Journal of microencapsulation最新文献

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Comparison of the radioprotective effects of the liposomal forms of five natural radioprotectants in alleviating the adverse effects of ionising irradiation on human lymphocytes and skin cells in radiotherapy. 五种天然放射性保护剂的脂质体形式在减轻放射治疗中电离辐射对人类淋巴结和皮肤细胞的不良影响方面的放射性保护作用的比较。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-12-01 Epub Date: 2023-11-09 DOI: 10.1080/02652048.2023.2268705
Ngoc-Duy Pham, Thi-Huynh-Nga Nguyen, Ngoc-Bich-Dao Vu, Thi-Ngoc-Mai Tran, Bao-Ngoc Pham, Hoang-Sinh Le, Kim-Hai Vo, Xuan-Cuong Le, Le-Bao-Ha Tran, Minh-Hiep Nguyen
{"title":"Comparison of the radioprotective effects of the liposomal forms of five natural radioprotectants in alleviating the adverse effects of ionising irradiation on human lymphocytes and skin cells in radiotherapy.","authors":"Ngoc-Duy Pham, Thi-Huynh-Nga Nguyen, Ngoc-Bich-Dao Vu, Thi-Ngoc-Mai Tran, Bao-Ngoc Pham, Hoang-Sinh Le, Kim-Hai Vo, Xuan-Cuong Le, Le-Bao-Ha Tran, Minh-Hiep Nguyen","doi":"10.1080/02652048.2023.2268705","DOIUrl":"10.1080/02652048.2023.2268705","url":null,"abstract":"<p><p>This study aims to evaluate the radioprotective effects of liposomes encapsulating curcumin (Lip-CUR), silibinin (Lip-SIL), α-tocopherol (Lip-TOC), quercetin (Lip-QUE) and resveratrol (Lip-RES) in alleviating the adverse effects of ionising irradiation on human lymphoctyes and skin cells in radiotherapy. Liposomes encapsulating the above natural radioprotectants (Lip-NRPs) were prepared by the film hydration method combined with sonication. Their radioprotective effects for the cells against X-irradiation was evaluated using trypan-blue assay and γ-H2AX assay. All prepared Lip-NRPs had a mean diameter less than 240 nm, polydispersity index less than 0.32, and zeta potential more than -23 mV. Among them, the radioprotective effect of Lip-RES was lowest, while that of Lip-QUE was highest. Lip-SIL also exhibited a high radioprotective effect despite its low DPPH-radical scavenging activity (12.9%). The radioprotective effects of Lip-NRPs do not solely depend on the free radical scavenging activity of NRPs but also on their ability to activate cellular mechanisms.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"613-629"},"PeriodicalIF":3.9,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41182835","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}
引用次数: 0
Polysorbate 80 surface modified PLGA nanoparticles: an in-vitro evaluation of cellular uptake and cytotoxicity on neuro-2a cells. 聚山梨醇酯80表面修饰的PLGA纳米颗粒:细胞摄取和对神经-2a细胞的细胞毒性的体外评估。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-08-23 DOI: 10.1080/02652048.2023.2244095
Surbhi Sharma, Shweta Dang
{"title":"Polysorbate 80 surface modified PLGA nanoparticles: an <i>in-vitro</i> evaluation of cellular uptake and cytotoxicity on neuro-2a cells.","authors":"Surbhi Sharma,&nbsp;Shweta Dang","doi":"10.1080/02652048.2023.2244095","DOIUrl":"10.1080/02652048.2023.2244095","url":null,"abstract":"<p><strong>Aim: </strong>Present study focuses on the development of P80 coated PLGA Nanoparticles loaded with drugs, paroxetine (P80-Par-PLGA-NPs) and clonidine (P80-CLD-PLGA-NPs) for <i>in-vitro</i> evaluation of Cellular Uptake & Cytotoxicity on Neuro-2a cells.</p><p><strong>Method: </strong>P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs were developed and characterised for zeta size, potential, PDI, EE%, DL%, TEM, SEM, FTIR, DSC, i<i>n-vitro</i> release, cytotoxicity, histopathological and cell uptake studies using rhodamine loaded P80-NPs.</p><p><strong>Result: </strong>Mean particle diameter of P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs was 204; 182.7 nm, ZP of -21.8; -18.72 mV and 0.275; 0.341 PDI, respectively. TEM and SEM images revealed homogenous surface morphology. <i>In-vitro</i> drug release showed sustained and complete release in 72 h. Cell viability (>90%) at C<sub>max</sub> and no cytotoxicity in histopathology was observed. Significant higher uptake (96.9%) of P80-modified-NPS was observed as compared to unmodified-NPs (81%) (p < 0.05).</p><p><strong>Conclusion: </strong>The finding clearly indicated a higher cell uptake of drugs via surface modified P80-coated PLGA-NPs as compared to unmodified particles.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"534-548"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10047753","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}
引用次数: 1
The management of osteoarthritis symptomatology through nanotechnology: a patent review. 通过纳米技术治疗骨关节炎症状:一项专利综述。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-09-12 DOI: 10.1080/02652048.2023.2258955
Mariana Mendonça Santos, Anamaria Mendonça Santos, José Adão Carvalho Nascimento Júnior, Tatianny de Araujo Andrade, Gomathi Rajkumar, Luiza Abrahão Frank, Mairim Russo Serafini
{"title":"The management of osteoarthritis symptomatology through nanotechnology: a patent review.","authors":"Mariana Mendonça Santos,&nbsp;Anamaria Mendonça Santos,&nbsp;José Adão Carvalho Nascimento Júnior,&nbsp;Tatianny de Araujo Andrade,&nbsp;Gomathi Rajkumar,&nbsp;Luiza Abrahão Frank,&nbsp;Mairim Russo Serafini","doi":"10.1080/02652048.2023.2258955","DOIUrl":"10.1080/02652048.2023.2258955","url":null,"abstract":"<p><p>Osteoarthritis is considered a degenerative joint disease that is characterised by inflammation, chronic pain, and functional limitation. The increasing development of nanotechnology in drug delivery systems has provided new ideas and methods for osteoarthritis therapy. This review aimed to evaluate patents that have developed innovations, therapeutic strategies, and alternatives using nanotechnology in osteoarthritis treatment. The results show patents deposited from 2015 to November 2021 in the online databases European Patent Office and World Intellectual Property Organisation. A total of 651 patents were identified for preliminary assessment and 16 were selected for full reading and discussion. The evaluated patents are focused on the intraarticular route, oral route, and topical route for osteoarthritis treatment. The intraarticular route presented a higher patent number, followed by the oral and topical routes, respectively. The development of new technologies allows us to envision a promising and positive future in osteoarthritis treatment.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"475-490"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10216637","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}
引用次数: 0
Development, systematic optimisation and biofilm disruption activity of eugenol-based nanosized emulsions stabilised with Tween 80. 吐温80稳定丁香酚基纳米乳液的开发、系统优化和生物膜破坏活性。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-08-11 DOI: 10.1080/02652048.2023.2244094
Chandra Lekha Putta, Syed Nazrin Ruhina Rahman, Payel Chakraborty, Tamilvanan Shunmugaperumal
{"title":"Development, systematic optimisation and biofilm disruption activity of eugenol-based nanosized emulsions stabilised with Tween 80.","authors":"Chandra Lekha Putta,&nbsp;Syed Nazrin Ruhina Rahman,&nbsp;Payel Chakraborty,&nbsp;Tamilvanan Shunmugaperumal","doi":"10.1080/02652048.2023.2244094","DOIUrl":"10.1080/02652048.2023.2244094","url":null,"abstract":"<p><p>The aims of this study were to systematically optimise a formula for eugenol emulsions via face-centered central composite design and to assess the activity against two-different bacterial strains (<i>Staphylococcus aureus</i> and <i>Propionibacterium acnes</i>) present at planktonic and biofilm forms. The molecular interaction of excipients, mean particle size (MPS) including zeta potential (ZP), drug entrapment efficiency (DEE) and <i>in vitro</i> drug release of optimised emulsions was done using FT-IR, Malvern Zetasizer, ultracentrifugation technique and membrane-free dissolution model, respectively. The emulsions consisted of 151.3 ± 1.45 nm MPS, -21.3 ± 1.25 mV ZP and 93.98 ± 1.41% DEE values. On storage of emulsions at 25 °C for 3 months, the value of DEE was found to be 72.12 ± 2.82%. The Tween 80 emulsifier film coverage onto the dispersed eugenol droplets of emulsions delayed significantly the drug release (12%-19%) compared to the drug release occurred from pure eugenol. The treatment of planktonic <i>S. aureus</i> and <i>P. acnes</i> with diluted eugenol emulsions showed the minimum inhibitory concentration and minimum bactericidal concentration values at 1.25-2.5 mg/ml whereas it occurred at 10 mg/ml for pure eugenol. Treating the biofilms with eugenol emulsions (1-2 mg/ml) yielded 59-70% minimum biofilm eradication concentration but 10 mg/ml pure eugenol showed 60%. Hence, the eugenol emulsions displayed antibacterial activity and could be projected as an antibiofilm or biofilm disruption agent.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"517-533"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10324864","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}
引用次数: 0
Microencapsulation of Bacillus subtilis and oat β-glucan and their application as a synbiotic in fish feed. 枯草芽孢杆菌和燕麦β-葡聚糖的微胶囊化及其作为合生素在鱼类饲料中的应用。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-06-08 DOI: 10.1080/02652048.2023.2220394
Angélica Priscila do Carmo Alves, Amanda do Carmo Alves, Rodney Alexandre Ferreira Rodrigues, Brunno da Silva Cerozi, José Eurico Possebon Cyrino
{"title":"Microencapsulation of <i>Bacillus subtilis</i> and oat β-glucan and their application as a synbiotic in fish feed.","authors":"Angélica Priscila do Carmo Alves,&nbsp;Amanda do Carmo Alves,&nbsp;Rodney Alexandre Ferreira Rodrigues,&nbsp;Brunno da Silva Cerozi,&nbsp;José Eurico Possebon Cyrino","doi":"10.1080/02652048.2023.2220394","DOIUrl":"10.1080/02652048.2023.2220394","url":null,"abstract":"<p><p>To improve survival during storage and exposure to adverse conditions, <i>Bacillus subtilis</i> was microencapsulated with oat β-glucan by spray-drying technology. The characterisation of the microcapsules was designed to compare free and microencapsulated cells through exposure to simulated gastric fluids (SGF) throughout storage for 90 days at different temperatures. The characterisation included analysis of efficiency, morphology, moisture, water activity, hygroscopicity, particle size, and zeta potential. The microcapsules presented a particle size of 1.5 ± 0.34 μm and an encapsulation efficiency of 77.9 ± 3.06%. After SGF, the survival of microencapsulated cells was 8.4 ± 0.07 log CFU mL<sup>-1</sup> while that of free cells was 7.6 ± 0.06 log CFU mL<sup>-1</sup>. After 90 days of storage, only microencapsulated cells remained above 6 log-unit of viability. In conclusion, spray-drying technique combined with the addition of oat β-glucan proved to be an efficient method to protect <i>B. subtilis</i> under storage and SGF with potential application in fish feed.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"491-501"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9588418","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}
引用次数: 0
Tacrolimus loaded nanostructured lipid carriers using Moringa oleifera seed oil: design, optimization and in-vitro evaluations. 使用辣木籽油负载他克莫司的纳米结构脂质载体:设计、优化和体外评价。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-07-05 DOI: 10.1080/02652048.2023.2231075
Rajat Garg, Anuj Garg
{"title":"Tacrolimus loaded nanostructured lipid carriers using Moringa oleifera seed oil: design, optimization and in-vitro evaluations.","authors":"Rajat Garg,&nbsp;Anuj Garg","doi":"10.1080/02652048.2023.2231075","DOIUrl":"10.1080/02652048.2023.2231075","url":null,"abstract":"<p><p>The proposed research aims to develop Tacrolimus-loaded nanostructured lipid carriers (TAC-loaded NLCs) to overcome poor aqueous solubility and dissolution rate to enhance its oral absorption. A central composite design was used to optimise the amount of Poloxamer 188 and D-α-Tocopherol-polyethylene-glycol-succinate (TPGS). The optimised TAC-loaded NLCs contain stearic acid (250 mg), <i>Moringa oleifera</i> (MO) seed oil (50 mg), TAC (Tacrolimus: 10 mg), TPGS (60 mg), and Poloxamer 188 (1% w/v) with a mean diameter of 393.3 ± 29.68 nm, a zeta potential of -18.3 ± 6.19 mV, high entrapment efficiency (92.12 ± 1.14% w/w), and desirability (0.989). TAC-loaded NLCs showed ∼12 times higher drug dissolution efficiency, while <i>in-vitro</i> anti-inflammatory studies showed ∼1.8 times lower IC<sub>50</sub> (half-maximal inhibitory concentration) than TAC suspension. The lyophilised TAC-loaded NLCs were found to be stable after 3 months. Thus, the present study concludes the successful encapsulation of TAC in NLCs made of stearic acid and MO seed oil.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"502-516"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9741303","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}
引用次数: 0
Diruthenium(II-III)-ibuprofen-loaded chitosan-based microparticles and nanoparticles systems: encapsulation, characterisation, anticancer activity of the nanoformulations against U87MG human glioma cells. Diruthenium(II-III)-布洛芬负载的壳聚糖基微粒和纳米颗粒系统:纳米制剂对U87MG人神经胶质瘤细胞的封装、表征和抗癌活性。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-09-12 DOI: 10.1080/02652048.2023.2258967
Hanif Ur-Rehman, Bárbara Fornaciari, Samara R Alves, Alison Colquhoun, Denise de Oliveira Silva
{"title":"Diruthenium(II-III)-ibuprofen-loaded chitosan-based microparticles and nanoparticles systems: encapsulation, characterisation, anticancer activity of the nanoformulations against U87MG human glioma cells.","authors":"Hanif Ur-Rehman,&nbsp;Bárbara Fornaciari,&nbsp;Samara R Alves,&nbsp;Alison Colquhoun,&nbsp;Denise de Oliveira Silva","doi":"10.1080/02652048.2023.2258967","DOIUrl":"10.1080/02652048.2023.2258967","url":null,"abstract":"<p><p>The aim of this work was to investigate novel formulations containing diruthenium(II-III)-ibuprofen (RuIbp) metallodrug encapsulated into the chitosan (CT) biopolymer. Microparticles (RuIbp/CT MPs, ∼ 1 µm) were prepared by spray-drying, and RuIbp/CT-crosslinked nanoparticles (NPs) by ionic gelation (RuIbp/CT-TPP, TPP = tripolyphosphate <b>(1)</b>, RuIbp/CT-TPP-PEG, PEG = poly(ethyleneglycol <b>(2)</b>) or pre-gel/polyelectrolyte complex method (RuIbp/CT-ALG, ALG = alginate <b>(3)</b>). Ru analysis was conducted by energy dispersive x-ray fluorescence or inductively coupled plasma atomic emission spectroscopy, and physicochemical characterisation by powder x-ray diffraction, electronic absorption and FTIR spectroscopies, electrospray ionisation mass spectrometry, thermal analysis, scanning electron, transition electron and atomic force microscopies, and dynamic light scattering. The RuIbp-loaded nanosystems exhibited encapsulation efficiency ∼ 20-37%, drug loading∼ 10-20% (w/w), hydrodynamic diameter (nm): 103.2 ± 7.9 <b>(1)</b>, 91.7 ± 12.6 <b>(2)</b>, 270.2 ± 58.4 <b>(3)</b>, zeta potential (mV): +(47.7 ± 2.8) <b>(1)</b>, +(49.2 ± 3.6) <b>(2)</b>, -(28.2 ± 2.0) <b>(3)</b>. Nanoformulation <b>(1)</b> showed the highest cytotoxicity with increased efficacy in relation to the RuIbp free metallodrug against U87MG human glioma cells.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"549-565"},"PeriodicalIF":3.9,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10564676","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}
引用次数: 0
Dual drug loaded polypeptide delivery systems for cancer therapy. 用于癌症治疗的双载药多肽递送系统。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-10-12 DOI: 10.1080/02652048.2023.2270064
Natalia Zashikhina, Erik Gandalipov, Apollinariia Dzhuzha, Viktor Korzhikov-Vlakh, Evgenia Korzhikova-Vlakh
{"title":"Dual drug loaded polypeptide delivery systems for cancer therapy.","authors":"Natalia Zashikhina,&nbsp;Erik Gandalipov,&nbsp;Apollinariia Dzhuzha,&nbsp;Viktor Korzhikov-Vlakh,&nbsp;Evgenia Korzhikova-Vlakh","doi":"10.1080/02652048.2023.2270064","DOIUrl":"10.1080/02652048.2023.2270064","url":null,"abstract":"<p><p>The present study was aimed to prepare and examine <i>in vitro</i> novel dual-drug loaded delivery systems. Biodegradable nanoparticles based on poly(L-glutamic acid-<i>co</i>-D-phenylalanine) were used as nanocarriers for encapsulation of two drugs from the paclitaxel, irinotecan, and doxorubicin series. The developed delivery systems were characterised with hydrodynamic diameters less than 300 nm (PDI < 0.3). High encapsulation efficiencies (≥75%) were achieved for all single- and dual-drug formulations. The release studies showed faster release at acidic pH, with the release rate decreasing over time. The release patterns of the co-encapsulated forms of substances differed from those of the separately encapsulated drugs, suggesting differences in drug-polymer interactions. The joint action of encapsulated drugs was analysed using the colon cancer cells, both for the dual-drug delivery sytems and a mixture of single-drug formulations. The encapsulated forms of the drug combinations demonstrated comparable efficacy to the free forms, with the encapsulation enhancing solubility of the hydrophobic drug paclitaxel.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"1-19"},"PeriodicalIF":3.9,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41203423","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}
引用次数: 2
In-vitro and in-vivo evaluation and anti-colitis activity of esculetin-loaded nanostructured lipid carrier decorated with DSPE-MPEG2000. DSPE-MPEG2000修饰的载脂质纳米载体体外和体内评价及其抗结肠炎活性。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-09-01 DOI: 10.1080/02652048.2023.2215345
Feng Shi, Wenxiong Yin, Michael Adu-Frimpong, Xiaoxiao Li, Xiaoli Xia, Weigang Sun, Hao Ji, Elmurat Toreniyazov, Wang Qilong, Xia Cao, Jiangnan Yu, Ximing Xu
{"title":"<i>In-vitro</i> and <i>in-vivo</i> evaluation and anti-colitis activity of esculetin-loaded nanostructured lipid carrier decorated with DSPE-MPEG2000.","authors":"Feng Shi,&nbsp;Wenxiong Yin,&nbsp;Michael Adu-Frimpong,&nbsp;Xiaoxiao Li,&nbsp;Xiaoli Xia,&nbsp;Weigang Sun,&nbsp;Hao Ji,&nbsp;Elmurat Toreniyazov,&nbsp;Wang Qilong,&nbsp;Xia Cao,&nbsp;Jiangnan Yu,&nbsp;Ximing Xu","doi":"10.1080/02652048.2023.2215345","DOIUrl":"https://doi.org/10.1080/02652048.2023.2215345","url":null,"abstract":"<p><strong>Objective: </strong>Encapsulation of esculetin into DSPE-MPEG2000 carrier was performed to improve its water solubility and oral bioavailability, as well as enhance its anti-inflammatory effect on a mouse model of ulcerative colitis that was induced with dextran sulphate sodium (DSS).</p><p><strong>Methods: </strong>We determined the <i>in-vitro</i> and <i>in-vivo</i> high-performance liquid chromatographic (HPLC) analysis method of esculetin; Esculetin-loaded nanostructure lipid carrier (Esc-NLC) was prepared using a thin-film dispersion method, wherein a particle size analyser was used to measure the particle size (PS) and zeta potential (ZP) of the Esc-NLC, while a transmission electron microscope (TEM) was employed to observe its morphology. Also, HPLC was used to measure its drug loading (DL), encapsulation efficiency (EE) and the <i>in-vitro</i> release of the preparation, as well as investigate the pharmacokinetic parameters. In addition, its anti-colitis effect was evaluated via histopathological examination of HE-stained sections and detection of the concentrations of tumour necrosis factor-alpha (TNF-α), interleukin (IL)-1 beta (β), and IL-6 in serum with ELISA kits.</p><p><strong>Results: </strong>The PS of Esc-NLC was 102.29 ± 0.63 nm with relative standard deviation (RSD) of 1.08% (with poly-dispersity index-PDI of 0.197 ± 0.023), while the ZP was -15.67 ± 1.39 mV with RSD of 1.24%. Solubility of esculetin was improved coupled with prolonged release time. Its pharmacokinetic parameters were compared with that of free esculetin, wherein the maximum concentration of the drug in plasma was increased by 5.5 times. Of note, bioavailability of the drug was increased by 1.7 times, while the half-life was prolonged by 2.4 times. In the anti-colitis efficacy experiment, the mice in Esc and Esc-NLC groups exhibited significantly reduced levels of TNF-α, IL-1β, and IL-6 in their sera comparable to the DSS group. Colon histopathological examination revealed that mice with ulcerative colitis in both Esc and Esc-NLC groups displayed improved inflammation, amid the Esc-NLC groups having the best prophylactic treatment effect.</p><p><strong>Conclusion: </strong>Esc-NLC could ameliorate DSS-induced ulcerative colitis by improving bioavailability, prolonging drug release time and regulating cytokine release. This observation confirmed the potential of Esc-NLC to reduce inflammation in ulcerative colitis, albeit the need for follow-up research to verify the application of this strategy to clinical treatment of ulcerative colitis.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 6","pages":"442-455"},"PeriodicalIF":3.9,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9995398","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}
引用次数: 2
Enhancement of ocular anti-glaucomic activity of agomelatine through fabrication of hyaluronic acid modified-elastosomes: formulation, statistical optimisation, in vitro characterisation, histopathological study, and in vivo assessment. 通过制备透明质酸修饰弹性体增强阿戈美拉汀抗青光眼活性:配方、统计优化、体外表征、组织病理学研究和体内评估。
IF 3.9 4区 医学
Journal of microencapsulation Pub Date : 2023-09-01 DOI: 10.1080/02652048.2023.2215326
Asmaa Ashraf Nemr, Galal Mohamed El-Mahrouk, Hany Abdo Badie
{"title":"Enhancement of ocular anti-glaucomic activity of agomelatine through fabrication of hyaluronic acid modified-elastosomes: formulation, statistical optimisation<i>, in vitro</i> characterisation, histopathological study, and <i>in vivo</i> assessment.","authors":"Asmaa Ashraf Nemr,&nbsp;Galal Mohamed El-Mahrouk,&nbsp;Hany Abdo Badie","doi":"10.1080/02652048.2023.2215326","DOIUrl":"https://doi.org/10.1080/02652048.2023.2215326","url":null,"abstract":"<p><strong>Aim: </strong>The aim of this manuscript was to fabricate agomelatine (AGM) loaded elastosomes to improve its corneal permeation and ocular bioavailability. AGM is a biopharmaceutical classification system (BCS) class II with low water solubility and high membrane permeability. It has a potent agonistic action on melatonin receptors, so it is used for glaucoma treatment.</p><p><strong>Methods: </strong>Elastosomes were made using modified ethanol injection technique according to a 2<sup>2</sup> × 4<sup>1</sup> full factorial design. The chosen factors were: edge activators (EAs) type, surfactant percent (SAA %w/w), and cholesterol:surfactant ratio (CH:SAA ratio). The studied responses were encapsulation efficiency percent (EE%), mean diameter, polydispersity index (PDI), zeta potential (ZP), percentage of drug released after two hours (<i>Q</i><sub>2h%</sub>), and 24 hours (<i>Q</i><sub>24h%</sub>).</p><p><strong>Results: </strong>The optimum formula with the desirability of 0.752 was composed of Brij98 as EA type, 15%w/w SAA%, and 1:1 CH:SAA ratio. It revealed EE% of 73.22%w/v and mean diameter, PDI, ZP, <i>Q</i><sub>2h%</sub>, and <i>Q</i><sub>24h%</sub> values of 484.25 nm, 0.31, -30.75 mV, 32.7%w/v, and 75.6%w/v, respectively. It demonstrated acceptable stability for three months and superior elasticity than its conventional liposome. The histopathological study ensured the tolerability of its ophthalmic application. Also, it was proven to be safe from the results of the pH and refractive index tests. The <i>in vivo</i> pharmacodynamic parameters of the optimum formula revealed dominance in a maximum % decrease in intraocular pressure (IOP), the area under the IOP response curve, and mean residence time with the value of 82.73%w/v, 820.69%h, and 13.98 h compared to that of the AGM solution (35.92%w/v, 181.30%h, and 7.52 h).</p><p><strong>Conclusions: </strong>Elastosomes can be a promising option to improve AGM ocular bioavailability.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 6","pages":"423-441"},"PeriodicalIF":3.9,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9995400","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}
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