ADMET and DMPK最新文献

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Predicting the acute aquatic toxicity of organic UV filters used in cosmetic formulations. 预测化妆品配方中使用的有机紫外线过滤剂的急性水生毒性。
IF 3.4
ADMET and DMPK Pub Date : 2024-09-11 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2364
Chrysanthos Stergiopoulos, Fotios Tsopelas, Maria Ochsenkühn-Petropoulou, Klara Valko
{"title":"Predicting the acute aquatic toxicity of organic UV filters used in cosmetic formulations.","authors":"Chrysanthos Stergiopoulos, Fotios Tsopelas, Maria Ochsenkühn-Petropoulou, Klara Valko","doi":"10.5599/admet.2364","DOIUrl":"https://doi.org/10.5599/admet.2364","url":null,"abstract":"<p><strong>Background and purpose: </strong>Organic UV filters are commonly used in sunscreen and cosmetic formulations to protect against harmful UV radiation. However, concerns have emerged over their potential toxic effects on aquatic organisms. This study aims to investigate the acute aquatic toxicity of 13 organic UV filters and determine whether phospholipid binding, measured through biomimetic chromatographic methods, is a better predictor of toxicity than the traditionally used octanol-water partition coefficient (log <i>P</i>).</p><p><strong>Experimental approach: </strong>The chromatographic retention of the 13 UV filters was measured on an immobilized artificial membrane (IAM) stationary phase to assess phospholipid binding. These measurements were then applied to previously established predictive models, originally developed for pharmaceutical compounds, to estimate acute aquatic toxicity endpoints of 48-hour LC<sub>50</sub> for fish and the 48-hour EC<sub>50</sub> (immobilization) for Daphnia magna.</p><p><strong>Key results: </strong>Phospholipid binding was found to be a more reliable predictor of the acute aquatic toxicity of UV filters compared to log <i>P</i>. The toxicity was primarily driven by lipophilicity and charge, with negatively charged compounds exhibiting lower toxicity.</p><p><strong>Conclusion: </strong>The study demonstrates that phospholipid binding is a better descriptor of UV filter toxicity than log <i>P</i>, providing a more accurate method for predicting the environmental risk of these compounds. This insight can guide the development of more environmentally friendly sunscreens by reducing the use of highly lipophilic and positively charged compounds, thus lowering their aquatic toxicity.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 5","pages":"781-796"},"PeriodicalIF":3.4,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11542717/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142612118","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}
引用次数: 0
Determination of methotrexate using carbon paste electrode modified with ionic liquid/Ni-Co layered double hydroxide nanosheets as a voltammetric sensor. 使用离子液体/镍钴层状双氢氧化物纳米片修饰的碳浆电极作为伏安传感器测定甲氨蝶呤。
IF 3.4
ADMET and DMPK Pub Date : 2024-09-04 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2460
Peyman Mohammadzadeh Jahani, Fariba Garkani Nejad, Reza Zaimbashi, Mohammad Reza Aflatoonian, Somayeh Tajik, Hadi Beitollahi
{"title":"Determination of methotrexate using carbon paste electrode modified with ionic liquid/Ni-Co layered double hydroxide nanosheets as a voltammetric sensor.","authors":"Peyman Mohammadzadeh Jahani, Fariba Garkani Nejad, Reza Zaimbashi, Mohammad Reza Aflatoonian, Somayeh Tajik, Hadi Beitollahi","doi":"10.5599/admet.2460","DOIUrl":"https://doi.org/10.5599/admet.2460","url":null,"abstract":"<p><strong>Background and purpose: </strong>Methotrexate (MTX) is a widely used anti-cancer drug, but its overuse can lead to significant side effects. Therefore, it is very vital to design simple and sensitive analytical methods for its determination.</p><p><strong>Experimental approach: </strong>In this work, an electrochemical sensor was prepared based on an ionic liquid (IL)/Ni-Co layered double hydroxide nanosheets (Ni-Co-LDH)-modified carbon paste electrode IL/Ni-Co-LDH/CPE. Cyclic voltammetry, differential pulse voltammetry, and chronoamperometry methods were applied to evaluate the performance of the designed sensor for MTX determination.</p><p><strong>Key results: </strong>The IL/Ni-Co-LDH/CPE sensor exhibits a linear relationship between the peak current of the differential pulse voltammetry and MTX concentrations in the linear dynamic range of 0.02 to 140.0 μM, with a detection limit of 0.006 μM. The IL/Ni-Co-LDH/CPE sensor exhibited relative standard deviation values between 1.7 to 3.7 % for recovery tests on real samples, indicating the precision of the method.</p><p><strong>Conclusion: </strong>The designed sensor with cost-effective and good performance could be valuable for therapeutic drug monitoring and clinical diagnostics.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"637-648"},"PeriodicalIF":3.4,"publicationDate":"2024-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517520/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543043","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}
引用次数: 0
Food and bile micelle binding of zwitterionic antihistamine drugs. 食物与胆汁胶束结合的齐聚物抗组胺药物。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-29 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2454
Rie Takeuchi, Kiyohiko Sugano
{"title":"Food and bile micelle binding of zwitterionic antihistamine drugs.","authors":"Rie Takeuchi, Kiyohiko Sugano","doi":"10.5599/admet.2454","DOIUrl":"https://doi.org/10.5599/admet.2454","url":null,"abstract":"<p><strong>Background and purpose: </strong>The food effects on oral drug absorption are challenging to predict from in vitro data. Food intake has been reported to reduce the oral absorption of several zwitterionic antihistamine drugs. However, the mechanism for this negative food effect has not been clear. The purpose of the present study was to evaluate the bile micelle and food binding of zwitterionic antihistamine drugs as a possible mechanism for the negative food effects on their oral drug absorption.</p><p><strong>Experimental approach: </strong>Bilastine (BIL), cetirizine (CET), fexofenadine (FEX), and olopatadine (OLO) were employed as model drugs. The fed/fasted AUC ratios of BIL, CET, FEX, and OLO after oral administration are reported to be 0.60 to 0.7, 0.92, 0.76 to 0.85, and 0.84, respectively. The unbound fraction (<i>f</i> <sub>u</sub>) of these drugs in the fasted and fed state simulated intestinal fluids (FaSSIF and FeSSIF, containing 3 and 15 mM taurocholic acid, respectively) with or without FDA breakfast homogenate (BFH) was measured by dynamic dialysis.</p><p><strong>Key results: </strong>The FeSSIF/ FaSSIF f<sub>u</sub> ratios were 0.90 (BIL), 0.46 (CET), 0.76 (FEX), and 0.78 (OLO). In the presence of BFH, the f<sub>u</sub> ratios were reduced to 0.52 (BIL), 0.22 (CET), 0.39 (FEX), and 0.44 (OLO).</p><p><strong>Conclusion: </strong>Despite being zwitterion at pH 6.5, the antihistamine drugs were bound to bile micelles. Bile micelle and food binding were suggested to cause a negative food effect on the oral absorption of these drugs. However, the AUC ratio was not quantitatively predicted by using FeSSIF + BFH.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"649-656"},"PeriodicalIF":3.4,"publicationDate":"2024-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517518/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543044","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}
引用次数: 0
Molecular properties, including chameleonicity, as essential tools for designing the next generation of oral beyond rule of five drugs. 分子特性(包括变色性)是设计下一代口服超越五项原则药物的重要工具。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-27 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2334
Diego García Jiménez, Maura Vallaro, Luigi Vitagliano, Lucía López López, Giulia Apprato, Giuseppe Ermondi, Giulia Caron
{"title":"Molecular properties, including chameleonicity, as essential tools for designing the next generation of oral beyond rule of five drugs.","authors":"Diego García Jiménez, Maura Vallaro, Luigi Vitagliano, Lucía López López, Giulia Apprato, Giuseppe Ermondi, Giulia Caron","doi":"10.5599/admet.2334","DOIUrl":"https://doi.org/10.5599/admet.2334","url":null,"abstract":"<p><strong>Background and purpose: </strong>The classical drug discovery toolbox continually expands beyond traditional rule of five (Ro5)-compliant small molecules to include new chemical modalities for difficult-to-drug targets. The paper focuses on the molecular properties essential to drive oral bioavailability within the bRo5 framework.</p><p><strong>Experimental approach: </strong>The first part outlines the concept and methodologies for characterizing bRo5 physicochemical properties, including considerations on chameleonicity; in particular, the paper summarizes the content of the last author's talk presented during the IAPC-10 Meeting held in Belgrade in September 2023 (https://iapchem.org/index.php/iapc-10-home). The second part of the manuscript presents novel experimental and computational data on three proteolysis targeting chimeras (PROTACs) currently in clinical trials.</p><p><strong>Key results: </strong>Molecular descriptors of ARV-110, ARV-471, and DT-2216 are reported and the main limitations of the applied experimental approaches are discussed. Moreover, a simple computational method shows how predicting the presence of chameleonic effects.</p><p><strong>Conclusion: </strong>A full complete physicochemical characterization of three degraders in clinical trials is reported to highlight the differences in physicochemical descriptors between PROTACs dosed orally and intravenously.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 5","pages":"721-736"},"PeriodicalIF":3.4,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11542721/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142612104","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}
引用次数: 0
Cerium oxide nanoparticles-assisted aptasensor for chronic myeloid leukaemia detection. 用于检测慢性骨髓性白血病的纳米氧化铈辅助传感器。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-18 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2404
Yuspian Nur, Muhammad Ihda Hl Zein, Irkham Irkham, Shabarni Gaffar, Toto Subroto, Yeni Wahyuni Hartati
{"title":"Cerium oxide nanoparticles-assisted aptasensor for chronic myeloid leukaemia detection.","authors":"Yuspian Nur, Muhammad Ihda Hl Zein, Irkham Irkham, Shabarni Gaffar, Toto Subroto, Yeni Wahyuni Hartati","doi":"10.5599/admet.2404","DOIUrl":"https://doi.org/10.5599/admet.2404","url":null,"abstract":"<p><strong>Background and purpose: </strong>Chronic myeloid leukaemia (CML) is one of the most lethal types of leukaemia and can rapidly progress if not treated properly. Therefore, having an effective diagnostic strategy is crucial. Various methods are available for diagnosis, including electrochemical biosensors with aptamer bioreceptors.</p><p><strong>Experimental approach: </strong>In this study, we immobilized the KK1D04 aptamer on a screen-printed carbon electrode (SPCE) supported by CeO<sub>2</sub> nanoparticles (CeO<sub>2</sub>NPs) to detect K562 cells, a type of CML cell line. Several parameters were optimized to enhance the aptasensor response using the Box-Behnken experimental design.</p><p><strong>Key results: </strong>The developed aptasensor demonstrated good performance with a limit of detection (LOD) and limit of quantification (LOQ) of 16 cells/mL and 3,882 cells/mL, respectively, in the K562 cell concentration range of 10<sup>2</sup> to 10<sup>6</sup> cells/mL. The optimum experimental conditions were an aptamer concentration of 0.8 ppm, an aptamer incubation time of 36 minutes, and a K562 aptamer-cell incubation time of 13 minutes. The aptasensor also exhibits selectivity for K562 cells compared to Vero cells, THP1 cells, and Raji cells.</p><p><strong>Conclusion: </strong>The aptasensor in this study demonstrated the potential to detect K562 cells. These results could contribute to the advancement of point-of-care (POC) devices for the detection of CML.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"623-635"},"PeriodicalIF":3.4,"publicationDate":"2024-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517519/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543042","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}
引用次数: 0
Ex vivo propofol permeation across nasal mucosa: A proof-of-concept study for outpatient light sedation via nasal route. 异丙酚通过鼻黏膜的体外渗透:通过鼻腔途径进行门诊轻度镇静的概念验证研究。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-16 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2403
Michele D Spampinato, Anna Costanzini, Roberto De Giorgio, Angelina Passaro, Nicola Realdon, Fabrizio Bortolotti, Sabrina Banella, Gaia Colombo
{"title":"<i>Ex vivo</i> propofol permeation across nasal mucosa: A proof-of-concept study for outpatient light sedation via nasal route.","authors":"Michele D Spampinato, Anna Costanzini, Roberto De Giorgio, Angelina Passaro, Nicola Realdon, Fabrizio Bortolotti, Sabrina Banella, Gaia Colombo","doi":"10.5599/admet.2403","DOIUrl":"https://doi.org/10.5599/admet.2403","url":null,"abstract":"<p><strong>Background and purpose: </strong>Aiming to achieve light sedation via intranasal administration, this study showed that propofol (PPF) did not permeate across the rabbit nasal mucosa ex vivo from its marketed emulsion for injection.</p><p><strong>Experimental approach: </strong>Dilution of the emulsion with methyl-β-cyclodextrin in saline solution increased propofol solubility in water and diffusion across the nasal epithelium.</p><p><strong>Key results and conclusion: </strong>Despite these positive effects of the cyclodextrin, the amount of PPF permeated was minimal in 3 h, exceeding the formulation residence time in the nose. These results highlight the key role of formulation and the need for innovation in solubility and transmucosal transport enhancement techniques to optimize drug delivery and therapeutic efficacy.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 5","pages":"759-768"},"PeriodicalIF":3.4,"publicationDate":"2024-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11542715/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142612097","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}
引用次数: 0
The biological applications of IPN hydrogels. IPN 水凝胶的生物应用。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-14 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2398
María I León-Campos, Juan J Mendoza, Hilda Aguayo-Morales, Luis E Cobos-Puc, Denis A Cabrera-Munguía, Jesús A Claudio-Rizo
{"title":"The biological applications of IPN hydrogels.","authors":"María I León-Campos, Juan J Mendoza, Hilda Aguayo-Morales, Luis E Cobos-Puc, Denis A Cabrera-Munguía, Jesús A Claudio-Rizo","doi":"10.5599/admet.2398","DOIUrl":"https://doi.org/10.5599/admet.2398","url":null,"abstract":"<p><strong>Background and purpose: </strong>Interpenetrating polymer network (IPN) hydrogels are an adaptable category of materials, exhibiting remarkable promise for various biological applications due to their distinctive structural and functional attributes. This review delves into the synthesis of IPN hydrogels through both physical and chemical methodologies, elucidating how these techniques allow for precise tailoring of mechanical properties, swelling behaviour, and biocompatibility.</p><p><strong>Experimental approach: </strong>We conducted an extensive literature review by searching well-established online research databases for articles published since 2009 to gather comprehensive data on IPN hydrogels.</p><p><strong>Key results: </strong>Our review highlights several critical applications of IPN hydrogels in the biomedical field; i) Tissue engineering: IPN hydrogels are evaluated for their capacity to emulate the extracellular matrix, making them excellent scaffolds for tissue engineering; ii) Controlled drug release: The ability of IPN hydrogels to modulate drug release rates and protect bioactive molecules is explored. Their structure enables sustained and targeted delivery of therapeutic agents, enhancing treatment efficacy; iii) 3D bioprinting: The use of IPN hydrogels as bioinks for 3D bioprinting is assessed, demonstrating their capability to construct intricate, biomimetic structures with high precision; and iv) Regenerative medicine: the development of biomimetic IPN hydrogels for regenerative medicine, emphasizing their potential to closely replicate natural biological environments, thereby promoting effective tissue repair and regeneration.</p><p><strong>Conclusion: </strong>IPN hydrogels emerge as a versatile and multifaceted platform with significant implications for advancing biomedical science and clinical therapies. Their diverse applications highlight their potential to revolutionize current biomedical practices and contribute to the development of innovative therapeutic solutions.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"581-621"},"PeriodicalIF":3.4,"publicationDate":"2024-08-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517517/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543046","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}
引用次数: 0
Analgesic effects of intraarticular anaesthetic lidocaine and methylprednisolone versus methylprednisolone alone following knee arthroscopy. 膝关节镜手术后关节内麻醉利多卡因和甲基强的松龙与单用甲基强的松龙的镇痛效果对比。
IF 3.4
ADMET and DMPK Pub Date : 2024-08-03 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2412
Wahid Mohammed Hassan, Anas Amer Mohammad
{"title":"Analgesic effects of intraarticular anaesthetic lidocaine and methylprednisolone versus methylprednisolone alone following knee arthroscopy.","authors":"Wahid Mohammed Hassan, Anas Amer Mohammad","doi":"10.5599/admet.2412","DOIUrl":"https://doi.org/10.5599/admet.2412","url":null,"abstract":"<p><strong>Background: </strong>Knee arthroscopy is a widely practiced orthopaedic procedure known for its minimally invasive approach, allowing quicker recovery times and less postoperative discomfort than traditional open surgeries. However, managing postoperative pain remains a critical aspect of patient care and satisfaction. The main objective of this research is to examine the relationships between patient demographics (age, gender, BMI) and early postoperative outcomes, including pain, physiotherapy, and walking.</p><p><strong>Method: </strong>Randomized data collection, clinical trial study of 2 groups of patients. The patients were split into lidocaine 1 % 16 ml + methylprednisolone 160 mg 4 ml) and (methylprednisolone only 160 mg 4 ml) groups. All patients in both groups were queried about age, gender, BMI, and pain on the first, third, and 15th days following surgery. All patients were tested for physiotherapy on the second, third, and fourth postop days. After surgery, walking was tested on the third, fourth, and fifth days.</p><p><strong>Results: </strong>Significant differences in postoperative pain relief and physiotherapy initiation times were observed. There are notable associations between treatment groups and recovery metrics, such as pain levels and mobility on various days' post-surgery. Significant demographic influences (age, gender, BMI) on recovery outcomes are observed, particularly in walking and pain at day 15 post-operation.</p><p><strong>Conclusion: </strong>lidocaine and methylprednisolone improve postoperative pain relief and functional recovery in knee arthroscopy patients, with most experiencing reduced pain early post-surgery (early physiotherapy) and an expedited return to walking (decreased morbidity). Patients taking just methylprednisolone recovered slower. Age, gender, and BMI affected pain and walking abilities post-operation but not physiotherapy time, underscoring the personalised approach needed in postoperative treatment.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"679-685"},"PeriodicalIF":3.4,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517516/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543041","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}
引用次数: 0
Optimizing gefitinib nanoliposomes by Box-Behnken design and coating with chitosan: A sequential approach for enhanced drug delivery. 通过盒-贝肯设计和壳聚糖包衣优化吉非替尼纳米脂质体:一种增强药物输送的连续方法。
IF 3.4
ADMET and DMPK Pub Date : 2024-07-31 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2366
Seema Rohilla, Rajendra Awasthi, Ankur Rohilla, Sachin Kumar Singh, Dinesh Kumar Chellappan, Kamal Dua, Harish Dureja
{"title":"Optimizing gefitinib nanoliposomes by Box-Behnken design and coating with chitosan: A sequential approach for enhanced drug delivery.","authors":"Seema Rohilla, Rajendra Awasthi, Ankur Rohilla, Sachin Kumar Singh, Dinesh Kumar Chellappan, Kamal Dua, Harish Dureja","doi":"10.5599/admet.2366","DOIUrl":"https://doi.org/10.5599/admet.2366","url":null,"abstract":"<p><strong>Background and purpose: </strong>This study aimed to improve the stability and prolonged gefitinib release from the nanoliposomes.</p><p><strong>Experimental approach: </strong>Nanoliposomes were prepared by reverse-phase evaporation and optimized using Box-Behnken design to investigate the influence of sonication time (<i>X</i> <sub>1</sub>), tween 80 / soya phosphatidylcholine ratio (<i>X</i> <sub>2</sub>), and cholesterol/soya phosphatidylcholine ratio (<i>X</i> <sub>3</sub>) on nanoliposomes.</p><p><strong>Key results: </strong>Optimized nanoliposomes were quasi-spherical shaped, with a mean dimension of 93.2 nm and an encapsulation efficiency of 87.56±0.17 %. Surface decoration of the optimized batch was done using different concentrations of chitosan. The optimal chitosan concentration required to adorn the nanoliposome surface was 0.01 %. In comparison to unadorned nanoliposomes (82.16±0.65 %), adorned nanoliposomes (78.04±0.35 %) released the drug consistently over 24 h via Fickian diffusion. The IC<sub>50</sub> values for surface-adorned nanoliposomes in A549 and H1299 cells were 6.53±0.75 and 4.73±0.46 μM, respectively. Cytotoxicity of the surface-decorated nanoliposomes may be due to their higher zeta potential and prolonged drug release. At the end of the sixth month, the samples stored at 4 °C were more stable than those stored at 25 °C and 45 °C. The stability of plain nanoliposomes has increased after chitosan coating. Thus, by using different concentrations of chitosan solution as coating material, we can develop a suitable sustained drug-release surface-adorned nanoliposomal formulation.</p><p><strong>Conclusion: </strong>The developed nanoliposomes may offer a new path for melanoma clinics.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"12 4","pages":"657-677"},"PeriodicalIF":3.4,"publicationDate":"2024-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11517515/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543045","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}
引用次数: 0
Impact of lactoferrin supplementation on cotrimoxazole pharmacokinetics: A preliminary clinical investigation. 补充乳铁蛋白对复方新诺明药代动力学的影响:初步临床研究。
IF 3.4
ADMET and DMPK Pub Date : 2024-06-27 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2358
Dion Notario, Angela Marietha Munzir, Yulina Novella, Linawati Hananta
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