Future Journal of Pharmaceutical Sciences最新文献

{"title":"Bioautography, synergistic effect and HPTLC-MS and SEM analysis of antimicrobial and antioxidant compounds of inflorescence extract of Sphaeranthus indicus","authors":"Dhananjay Tandon,&nbsp;Ashwini Kumar Gupta","doi":"10.1186/s43094-023-00518-9","DOIUrl":"10.1186/s43094-023-00518-9","url":null,"abstract":"<div><h3>Background</h3><p><i>Sphaeranthus indicus</i> L. is a well-known medicinal plant in folk medicine. A variety of biological activities and chemical substances in this plant have been reported. The phytochemical content and activity may vary according to geographic location. This study aims to determine the geographical significance, the analysis of the synergistic effect of phytochemicals, the identification of active compounds, and the determination of the action mechanism of <i>S</i>. <i>indicus</i> inflorescence methanolic extract against <i>Staphylococcus aureus</i> and <i>Klebsiella pneumonia</i>.</p><h3>Results</h3><p>The bands with Rf values of 0.92 and 1.0 showed antimicrobial activity, while all bands showed antioxidant activity. The first fraction showed the highest antimicrobial activity, and the pool of the second fraction showed the highest antioxidant activity. The kinetics of the antioxidants differed among the fractions. Analysis of synergistic effects showed that several compounds were involved in the activities. The bands with Rf 0.45, 0.55, 0.68, 0.79, and 0.85 were active components of the extract. Leakage of cell contents was detected at 260 and 280 nm wavelengths. Six different proteins and one nucleic acid band were detected after electrophoresis. The SEM analysis showed that the phytochemicals caused severe membrane damage.</p><h3>Conclusion</h3><p> The study revealed that the photochemical present in methanol extract of the inflorescence of <i>S. indicus</i> has a synergistic effect and acts on bacterial cell envelope. The five compounds were identified as active molecules belonging to the class of terpenoids. The result also signified the geographical area since thymol was identified for the first time in this plant at this location.</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":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00518-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44884574","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":"Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation","authors":"Prerna Hemant Sidwadkar,&nbsp;Nitin Hindurao Salunkhe,&nbsp;Kailas Krishnat Mali,&nbsp;Vijay Bapu Metkari,&nbsp;Durgesh Paresh Bidye","doi":"10.1186/s43094-023-00521-0","DOIUrl":"10.1186/s43094-023-00521-0","url":null,"abstract":"<div><h3>Background</h3><p>The objective of the present investigation was to obtain directly compressible agglomerates of ibuprofen with nicotinamide by a quasi-emulsification solvent diffusion technique. Ibuprofen-nicotinamide agglomerates were prepared by quasi-emulsification solvent diffusion technique using ethanol (good solvent), water (poor solvent), and chloroform (bridging liquid). The prepared agglomerates were characterized by ATR-FTIR, powder X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy and were evaluated for tableting performance and in vitro drug release. To appropriately identify the hydrogen bonding sites, a thorough understanding of the structures of API and coformer is necessary, hence molecular docking approach was implemented to depict the interaction between the proposed coformer and COX-2 protein (PDB Id:4PH9).</p><h3>Results</h3><p>The percent yield of agglomerates was in the range of 85–98 w/w%, and drug content for all batches was in the range of 96–99%. The microphotographs showed irregular circularly shaped agglomerates. ATR-FTIR study showed a strong possibility of hydrogen bonding between ibuprofen and nicotinamide. The crystallinity of ibuprofen was slightly reduced and confirmed by P-XRD and DSC. Crushing strength and friability studies showed good handling qualities of ibuprofen agglomerates. Heckel plot studies showed low mean yield pressure and high tensile strength, indicating excellent compressibility and compactibility of ibuprofen agglomerates. More than 90% drug release was obtained within 60 min in PBS (pH 7.4). The docking studies revealed that nicotinamide individually has –CDOCKER energy 16.8109 where coformer showed 29.0584, which indicates coformer has a better binding affinity to target as compared to nicotinamide individual.</p><h3>Conclusions</h3><p>It can be concluded that the agglomerates improved the dissolution, tableting performance, and solid-state properties of ibuprofen and hence can be useful to improve the therapeutic performance of ibuprofen.</p><h3>Graphic 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":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00521-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42398782","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":"Development of a robust and reliable reverse-phase high-performance liquid chromatography (RP-HPLC) method using analytical quality by design principles for the accurate determination of esculin in its bulk form","authors":"Sarvesh Patil,&nbsp;Anjana Adhyapak,&nbsp;Priya Shetti,&nbsp;Rohan Gurao","doi":"10.1186/s43094-023-00524-x","DOIUrl":"10.1186/s43094-023-00524-x","url":null,"abstract":"<div><h3>Background</h3><p>Analytical quality by design is a proactive, holistic, and data-driven approach to quality that emphasizes risk assessment and management. This can lead to more robust and reliable methods than traditional approaches. Using principles of analytical quality by design for method development can help to assure the quality and consistency of analytical methods. This is important for the pharmaceutical industry, where accurate and reproducible analytical methods are essential for ensuring drug safety, shelf life, and efficacy. Esculin is a naturally occurring derivative of coumarin that is found in the stems of the plant Aesculus indica. The present study describes the use of an analytical quality by design approach to develop and validate a reliable RP-HPLC method for the analysis of esculin bulk form.</p><h3>Result</h3><p>A central composite design was employed to optimize the percent of methanol in the mobile phase and flow rate for the analysis of a compound esculin using the RP-HPLC method. The optimized conditions were 43% methanol and 0.9 ml/min flow rate, with a retention time of 3.78 min, and Phenomenex Luna (5 µm × 250 mm, 4.6 mm) column was used. The method was found to be linear with a correlation coefficient of 0.9998 for a concentration range of 4–20 μg/ml. The parameters of the system suitability test were within the acceptable range (0.0612–0.1398%), and the precision for both intra-day and inter-day measurements was below 2%. The robustness and ruggedness of the method were also good, with changes in the flow rate and mobile phase composition having a minimal impact on the method's performance. The limit of detection (LOD) and limit of quantification (LOQ) values were reported to be 0.82891 μg/ml and 2.511 μg/ml, respectively. The validation parameters of the method adhered to the specified limit following the ICH guidelines.</p><h3>Conclusion</h3><p>In summary, an AQbD-based efficient and robust RP-HPLC chromatographic method has been developed for the quantification of the esculin compound. The method is linear, precise, and reproducible, and it has good LOD and LOQ values. The method could be used for repetitive analysis of the compound in pharmaceutical formulations.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00524-x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43801160","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":"Critical variables affecting the layering method of pelletization","authors":"Drashti Maniyar,&nbsp;Pramod Kadu,&nbsp;Mirza Ilyas Rahim Baig","doi":"10.1186/s43094-023-00522-z","DOIUrl":"10.1186/s43094-023-00522-z","url":null,"abstract":"<div><p>The oral route of delivery is the most preferred route for administering most of the drugs. Pellets have gained importance since they offer numerous advantages like decreased dose dumping, improved patient compliance since dosing frequency is reduced, and ease of administering multiple chemically incompatible drugs immediately without the possibility of them interacting with each other. The critical variables related to process and equipment are identified and what impact they have on the quality of pellets formed is discussed. The position of the spray nozzle also affects the pellets and their yield. A complete guideline has been drawn which makes the process of pelletization using the Wurster method easier. The process variables affecting the pelletization process include inlet and product temperature, relative humidity, batch size; spray rate, and atomization air pressure and the equipment variables include column height, air distribution plate, a type of filter, and shaking interval. All these variables have a low, medium, or high impact on the process and they all together contribute to the quality of pellets formed. This review article focuses on critical process and equipment variables affecting the process of pelletization and the quality of pellets formed when using the Wurster equipment. The main objective is to review critical variables affecting the layering method of palletization and to sketch some basic problems encountered during pelletization and their troubleshooting.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00522-z","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44304054","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":"Suzuki–Miyaura cross-couplings for alkyl boron reagent: recent developments—a review","authors":"Adnan Ahmed,&nbsp;Irfan Mushtaq,&nbsp;Sampath Chinnam","doi":"10.1186/s43094-023-00520-1","DOIUrl":"10.1186/s43094-023-00520-1","url":null,"abstract":"<div><p>In the history of catalysis and organic synthesis, boric chemistry has been developed into one of the most varied and practical disciplines. Several useful Suzuki–Miyaura cross-coupling (SMC) reactions as well as hydroborylation reactions are regarded the essential tools inside the chemical synthesis toolkit accompanied by researchers of the industry or the academia. Novel synthesis of the less electrically and sterically ongoing carbon–boron synthetic reagents is carried out to ensure a unique coupling reaction utilizing metals along with these reagents which draws considerable interest in accelerating the discovery of creative uses for otherwise difficult organic adducts in many disciplines. This article details the noteworthy advancements in the use of traditional metal-catalyzed carbon–carbon coupling processes with cutting-edge coupling partners such as carbon–boron reagents often the beta-alkyl Suzuki–Miyaura coupling since 2001. The current review covers alkylboranes, organotrifluoroborates, 9-BBN, alkylboronic acids and boronic esters as useful reagents in SMCs that will help synthetic chemists in developing new compounds.</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":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00520-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43103902","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":"Emerging of artificial intelligence and technology in pharmaceuticals: review","authors":"Ayesha Sultana,&nbsp;Rahath Maseera,&nbsp;Abdul Rahamanulla,&nbsp;Alima Misiriya","doi":"10.1186/s43094-023-00517-w","DOIUrl":"10.1186/s43094-023-00517-w","url":null,"abstract":"<div><h3>Background</h3><p>The review covers a variety of Artificial intelligence (AI) related topics in medication development. Additionally, it gives a quick account of the recent advances made in drug development by the pharmaceutical industry in cooperation with various AI. All facts of science have been impacted by advances in computing and technology. In all fields of science and technology, from fundamental engineering to medicine, AI has become a crucial component. AI has so influenced pharmaceutical chemistry and health care.</p><h3>Main body</h3><p>The use of computers to assist in drug creation has overtaken more conventional approaches in recent years. AI is frequently utilised to reduce the amount of time and improve drug design processes. The success rate of the developed medicine is further increased by the ease with which the target proteins may be discovered utilising AI. Every step of the medication design process involves the use of AI technology, which lowers the cost and greatly lowers the health hazards related to preclinical studies. AI is a powerful data mining technique that is based on vast amounts of pharmaceutical data and the machine learning process.</p><h3>Conclusion</h3><p>The use of AI in de novo drug design, activity scoring, virtual screening, and In silico evaluation of drug molecule characteristics is the consequence (absorption, distribution, metabolism, excretion, and toxicity). To speed up drug research and the healthcare system, pharmaceutical companies have joined with AI firms.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00517-w","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41683680","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":"In silico prediction of siRNA to silence the SARS-CoV-2 omicron variant targeting BA.4, BA.5, BQ.1, BQ1.1. and XBB: an alternative to traditional therapeutics","authors":"Rahatul Islam,&nbsp;Asif Shahriar,&nbsp;Nour Fatema,&nbsp;Muhammad Ramiz Uddin,&nbsp;Mrityunjoy Acharjee,&nbsp;Md Mukhlesur Rahman Shepon,&nbsp;Avishek Sarkar,&nbsp;Khosnur Jahan Aurin","doi":"10.1186/s43094-023-00510-3","DOIUrl":"10.1186/s43094-023-00510-3","url":null,"abstract":"<div><h3>Background</h3><p>After the first infection in December 2019, the mutating strains of SARS-CoV2 have already affected a lot of healthy people around the world. But situations have not been as devastating as before the first pandemic of the omicron strains of SARS-CoV2. As of January 2023, five more Omicron offshoots, BA.4, BA.5, B.Q.1, B.Q.1.1 and XBB are now proliferating worldwide. Perhaps there are more variants already dormant that require only minor changes to resurrect. So, this study was conducted with a view to halting the infection afterwards. The spike protein found on the virus outer membrane is essential for viral attachment to host cells, thus making it an attractive target for vaccine, drug, or any other therapeutic development. Small interfering RNAs (siRNAs) are now being used as a potential treatment for various genetic conditions or as antiviral or antibacterial therapeutics. Thus, in this study, we looked at spike protein to see if any potential siRNAs could be discovered from it.</p><h3>Results</h3><p>In this study, by approaching several computational assays (e.g., GC content, free energy of binding, free energy of folding, RNA–RNA binding, heat capacity, concentration plot, validation, and finally molecular docking analysis), we concluded that two siRNAs could be effective to silence the spike protein of the omicron variant. So, these siRNAs could be a potential target for therapeutic development against the SARS-CoV2 virus by silencing the spike protein of this virus.</p><h3>Conclusion</h3><p>We believe our research lays the groundwork for the development of effective therapies at the genome level and might be used to develop chemically produced siRNA molecules as an antiviral drug against SARS-CoV2 virus infection.</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":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00510-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44128903","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":"Medicament testing on acupuncture points as a non-invasive diagnostic tool for determining the daily doses of sofosbuvir in patients with chronic hepatitis C virus infection","authors":"Naylya Djumaeva,&nbsp;Gulnara Akhundjanova,&nbsp;Leyla Djumaeva,&nbsp;Dilbar Urunova","doi":"10.1186/s43094-023-00514-z","DOIUrl":"10.1186/s43094-023-00514-z","url":null,"abstract":"<div><h3>Background</h3><p>Acupuncture points are known for their unique bioelectric properties. Medication testing at acupuncture points has not previously been used to determine the daily doses of sofosbuvir in patients with chronic hepatitis C virus infection.</p><h3>Results</h3><p>This pilot study included 61 patients with a confirmed diagnosis of chronic hepatitis C virus infection. Medicament testing of acupuncture points of the liver meridian (“Xing-jian”) and Voll’s circulation meridian (“Cells and lobules of the liver”) was performed to determine the daily doses of sofosbuvir. A correlation analysis was carried out between the tested doses of the drug and the viral load in the blood of patients to confirm the results of testing the daily doses of sofosbuvir. Patients with chronic hepatitis C virus infection showed a significant positive correlation between tested daily doses of sofosbuvir and viral load in their blood. The mean values of the tested doses of sofosbuvir did not vary at different acupuncture points and significantly differed depending on viral load.</p><h3>Conclusions</h3><p>This study showed that acupuncture points can serve as a diagnostic tool in the process of medicament testing and allow the determination of daily doses of sofosbuvir in patients with chronic hepatitis C virus infection. To further assess the clinical applications and physiological basis of medicament testing methods, additional clinical and instrumental studies are needed with a large sample of patients.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00514-z","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43655806","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":"Nanovaccines to combat drug resistance: the next-generation immunisation","authors":"K. Manju,&nbsp;S. Niranjan Raj,&nbsp;H. K. Ranjini,&nbsp;S. Chandra Nayaka,&nbsp;P. Ashwini,&nbsp;S. Satish,&nbsp;M. N. Nagendra Prasad,&nbsp;Raghuraj Singh Chouhan,&nbsp;Syed Baker","doi":"10.1186/s43094-023-00515-y","DOIUrl":"10.1186/s43094-023-00515-y","url":null,"abstract":"<div><h3>Background</h3><p>The present review envisages the role of nanovaccines to combat the global challenges of antimicrobial resistance. Nanovaccines are a novel formulation comprised of nanomaterials coupled with an immunogenic component to elicit the immune response and provide protection against the desired infectious disease. The nanovaccines with unique physicochemical properties can be more efficient against targeting the desired tissues in the body, aids in prolong circulation to promote antigen-presenting cells to act upon the target antigens.</p><h3>Main content</h3><p>The present review envisages the development of nanovaccines against antimicrobial-resistant pathogens. The use of nanovaccines can exhibit potent antigenicity with prolonged retention and controlled release to induce both cell- and antibody-mediated responses. Nanovaccines usage is still in the early stages and can be next-generation immunisation for prophylactic and therapeutic efficiency. The future development of nanovaccines against multi-drug-resistant pathogens can explore new avenues. Based on these facts, the present review is designed from the previously reported scientific studies and compiled with the fact that nanovaccines can revolutionise vaccine strategies. The articles were extracted from reputed databases like PubMed, Scopus, and ESCI. The size and conjugating chemistry of nanomaterials can be beneficial in developing novel multi-nanovaccine formulations that can target pools of antimicrobial resistance mechanisms.</p><h3>Conclusion</h3><p>Overall, the nanovaccines can form one of the best effective modes of targeting multi-drug-resistant pathogens. The nanovaccines can stimulate the innate immune response and generate effective immune-therapeutic novel formulation against infectious pathogens. Based on these facts and considerations, the present article makes an alarming call to develop nanovaccines to counter multi-drug resistance.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00515-y","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44864875","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":"Characterization, cellular uptake in Caco-2 cells and physiologically based pharmacokinetic modeling of baicalin-loaded solid lipid nanoparticles","authors":"Hussein O. Ammar,&nbsp;Rehab N. Shamma,&nbsp;Carol Yousry,&nbsp;Rasha S. Elbatanony,&nbsp;Basma Khater,&nbsp;Amira M. Ghoneim","doi":"10.1186/s43094-023-00512-1","DOIUrl":"10.1186/s43094-023-00512-1","url":null,"abstract":"<div><h3>Background</h3><p>Baicalin is a natural compound having intriguing and useful pharmacological properties that may be used alone or in conjunction with other treatments in a variety of therapeutic areas. However, the drug has low aqueous solubility and poor absorption. The aim of this research was to optimize the bioavailability of baicalin through incorporation into solid lipid nanoparticles.</p><h3>Results</h3><p>The particle size of the prepared baicalin-loaded solid lipid nanoparticles ranged between 248.2 ± 1.72 nm and 291.9 ± 30.9 nm. The speed, duration of homogenization and the content of both the surfactant and soy lecithin affected the particle size and the entrapment efficiency. The optimized formula showed superiority in drug release over the drug suspension, with biphasic release profile. Cell culture results showed good accumulation of the drug into the Caco-2 cells that increases over time in the case of the optimized formula. Physiologically based pharmacokinetic (PBPK) modeling simulated enhanced bioavailability of the optimized formula, compared to the drug suspension.</p><h3>Conclusion</h3><p>Solid lipid nanoparticles have demonstrated potential as cancer therapy nanocarriers. Reduced toxicity, improved drug absorption and flexibility in combining hydrophilic and lipophilic medications are all significant advantages of this system. The PBPK simulation suggested the safety of the optimized BA-SLNs in cancer patients and in geriatric populations.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-023-00512-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47996871","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}