Hasil untuk "Pharmacy and materia medica"

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DOAJ Open Access 2026
Flavonoids as chemopreventive agents: metabolism, apoptosis, and oxidative stress modulation

Faruk Alam, Surabhi Mandal, Bhupendra Shrestha et al.

Background: Liposomes are widely used as drug delivery systems because of their reduced systemic toxicity. Over the past few decades, numerous drug-loaded liposomes have been approved for clinical use in the treatment of cancer, viral, and fungal infections. Various liposomal formulations have progressed to later phases of clinical trials. Liposomes are spherical vesicles composed of a single or multiple phospholipid bilayers surrounding an aqueous core. Drug-loaded liposomes can exhibit controlled or targeted drug delivery, low immunogenicity, high biocompatibility, biodegradability, prolonged drug half-life, increased efficiency, reduced systemic toxicity, and enhanced pharmacokinetic properties. Methodology: This review article addresses the characteristics and types of liposomes; novel methods for their preparation, such as the Supercritical Anti-solvent Method and the Dual Asymmetric Centrifugation Method; lipid preferences; future directions for liposomes; marketed liposomal formulations; and associated patents. Results and Discussion: It has the potential to protect the drug against degradation. The aforementioned drug delivery system increases in vivo drug distribution toward target sites. PEGylated liposomes can prolong circulation time. It requires expertise in techniques, such as thin-film hydration and reverse-phase evaporation, for preparation. It has been utilized in nanomedicine. This particular delivery system requires characterizations like size, drug loading, drug release, etc. Conclusion: Liposome-embedded delivery systems advance nanotechnology and biopharmaceutics. The role of modern medicine has continued to expand, particularly in the management of chronic diseases.

Pharmacy and materia medica, Therapeutics. Pharmacology
S2 Open Access 2025
Strategies for Tag Design and Removal in the Expression and Purification of Recombinant Proteins

Jiayi Xie, Hongying Fan, Qingshan Bill Fu

Review Strategies for Tag Design and Removal in the Expression and Purification of Recombinant Proteins Jiayi Xie 1,2, Hongyi Fan 3, and Qingshan Bill Fu 1,2,* 1 School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China 2 Shanghai Institute of Materia Medica, Zhongshan Institute for Drug Discovery, Chinese Academy of Sciences, Zhongshan 528400, China 3 School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 511400, China * Correspondence: fuqingshan@simm.ac.cn Received: 19 December 2024; Revised: 10 January 2025; Accepted: 14 February 2025; Published: 8 April 2025 Abstract: Recombinant proteins find extensive applications in the biomedical and industrial fields, and efficient protein purification is often critical for achieving their functional value. Adding specific tags to the target proteins significantly enhances expression and purification efficiency and reduces time and costs. Tags can be classified into interfering and non-interfering tags, based on their effect on protein function during purification. However, interfering tags may need to be removed after purification to prevent interference with the protein’s function in downstream applications, presenting challenges for the design and utilization of tagged fusion proteins. In this article, we discuss the recent advancements in solubility tags and controllable aggregation tags, which have emerged as powerful tools to improve purification efficiency and address these challenges. We further outline strategies for optimal tag design and on-demand cleavage, and emphasize emerging trends, technical features, and forthcoming challenges that are shaping the future of tagged fusion protein production.

DOAJ Open Access 2025
ROS/Enzyme Dual-Responsive Drug Delivery System for Targeted Colorectal Cancer Therapy: Synergistic Chemotherapy, Anti-Inflammatory, and Gut Microbiota Modulation

Xin Zhang, Ruonan Lian, Bingbing Fan et al.

<b>Objectives:</b> Colorectal cancer (CRC) is a leading cause of cancer-related mortality, driven by chronic inflammation, gut microbiota dysbiosis, and complex tumor microenvironment interactions. Current therapies are limited by systemic toxicity and poor tumor accumulation. This study aimed to develop a ROS/enzyme dual-responsive oral drug delivery system, KGM-CUR/PSM microspheres, to achieve precise drug release in CRC and enhance tumor-specific drug accumulation, which leverages high ROS levels in CRC and the β-mannanase overexpression in colorectal tissues. <b>Methods:</b> In this study, we synthesized a ROS-responsive prodrug polymer (PSM) by conjugating polyethylene glycol monomethyl ether (mPEG) and mesalazine (MSL) via a thioether bond. CUR was then encapsulated into PSM using thin-film hydration to form tumor microenvironment-responsive micelles (CUR/PSM). Subsequently, konjac glucomannan (KGM) was employed to fabricate KGM-CUR/PSM microspheres, enabling targeted delivery for colorectal cancer therapy. The ROS/enzyme dual-response properties were confirmed through in vitro drug release studies. Cytotoxicity, cellular uptake, and cell migration were assessed in SW480 cells. In vivo efficacy was evaluated in AOM/DSS-induced CRC mice, monitoring tumor growth, inflammatory markers (TNF-α, IL-1β, IL-6, MPO), and gut microbiota composition. <b>Results:</b> In vitro drug release studies demonstrated that KGM-CUR/PSM microspheres exhibited ROS/enzyme-responsive release profiles. CUR/PSM micelles demonstrated significant anti-CRC efficacy in cytotoxicity assays, cellular uptake studies, and cell migration assays. In AOM/DSS-induced CRC mice, KGM-CUR/PSM microspheres significantly improved survival and inhibited CRC tumor growth, and effectively reduced the expression of inflammatory cytokines (TNF-α, IL-1β, IL-6) and myeloperoxidase (MPO). Histopathological and microbiological analyses revealed near-normal colon architecture and microbial diversity in the KGM-CUR/PSM group, confirming the system’s ability to disrupt the “inflammation-microbiota-tumor” axis. <b>Conclusions:</b> The KGM-CUR/PSM microspheres demonstrated a synergistic enhancement of anti-tumor efficacy by inducing apoptosis, alleviating inflammation, and modulating the intestinal microbiota, which offers a promising stimuli-responsive drug delivery system for future clinical treatment of CRC.

Pharmacy and materia medica
DOAJ Open Access 2025
The effects of judicialization on the budget of the Municipal Health Department of Canguçu/RS

Cristiano Manetti da Cruz, Mercia Pandolfo Provin, Ana Laura de Sene Amâncio Zara

Objectives: To identify expenses with the purchase of medicines and supplies by the Municipal Health Department of Canguçu/RS, through legal proceedings, from 2017 to 2021. Methods: It is a quantitative, descriptive, and retrospective study, using the docu-ment analysis technique. Secondary data on public costs, available on the Transparency Portal, were used. The amounts spent and the origins of the resources used for the acqui-sition of these drugs were analyzed. Results: There was an increase of 297.93% in spen-ding on legal proceedings for the acquisition of medicines and pharmaceutical supplies through judicial blockades. Of these, more than 76% refer to antineoplastic medications. The basic care budget increased by 132.41% in this period and the costs of pharmaceu-tical assistance almost doubled from R$ 854,248.86, in 2017, to R$ 1,524,871.92, in 2021, with a significant increase during the pandemic period. Comparing the expen-diture on purchasing medicines through blockages by court permits in 2021 and the amount spent on pharmaceutical assistance in the same period, it is noted that the cost is very similar, but a small portion of the population is served through judicialization. Conclusions: There was a considerable increase in spending on purchasing medicines due to court decisions. The Municipal Health Department is obliged to acquire medicines that do not belong to the Municipal Medication List, through judicial blocking of public accounts, because the government of the State of Rio Grande do Sul does not send these medicines to users with approved lawsuits.

Pharmacy and materia medica, Pharmaceutical industry
DOAJ Open Access 2024
Real-Time Fluorescence Monitoring System for Optimal Light Dosage in Cancer Photoimmunotherapy

Hideki Tanaka, Yoshikatsu Koga, Mayumi Sugahara et al.

<b>Background/Objectives</b>: Near-infrared photoimmunotherapy (NIR-PIT) was recently approved for the treatment of unresectable locally advanced or recurrent head and neck cancers in Japan; however, only one clinical dose has been validated in clinical trials, potentially resulting in excessive or insufficient dosing. Moreover, IRDye700X (IR700) fluorescence intensity plateaus during treatment, indicating a particular threshold for the antitumor effects. Therefore, we investigated the NIR laser dose across varying tumor sizes and irradiation methods until the antitumor effects of the fluorescence decay rate plateaued. <b>Methods</b>: Mice were subcutaneously transplanted with A431 xenografts and categorized into control, clinical dose (cylindrical irradiation at 100 J/cm², frontal irradiation at 50 J/cm²), and evaluation groups. The rate of tumor IR700 fluorescence intensity decay to reach predefined rates (−0.05%/s or −0.2%/s) until the cessation of light irradiation was calculated using a real-time fluorescence imaging system. <b>Results</b>: The evaluation group exhibited antitumor effects comparable to those of the clinical dose group at a low irradiation dose. Similar results were observed across tumor sizes and irradiation methods. <b>Conclusions</b>: In conclusion, the optimal antitumor effect of NIR-PIT is achieved when the fluorescence decay rate reaches a plateau, indicating the potential to determine the appropriate dose for PIT using a real-time fluorescence monitoring system.

Medicine, Pharmacy and materia medica
DOAJ Open Access 2024
Antiangiogenic activity of 5-bromoindole carbothioamide derivative in ex vivo, in vivo, and in vitro experimental study

Zainab M. Ali, Haitham Mahmood Kadhim, Omeed M. Hassan et al.

The study aimed to investigate the antiangiogenic, antioxidant, and cytotoxicity activity of a carbothioamide indole derivative. The 2-NPHC activity was evaluated using the ex vivo rat aorta ring assay, the in vivo chick chorioallantois membrane assay, the DPPH assay for scavenging activity, and the expression of the VEGF gene in colon cancer cell line (HCT116). The 2-NPHC had significant antiangiogenic activity in a dose-dependent manner in the rat aorta assay. 2-NPHC managed to reduce the DPPH free radical in a concentration-dependent, 2-NPHC had low to non-toxic effects on the HUVEC cell line, with an IC50 value of 711.7 μg/ml. The VEGF gene expression in the HCT116 cell line reduced the target gene expression compared to control cells. In conclusion, 2-NPHC exhibited significant inhibition of the angiogenesis process, either directly by inhibiting the release or activity of VEGF or indirectly through its antioxidant properties.

Pharmacy and materia medica
DOAJ Open Access 2024
The impact of medical malpractice on community

Tayyab Javed , Usama Muhammad Zahid, Liaqat Ali

Medical malpractice refers to mistakes made by medical providers in their treatment of patients. This study aimed to investigate the impact of substandard medical treatment on patients' legal rights. A qualitative research approach was chosen, using primary and secondary sources of information. The study revealed that medical malpractice significantly affects patients' rights, underscoring the need for a high-quality healthcare system that protects and enhances patient rights. It has been proven that medical errors cause medical providers to view their patients as potential plaintiffs and practice defensive medicine. This approach has negative consequences for patient care, leading to unnecessary and often harmful outcomes. Furthermore, it has been shown that medical malpractice has particularly adverse effects on patients, affecting them physically, mentally, socially, and financially.

Pharmacy and materia medica
DOAJ Open Access 2022
Atractylone Alleviates Ethanol-Induced Gastric Ulcer in Rat with Altered Gut Microbiota and Metabolites

Li L, Du Y, Wang Y et al.

Ling Li,1,2,&ast; Yaoyao Du,1,&ast; Yang Wang,3 Ning He,2 Bing Wang,1,4 Tong Zhang1 1School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of China; 2School of Pharmacy, Anhui University of Chinese Medicine, Hefei, People’s Republic of China; 3Metabo-Profile Biotechnology (Shanghai) Co. Ltd, Shanghai, People’s Republic of China; 4Chinese Academy of Sciences, Shanghai Institute of Materia Medica, Shanghai, People’s Republic of China&ast;These authors contributed equally to this workCorrespondence: Bing Wang; Tong Zhang, Email bwang@simm.ac.cn; zhangtdmj@hotmail.comBackground: Gastric ulcer (GU) is the most common multifactor gastrointestinal disorder affecting millions of people worldwide. There is evidence that gut microbiota is closely related to the development of GU. Atractylone (ATR) has been reported to possess potential biological activities, but research on ATR alleviating GU injury is unprecedented.Methods: Helicobacter pylori (H. pylori)-induced GU model in zebrafish and ethanol-induced acute GU model in rat were established to evaluate the anti-inflammatory and ulcer inhibitory effects of ATR. Then, 16S rRNA sequencing and metabolomics analysis were performed to investigate the effect of ATR on the microbiota and metabolites in rat feces and their correlation.Results: Therapeutically, ATR inhibited H. pylori-induced gastric mucosal injury in zebrafish. In the ulceration model of rat, ATR mitigated the gastric lesions damage caused by ethanol, decreased the ulcer area, and reduced the production of inflammatory factors. Additionally, ATR alleviated the gastric oxidative stress injury by increasing the activity of superoxide dismutase (SOD) and decreasing the level of malondialdehyde (MDA). Furthermore, ATR played a positive role in relieving ulcer through reshaping gut microbiota composition including Parabacteroides and Bacteroides and regulating the levels of metabolites including amino acids, short-chain fatty acids (SCFAs), and bile acids.Conclusion: Our work sheded light on the mechanism of ATR treating GU from the perspective of the gut microbiota and explored the correlation between gut microbiota, metabolites, and host phenotype.Keywords: atractylone, gastric ulcer, inflammation, oxidative stress, gut microbiota, metabolomics

Pathology, Therapeutics. Pharmacology
DOAJ Open Access 2022
Wound-Healing Effects of Curcumin and Its Nanoformulations: A Comprehensive Review

Amrita Kumari, Neha Raina, Abhishek Wahi et al.

Wound healing is an intricate process of tissue repair or remodeling that occurs in response to injury. Plants and plant-derived bioactive constituents are well explored in the treatment of various types of wounds. Curcumin is a natural polyphenolic substance that has been used since ancient times in Ayurveda for its healing properties, as it reduces inflammation and acts on several healing stages. Several research studies for curcumin delivery at the wound site reported the effectiveness of curcumin in eradicating reactive oxygen species and its ability to enhance the deposition of collagen, granulation tissue formation, and finally, expedite wound contraction. Curcumin has been widely investigated for its wound healing potential but its lower solubility and rapid metabolism, in addition to its shorter plasma half-life, have limited its applications in wound healing. As nanotechnology has proven to be an effective technique to accelerate wound healing by stimulating appropriate mobility through various healing phases, curcumin-loaded nanocarriers are used for targeted delivery at the wound sites. This review highlights the potential of curcumin and its nanoformulations, such as liposomes, nanoparticles, and nano-emulsions, etc. in wound healing. This paper emphasizes the numerous biomedical applications of curcumin which collectively prepare a base for its antibiofilm and wound-healing action.

Pharmacy and materia medica
DOAJ Open Access 2021
Co-Occurring Depression and Associated Healthcare Utilization and Expenditure in Individuals with Respiratory Condition: A Population-Based Study

Prashant Sakharkar, Thanh Mai

The existing literature is limited on the prevalence of depression among people with respiratory conditions and person-level factors that are associated with increased healthcare utilization and expenditures. The aim of this study was to explore the prevalence, pattern of healthcare use, and expenditures in noninstitutionalized individuals having co-occurring depression with respiratory conditions. The Medical Expenditure Panel Survey (MEPS) data from 2011 to 2017 was used in this study. Our sample included individuals having respiratory conditions (asthma, emphysema, and chronic bronchitis) with and without depression. Healthcare use and expenditure data were analyzed using a chi-square test, <i>t</i>-tests, and multiple linear regression analyses. There were 8848 individuals in the study. The prevalence of comorbid depression was 20%. Individuals with co-occurring depression with respiratory conditions differed significantly from individuals without co-occurring depression for age ≥ 45 years, white, and with ≤2 chronic disease conditions. Depressed individuals with respiratory conditions had higher healthcare utilization and expenditures. The presence of co-occurring depression with respiratory conditions increases the treatment complexity, healthcare utilization, and expenditure. Better treatment and management of these patients may reduce healthcare use and expenditures in the future.

Pharmacy and materia medica
DOAJ Open Access 2021
The Development and Optimization of Hot-Melt Extruded Amorphous Solid Dispersions Containing Rivaroxaban in Combination with Polymers

Jong-Hwa Lee, Hyeong Sik Jeong, Jong-Woo Jeong et al.

Rivaroxaban (RXB), a novel oral anticoagulant that directly inhibits factor Xa, is a poorly soluble drug belonging to Biopharmaceutics Classification System (BCS) class II. In this study, a hot-melt extruded amorphous solid dispersion (HME-ASD) containing RXB is prepared by changing the drug:polymer ratio (Polyvinylpyrrolidione-vinyl acetate 64, 1:1–1:4) and barrel temperature (200–240 °C), fixed at 20% of Cremophor<sup>®</sup> RH 40 and 15 rpm of the screw speed, using the hot-melt extruding technique. This study evaluates the solubility, dissolution behavior, and bioavailability for application to oral drug delivery and optimizes the formulation of rivaroxaban amorphous solid dispersion (RXB-ASD). Based on a central composite design, optimized RXB-ASD (PVP VA 64 ratio 1:4.1, barrel temperature 216.1 °C, Cremophor<sup>®</sup> RH 40 20%, screw speed 15 rpm) showed satisfactory results for dependent variables. An in vitro drug dissolution study exhibited relatively high dissolution in four media and achieved around an 80% cumulative drug release in 120 min. Optimized RXB-ASD was stable under the accelerated condition for three months without a change in crystallinity and the dissolution rate. A pharmacokinetic study of RXB-ASD in rats showed that the absorption was markedly increased in terms of rate and amount, i.e., the systemic exposure values, compared to raw RXB powder. These results showed the application of quality by design (QbD) in the formulation development of hot-melt extruded RXB-ASD, which can be used as an oral drug delivery system by increasing the dissolution rate and bioavailability.

Pharmacy and materia medica
DOAJ Open Access 2019
L-Ferritin: One Gene, Five Diseases; from Hereditary Hyperferritinemia to Hypoferritinemia—Report of New Cases

Beatriz Cadenas, Josep Fita-Torró, Mar Bermúdez-Cortés et al.

Ferritin is a multimeric protein composed of light (L-ferritin) and heavy (H-ferritin) subunits that binds and stores iron inside the cell. A variety of mutations have been reported in the L-ferritin subunit gene (<i>FTL</i> gene) that cause the following five diseases: (1) hereditary hyperferritinemia with cataract syndrome (HHCS), (2) neuroferritinopathy, a subtype of neurodegeneration with brain iron accumulation (NBIA), (3) benign hyperferritinemia, (4) L-ferritin deficiency with autosomal dominant inheritance, and (5) L-ferritin deficiency with autosomal recessive inheritance. Defects in the <i>FTL</i> gene lead to abnormally high levels of serum ferritin (hyperferritinemia) in HHCS and benign hyperferritinemia, while low levels (hypoferritinemia) are present in neuroferritinopathy and in autosomal dominant and recessive L-ferritin deficiency. Iron disturbances as well as neuromuscular and cognitive deficits are present in some, but not all, of these diseases. Here, we identified two novel <i>FTL</i> variants that cause dominant L-ferritin deficiency and HHCS (c.375+2T &gt; A and 36_42delCAACAGT, respectively), and one previously reported variant (Met1Val) that causes dominant L-ferritin deficiency. Globally, genetic changes in the <i>FTL</i> gene are responsible for multiple phenotypes and an accurate diagnosis is useful for appropriate treatment. To help in this goal, we included a diagnostic algorithm for the detection of diseases caused by defects in <i>FTL</i> gene.

Medicine, Pharmacy and materia medica
DOAJ Open Access 2018
Uji Aktivitas Antioksidan Ekstrak Etanol Buah dan Biji Buah Kalangkala (Litsea angulata) asal Kalimantan Selatan

Revita Saputri, Eka Fitri Susiani

Free radicals are atoms or molecules, having one or more unpaired electrons. Increased production of free radicals can cause oxidative stress and cause many pathological conditions, e.g. cancers, heart diseases, and other diseases. The antioxidant can inhibit oxidative stress. Kalangkala (Litsea angulata) usually found in the South Kalimantan that can be used as an antioxidant. The study aimed to determine the antioxidant activity of ethanolic extract of Kalangkala fruits and seeds from South Kalimantan. Antioxidant activity was conducted qualitatively and quantitative uses the method DPPH. The result of the antioxidant activity of ethanolic extract of Kalangkala fruits and seeds qualitatively showed the presence of yellow spots on a purple background at Thin Layer Chromatography (TLC). The result of the activity of ethanolic extract of Kalangkala seeds quantitatively obtained IC50 value was 48.78 ppm and activity of ethanolic extract of Kalangkala fruits quantitatively obtained IC50 value was 243.14 ppm. Ethanolic extract of Kalangkala fruits and seeds from South Kalimantan has antioxidant activity.

Pharmacy and materia medica

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