Future Journal of Pharmaceutical Sciences最新文献

{"title":"Exploring the protective effect exhibited by curcumin-loaded coconut oil microemulsion in the experimental models of neurodegeneration: an insight of formulation development, in vitro and in vivo study","authors":"Vijay Patil,&nbsp;Shruti Mhamane,&nbsp;Suraj More,&nbsp;Atmaram Pawar,&nbsp;S. Arulmozhi","doi":"10.1186/s43094-022-00441-5","DOIUrl":"10.1186/s43094-022-00441-5","url":null,"abstract":"<div><h3>Background</h3><p>Neurodegenerative diseases are a major health concern which requires promising drugs with appropriate drug delivery systems. The aim of the present study was development and characterization of curcumin-loaded coconut oil microemulsion (Cur-ME) and to improve the pharmacokinetic and pharmacodynamics performance. Initially, solubility study and emulsification study were performed for preliminary screening of the components. Pseudoternary phase diagram was constructed using selected components, and composition of Cur-ME was finalized. Furthermore, in vitro drug release in vivo pharmacokinetics and pharmacodynamic was performed.\u0000</p><h3>Results</h3><p>The final formulation exhibited globule size less than 20 nm with PDI and zeta potential as 0.24 and −17 mV, respectively. The formulation showed more than 90% drug content with no signs of precipitation upon dilution and centrifugation. In vitro drug release revealed 2.12-fold improvement in dissolution. In vivo plasma pharmacokinetics of Cur-ME revealed twofolds and 2.48-fold improvement in AUC and Cmax, respectively, than that of Cur-Sol. In vivo pharmacokinetics in adult zebrafish revealed significant enhancement (<i>p</i> &lt; 0.01) in curcumin delivery to the brain with 1.96-fold and 1.92-fold improvement in Cmax and AUC, respectively. Furthermore, the pharmacodynamics of the formulation was evaluated using trimethyl tin (TMT)-induced neurodegeneration in wistar rats. The results revealed that Cur-ME treated group significantly decreased the escape latency and pathlength as compared to the neurodegeneration control group. The observed effects were also markedly significant than Cur-Sol treated group. Further, the brain malondialdehyde (MDA) and glutathione (GSH) levels were found to be increased significantly as compared to Cur-Sol treated group.</p><h3>Conclusion</h3><p>The encouraging results exhibited by Cur-ME can be regarded as a mark of an effective formulation that can be used in neurodegeneration. Overall, these findings indicate that an orally delivered microemulsion has enormous potential for drug delivery to the brain.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00441-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41464781","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A comprehensive review on invasomal carriers incorporating natural terpenes for augmented transdermal delivery","authors":"Bhumika Kumar,&nbsp;Mukesh Pandey,&nbsp;Rohan Aggarwal,&nbsp;Pravat Kumar Sahoo","doi":"10.1186/s43094-022-00440-6","DOIUrl":"10.1186/s43094-022-00440-6","url":null,"abstract":"<div><h3>Background</h3><p>Transdermal drug delivery is one of the most widely used drug administration routes, which offer several advantages over other routes of drug delivery. The apical layer of the skin called the <i>stratum corneum</i> is the most dominant obstacle in the transdermal drug delivery, which restricts the passage of drugs across the skin. Considerable strategies have been applied to enhance the rate of permeation across the epithelial cells; however, the most widely used strategy is the use of sorption boosters, also known as permeation enhancers.</p><h3>Main body</h3><p>Terpenes were considered as efficient skin permeation enhancers and are generally recognized as safe as per Food and Drug Administration. Terpenes improve the permeability of drugs either by destructing the <i>stratum corneum</i>’s tightly packed lipid framework, excessive diffusivity of drug in cell membrane or by rampant drug partitioning into epithelial cells. Various vesicular systems have been developed and utilized for the transdermal delivery of many drugs. Invasomes are one such novel vesicular system developed which are composed of phospholipids, ethanol and terpenes. The combined presence of ethanol and terpenes provides exceptional flexibility to the vesicles and improves the permeation across the barrier offered due to the <i>stratum corneum</i> as both ethanol and terpenes act as permeation enhancers. Therefore, utilization of invasomes as carriers to facilitate higher rate of drug permeation through the skin can be a very useful approach to improve transdermal drug delivery of a drug.</p><h3>Conclusion</h3><p>The paper focuses on a broad updated view of terpenes as effective permeation enhancers and invasomes along with their applications in the pharmaceutical formulations.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00440-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42830873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring Clinacanthus nutans leaf different solvent extracts on antiproliferative effects induced metastasis through apoptosis and cell cycle against MCF-7 human breast cancer cell lines","authors":"Zaleha Md Toha,&nbsp;Nor Hasyimah Haron,&nbsp;Nik Nur Syazni Nik Mohamed Kamal,&nbsp;Melati Khairuddean,&nbsp;Hasni Arsad","doi":"10.1186/s43094-022-00437-1","DOIUrl":"10.1186/s43094-022-00437-1","url":null,"abstract":"<div><h3>Background</h3><p>Medicinal herbs in Malaysia like <i>Clinacanthus nutans</i> (CN) traditionally are used in the treatment of various diseases and cancers. The present research was conducted to determine the effects of <i>C. nutans</i> leaf different solvent extracts on the human breast cancer cell lines (MCF-7). The antiproliferative growth and survival effects of dichloromethane CN leaf extracts (CNDCM), as well as the short- and long-term effects through metastasis, apoptosis and cell cycle effects, were observed. The chemical profiles were done to evaluate the properties of the CNDCM.</p><h3>Results</h3><p>The evaluation of GC–MS identified 16 major phytochemical compounds present in this extract with biological activities. Antiproliferative assay used is the SRB assay, which showed the CNDCM induced strong antiproliferative property compared with the other extracts, so its IC₅₀ dose was selected for further testing with value 108 µg/mL at 72 h after exposure on MCF-7 and MCF-10A cell lines. The clonogenic survival effects of CNDCM in various concentrations (31.25, 62.5, 125, 250 and 500 µg/mL) inhibited the ability of MCF-7 cells to form colonies, and the metastasis result was indicated in an image of wound healing assay. Moreover, the CNDCM extract significantly induced apoptosis in all the cell cycle phases. Finally, the experiments with various extract concentrations on normal human breast cell lines showed no antiproliferative effects for all the extracts tested.</p><h3>Conclusion</h3><p>Among all the extracts of CN, the CNDCM extracts demonstrated the highest antiproliferative activity and survival against the MCF-7 cell lines tested.\u0000</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00437-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49220447","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"3D printing of pharmaceuticals: approach from bench scale to commercial development","authors":"Ranjitsinh Pawar,&nbsp;Atmaram Pawar","doi":"10.1186/s43094-022-00439-z","DOIUrl":"10.1186/s43094-022-00439-z","url":null,"abstract":"<div><h3>Background</h3><p>The three-dimensional (3D) printing is paradigm shift in the healthcare sector. 3D printing is platform technologies in which complex products are developed with less number of additives. The easy development process gives edge over the conventional methods. Every individual needs specific dose treatment. ‘One size fits all’ is the current traditional approach that can shift to more individual specific in 3D printing. The present review aims to cover different perspectives regarding selection of drug, polymer and technological aspects for 3D printing. With respect to clinical practice, regulatory issue and industrial potential are also discussed in this paper.</p><h3>Main body</h3><p>The individualization of medicines with patient centric dosage form will become reality in upcoming future. It provides individual’s need of dose by considering genetic profile, physiology and diseased condition. The tailormade dosages with unique drug loading and release profile of different geometrical shapes and sizes can easily deliver therapeutic dose. The technology can fulfill growing demand of efficiency in the dose accuracy for the patient oriented sectors like pediatric, geriatric and also easy to comply with cGMP requirements of regulated market. The clinical practice can focus on prescribing each individual’s necessity of dose.</p><h3>Conclusion</h3><p>In the year 2015, FDA approved first 3D printed drug product, which is initiator in the new phase of manufacturing of pharmaceuticals. The tailormade formulations can be made in future for personalized medications. Regulatory approval from agencies can bring the 3DP product into the market. In the future, formulators can bring different sector-specific products for personalized need through 3DP pharmaceutical product.</p><h3>Graphical Abstract</h3>\u0000 <div><figure><div><div><picture><source><img></source></picture></div></div></figure></div>\u0000 </div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-11-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9702622/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35208453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artemisia vulgaris Linn: an updated review on its multiple biological activities","authors":"Deepali Siwan,&nbsp;Dipali Nandave,&nbsp;Mukesh Nandave","doi":"10.1186/s43094-022-00436-2","DOIUrl":"10.1186/s43094-022-00436-2","url":null,"abstract":"<div><h3>Background</h3><p><i>Artemisia vulgaris </i>Linn, an annual herb, is also known as Mugwort or Wormwood in English, Nagadouna in Hindi, Mashibattiri, or Machipatri in Tamil. Native habitats are temperate Asia, Europe, Northern Africa and Alaska. Ethnomedicinally, it is used in traditional treatments to treat depression, epilepsy, irritability, insomnia and stress. This plant is called Herbaka in the Philippines and is used to alleviate hypertension. It is utilized as a culinary herb in western countries and is often used to flavor rice dishes and tea in Asia.</p><h3>Main body of the abstract</h3><p>Botanical description, holistic approaches, ethnomedical uses and phytochemical screening of <i>A. vulgaris</i> along with its various <i>in vitro</i>/<i>in vivo</i> pharmacological activities reported are the prime focus of this literature. The primary phytoconstituents and diverse pharmacology of this plant have been fully uncovered in order to learn about its previously unrecognized ethnomedicinal uses and provide scientists with new knowledge to advance their study of this plant.</p><h3>Short conclusion</h3><p>This review includes various principle phytoconstituents (hydroxybenzoic acid, rutoside, camphen, 1, 8-cineole and α-thujone) which are extensively shown biological activities such as analgesic, anti-fungal and anti-bacterial. However, further investigations are needed for identifying chemical constituents responsible for the claimed ethnomedicinal uses along with their mechanism of action. It is also anticipated here that the review will be the current understanding of <i>Artemisia vulgaris</i> application in complementary and alternative medicine.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-11-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00436-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46874624","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation development, optimization and characterization of Pemigatinib-loaded supersaturable self-nanoemulsifying drug delivery systems","authors":"Muthadi Radhika Reddy,&nbsp;Kumar Shiva Gubbiyappa","doi":"10.1186/s43094-022-00434-4","DOIUrl":"10.1186/s43094-022-00434-4","url":null,"abstract":"<div><h3>Background</h3><p>Pemigatinib is a small molecule tyrosine kinase inhibitor of fibroblast growth factor receptor inhibitors. The oral bioavailability of Pemigatinib is constricted due to its limited solubility at physiological pH. It is essential to develop a novel formulation of Pemigatinib to improve the intrinsic solubility and to reduce the pharmacokinetic variability. Self-nanoemulsifying drug delivery system is an effective, smart and more adequate formulation approach for poorly soluble drugs. Different from conventional self-nanoemulsifying drug delivery system, a supersaturable self-nanoemulsifying drug delivery system of Pemigatinib was prepared by using a supersaturation promoter.</p><h3>Results</h3><p>Among all the oils, Captex® 300 have shown maximum solubility of Pemigatinib. Considering the solubilization potential and emulsification ability Kolliphor®RH 40 was selected as surfactant. Transcutol®HP was selected as co-surfactant. The composition of oil, surfactant and co-surfactant was identified using phase diagrams and further adjusted by simplex-lattice design. HPMC K4M as precipitation inhibitor at 5% concentration resulted in effective supersaturating with increased self-emulsification time. The droplet of sSNEDDS ranges from 166.78 ± 3.14 to 178.86 ± 1.24 nm with PDI 0.212 – 0.256, which is significantly smaller than that observed with plain SNEDDS. TEM images revealed the spherical shape of the nanodroplets. The final optimized formulation formed spontaneous nanoemulsion within 15 secs when added to physiological fluids. The percent transmittance of the diluted formulation was found to be 99.12 ± 0.46. The viscosity was found to be 574 ± 26 centipoises indicating the good flow ability. FTIR and DSC studies indicated the amorphization of the drug. The dissolution profile of sSNEDDS indicated the faster release of drug compared to both pure drug suspension and SNEDDS formulation. The drug release rate is directly proportional to the concentration of the drug. The drug release from the insoluble matrix is a square root of time-dependent Fickian diffusion process. The formulation was found to be stable and transparent at all pH values and the percent transmittance was more than 95%. Any kind of separation or precipitation was not observed at different temperatures cycles. No significant difference was observed with all the samples exposed at different storage conditions.</p><h3>Conclusions</h3><p>This study demonstrated the feasibility of stabilizing and improving the in-vitro performance of self-nanoemulsifying drug delivery systems of Pemigatinib by incorporating HPMC K4M as precipitation inhibitor.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00434-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47865880","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research-based findings on scope of liposome-based cosmeceuticals: an updated review","authors":"Tapan Kumar Shaw,&nbsp;Paramita Paul,&nbsp;Bappaditya Chatterjee","doi":"10.1186/s43094-022-00435-3","DOIUrl":"10.1186/s43094-022-00435-3","url":null,"abstract":"<div><h3>Background</h3><p>Cosmeceuticals are cosmetic products with biologically active components that have drug-like benefits. Cosmeceuticals are currently rapidly growing segments encompassing the personal care industry and numerous topical cosmetics-based therapies for treating different skin conditions. The barrier nature of skin causes limitations to topical treatment. The effectiveness of this cosmeceutical product has been enhanced a few folds by using nanotechnological modifications. \u0000</p><h3>Main body</h3><p>PubMed electronic searches for the literature were performed using combinations of the following terms: “cosmeceutical,” “liposome-based cosmeceuticals,” “acne and liposome,” “photo-aging and liposome,” “hyperpigmentation and liposome,” “wrinkles and liposome,” “fungal infections and liposome,” and “hair damage and liposome” from the earliest publication date available to January 5, 2022. Among the various nanotechnological approaches, liposomes offer numerous advantages such as topical cosmeceutical products, starting from improved moisturization, biodegradability, biocompatibility, enhanced permeation and retention, improved bioavailability of the active ingredients, increased esthetic appeal of cosmeceutical products, slow and extended dermal release. This review outlines various liposome-based cosmeceutical products that has been investigated to treat skin disorders such as photoaging, wrinkles, hyperpigmentation, hair damage and fungal infections.</p><h3>Conclusion</h3><p>Liposome-based cosmeceuticals provide a better opportunity to deliver therapeutic moiety for various skin conditions and offer potential promise for future clinical applications.</p><h3>Graphical Abstract</h3>\u0000 <div><figure><div><div><picture><source><img></source></picture></div></div></figure></div>\u0000 </div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00435-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46405867","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Primaquine-loaded transdermal patch for treating malaria: design, development, and characterization","authors":"Pankaj Sharma,&nbsp;Mukul Tailang","doi":"10.1186/s43094-022-00433-5","DOIUrl":"10.1186/s43094-022-00433-5","url":null,"abstract":"<div><h3>Background</h3><p>The goal of the current study was to create, improve, and test a transdermal patch loaded with primaquine for the treatment of malaria. Several ingredients were used to create the transdermal patch. For the choosing of polymers, placebo patches were created. The optimization of polymer ratios for patch development and testing their impact on tensile strength, in vitro drug release, in vitro drug permeation, and ex vivo drug permeation employed response surface methods. The F5 formulation was chosen as the optimal formulation based on these answers to the data. The stability of the F5 formulation was examined. According to the findings of trials on acute skin irritation, no place where transdermal patches were given showed any signs of clinical abnormalities or a change in body weight. No erythema or edema of the skin was seen in the rabbit’s skin.</p><h3>Results</h3><p>It was observed that tensile strength of the transdermal films formulated with Eudragit RL100 and hydroxypropyl methylcellulose (<i>P</i>_mix) was found between 0.32 ± 0.017 and 0.59 ± 0.013 kg/cm², which were 0.32 ± 0.017 (F1), 0.36 ± 0.012 (F2), 0.35 ± 0.015 (F3) for <i>P</i>_mix ratio 1:1, 0.42 ± 0.011 (F4), 0.49 ± 0.010 (F5), 0.55 ± 0.016 (F6) for <i>P</i>_mix ratio 1:2 and 0.56 ± 0.014 (F7), 0.57 ± 0.010 (F8), 0.59 ± 0.013 (F9) for <i>P</i>_mix ratio 1:3. Data fitting to the Peppas, Hixon–Crowell, Higuchi, and Zero-order models was used to examine the optimized transdermal patch (F5) release kinetic mechanism. Data comparison was done using the correlation coefficient (<i>R</i>²). Zero-order had an observed correlation coefficient (<i>R</i>²) of 0.9988, which was greater than that for other models. Therefore, it was clear that the medication was released from the formulation after the Zero-order release.</p><h3>Conclusion</h3><p>The ideal thickness, percent elongation, and tensile strength of the primaquine therapeutic transdermal patches were prepared for transdermal delivery. The therapeutic transdermal patch was prepared by using Eudragit RL100: HPMC K15M (1:2) into the patch because this combination was responsible for the significant delivery of the drug into the bloodstream. The therapeutic transdermal patch has a notable penetration rate. Dimethyl sulfoxide was used as a permeation enhancer, which helped to obtain a high penetration rate. The statistical analysis was used to support the improved formulation. The therapeutic transdermal patch is a potential vehicle for the administration of primaquine, according to stability studies.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-10-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00433-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41296550","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Genetic abnormality of cytochrome-P2C9*3 allele predisposes to epilepsy and phenytoin-induced adverse drug reactions: genotyping findings of cytochrome-alleles in the North Indian population","authors":"Vivek Kumar Garg,&nbsp; Supriya,&nbsp;Ritu Shree,&nbsp;Ajay Prakash,&nbsp;Aastha Takkar,&nbsp;Madhu Khullar,&nbsp;Biman Saikia,&nbsp;Bikash Medhi,&nbsp;Manish Modi","doi":"10.1186/s43094-022-00432-6","DOIUrl":"10.1186/s43094-022-00432-6","url":null,"abstract":"<div><h3>Background</h3><p>This research aims to study the association of genetic polymorphism in genes coding for CYP2C9 and CYP2C19 in phenytoin-induced dose-related toxicity and to assess if the presence of allele CYP2C9*3 plays a role in phenytoin-induced idiosyncratic adverse effects. Current observational case control study included 142 patients with phenytoin-induced adverse drug reactions (ADRs) and 100 controls. All these patients underwent genotyping to determine the type of CYP2C9 allele [CYP2C9*1, CYP2C9*2 or CYP2C9*3) and CYP2C19 allele (CYP2C19*1, CYP2C19*2 or CYP2C19*3] by real-time polymerase chain reaction (RT-PCR) using Applied Biosystems (ABI) 7500 Real-Time PCR System (USA).\u0000</p><h3>Results</h3><p>Presence of homozygous status for allele CYP2C9*3 was associated with significantly higher risk of phenytoin-induced dose-dependent ADRs, dose-independent ADRs, gum hyperplasia, and skin rash. Presence of heterozygous status for allele CYP2C9*3 was associated with significantly higher risk of phyenytoin-induced dose-dependent ADRs and dose-independent ADRs. Presence of either heterozygous or homozygous status for CYP2C9*2 and CYP2C19*2 did not have any bearing on dose-related side effects. None of the patients showed CYP2C19*3 allele.\u0000</p><h3>Conclusion</h3><p>Variant alleles of CYP2C9*3 are significantly overexpressed among patients with phenytoin-induced ADRs, thereby suggesting the role for CYP2C9 genotype testing to predict risk of phenytoin-related ADRs.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-10-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00432-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49618573","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Elucidation of possible mechanisms of the antidiabetic potential of Zn-loaded Bryophyllum pinnatum (Lam.) extracts in experimental animal models","authors":"Varsha Tiwari,&nbsp;Abhishek Tiwari,&nbsp;Anita Singh,&nbsp;Navneet Verma,&nbsp;Manish Kumar,&nbsp;Ajay Sharma","doi":"10.1186/s43094-022-00431-7","DOIUrl":"10.1186/s43094-022-00431-7","url":null,"abstract":"<div><h3>Background</h3><p>The present study focused on the antidiabetic potential and fingerprinting analysis of <i>Bryophyllumc</i> <i>pinnatum</i> stems as well as its possible mechanisms of action along with identification of its major phytoconstituents. The oral glucose tolerance test has been performed administering a glucose solution (2000 mg/kg) to induce hyperglycemia. Diabetes have been instigated by single intra-peritoneal injection of streptozotocin (65 mg/kg).</p><h3>Results</h3><p>Alcohol and aqueous extracts were found to be safe up to a dose of 3000 mg/kg. Oral glucose tolerance test results showed significant reduction in fasting blood glucose level. Alcohol and aqueous extracts (200, 400 mg/kg b.w.) showed significant reduction in fasting blood glucose among all groups. Groups receiving zinc sulfate-loaded extracts showed a statistically significant reduction in low-density lipoproteins, triglycerides and total cholesterol levels and enhanced levels of high density lipoproteins. Fingerprinting analysis has been performed to identify the major phytoconstituents of flavonoid category morin, chrysin, and 6-hydroxy flavones, as well as iso-quercetin, hyperosides and terpenoids present in the extracts possess antidiabetic potential.</p><h3>Conclusions</h3><p>Both alcohol and aqueous extracts found to possess significant antidiabetic activity in diabetic rats. Zinc sulfate synergistically potentiates the antidiabetic potential of alcohol extract. Fingerprinting analysis revealed the presence of flavonoids such as morin, chrysin, and 6-hydroxy flavones, as well as iso-quercetin, hyperosides, and terpenoids. The possible mechanisms of antidiabetic activity have been elucidated, although further studies are required to give more elaborated mechanism on molecular basis.</p><h3>Graphical abstract</h3>\u0000 <div><figure><div><div><picture><source><img></source></picture></div></div></figure></div>\u0000 </div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2022-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-022-00431-7","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45493774","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}