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":"<p><p>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.</p>","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}
{"title":"A Time of Transition: Looking Back with Gratitude, Forward with Optimism.","authors":"Bruce J Melancon","doi":"10.1089/adt.2024.123","DOIUrl":"10.1089/adt.2024.123","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"395-396"},"PeriodicalIF":1.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142613866","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}
{"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":"<p><p>\u0000 <i>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 <i>in vitro</i> 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.</i>\u0000 </p>","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}
{"title":"Unlocking Antioxidant-Anticancer Synergy: An Exploration of Therapeutic Bioactives from Methanolic Extracts of <i>Rubus ellipticus</i> and <i>Boerhavia diffusa</i> 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":"<p><p>\u0000 <i>This study aimed to assess the synergistic antioxidant and anticancer effects of methanolic extracts derived from <i>Rubus ellipticus</i> and <i>Boerhavia diffusa</i> fruits against the HeLa cell line. The methanolic extracts were prepared from the fruits of <i>R. ellipticus</i> and <i>B. diffusa</i>, 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. <i>R. ellipticus</i> exhibited higher antioxidant potential as revealed by higher DPPH scavenging activity and FRAP value compared with <i>B. diffusa</i>. The benzoic acid extracted from <i>R. ellipticus</i> demonstrated potent anticancer activity against the HeLa cell line, with an IC<sub>50</sub> of 1.07 µg/mL. Similarly, rutin extracted from <i>B. diffusa</i> displayed moderate anticancer activity with an IC<sub>50</sub> 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 <i>R. ellipticus</i> and <i>B. diffusa</i> 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.</i>\u0000 </p>","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}
{"title":"Drug Repurposing Patent Applications: April-June 2024.","authors":"Hermann A M Mucke","doi":"10.1089/adt.2024.081","DOIUrl":"10.1089/adt.2024.081","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"387-394"},"PeriodicalIF":1.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142340180","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}
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}
{"title":"Latest Delivery Advancements of Lipid Nanoparticles for Cancer Treatment.","authors":"Somia Chauhan, Kalpana Nagpal","doi":"10.1089/adt.2024.019","DOIUrl":"10.1089/adt.2024.019","url":null,"abstract":"<p><p>\u0000 <i>As one of the primary causes of illness and death globally, cancer demands novel and potent treatment approaches, which is why lipid nanoparticles (LNPs) have gained attention as a promising delivery system for anticancer drugs with precision and efficacy. The article discusses the salient characteristics of LNPs, such as the lipid components, particle size, polydispersity index, and encapsulation efficiency, followed by strategies that enhance their remarkable drug delivery capabilities. The articles explore LNPs ability to improve the solubility, stability, and bioavailability of various chemotherapeutics, nucleic acids, and immunotherapeutic modalities. It also highlights the recent advancement in surface modification of LNPs, which is essential to improve their effectiveness. Tailored coatings of LNPs improve targeting precision, stability, and biocompatibility; enhancing their transport to boost therapeutic efficacy for cancer targeting. The review summarizes the recent advancements made in using LNPs to treat different forms of cancer and focuses on the most recent clinical studies. Overall, the review highlights that the LNPs can target and treat cancer in a tailored manner through gene therapy, RNA interference, and immunotherapy.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"340-360"},"PeriodicalIF":1.6,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141537447","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}
Amala Maxwell, Prachi Modi, Karishma Sequeira, Masuma Punja, Shaila Lewis
{"title":"A Novel <i>In Situ</i> Gelling System of Quercetin/Sulfobutyl-Ether-β-Cyclodextrin Complex-Loaded Chitosan Nanoparticles for the Treatment of Vulvovaginitis.","authors":"Amala Maxwell, Prachi Modi, Karishma Sequeira, Masuma Punja, Shaila Lewis","doi":"10.1089/adt.2024.042","DOIUrl":"10.1089/adt.2024.042","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"308-324"},"PeriodicalIF":1.6,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141726814","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}
{"title":"Synthesis of Novel Acrylamide Graft Copolymer of <i>Acacia nilotica</i> Gum for the Stabilization of Melatonin Nanoparticles for Improved Therapeutic Effect: Optimization Using (3)<sup>2</sup> Factorial Design.","authors":"Sonali Sundram, Neerupma Dhiman, Rishabha Malviya, Rajendra Awasthi","doi":"10.1089/adt.2024.013","DOIUrl":"10.1089/adt.2024.013","url":null,"abstract":"<p><p>\u0000 <i>The objective of the present study was to optimize the microwave-assisted synthesis of the acrylamide graft copolymer of <i>Acacia nilotica</i> gum (AM-co-ANG). Furthermore, graft copolymer was used for the formulation of a nanoparticulate system using a novel top to bottom solvent antisolvent technique for the delivery of melatonin. Grafting of ANG was optimized by using 3<sup>2</sup> factorial design, where concentrations of polymer and monomer (acrylamide) were used as independent variables and swelling index in acidic (0.1 N HCl) and basic (1 N NaOH) pH. Grafted polymers were further used to develop and optimize nanoparticulate system using concentration of the graft copolymer and concentration of drug as independent variables. The size of the nanoformulation and entrapment efficiency were selected as dependent variables. Difference in infrared spectrum and absorbance maxima in the ultraviolet region confirm that grafting has taken place. Porous structure and a higher contact angle confirmed hydrophobic nature of AM-co-ANG as compared with the native polymer. Acrylamide graft copolymers show more swelling in 1 N NaOH as compared with 0.1 N HCl. <i>In vitro</i> toxicity studies in hepatic (HepG2 cell line), brain (SHSY5Y cell line), and skin (HaCaT cell line) cells easily predict that synthesized polymer have no cytotoxicity. The entrapment efficiency ranged from 55.24 ± 1.35% to 73.21 ± 1.83%. A nonlinear correlation was observed between independent and dependent variables, as confirmed by multivariate analysis of variance, surface regression, and the correlation report. The prepared formulations were able to release drug up to 12 h. The regression coefficient easily predicted that most of the formulations followed Baker-Lonsdale drug release kinetics.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"278-307"},"PeriodicalIF":1.6,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141496958","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}