{"title":"Recent advances in ruthenium (III) complex-loaded nanomaterial for enhanced cancer therapy efficacy.","authors":"Xuemei Zhong, Ye Zhang, Jianhua Wei","doi":"10.1080/03639045.2025.2455428","DOIUrl":"10.1080/03639045.2025.2455428","url":null,"abstract":"<p><strong>Objective: </strong>Amid the escalating global cancer incidence, the development of effective and safe anticancer drugs is a critical priority in medical research. Addressing the clinical shortcomings of ruthenium-based anticancer drugs are currently a prominent focus of research.</p><p><strong>Significance and methods: </strong>Since the pioneering work with platinum derivatives, significant progress has been made in the fundamental studies of metal complexes for the treatment of a wide range of cancers, and there has been a growing interest in their properties and biomedical applications. Although chemotherapy is crucial in clinical tumor management, platinum(II) anticancer drugs like cisplatin and carboplatin suffer from severe toxicity and drug resistance issues. Among various metal-based drugs, ruthenium(III) complexes are notable for their selectivity, cytotoxic activity <i>in vitro</i>, and effective anticancer properties <i>in vivo</i>. Despite some drug candidates reaching late-stage clinical trials, their clinical application remains constrained by problems such as low solubility, poor stability, and inadequate cellular uptake.</p><p><strong>Results: </strong>The development of efficient and stable nanocarrier-based drug delivery systems for ruthenium(III) complexes, enhancing pharmacokinetic properties, and enabling slow, controlled release and targeted drug delivery, offers potential solutions to these limitations.</p><p><strong>Conclusions: </strong>This review delves into the recent strides in nanomaterial-based drug delivery for ruthenium complexes, encompassing research on platinum (II) and ruthenium (III) metal complexes, nano-delivery system designs, and addresses pivotal challenges and future trajectories in this domain.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"169-179"},"PeriodicalIF":2.4,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001908","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 characterization of a <i>Vaccinium vitis-idaea</i> liposomal gel for the treatment of atopic dermatitis.","authors":"Zhuoqun Zhang, Jinhai Huo, Lina Feng, Jing Wang, Xinyu Fan, Weiming Wang","doi":"10.1080/03639045.2025.2467857","DOIUrl":"10.1080/03639045.2025.2467857","url":null,"abstract":"<p><strong>Objective: </strong>In this study, a liposomal gel with anti-inflammatory, antibacterial, and antioxidant effects and improving atopic dermatitis (AD) was prepared using <i>Vaccinium vitis-idaea</i> polyphenol as the main active ingredient, which is safe, effective, of stable quality and has anti-inflammatory and antimicrobial effects.</p><p><strong>Methods: </strong>The polyphenol extract from <i>Vaccinium vitis-idaea</i> was obtained through ultrasonic extraction and subsequently purified using macroporous resin. A liposome gel incorporating this extract was formulated using poloxamer 188 and poloxamer 407 as the base materials. The gel's physical characteristics, including appearance, vesicle size, and zeta potential, were systematically characterized. Furthermore, its anti-inflammatory, antioxidant, anti-aging, and anti-AD effects were assessed through both <i>ex vivo</i> and <i>in vivo</i> studies.</p><p><strong>Results: </strong>After process optimization, the yield of <i>Vaccinium vitis-idaea</i> polyphenol was 4.33%; the encapsulation rate of <i>Vaccinium vitis-idaea</i> liposome was 90.45%. The liposome gel prepared by the optimal process had a zeta potential of -33.67 mV, a particle size of 119 nm, a PDI of 0.147, and showed good stability under the conditions of 60 °C, 75% relative humidity, and light intensity of 4500 ± 500 Lux. The results of <i>in vitro</i> studies showed that <i>Vaccinium vitis-idaea</i> polyphenols have antibacterial and antioxidant effects, and the results of <i>in vivo</i> studies showed that the <i>Vaccinium vitis-idaea</i> liposome gel is safe for skin application, effectively reduces dandruff and erythema, reduces the degree of keratinization, reduces the degree of congestion and inflammatory infiltration of local tissues as well as increasing the content of collagen fibers in skin tissues, promotes the restoration of the structural integrity of the skin, and by reducing the inflammatory factors TNF-α, IL-4. By reducing the expression level of inflammatory factors TNF-α, IL-4, IL-13, and MDA, increasing the expression level of SOD, and reducing the diversity of bacterial flora in AD tissues, it can play the role of anti-inflammatory, anti-bacterial, and antioxidant effects and improve the symptoms of AD.</p><p><strong>Conclusion: </strong>The present study demonstrated that the prepared <i>Vaccinium vitis-idaea</i> liposome gel had an ameliorating effect on AD.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"273-283"},"PeriodicalIF":2.4,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143432346","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":"Tumor microenvironment as a target for developing anticancer hydrogels.","authors":"Suman Khurana, Shrestha Sharma, Parveen Kumar Goyal","doi":"10.1080/03639045.2025.2455424","DOIUrl":"10.1080/03639045.2025.2455424","url":null,"abstract":"<p><strong>Objective: </strong>It has been reported that cancer cells get protected by a complex and rich multicellular environment i.e. the tumor microenvironment (TME) consisting of varying immune cells, endothelial cells, dendritic cells, fibroblasts, etc. This manuscript is aimed at the characteristic features of TME considered as potential target(s) for developing smart anticancer hydrogels.</p><p><strong>Significance: </strong>The stimuli-specific drug delivery systems especially hydrogels that can respond to the characteristic features of TME are fabricated for treating cancer. For developing anticancer formulations, TME targeting can be considered an alternative way as it enhances the cytotoxic potential and reduces the unwanted effects. This manuscript shall be of quite interest to academicians, researchers, and clinicians engaged in oncology.</p><p><strong>Methods: </strong>The manuscript was prepared by using the data available in the public domain in online resources such as Google Scholar, PubMed, Science Direct, Scopus, Web of Science, Research Gate, etc.</p><p><strong>Results: </strong>Smart hydrogels, sensitive to some specific features of TME such as low pH, high concentration of glutathione, specific enzymes, etc., are promising anticancer formulations as these improve the efficacy and lower the side effects of chemotherapy.</p><p><strong>Conclusion: </strong>The stimuli-responsive hydrogels have been gaining more attention for delivering cytotoxic drugs to the TME in response to specific stimuli. The stimuli-responsive hydrogels, comprising of cytotoxic drug(s) and specific polymers have some special features such as similarity with biological matrix, ability to respond to various internal as well as external stimuli, improved permeability, porosity, biocompatibility, resemblance with soft living tissues, etc.; and are considered as the promising anticancer candidates.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"157-168"},"PeriodicalIF":2.4,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001909","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":"Docetaxel and niclosamide-loaded nanofiber systems for improved chemo-therapeutic activity and resistance reversal in prostate cancer.","authors":"Saurabh Shah, Paras Famta, Ganesh Vambhurkar, Rahul Kumar, Giriraj Pandey, Gurpreet Singh, Suraj Wagh, Shubham Kanaujiya, Dilip Kumar Arya, Abhishek Sharma, Akshay Shinde, Sajja Bhanu Prasad, Sachin Chandankar, Swapnil Shinde, Anamika Sharma, P S Rajinikanth, Dharmendra Kumar Khatri, Amit Asthana, Saurabh Srivastava","doi":"10.1080/03639045.2025.2453533","DOIUrl":"10.1080/03639045.2025.2453533","url":null,"abstract":"<p><strong>Objective: </strong>The objective of the study was to tackle the recurrence of prostate cancer (PCa) post-surgery and to re-sensitize the docetaxel (DTX)-resistant PC-3 cells to chemo-therapy using NIC.</p><p><strong>Significance: </strong>Prolonged DTX therapy leads to the emergence of chemo-resistance by overexpression of PI3K-AKT pathway in PCa along with tumor recurrence post-surgery. Suppression of this pathway could be essential in improving the anticancer activity of DTX and re-sensitizing the resistant cells.</p><p><strong>Method: </strong>Niclosamide (NIC), an anthelmintic drug has shown tremendous anticancer potential and has re-sensitized the resistant cells to various drugs. To mitigate the post-surgical tumor recurrence, an implant-based system facilitating the sustained release of DTX and NIC could be beneficial. DTX and NIC were incorporated within a nanofiber (NF) system to prevent on-site recurrence by local release and re-sensitize the DTX-resistant cells.</p><p><strong>Key findings: </strong>The fabricated DTX-NIC NF <i>via</i> electrospinning were 334 ± 96.14 nm in diameter and demonstrated sustained release profile till 6 d. Elevated mitochondrial damage, reactive oxygen species levels and apoptotic index revealed improvement in the cytotoxicity of DTX-NIC post incorporation into the NF owing to their sustained release profile. Re-sensitization of PC-3/DTX cells was observed by introduction of NIC which could be due to the suppression of p-Akt1, which was overexpressed in resistant cells.</p><p><strong>Conclusion: </strong>From superior activity of DTX-NIC NF and re-sensitization of resistant cells, we conclude that DTX-NIC NF could be a beneficial therapeutic regimen in preventing tumor recurrence in PCa.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"132-143"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001905","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}
Ranieli Paiva Lopes, Millena Alves Máximo Vaz, Fernanda Lopes Ferreira, Grasiely Faria de Sousa, Cintia Lopes de Brito Magalhães, Sidney Augusto Vieira-Filho, Jaqueline Maria Siqueira Ferreira, Antônio Helvécio Tótola, Lucienir Pains Duarte, José Carlos de Magalhães
{"title":"Potent antiviral action detected in <i>Tontelea micrantha</i> extracts against <i>Alphavirus chikungunya</i>.","authors":"Ranieli Paiva Lopes, Millena Alves Máximo Vaz, Fernanda Lopes Ferreira, Grasiely Faria de Sousa, Cintia Lopes de Brito Magalhães, Sidney Augusto Vieira-Filho, Jaqueline Maria Siqueira Ferreira, Antônio Helvécio Tótola, Lucienir Pains Duarte, José Carlos de Magalhães","doi":"10.1080/03639045.2024.2449130","DOIUrl":"10.1080/03639045.2024.2449130","url":null,"abstract":"<p><strong>Background: </strong><i>Tontelea micrantha</i>, a notable plant species, has garnered interest for its medicinal properties, including anti-inflammatory, antibacterial and antiviral effects. A vaccine for Chikungunia virus is still under evaluation and no specific antiviral drug has been licensed to date.</p><p><strong>Objective: </strong>The work investigated antiviral activity of ethyl acetate (EAEF) and methanolic (EMF) extracts from <i>T. micrantha</i> leaves in mammalian cells exposed to <i>Alphavirus chikungunya</i> (CHIKV).</p><p><strong>Methods: </strong>The cytotoxicity, antiviral activity, selectivity index, effect on viral gene expression, virus production, and mechanisms of action were evaluated.</p><p><strong>Results: </strong>EAEF and EMF extracts showed anti-CHIKV effects at non-cytotoxic concentrations, with CC<sub>50</sub> above 300 μg/mL, EC<sub>50</sub> of 18 and 43 μg/mL respectively, and selectivity Index above 4. These concentrations drastically reduce viral yields and CHIKV gene expression and have shown activity both directly on viral particles and at different stages of the viral cycle.</p><p><strong>Conclusion: </strong>EAEF and EMF showed robust antiviral activity against CHIKV, making them promising candidates for the development of anti-CHIKV drugs.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"102-110"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142926586","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":"Formulate a concentrated highly branched poly(β-amino ester)/DNA polyplex - one step closer to application in lung cystic fibrosis disease.","authors":"Bei Qiu, Yinghao Li, Zhonglei He, Zishan Li, Sébastien Terreau, Xianqing Wang, Jing Lyu, Wenxin Wang, Irene Lara-Sáez","doi":"10.1080/03639045.2024.2448271","DOIUrl":"10.1080/03639045.2024.2448271","url":null,"abstract":"<p><strong>Objective: </strong>Highly branched poly(β-amino ester) (HPAEs)-based gene therapy holds promise for treating lung cystic fibrosis (CF). However, the translation of HPAEs/DNA nanoparticles into clinical applications poses a significant challenge due to the requirement for high concentrations of the formulation.</p><p><strong>Methods: </strong>In this work, a straightforward and scalable concentration method was developed for concentrating HPAEs/DNA polyplexes. A series of different buffers with various pH values and ionic components were initially tested to develop the optimized HPAEs/DNA polyplex formulation. Subsequently, the optimized HPAEs/DNA polyplex formulation was concentrated through lyophilization and ultrafiltration.</p><p><strong>Results: </strong>The ultrafiltration outperformed the lyophilization in concentration capacity, showing a 24-fold increase in the concentrated formulation compared to the original non-concentrated formulation. The concentration does not disturb the transfection efficiency in lung CF epithelial cells, indicating its potential for lung delivery applications. Moreover, the concentrated HPAEs/DNA polyplex successfully restored the production of CF transmembrane conductance regulator (CFTR) protein in primary lung CF epithelial cells, surpassing the performance of the non-concentrated common gene transfection reagents such as Lipofectamine 3000 and Xfect.</p><p><strong>Conclusion: </strong>The concentrated HPAEs/DNA formulation represents a promising step forward for preclinical testing (e.g. <i>in vivo</i> evaluation), with further research needed to confirm its potential for clinical use.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"91-101"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142914007","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}
Shama Parveen, Jasveer Kaur, Om Silakari, Bharti Sapra
{"title":"Optimizing voriconazole-loaded thermoresponsive hydrogel: <i>in silico</i> tools and <i>ex vivo</i> studies.","authors":"Shama Parveen, Jasveer Kaur, Om Silakari, Bharti Sapra","doi":"10.1080/03639045.2025.2453967","DOIUrl":"10.1080/03639045.2025.2453967","url":null,"abstract":"<p><strong>Objective: </strong>The present study aims to develop and evaluate the voriconazole-loaded thermoresponsive hydrogel using <i>in silico</i> tools.</p><p><strong>Methods: </strong>Poloxamer 407 and PEG 400 were selected as the components from <i>in silico</i> studies for thermoresponsive hydrogel of voriconazole. The cohesive energy density (CED) and solubility parameters (SP) were calculated using Biovia Material Studio 2022 software to predict the polymer-polymer miscibility and drug-polymer miscibility. Different evaluation techniques used to select the optimized formulation. The <i>in vitro</i> antimicrobial activity against <i>Candida albicans</i> was determined for the optimized formulation to illustrate the efficacy of the developed formulation.</p><p><strong>Results: </strong>Hydrogel containing 15% poloxamer exhibited gelation time of 92.67 ± 3.51 s, and gelation temperature of 36.67 °C with good spreadability of 13.00 ± 0.02 cm<sup>2</sup>. CED values for poloxamer 407, PEG 400, and Voriconazole individually were found to be 3.23 × 10<sup>-8</sup>, 3.21 × 10<sup>-8</sup>, 4.84 × 10<sup>-8</sup>, respectively, whereas in the combination of poloxamer 407 and PEG 400 was found to 3.85 × 10<sup>-8</sup> and in ratio 9:1 was found to be 3.81 × 10<sup>-8</sup> indicated the best miscibility between poloxamer 407 and PEG 400 in 9:1 ratio. Based on solvation-free energy of voriconazole (-48.343 kJ/mol) ethanol was selected as the solvent system. Optimized formulation showed the sustained release over the 36 h and good antimicrobial effect.</p><p><strong>Conclusion: </strong>A thermoresponsive hydrogel of voriconazole was developed using Biovia Material Studio 2022, integrating computational predictions and molecular dynamics simulations to streamline polymer and solvent selection. This approach minimized trial-and-error experiments, enabling efficient formulation while enhancing understanding of polymer-polymer and drug-polymer interactions.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"144-155"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001907","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":"AQbD integrated high-performance thin layer chromatographic method for quantitative estimation of Tavaborole in the presence of its degradants and the matrix of nanostructured lipid carriers.","authors":"Rashmin Patel, Savaliya Neel, Patel Mrunali, Yash Patel, Richa Dave, Agrawal Vikas","doi":"10.1080/03639045.2024.2449148","DOIUrl":"10.1080/03639045.2024.2449148","url":null,"abstract":"<p><strong>Background: </strong>Tavaborole (TAV), a benzoxaborole derivative, is an FDA-approved antifungal agent for treating onychomycosis, a common and persistent fungal infection of the toenails.</p><p><strong>Objective: </strong>This study aimed to develop a robust stability-indicating HPTLC method to determine TAV in nanostructured lipid carriers (NLC) using a comprehensive approach that includes risk assessment, and Analytical Quality by Design.</p><p><strong>Methods: </strong>The critical method parameters influencing the HPTLC results were screened using a Plackett-Burman screening design followed by its optimization using a central composite optimization design. The developed method was validated as per ICH recommendation.</p><p><strong>Results: </strong>Optimized method utilized pre-coated aluminum-backed HPTLC plates using 10 µL/band injection volume, and the plate was developed using an isocratic mobile phase consisting of toluene: ethyl acetate: formic acid (75:25:1%v/v/v) in twin trough chamber pre-saturated for 20 mins with vapors of 10 mL of mobile phase. The separated components were detected at a wavelength of 221 nm. The developed HPTLC method resulted in a retardation factor of 0.49 ± 0.04 for TAV. Validation results revealed the HPTLC method's specificity (peak purity ≥ 0.999), linearity over a concentration range of 2-10 μg/band, sensitivity (LOD 0.21 μg and LOQ 0.64 μg), accuracy (99.68 - 101.43%w/w), and precision (%RSD < 2.0).</p><p><strong>Conclusion: </strong>The developed robust stability-indicating HPTLC method was successfully implemented for the sustainable testing of the TAV in the NLC formulations and stability testing.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"111-122"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142921282","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":"Polyethylene glycol complexed with boronophenylalanine as a potential alternative to fructose-boronophenylalanine complexation to increase cellular uptake for BNCT treatment.","authors":"Yaxin Qin, Qi Dai, Zhicheng Zhang, Xiaoyan Sun, Ruolin Jiang, Xiaoyan Bao, Linjie Wu, Xin Tan, Xufang Ying, Zhiqing Ben, Qichun Wei, Min Han","doi":"10.1080/03639045.2025.2452607","DOIUrl":"10.1080/03639045.2025.2452607","url":null,"abstract":"<p><strong>Objective: </strong>Boron Neutron Capture Therapy (BNCT) is a novel precision radiotherapy. The key to BNCT application lies in the effective targeting and retention of the boron-10 (<sup>10</sup>B) carrier. Among the various compounds studied in clinical settings, 4-boronophenylalanine (BPA) become the most prevalent one currently. However, challenges such as inadequate solubility and restricted tumor accumulation have affected the clinical efficacy of treatment with BPA. Therefore, there is an urgent need to prepare formulations with higher tumor uptake efficiency and increased intratumoral accumulation.</p><p><strong>Methods: </strong>polyethylene glycol 400 and BPA were added to methanol and stirred until completely dissolved. The solution was then evaporated to remove methanol, yielding a pale-yellow clear liquid of the PEG400-BPA complex. This complex was then used for <i>in vitro</i> and <i>in vivo</i> experiments, and it was evaluated for inhibition effects after BNCT irradiation in GL261 cells.</p><p><strong>Results: </strong>Compared to the clinically used fructose-BPA, PEG400-BPA increased the boron uptake in tumor cells nearly twice and exhibited a better tumor-to-normal tissue ratio (T/N) in the <i>in vivo</i> studies. Due to the BNCT efficacy with PEG400-BPA through <i>in vitro</i> experiments, the PEG400-BPA group also had showed significant cell-killing effects.</p><p><strong>Conclusion: </strong>We discovered that PEG400 can form a complex with BPA, significantly improving its water solubility. It provides a simple, long-term stable, easily convertible, and injectable formulation method for the delivery of BPA in BNCT treatment. It also offers new insights for BPA solubilization and formulation as well as compound forms of administration of boron drugs on the delivery of boron drugs in BNCT.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"123-131"},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142964254","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}
Narahari N Palei, Mohanalakshmi Sabapati, Vijayaraj S, Saptarshi Samajdar, Arghya K Dhar
{"title":"Formulation of <i>Morus alba</i> extract loaded solid lipid nanoparticles: <i>in silico</i>, characterizations, and <i>in vitro</i> cytotoxicity study.","authors":"Narahari N Palei, Mohanalakshmi Sabapati, Vijayaraj S, Saptarshi Samajdar, Arghya K Dhar","doi":"10.1080/03639045.2024.2439930","DOIUrl":"10.1080/03639045.2024.2439930","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to formulate <i>Morus alba</i> leaf extract (MAE) loaded solid lipid nanoparticles (SLNs) and investigate its cytotoxic potential using MDA-MB231 cell line.</p><p><strong>Significance: </strong>SLNs can protect MAE from degradation, enhance cytotoxicity potential, and making them suitable for various therapeutic areas.</p><p><strong>Methods: </strong>SLNs were developed using high-pressure homogenization method, and the formulations were optimized based on particle size, zeta potential, % entrapment efficiency (EE), and % cumulative drug release (CDR). The <i>in vitro</i> cytotoxic efficacy of MAE-loaded SLNs was evaluated through apoptosis assays and compared to that of free MAE.</p><p><strong>Results: </strong>The particle size, zeta potential, % EE, and % CDR of optimized SLNs were found 116.3 nm, -26.18 mV, 89.30%, and 79.4%, respectively. MAE-loaded SLNs demonstrated significantly greater cytotoxic effects than the MAE (<i>p</i> < 0.05). SLNs induced less inhibition in the G0/G1 phase but showed marked inhibition in the S phase (9.7 ± 1.7%) and G2/M phase (2.2 ± 0.6%), indicating effective disruption of DNA replication and cell division, with significant cytotoxicity compared to control cells. The percentage of total apoptosis was 72.49 ± 2.7% for MAE alone and 81.46 ± 2.9% for MAE loaded SLNs, demonstrating a notably higher apoptosis rate for the SLNs formulation (<i>p</i> < 0.05). These findings indicated that MAE loaded SLNs significantly enhance the apoptotic and cytotoxic impact compared to MAE.</p><p><strong>Conclusion: </strong>These results proved that MAE loaded SLNs as a promising nano carrier system to improve the therapeutic performance of MAE.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"14-28"},"PeriodicalIF":2.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142799739","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}