{"title":"Silibinin-Loaded Nanostructured Lipid Carriers for Growth Inhibition of Cisplatin-Resistant Ovarian Cancer Cells.","authors":"Sevda Jafari, Atabak Bakhshaei, Morteza Eskandani, Ommoleila Molavi","doi":"10.1089/adt.2022.060","DOIUrl":"https://doi.org/10.1089/adt.2022.060","url":null,"abstract":"<p><p>Cisplatin is the most often used chemotherapy in the treatment of ovarian cancer (OC), however long-term usage leads to drug resistance and treatment failure. Silibinin is a sparingly water-soluble natural compound with well-known anticancer effects. The use of lipid-based delivery systems is a potential approach for enhancing silibinin's water solubility. In this study, nanostructured lipid carriers (NLCs) containing silibinin were prepared and their inhibitory effects were tested in combination with cisplatin against sensitive/resistant A2780 OC cells. Silibinin-loaded NLCs (silibinin-NLCs) were prepared by the hot homogenization method, and their size, shape, zeta potential (ZP), and encapsulation efficiency (EE), as well as their inhibitory effects, were examined in combination with cisplatin against sensitive/resistant A2780 OC cells. Formulation of silibinin-NLCs using cocoa butter led to spherical-shaped NLCs with a size of 95 nm and EE of 98%. The ZP and the dispersion index of the silibinin-NLCs were -27.12 ± 0.13 mv and 0.12 ± 0.04, respectively. The release kinetics of silibinin-NLCs was best fitted with the zero-order model. The combination of cisplatin and silibinin-NLCs sensitized the cisplatin-resistant A2780 OC cells and exhibited a more synergistic inhibitory effect on A2780 cells as compared with the combination of cisplatin and plain silibinin. The optimized silibinin-NLCs can be considered a suitable drug delivery system for the inhibition of cisplatin-resistant OC cells.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"339-348"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10412200","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":"Development and Validation of Reverse-Phase High-Performance Liquid Chromatography Based Bioanalytical Method for Estimation of Simvastatin in Rat's Plasma.","authors":"Narendra Kumar Pandey, Sachin Kumar Singh, Bimlesh Kumar, Leander Corrie, Umesh Goutam, Dileep Singh Baghel","doi":"10.1089/adt.2022.080","DOIUrl":"https://doi.org/10.1089/adt.2022.080","url":null,"abstract":"<p><p>Simvastatin (SIM) is known to lower cholesterol levels and is speculated in the pathogenesis of Alzheimer's disease. In this study, the bioanalytical method of SIM SNEDDS was developed and validated for the estimation of SIM in the rat's plasma using reverse-phase high-performance liquid chromatography. C-18 reverse-phase octadecylsilyl column was used to validate the method. Atorvastatin (ATV) was used as an internal standard. Gradient elution was performed using acetonitrile and water in a ratio of 90:10 with a flow rate of 1 mL/min. The chromatogram of these both compounds SIM and ATV was detected at a wavelength of 238 and 244 nm. The drugs were extracted from the plasma samples using the protein precipitation method. The retention time of SIM and ATV was found to be 3.720 and 8.331 min, respectively. The developed method was found to be linear in the range between 50 and 250 ng/mL, with a regression coefficient (r<sup>2</sup>) of 0.9994. According to ICH M10 guidelines, the method was validated. The percent of drug recovery was more than 95% and the % relative standard deviation was <2% in the replicate studies, which showed that the method was accurate and precise. The limit of detection and limit of quantification were found in rat plasma to be 0.12 and 0.38 ng/mL, respectively. The obtained result indicated that the developed method was successful in estimating SIM in rat plasma and passed all validation test parameters.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"349-358"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10762625","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 July-September 2022.","authors":"Hermann A M Mucke","doi":"10.1089/adt.2022.097","DOIUrl":"https://doi.org/10.1089/adt.2022.097","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"359-366"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10412199","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":"Potential Assessment of Topical Felbinac-Loaded Cubosomal Gel in Soft Tissue Injury in Albino Rats.","authors":"Snigdha Bhardwaj, Anshul, Praveen Kumar Gaur, Sonam Bhatia","doi":"10.1089/adt.2022.063","DOIUrl":"https://doi.org/10.1089/adt.2022.063","url":null,"abstract":"<p><p>Muscle strain is one of the most common injuries with high intermittence rate. Due to diverseness of strain injuries, different experimental animal models are employed to investigate such injuries with reproducible results. Cubosomes, an emerging nano drug delivery tool, are considered ideal carriers for the topical delivery of lipophilic drugs to treat local inflammations with reduced frequency of application for prolonged periods. This work describes the development of Felbinac-loaded cubosomal gel and investigated the treatment of inflammation and tissue injury <i>in vivo</i>. Sciatic Function Index (SFI) is a simple clinical method to observe hind limb recovery in rats after induced injuries. First, cubosomes were fabricated by high-pressure homogenization process and evaluated for <i>in vitro</i> parameters. The optimized cubosome formulation was chosen to develop cubosomal gel and evaluated for <i>in</i> vitro parameters and also investigated time to recovery of SFI after strain induction in tibialis anterior muscles in rats. The cubosome formulation (F4) exhibited low droplet size (51.04 ± 1.37 nm)and polydispersity index (0.085 ± 1.13), and negative zeta potential (-32.8 ± 0.67 mV). In rats, topical application of cubosomal gel formulation (CGF) exhibited significant improvement in skin permeation (402 ± 6.08 μg) and drug flux (15.71 ± 0.82 μg/cm<sup>2</sup> h) compared to plain gel. Also, CGF demonstrated significant difference in SFI from first to seventh day. The histology of rat skin showed significant effect for groups treated with Felbinac-loaded CGF compared to a negative control group.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"367-376"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10413074","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":"Healing Potential of Propolis Extract-<i>Passiflora edulis</i> Seed Oil Emulgel Against Excisional Wound: Biochemical, Histopathological, and Cytokines Level Evidence.","authors":"Puneet Gupta, Ashish Singh, Neelam Singh, Faraat Ali, Ayushi Tyagi, Sadish K Shanmugam","doi":"10.1089/adt.2022.075","DOIUrl":"https://doi.org/10.1089/adt.2022.075","url":null,"abstract":"<p><p>Propolis is rich in natural bioactive compounds, and considering its importance for many skin therapies, emulgel was prepared. This study examines how a propolis extract (PE) and Passiflora edulis seed (PS) oil emulgel affect rat deep skin wound healing. Based on preset criteria of maximum drug content and optimum drug permeation through the stratum corneum along with drug retention in the skin layers, an optimized emulgel formula based on Box-Behnken factorial design was prepared and used for subsequent <i>in vitro</i> and <i>in vivo</i> evaluations. <i>In vivo</i> wound-healing activities of emulgel and control treatments were investigated in a rat model. The optimized emulgel formula exhibited superior healing activity compared with plain PE suspension-treated rats on day 14 of wounding. Histopathological investigations of hematoxylin and eosin and Masson's Trichrome-stained skin sections supported this effect. Emulgel promotes cutaneous wound healing through a variety of mechanisms, including anti-inflammatory through modulation of cytokines tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production, and promotion of collagen fiber formation, all of which contribute to tissue remodeling. Furthermore, when compared with propolis suspension, emulgel showed significant antioxidant and anti-inflammatory effects. Emulgel significantly increased the skin's hydroxyproline level, antioxidant potential, wound contraction, increased penetration, and localized propolis deposition across the skin. Incorporation of PS oil into the emulgel accelerates the tissue regeneration process. The findings suggest that 5% propolis emulgel could be used as an alternative to treat wounds.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 7","pages":"300-316"},"PeriodicalIF":1.8,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40561376","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":"<i>Letter to the Editor:</i> 3D Printing Has an Imperative Role in Colitis Management.","authors":"Sarmili Sahoo, Amandeep Singh","doi":"10.1089/adt.2022.078","DOIUrl":"https://doi.org/10.1089/adt.2022.078","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 7","pages":"295-297"},"PeriodicalIF":1.8,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40561373","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":"Editor's Response to a Letter on \"3D Printing Has an Imperative Role in Colitis Management\" by Sahoo and Singh.","authors":"Bruce J Melancon","doi":"10.1089/adt.2022.29101.bjm","DOIUrl":"https://doi.org/10.1089/adt.2022.29101.bjm","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 7","pages":"298-299"},"PeriodicalIF":1.8,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40561375","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":"Computational Design of Phosphatidylinositol 3-Kinase Inhibitors.","authors":"Isha Rani, Anju Goyal, M Sharma","doi":"10.1089/adt.2022.057","DOIUrl":"https://doi.org/10.1089/adt.2022.057","url":null,"abstract":"<p><p>\u0000 <i>One of the most sought-after therapeutic targets for treating human cancers is the phosphoinositide 3-kinase; PI3k is an integral part of the PI3K/protein kinase B signaling arcade. This pathway is frequently activated in malignancies. Drug resistance and dose-limiting adverse effects are currently associated challenges with the existing anticancer chemotherapy. Therefore, in this research, a series of pyrimidine derivatives were designed and evaluated against human PI3K by using molecular docking analysis. The docking results were further verified by molecular dynamic simulation, which analyzed the strength of the macromolecular complex with respect to time. Compounds IV and XIV were found to be the most potent inhibitors of the human PI3K receptor with a high degree of stability within the active site of the target receptor for a timeframe of 50 ns. Thus, both of these compounds could be important drug candidates for the development of PI3K inhibitors as a prospective anticancer agent.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 7","pages":"317-337"},"PeriodicalIF":1.8,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40561374","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 March: June 2022.","authors":"H. Mucke","doi":"10.1089/adt.2022.065","DOIUrl":"https://doi.org/10.1089/adt.2022.065","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2022-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42502329","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 Review on Delivery and Bioavailability Enhancement Strategies of Azithromycin.","authors":"Pallavi Swarup, Gopal Prasad Agrawal","doi":"10.1089/adt.2022.036","DOIUrl":"https://doi.org/10.1089/adt.2022.036","url":null,"abstract":"<p><p>Azithromycin (AZI) belongs to the class of macrolide antibiotics that has limited water solubility and belongs to Biopharmaceutical Classification System Class II. Dissolution is the rate-limiting step in the absorption process of AZI. Several approaches have been investigated for enhancing the bioavailability of poorly soluble drugs. This review intends to explore the various strategies that have been investigated for improving the solubility and/or bioavailability of AZI and the delivery systems that have been designed for delivery of AZI in ocular fluid.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 6","pages":"251-257"},"PeriodicalIF":1.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33449341","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}