCJ and 3OG7 are Arbortristoside D and Nicotiflorin respectively. The compound that interacted with both the proteins wasArbortristoside B. These phytochemicals appear to be more effective to the FDA-approved V600E-BRaf inhibitor Vemurafenib and Hsp90 Chaperone Inhibitor Diclonine.
Conclusion: One of the most common, deadly, and dangerous malignant diseases with a high global prevalence rate is melanoma (skin cancer). The present study may prove more helpful in developing an ideal targeted drug delivery system of phytochemicals obtained from plant Nyctanthesarbor-tristisfor treatment of melanoma. This suggests that these substances could be evolved into highly effective anti-melanoma drugs.
CHARACTERISATION, EVALUATION AND DENSITY FUNCTIONAL ANALYSIS OF CILNIDIPINE-NICOTINAMIDE COCRYSTALS DEVELOPED BY LIQUID ASSISTED GRINDING TECHNIQUE: A SUSTAINABLE APPROACH FOR ENHANCED SOLUBILITY
Authors: CHERUKKOTH RENJISH , ITTIYAVIRAH SIBI P. , HARINDRAN JYOTI , NAIR C. R. SUDHAKARAN
Published: March 2024

Objective: Improving the solubility of poorly water-soluble drugs has always been a challenge in drug development. This study aimed to enhance the aqueous solubility of a poorly water-soluble drug, Cilnidipine, by cocrystallisation method using liquid-assisted grinding (LAG) technique with Nicotinamide as the coformer. The study also aimed to understand the mechanism of cocrystal formation by quantum mechanical calculations.
Methods: The Cilnidipine-Nicotinamide cocrystals were prepared in various stoichiometric ratios using the liquid-assisted grinding (LAG) technique. The cocrystals obtained were characterised by vibrational spectroscopy, thermal methods such as differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and surface morphology by field emission scanning electron microscopy (FE-SEM). The cocrystals were evaluated for saturation solubility, and the mechanistic study of cocrystal formation was performed using the Gaussian 09 software package.
Results: FT-IR spectra of the formulated cocrystal indicated the intermolecular hydrogen bond formation between-N-H of Nicotinamide and the nitro group of Cilnidipine. DSC analysis showed a single endotherm at 96.76 °C, PXRD patterns were different from that of the reactants, and FE-SEM analysis revealed the changes in the surface morphology of the obtained cocrystal. The prepared cocrystal showed a 26.36-fold enhancement in the aqueous solubility of Cilnidipine. The DFT study demonstrated the formation of a strong intermolecular hydrogen bonding between the nitro-oxygen atom of Cilnidipine and the amide hydrogen atom of Nicotinamide in cocrystal formed.
Conclusion: This study highlights the potential of the liquid-assisted grinding method for preparing cocrystals as a sustainable and reliable approach to address the challenges posed by poorly water-soluble drugs.
EXPLORATION OF THE ACTIVE COMPOUNDS OF MORINGA OLEIFERA LAM AS HIV-1 REVERSE TRANSCRIPTASE INHIBITOR: A NETWORK PHARMACOLOGY AND MOLECULAR DOCKING APPROACH
Authors: FITRIANA MELANDA , MUN’IM ABDUL , FIRDAYANI  , ADIKUSUMA WIRAWAN
Published: March 2024

Objective: This study aims to predict the active compound of Moringa oleifera for the treatment of Human Immunodeficiency Virus (HIV), specifically targeting the HIV-1 reverse transcriptase (HIV-1 RT) enzyme using network pharmacology and molecular docking approach.
Methods: The active ingredients of M. oleifera, were screened from the Knapsack database. Subsequently, HIV-1 RT and its related target compounds were retrieved from the Genecard database. The analysis of common targets involved protein-protein interactions (PPI) analysis using string databases and constructing interaction IDs using Cytoscape software. Gene Ontology (GO) functional and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed. Molecular docking studies were conducted using AutoDock Vina software to validate the results of the network pharmacological analysis.
Results: A total of 63 active ingredients and 8601 targets related to HIV-1 RT were identified. The network analysis, encompassing GO and KEGG enrichment, revealed strong associations of common targets with key signaling pathways such as Tumor Necrosis Factor (TNF), Toll Like Receptor (TLR), and apoptosis. Additionally, 11 compounds of M. oleifera including apigenin, benzyl isothiocyanate, benzylamine, caffeic acid, ferulic acid, epicatechin, kaempferol, gallic acid, luteolin, syringic acid and vanillin were identified as potential vital compounds. Molecular docking analysis highlighted apigenin and kaempferol as the most promising compounds, exhibiting the lowest binding affinity to the HIV-1 RT enzyme. These compounds correlated with caspase-3(CASP3), caspase-9 (CASP9), and BCL2 Apoptosis Regulator (BAX) protein, stimulating cell apoptosis through multiple pathways. 
Conclusion: The study highlighted that apigenin and kaempferol are potential compound of M. oleifera in HIV-1 treatment through inhibition activity at HIV-1 RT Enzyme.
STUDY ON FORMULATION OF BACTERIAL CELLULOSE NANOFIBERS-COATED NANOLIPOSOMES CONTAINING PACLITAXEL FOR ORAL ADMINISTRATION
Authors: CAO CUONG BA , XUAN ONG PHONG , NGUYEN THANH XUAN
Published: March 2024

Objective: The low oral bioavailability of paclitaxel (PAC) because of its limited aqueous solubility and poor intestinal permeability after being administered orally suggests the need for a sustained release system. The aim of this study is to produce and evaluate in vitro a nanoliposome system that carries paclitaxel (BCN-LIP-PAC) for oral administration.
Methods: Thin-film evaporation and electrostatic deposition methods were used to obtain LIP-PAC and BCN-LIP-PAC. Particle size, polydispersity index (PDI), zeta potential, morphological analysis, entrapment efficiency percentage (EE%), and in vitro dissolution studies were used to characterize the developed systems.
Results: The nano-range sizes of LIP-PAC and BCN-LIP-PAC (0.1 % BCN) were 112±4.2 nm and 154±6.4 nm, respectively, where EE % were 80.6±2.3 % and 84.6±1.7 %, respectively. BCN-LIP-PAC exhibited good stability in simulated gastrointestinal ﬂuids. The drug release experiments conducted in vitro showed that BCN-LIP-PAC had obvious sustained release behaviors when compared to LIP-PAC. Furthermore, the release rate of PAC from all LIP-PAC and BCN-LIP-PAC was higher in SIF than in SGF.
Conclusion: The preparation, characterization, and evaluation of BCN-LIP-PAC (0.1 % BCN) for oral PAC delivery were all successful. In conclusion, the approach presented herein is a promising option for delivering oral sustained-release PAC.
QUALITY BY DESIGN SUPPORTED CONSTRUCTION OF ORAL FAST-DISSOLVING FILMS FOR TELMISARTAN: RECONNOITERING THE QUALITY ATTRIBUTES
Authors: GAYATRI DEVI MEDISETTY , KUMAR R. SANTHOSH
Published: March 2024

Objective: The angiotensin II receptor antagonist telmisartan (TMS) is often used to treat hypertension. The BCS class II antihypertensive drug TMS has a low solubility, poorly absorbed when taken orally. The goal of this study was to formulate an oral fast-dissolving film (OFDF) of TMS. In recent years, the concept of a rapidly dissolving dosage form as an innovative delivery system has gained popularity. By decreasing dosing frequency, maximize therapeutic effectiveness, bioavailability, and stability. It will also prevent the drugs from being metabolized in the first place. This technique allows for faster drug absorption from the gastrointestinal tract (GIT), which might result in a more rapid onset of action.
Methods: An experimental design known as Box-Behnken was employed to optimize a OFDF. Mango kernel (100-300 mg), maltodextrin (200-350 mg), and propylene glycol (PG) (15-30%) were chosen as independent variables with the highest preference. Included measurements of T5 tensile strength, disintegration time, folding endurance, elongation, and drug release efficiency as dependent variables.
Results: The physical properties of the films were found to be satisfactory, and Fourier transform infrared (FTIR) analysis failed to detect any drug-polymer interaction. F4 was found to have the greatest bioadhesive strength of 49.82 gm and the longest ex-vivo mucoadhesion duration of 189 min. A higher concentration of mango kernel in the formulation resulted in a greater rate of drug release. More than 60% of the drug was discharged within 10 min.
Conclusion: The oral mucosa of a rat was used for ex-vivo for irritation studies. Based on the pharmacokinetic plasma parameters, which is made into quick-dissolving films that are taken by mouth, is much better absorbed than aqueous suspensions. Studies of the enhanced formulation's stability showed that F4 may be stored for up to three months without deterioration.
DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF LORATADINE SUSTAINED RELEASED BUCCAL FILM: IN VITRO AND IN VIVO STUDY IN BEAGLE DOGS
Authors: ABDOUN SIHAM A. , ALTUWAYJIRI AMLAK S. , ALFURAYDI BUSHRA A. , ALBURAYH KHAWLAH A. , ELHASSAN GAMAL O. , GABER DALIA A.
Published: March 2024

Objective: The aim of this work was to develop and evaluate bucco-adhesive films of Loratadine (LTD) for sustained release use.
Methods: Design of twelve different sustained released buccal film formulas using Carbopol, pectin, sodium alginate, glycerol, carboxymethyl cellulose (CMC), hydroxypropyl cellulose (HPC), Gelatin, Hydroxyethyl cellulose (HEC), and Hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers. Films were evaluated for physicochemical properties, thickness, swelling, moisture content, drug content, in vitro dissolution. The pharmacokinetic parameters of optimal formula were evaluated in beagle dogs.
Results: The selected film formula (F6) showed accepted content and muco-adhesion properties. The in vitro release study showed prolonged release of drug from films over 10 h in optimal formulation. The bioavailability studies performed using beagle dogs model showed that there was 113.45% increase in the AUC0-24 of selected film compared with oral market tablets.
Conclusion: Bucco-adhesive films is a promising dosage form for improving the bioavailability of loratadine.