Journal of Pharmaceutical Innovation最新文献

{"title":"Formulation, Optimization, and Antioxidant Evaluation of Tetrahydrocurcumin-Loaded Ultradeformable Nanovesicular Cream","authors":"Ankita Kanshide,&nbsp;Malleswara Rao Peram,&nbsp;Nagesh Chandrasekhar,&nbsp;Arzoo Jamadar,&nbsp;Vijay Kumbar,&nbsp;Manohar Kugaji","doi":"10.1007/s12247-022-09696-0","DOIUrl":"10.1007/s12247-022-09696-0","url":null,"abstract":"<div><h3>Purpose</h3><p>Tetrahydrocurcumin (THC) has excellent anti-inflammatory and antioxidant properties, but its poor aqueous solubility limits its use in pharmaceutical and cosmetic formulations. The present study aimed to develop, optimize, and characterize a nanovesicular cream-loaded tetrahydrocurcumin transfersomes (THC-TFs) to improve its topical delivery and enhance its antioxidant activity.</p><h3>Methodology</h3><p>THC-TFs were prepared using the thin-film hydration technique and characterized for vesicle size, zeta potential, entrapment efficiency, and skin penetration. The optimized transfersomal formulation was incorporated into a cream base and characterized for various parameters.</p><h3>Results</h3><p>The optimized THC-TF (OPT-THC-TF) suspension showed a vesicle size of 212 ± 4.78 nm, a zeta potential of –40.3 mV, and percentage entrapment efficiency of 83.74 ± 0.21. Fluorescence microscopy revealed that transfersomes penetrated the deeper layers of skin. Ex vivo skin permeation demonstrated that OPT-THC-TF cream has better skin permeation and deposition potential compared to the THC conventional cream. The α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activity assay revealed that the antioxidant potential of THC-TF cream (77%) was comparable to that of pure THC (81%), demonstrating that THC antioxidant activity is unaffected by its encapsulation into transfersomes. The cell viability study revealed that THC-TF cream (***<i>p</i> &lt; 0.001) significantly decreased the cytotoxicity toward normal cells (L-929) compared to pure THC solution.</p><h3>Conclusion</h3><p>Based on these findings, it was concluded that the OPT-THC-TF cream could be a promising strategy for the topical delivery of encapsulated drugs for the effective treatment of various dermatological disorders.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"980 - 998"},"PeriodicalIF":2.6,"publicationDate":"2022-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48486836","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":"Editorial: December 2022: Welcome to the Postmodern World","authors":"Stephen Scypinski","doi":"10.1007/s12247-022-09700-7","DOIUrl":"10.1007/s12247-022-09700-7","url":null,"abstract":"","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"17 4","pages":"1073 - 1073"},"PeriodicalIF":2.6,"publicationDate":"2022-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"4204235","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":"Content Analysis of US FDA Warning Letters Issued to Compounding Pharmacies Regarding Violations of Current Good Manufacturing Practices Between 2017 and 2022","authors":"Isra Dmour","doi":"10.1007/s12247-022-09692-4","DOIUrl":"10.1007/s12247-022-09692-4","url":null,"abstract":"<div><h3>Purpose</h3><p>Assessment of the US FDA-issued WLs content is an educational tool that can be used in the continuous training program of community pharmacists in compounding pharmacies. The study was designed to critically assess FDA warning letters (WLs) issued to compounding pharmacies in 2017–2022 for violations of Current Good Manufacturing Practices (cGMP).</p><h3>Methods</h3><p>Content analysis was used to evaluate WLs issued concerning (1) type of violations; (2) frequency of violations mentioned in the WLs; (3) specific evaluations of the deviations related to compounded sterile products, and (4) evaluation of corrective measures requested by the US FDA.</p><h3>Results</h3><p>A total of 141 WLs were evaluated. The main observed violations in the analyzed WLs were adulterated drug products (130), misbranded drugs (103), unapproved new drug products (42), failure to report adverse events (22), and failure to report drugs (11). Other violations were evaluated related to sterile product compounding with emphasis on personnel qualifications, quality control procedures, equipment, etc.</p><h3>Conclusion</h3><p>The continuous issuance of WLs by the FDA indicates the need for compounding pharmacies become more vigilant to reduce the recurrence of the addressed violations through establishing adequate training/retraining programs. The analysis of issued WLs can serve as a learning tool to help improve compounding procedures, reduce the recurrence of these violations, and enhance patient safeguards.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"965 - 979"},"PeriodicalIF":2.6,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40698293","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":"Formulation Development, Optimization by Box-Behnken Design, and In Vitro Characterization of Gefitinib Phospholipid Complex Based Nanoemulsion Drug Delivery System","authors":"Mohit,&nbsp;Pankaj Kumar,&nbsp;Pavitra Solanki,&nbsp;Bharti Mangla,&nbsp;Geeta Aggarwal","doi":"10.1007/s12247-022-09690-6","DOIUrl":"10.1007/s12247-022-09690-6","url":null,"abstract":"<div><h3>Purpose</h3><p>Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that has been authorized for the treatment of non-small lung cancer; however, its applications are not restricted. Instead, it can also be utilized for the treatment of other ailments, such as arthritis, breast cancer, and skin cancer. Their application is limited due to biopharmaceutical issues, as they belong to the second class of BCS and trigger first-pass metabolism.</p><h3>Methods</h3><p>In the present study, a gefitinib-phospholipid complex (GB-PC-90G) was developed using the solvent evaporation method through a job plot. The FTIR, DSC, and SEM morphologies confirmed and characterized the complexes. A dissolution study was performed at pH 1.2 and revealed improved drug release through complexation. The complex was loaded into a nanoemulsion (GB-PC90G@NE) using caproyl 90, Transcutol HP, and Tween 80 as the oil, surfactant, and co-surfactant, respectively. These parameters were optimized using Box–Behnken design (BBD) software, and the formulation underwent in vitro characterization.</p><h3>Results</h3><p>Globule size and zeta potential for optimized batch were 165.6 nm and − 24.4 mV respectively. The SEM morphology indicated spherical nanoparticles. In vitro release at pH 7.4 showed the sustained release behavior of the drug from the nanoemulsion within 24 h compared to a non-complexed drug.</p><p>Moreover, stability study data confirmed that complex-loaded nanoemulsions were stable for at least 3 months at 4 ℃ and 25 ℃.</p><h3>Conclusion</h3><p>Finally, it was concluded that GB-PC90G@NE enhanced gefitinib’s biopharmaceutical performance and hydrophilicity. In the future, this complex-loaded nanoemulsion will be subjected to ex vivo and in vivo studies to manage arthritis.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"952 - 964"},"PeriodicalIF":2.6,"publicationDate":"2022-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49290450","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":"Nanosized Intranasal Delivery of Novel Self-Assembled Cubic Liquid Crystals: Formulation and Evaluation","authors":"Gurudatta N. Desai,&nbsp;Panchaxari M. Dandagi,&nbsp;Taufik M. Kazi","doi":"10.1007/s12247-022-09695-1","DOIUrl":"10.1007/s12247-022-09695-1","url":null,"abstract":"<div><h3>Purpose</h3><p>The focus of this research was to develop Almotriptan malate (ALM)-loaded cubosomal in situ gel to improve its permeation through the blood–brain barrier (BBB) with an efficient and quick action when administered through the intranasal route.</p><h3>Method</h3><p>Cubosomes were developed by emulsifying and homogenizing various proportions and concentrations of pluronics F127 (PF127) and glyceryl monooleate (GMO) along with polyvinyl alcohol (PVA) as suggested by the Box–Behnken design (BBD). The desirability function was used to select the optimum cubosomal formula. The developed cubosomes morphology was validated by high resolution transmission electron microscopy (HR-TEM) analysis. Differential scanning calorimetry (DSC) peaks served as proof that the drug was enclosed within the nanocarrier system. A range of concentrations of PF127 (15–21% w/v) were used to formulate and optimize the in situ gel. Ex vivo permeation experiments followed by histopathology studies were also conducted.</p><h3>Results</h3><p>It was observed that particle size (PS) of 177.15 ± 7.85 nm, polydispersity index (PDI) of 0.36 ± 2.55, zeta potential (ZP) of − 21.26 ± 0.19 mV, and entrapment efficiency percentage (EE%) of 72.58 ± 8.82% was obtained with a percent deviation of less than 5. G4 batch consisting of 18% w/v of PF127 demonstrated satisfactory results. Furthermore, the results were in accordance with the phase transition and the formulation displayed a pseudoplastic rheological behavior confirmed by the rheogram. The optimized formulation’s in vitro drug permeation measurements demonstrated 90.69% release after 5 h. The ex vivo permeation also revealed a 2.52 enhancement ratio when compared to plain in situ gel. Histopathology analyses showed a non-toxic effect of the optimized composition on the cellular structure of sheep’s nasal mucosa. A short-term stability analysis revealed that the formulation was stable at room temperature for 3 months.</p><h3>Conclusion</h3><p>ALM-loaded intranasal cubosomal in situ gel is likely to promote patient compliance by delivering immediate relief from migraine pain due to its rapid onset of action and safe dosage form.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"934 - 951"},"PeriodicalIF":2.6,"publicationDate":"2022-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41721556","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":"Appraisal of Surelease Clear E-7–19040, an Ethylcellulose Aqueous Dispersion, as a Release Modifier for the Hydrophilic Core","authors":"Pramod Parshuramkar,&nbsp;Deepak Khobragade,&nbsp;Pranita Kashyap","doi":"10.1007/s12247-022-09693-3","DOIUrl":"10.1007/s12247-022-09693-3","url":null,"abstract":"<div><h3>Purpose</h3><p>This study evaluated the efficacy of ethylcellulose aqueous dispersion type B (surelease clear E-7–19040) in modifying the drug release from the hydrophilic cores. Because of its ideal physicochemical and biological properties for the controlled-release formulation, Pindolol was selected as the model drug.</p><h3>Methods</h3><p>The final modified-release drug product comprises the immediate-release loading dose and the controlled-release maintenance dose. The tablet formulation was designed to have a seal-coated hydrophilic core with 75% of the drug, followed by a controlled-release polymer coating, immediate-release drug coating with 25% of the drug, followed by a color film coating.</p><h3>Results</h3><p>The controlled-release polymer coating was the critical step to achieving the desired product characteristics. During the coating of aqueous polymer dispersions, the adjustment of the controlled-release polymer to the pore former ratio, the control of the manufacturing process parameters, and the curing conditions are vital to developing a robust and stable end product. The final drug product achieved a targeted drug release profile in the selected dissolution method without a dose-dumping effect in the presence of alcohol and was unaffected by the accelerated stability study condition.</p><h3>Conclusion</h3><p>The ethylcellulose aqueous dispersion type B is very effective in modulating the release of hydrophilic drug core for achieving a desired drug release profile as per the drug product’s quality target product profile and the material of choice for the organic solvent-free, eco-friendly, controlled-release polymer coating system.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"923 - 933"},"PeriodicalIF":2.6,"publicationDate":"2022-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48241783","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":"Fabrication of Zein-Chitosan-Zein Sandwich-Like Nanofibers Containing Teicoplanin as a Local Antibacterial Drug Delivery System","authors":"Jebrail Movaffagh,&nbsp;Tanin Nourollahian,&nbsp;Saeed Khalatbari,&nbsp;Nafise Amiri,&nbsp;Bibi Sedigheh Fazly Bazzaz,&nbsp;Fatemeh Kalalinia","doi":"10.1007/s12247-022-09686-2","DOIUrl":"10.1007/s12247-022-09686-2","url":null,"abstract":"<div><h3>Purpose</h3><p>The parenteral antibiotic therapies have always been associated with several limitations that could be overcome by nano-based drug delivery systems. In this study, we aimed to fabricate teicoplanin-loaded zein-chitosan (CS)-zein sandwich-like electrospun nanofibers for targeted drug delivery.</p><h3>Methods</h3><p>The sandwich-like structures of zein-CS/teicoplanin-zein nanofibers were fabricated by the electrospinning process. Nanofiber membranes were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), drug encapsulation efficiency, in vitro release profile, and tensile strength studies. Finally, the antibacterial activity of the neat teicoplanin and zein-CS/teicoplanin-zein nanofibers was evaluated in static and dynamic conditions.</p><h3>Results</h3><p>SEM images demonstrated the use of suitable electrospinning conditions that led to the fabrication of the smooth and bead-free nanofibers with nanoscale diameter formation. FTIR and DSC analysis confirmed the presence and uniform distribution of the drug and also the interaction between the teicoplanin and chitosan in the formulation. The concentration of teicoplanin has a direct effect on the increase of mechanical tensile properties of sandwich-like nanofibers. In vitro release profile assay showed a burst release of teicoplanin during the first 24 h followed by a slow-release profile for 19 days. Finally, zein-CS/teicoplanin-zein nanofiber membranes showed significantly higher antibacterial activity compared with neat zein-CS-zein nanofibers and teicoplanin alone at the same concentration.</p><h3>Conclusion</h3><p>These results indicate that zein-CS-zein nanofibers would be a prospective candidate for targeted drug delivery in the treatment of local infections.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"911 - 922"},"PeriodicalIF":2.6,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48903488","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":"Box–Behnken Design-Based Optimized Kinetic Approach to Develop an Eco-friendly Analytical Method for the Quantitation of Glimepiride Using Spectrophotometry","authors":"Habibur Rahman","doi":"10.1007/s12247-022-09691-5","DOIUrl":"10.1007/s12247-022-09691-5","url":null,"abstract":"<div><h3>Purpose</h3><p>The prevalence of type 2 diabetes mellitus is one of the global concerns and almost 80% of diabetic patients are treated with oral antidiabetic drugs. GLMP as a prescribed oral antidiabetic drug for diabetic patients enhanced its necessity. Therefore, it is essential to quantify it in several drug formulations and biological samples. Hence, a simple, eco-friendly, validated kinetic spectrophotometric method was developed for quantifying GLMP in commercial dosage forms.</p><h3>Methods</h3><p>The method was based on the oxidation of the GLMP with potassium permanganate. The reaction was followed spectrophotometrically, measuring an increase in absorbance with time at 605 nm. RSM optimized the influence of preliminary experimental variables for the proposed procedure via BBD, a frequently used DoE. Under the optimized conditions, initial rate, fixed-time (at 6.0 min), and equilibrium method (25.0 min) were adopted for constructing the calibration graphs to determine the amount of GLMP. The robustness of the proposed method was performed, and the effect of selected analytical parameters was investigated with alternative conditions employing Youden and Steiner’s test.</p><h3>Results</h3><p>The outcomes of the model were significant. Hence, the performance of the analytical method was validated statistically and through recovery studies using ICH guidelines. Calibration curves were linear in the concentration ranges of 4.0–36.0 µg/ml with a detection limit of 1.60, 1.02, and 1.13 µg/ml for the initial rate, fixed-time, and equilibrium method, respectively. The proposed method’s greenness profile was assessed using the analytical Eco-Scale and found greener in terms of using harmful reagents, energy consumption, and waste production. Statistical comparison of the results is shown in good agreement with the results found by the reference method, indicating no significant difference in accuracy and precision.</p><h3>Conclusion</h3><p>The proposed validated kinetic method is simple, accurate, low cost, safe, and eco-friendly and might be used in research laboratories, hospitals, and pharmaceutical industries for the routine quality control analysis of GLMP in commercial dosage forms.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"893 - 910"},"PeriodicalIF":2.6,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41251059","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":"Pharma 4.0: Use of Advanced Multivariate Analytics at Industrial Scale for Process Troubleshooting, Establishing Material Control and Improving Process Robustness in Pharmaceutical Industrial setting: Case Study","authors":"Vaidehi Soman,&nbsp;Akshay Hatewar,&nbsp;Adolf Miranda,&nbsp;Abhaykumar Nalawade,&nbsp;Hansraj Gocher,&nbsp;Ram Kumar","doi":"10.1007/s12247-022-09689-z","DOIUrl":"10.1007/s12247-022-09689-z","url":null,"abstract":"<div><h3>Purpose</h3><p>This project aimed to use advanced multivariate analytics at scale for troubleshooting and improving the process robustness of pharmaceutical products. Additionally, the project aimed to make technology more accessible and empower people to use advanced analytics on the roadmap of Industry 4.0.</p><h3>Methods </h3><p>A web-based platform based on advanced analytics was designed and implemented. Using this platform, data was accessed from the cloud database with a few clicks, analyzed and interpreted using Advanced Analytics by end users who are Process Subject Matter Experts without much background in Data Science.</p><h3>Results</h3><p>This article highlights how Advanced Analytics is used at an industrial scale in Pharmaceutical Industrial Setting for troubleshooting a process and ultimately making the processes and products more robust thus ensuring that the drug supply to the patient is uninterrupted. Three application case studies are demonstrated, where conclusions drawn from the process models combined with the subject matter expertise successfully solved problems in a pharmaceutical industrial setting.</p><h3>Conclusion</h3><p>Considering the criticality of the drug product and the complex manufacturing processes in the pharmaceutical industry, this article establishes how historical data can be leveraged at scale to get value and meaningful conclusions using multivariate models and machine learning algorithms.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"1560 - 1574"},"PeriodicalIF":2.6,"publicationDate":"2022-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43534464","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":"Design, Development, In Silico, and In Vitro Characterization of Camptothecin-Loaded Mixed Micelles: In Vitro Testing of Verapamil and Ranolazine for Repurposing as Coadjuvant Therapy in Cancer","authors":"Kiran S. Patil,&nbsp;Ashok A. Hajare,&nbsp;Arehalli S. Manjappa,&nbsp;Harinath N. More,&nbsp;John I. Disouza","doi":"10.1007/s12247-022-09688-0","DOIUrl":"10.1007/s12247-022-09688-0","url":null,"abstract":"<div><h2>Abstract\u0000</h2><div><h3>Purpose</h3><p>Camptothecin has poor solubility, high systemic toxicity, and intrinsic structural instability. To deal with these challenges, present research aimed to develop camptothecin-loaded mixed micelles (CPT MMs) using TPGS and Pluronic^® F108 copolymers. Furthermore, our research aimed to test in vitro anticancer activities of non-micellar verapamil and ranolazine for repurposing as coadjuvant therapy with CPT MMs in cancer.</p><h3>Methods</h3><p>CPT MMs were fabricated by solvent evaporation method and optimized using 3² full factorial design. CPT MMs were characterized for % entrapment efficiency (%EE), mean particle size (MPS), zeta potential, surface morphology, % drug loading capacity (%DLC), in vitro drug release, and in vitro cytotoxicity and cell cycle arresting behaviors.</p><h3>Result</h3><p>The in silico studies revealed decent camptothecin interaction with a cavity of mixed micelles (MMs). CPT MMs composition (H5) is considered optimum based on %EE (94.92 ± 2.46%), MPS (136.9 ± 1.71 nm), zeta potential (− 22.9 ± 0.87 mV), and %DLC (1.810 ± 0.02%). TEM image shows self-assembled micelles with spherical shape. CPT MMs showed sustained release profile. The drug-excipient compatibility study revealed no primary incompatibilities. The CPT MMs showed moderately higher IC₅₀ values than camptothecin against A549 and B16F10 cells. The non-micellar verapamil and ranolazine when combined with CPT MMs at lower concentrations have resulted in substantially higher cytotoxicity. Whereas, the CPT MMs + ranolazine combination has shown higher cell cycle arresting behavior than CPT MMs + verapamil combination.</p><h3>Conclusion</h3><p>Elaborative and molecular mechanism–based studies are further needed to validate the repurposing potential of non-micellar verapamil and ranolazine as coadjuvant with CPT MMs in cancer.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"874 - 892"},"PeriodicalIF":2.6,"publicationDate":"2022-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44742536","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}