Assay and drug development technologies最新文献_第3页

Acknowledgment of Reviewers 2024. 审稿人致谢

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-01-01 DOI: 10.1089/adt.2024.10910.revack

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Nanocarrier-Mediated Dermal Drug Delivery System of Antimicrobial Agents for Targeting Skin and Soft Tissue Infections. 针对皮肤和软组织感染的纳米载体皮肤给药系统。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-01-01 Epub Date: 2024-11-26 DOI: 10.1089/adt.2024.060

Priya, Praveen Kumar Gaur, Shobhit Kumar

{"title":"Nanocarrier-Mediated Dermal Drug Delivery System of Antimicrobial Agents for Targeting Skin and Soft Tissue Infections.","authors":"Priya, Praveen Kumar Gaur, Shobhit Kumar","doi":"10.1089/adt.2024.060","DOIUrl":"10.1089/adt.2024.060","url":null,"abstract":"\u0000 Antimicrobial resistance in disease-causing microbes is seen as a severe problem that affects the entire world, makes therapy less effective, and raises mortality rates. Dermal antimicrobial therapy becomes a desirable choice in the management of infectious disorders since the rising resistance to systemic antimicrobial treatment frequently necessitates the use of more toxic drugs. Nanoparticulate systems such as nanobactericides, which have built-in antibacterial activity, and nanocarriers, which function as drug delivery systems for conventional antimicrobials, are just two examples of the treatment methods made feasible by nanotechnology. Silver nanoparticles, zinc oxide nanoparticles, and titanium dioxide nanoparticles are examples of inorganic nanoparticles that are efficient on sensitive and multidrug-resistant bacterial strains both as nanobactericides and nanocarriers. To stop the growth of microorganisms that are resistant to standard antimicrobials, various antimicrobials for dermal application are widely used. This review covers the most prevalent microbes responsible for skin and soft tissue infections, techniques to deliver dermal antimicrobials, topical antimicrobial safety concerns, current issues, challenges, and potential future developments. A thorough and methodical search of databases, such as Google Scholar, PubMed, Science Direct, and others, using specified keyword combinations, such as \"antimicrobials,\" \"dermal,\" \"nanocarriers,\" and numerous others, was used to gather relevant literature for this work.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"2-28"},"PeriodicalIF":1.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142715091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Preparation, Characterization, and In Vitro Evaluation of Chlorogenic Acid Loaded Hydrogel Beads for the Management of Ulcerative Colitis. 绿原酸负载水凝胶珠治疗溃疡性结肠炎的制备、表征和体外评价。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-01-01 Epub Date: 2024-12-04 DOI: 10.1089/adt.2024.072

Ranjit K Harwansh, Hemant Bhati, Rohitas Deshmukh, Mohammad Akhlaquer Rahman

{"title":"Preparation, Characterization, and In Vitro Evaluation of Chlorogenic Acid Loaded Hydrogel Beads for the Management of Ulcerative Colitis.","authors":"Ranjit K Harwansh, Hemant Bhati, Rohitas Deshmukh, Mohammad Akhlaquer Rahman","doi":"10.1089/adt.2024.072","DOIUrl":"10.1089/adt.2024.072","url":null,"abstract":"\u0000 Ulcerative colitis (UC) is a chronic inflammatory colon disorder. Several modern medicines have been used for UC treatment but are associated with side effects. Hence, herbal medicine-inspired lead molecules are promising for managing UC. Chlorogenic acid (CGA), an herbal bioactive, has been reported for anti-inflammatory, anticancer, antioxidant, and immunomodulatory activity. The current study aimed to develop enteric-coated mucoadhesive beads of CGA for colon targeting. CGA-loaded beads were prepared using chitosan and carrageenan as polymers through an ionic gelation technique. Furthermore, beads were coated with Eudragit S-100. The formulations were characterized by particle size analyzer, ultraviolet (UV)-spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), and in vitro drug release study. The optimized formulation (CGA-F2) showed particle size (440.6 ± 6.1 μm), zeta potential (-31.12 ± 2.16 mV), entrapment efficiency (83.56 ± 5.46), %yield (86.87 ± 4.19), and drug loading (1.14 ± 0.09). SEM indicated that the morphologies of CGA-F2 were spherical and ellipsoidal. The FTIR study confirmed the compatibility of the drug with polymers used in the formulations. CGA-F2 exhibited mucoadhesive efficiency (94.33 ± 2.1%) and swelling index (0.98 ± 0.03) at simulated colonic fluid (SCF) pH 7.4 (***p < 0.001) significantly. In an in vitro drug release study, CGA-F2 (95.07 ± 3.85%) showed a sustained drug release profile in SCF (pH 7.4) at 37 ± 0.5°C for 24 h. Optimized formulation exhibited drug release in a sustained manner for 24 h, which may be due to the effect of mucoadhesive and enteric coating polymer. Hence, CGA-loaded beads would be promising for treating the UC.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"29-43"},"PeriodicalIF":1.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142765646","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Ligandrol Ameliorates High-Fat Diet- and Streptozotocin-Induced Type 2 Diabetes Mellitus and Prevents Pancreatic Islets Degeneration. 利甘定能改善高脂饮食和链脲佐菌素诱发的 2 型糖尿病并防止胰岛退化

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-11-01 Epub Date: 2024-11-06 DOI: 10.1089/adt.2024.029

Deepa Sugumar, Ritaban Ghosh, Emdormi Rymbai, Jaikanth Chandrasekaran, Praveen Thaggikuppe Krishnamurthy, Ranjith S P, Shreya Sahu, Divakar Selvaraj

{"title":"Ligandrol Ameliorates High-Fat Diet- and Streptozotocin-Induced Type 2 Diabetes Mellitus and Prevents Pancreatic Islets Degeneration.","authors":"Deepa Sugumar, Ritaban Ghosh, Emdormi Rymbai, Jaikanth Chandrasekaran, Praveen Thaggikuppe Krishnamurthy, Ranjith S P, Shreya Sahu, Divakar Selvaraj","doi":"10.1089/adt.2024.029","DOIUrl":"10.1089/adt.2024.029","url":null,"abstract":"Androgen therapy has been shown to alleviate type 2 diabetes mellitus (T2DM) but is also associated with severe side effects such as prostate cancer. The present study aims to identify the best hit selective androgen receptor (AR) modulator by in silico studies and then investigates its antidiabetic effects in high-fat diet- and streptozotocin (STZ)-induced T2DM male rat model. Molecular docking and molecular dynamics (MD) studies were carried out using Maestro 13.1 and Desmond (2023-2024). Cytotoxicity and insulin secretion were measured in MIN6 cell lines. T2DM was induced using high-fat diet (HFD) for 4 weeks, followed by single STZ (40 mg/kg, intraperitoneally). OneTouch Ultra glucometer was used to measure fasting blood glucose. Gene expression was determined using reverse transcription polymerase chain reaction. Histopathology was carried out using hematoxylin and eosin stain. Through molecular docking, we identify ligandrol as a potential hit. Ligandrol showed a good binding affinity (-10.74 kcal/mol). MD showed that ligandrol is stable during the 100 ns simulation. Ligandrol increases insulin secretion in a dose-dependent manner in vitro in 2 h. Ligandrol (0.3 and 1 mg/kg, orally) significantly decreased the body weight and fasting blood glucose levels compared with the HFD and STZ group. Gene expression showed that ligandrol significantly increased the AR-targeted gene, neurogenic differentiation 1, compared with the HFD and STZ group. Histopathological staining studies showed that ligandrol prevents pancreatic islet degeneration compared with the HFD and STZ group. Our findings suggest that ligandrol's protective effect on pancreatic islets leading to its antidiabetic effect occurs through the activation of AR.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"397-408"},"PeriodicalIF":1.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142581919","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Reverse Phase-High-Performance Liquid Chromatography (RP-HPLC) Method Development and Validation Using Analytical Quality-by-Design Approach for Determination of Isoliquiritigenin in Bulk and Biological Sample. 采用 "分析质量源于设计 "方法开发和验证反相高效液相色谱 (RP-HPLC) 方法，用于测定大宗样品和生物样品中的异桔梗苷元。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-11-01 Epub Date: 2024-11-25 DOI: 10.1089/adt.2024.050

Mohamed Nihal P, Debasish Mohapatra, Alam Mohd Adil Alam Manir, Vancha Harish, Sachin Kumar Singh, Sakshi Upendra Lad, Srinivas Sutrapu, Sumant Saini, Sharfuddin Mohd

{"title":"Reverse Phase-High-Performance Liquid Chromatography (RP-HPLC) Method Development and Validation Using Analytical Quality-by-Design Approach for Determination of Isoliquiritigenin in Bulk and Biological Sample.","authors":"Mohamed Nihal P, Debasish Mohapatra, Alam Mohd Adil Alam Manir, Vancha Harish, Sachin Kumar Singh, Sakshi Upendra Lad, Srinivas Sutrapu, Sumant Saini, Sharfuddin Mohd","doi":"10.1089/adt.2024.050","DOIUrl":"10.1089/adt.2024.050","url":null,"abstract":"The primary objective of the present investigation is to develop and validate a simple, robust, and cost-effective isocratic reverse phase-high-performance liquid chromatography (RP-HPLC) method for determining isoliquiritigenin (ISL) in both bulk and biological samples using an analytical quality-by-design (AQbD) approach. The central composite design was employed for method optimization using Design Expert® software, by taking mobile phase ratio and flow rate as independent variables and peak area, retention time, tailing factor, and theoretical plates as dependent variables. The design suggested the use of a mobile phase consisting of acetonitrile:0.2% ortho-phosphoric acid (75:25, v/v) and a flow rate of 0.9 mL/min as optimal chromatographic conditions. The detection of ISL was performed at 364 nm. The optimized method was validated in accordance with International Conference on Harmonization (ICH) Q2(R1) guidelines. The method showed excellent linearity, limit of detection, limit of quantification, accuracy, precision, robustness, and system suitability. All validation parameters fell within the acceptable limits set by ICH. Additionally, the applicability of the method in biological samples were analyzed. In conclusion, the results suggest that the developed and validated AQbD-based RP-HPLC method was well-suited for the estimation of ISL in bulk and biological sample.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"409-424"},"PeriodicalIF":1.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142715098","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A Time of Transition: Looking Back with Gratitude, Forward with Optimism. 过渡时期：感恩回首，乐观前行。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-11-01 Epub Date: 2024-11-12 DOI: 10.1089/adt.2024.123

Bruce J Melancon

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Novel Pharmaceutical Cocrystal Consisting of Chlorzoxazone and Nicotinamide: A New Promising Carrier for Solubility Augmentation. 由氯唑沙宗和烟酰胺组成的新型药用共晶体：一种用于增加溶解度的新型载体。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-11-01 Epub Date: 2024-11-08 DOI: 10.1089/adt.2024.051

Arzoo Sekhani, Rahul Jha, Pranav J Shah

{"title":"Novel Pharmaceutical Cocrystal Consisting of Chlorzoxazone and Nicotinamide: A New Promising Carrier for Solubility Augmentation.","authors":"Arzoo Sekhani, Rahul Jha, Pranav J Shah","doi":"10.1089/adt.2024.051","DOIUrl":"10.1089/adt.2024.051","url":null,"abstract":"\u0000 Chlorzoxazone (CHZ) is a centrally acting muscle relaxant used to treat muscle spasms. It is employed as a first-line medication for treating muscle spasms, offering both musculoskeletal relaxation and mild sedative effects. According to the biopharmaceutics classification system, it belongs to class II drug having poor solubility and high permeability. In order to improve the flow property, water solubility, and dissolution of CHZ, CHZ-nicotinamide (NA) cocrystal was prepared by liquid-assisted grinding cocrystallization (LAG CC) method using methanol as the choice of solvent. CHZ-NA cocrystal was characterized by differential scanning calorimeter (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectrometry, and scanning electron microscopy (SEM). DSC scan showed a sharp endothermic peak shift, which is caused by the formation of a new crystal form with altered physical properties, which was further confirmed by PXRD. Also, a change in the surface morphology of LAG CC compared to CHZ was observed in SEM. The resultant CHZ-NA cocrystal displayed improved powder flow properties compared to the native form of CHZ. LAG CC demonstrated a 3.1- and 2.6-fold increase in saturated solubility and intrinsic dissolution rate, respectively, compared to CHZ alone. Furthermore, the in vitro dissolution study showed that the cumulative dissolution of CHZ in 2 h was about 53%. Whereas, dissolution of LAG CC reached 99% in 2 h, showing obvious dissolution improvement. Thus, CHZ-NA cocrystal could significantly improve the flow properties, solubility and dissolution of CHZ.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"425-434"},"PeriodicalIF":1.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142602923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Unlocking Antioxidant-Anticancer Synergy: An Exploration of Therapeutic Bioactives from Methanolic Extracts of Rubus ellipticus and Boerhavia diffusa Using HeLa Cell Line. 揭示抗氧化剂与抗癌剂的协同作用：利用 HeLa 细胞系探索椭圆茜草和白苧麻甲醇提取物中的治疗生物活性物质

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-10-01 Epub Date: 2024-07-31 DOI: 10.1089/adt.2024.040

Vipresh Bhardwaj, G T Kulkarni, Kalpana Nagpal

{"title":"Unlocking Antioxidant-Anticancer Synergy: An Exploration of Therapeutic Bioactives from Methanolic Extracts of Rubus ellipticus and Boerhavia diffusa Using HeLa Cell Line.","authors":"Vipresh Bhardwaj, G T Kulkarni, Kalpana Nagpal","doi":"10.1089/adt.2024.040","DOIUrl":"10.1089/adt.2024.040","url":null,"abstract":"\u0000 This study aimed to assess the synergistic antioxidant and anticancer effects of methanolic extracts derived from Rubus ellipticus and Boerhavia diffusa fruits against the HeLa cell line. The methanolic extracts were prepared from the fruits of R. ellipticus and B. diffusa, and their antioxidant potential was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity assay and the ferric reducing antioxidant power (FRAP) assay. The anticancer effects of benzoic acid and rutin extracted from the aforementioned fruits were also investigated against the HeLa cell line using the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide assay to measure the cell metabolic activity. Using Synergy Finder plus software, the bioactive compounds were tested to explore any synergistic effects. R. ellipticus exhibited higher antioxidant potential as revealed by higher DPPH scavenging activity and FRAP value compared with B. diffusa. The benzoic acid extracted from R. ellipticus demonstrated potent anticancer activity against the HeLa cell line, with an IC50 of 1.07 µg/mL. Similarly, rutin extracted from B. diffusa displayed moderate anticancer activity with an IC50 of 1.4 µg/mL while exhibiting minimal impact on normal cell lines. The combination studies of the extracted bioactive compounds revealed a synergistic effect. These findings suggest the therapeutic potential of R. ellipticus and B. diffusa in combating the oxidative stress and cancer. Their bioactive compounds like benzoic acid and rutin were observed to act synergistically. Further investigations are warranted to elucidate the underlying mechanisms and evaluate their applicability in clinical settings.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"361-372"},"PeriodicalIF":1.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141858935","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Drug Repurposing Patent Applications: April-June 2024. 药物再利用专利申请：2024 年 4 月至 6 月。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2024-10-01 Epub Date: 2024-09-24 DOI: 10.1089/adt.2024.081

Hermann A M Mucke

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Polyherbal Antiacne Gel: In Vitro Antibacterial Activity and Efficacy Evaluation Against Cutibacterium acnes. 多草本祛痘凝胶：针对痤疮杆菌的体外抗菌活性和功效评估

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2024-09-10 DOI: 10.1089/adt.2024.031

Praveen Kumar Gaur,Rosaline Mishra,Rahul Kaushik,Krishan Kumar Verma,Nitin Kumar,Kank Lata

{"title":"Polyherbal Antiacne Gel: In Vitro Antibacterial Activity and Efficacy Evaluation Against Cutibacterium acnes.","authors":"Praveen Kumar Gaur,Rosaline Mishra,Rahul Kaushik,Krishan Kumar Verma,Nitin Kumar,Kank Lata","doi":"10.1089/adt.2024.031","DOIUrl":"https://doi.org/10.1089/adt.2024.031","url":null,"abstract":"Acne is a common skin condition that affects people of all ages and can lead to significant physical and psychological distress. The first line of action against acne is topical products, though the most effective are topical antibiotics. In such a scenario, the development of effective and safe herbal formulations for the treatment of acne is of great importance. Rubia cordifolia, Aloe barbadensis, and Allium cepa extracts are rich sources of bioactive metabolites and are safe compared with antibiotics, in addition to being cost effective, sustainable, and eco-friendly. Also, their combination has not been studied for treating acne, and their potential benefits need to be investigated. The present study aimed to develop an effective polyherbal gel formulation of R. cordifolia, A. barbadensis, and A. cepa combined extract for treating acne and validate its effect with reference to conventional antibiotics. Plant materials were extracted in water by the reflux method, and phytochemical analysis was done for flavonoid, anthraquinone, and phenolic contents. The combined extract (R. cordifolia, A. barbadensis, and A. cepa extracts) was formulated in gel. The selected polyherbal gel was evaluated for in vitro antibacterial activity using agar well diffusion against Cutibacterium acnes (P. acnes) culture. Phytochemical analysis of the composite extract revealed the rich presence of flavonoids, phenolics, and anthraquinones. The polyherbal gels showed good physicochemical properties; however, FCEG-4 was selected for further studies. It was found to be effective against C. acnes (MTCC 1951) in agar well diffusion, as it showed a similar zone of inhibition as that of standard. Also, during in vivo studies, FCEG-4 showed comparable efficacy with clindamycin gel. It was concluded from the study that composite extracts incorporated in an aqueous-based gel system were effective in topical therapy of mild acne vulgaris, showing similar efficacy to that of clindamycin cream.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"1 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142202113","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0