Pub Date : 2023-03-01DOI: 10.1080/02652048.2023.2178537
Malik Muhammad Irfan, Shefaat Ullah Shah, Kifayat Ullah Shah, Nicolas Anton, Idoux-Gillet Ysia, Guillaume Conzatti, Kifayat Ullah Shah, Perennes Elise, Thierry Vandamme
The fundamental purpose of this study was to develop a stable lyophilised finasteride nanosystem (FNS-NS) for topical delivery. The FNS-NS was fabricated using an ultrasonication technique. The impact of two different cryoprotectants on the physicochemical characteristics of FNS-NS before and after lyophilisation was thoroughly investigated. The lyophilised FNS-NS had spherical shape with particle size lied between 188.6 nm ± 4.4 and 298.7 nm ± 4.7, low PDI values (0.26 ± 0.02 to 0.32 ± 0.02) and zeta potential ranging from -38.3 to +53.3 mV. The confocal laser microscopy depicted a comparatively higher cellular internalisation achieved for undecorated FNS-NS with respect to its chitosan-decorated counterpart. The lyophilised FNS-NS was stable for 90 days at proper storage conditions. The FNS-NS with 15% trehalose had appropriate physicochemical attributes that could be a promising carrier for topical delivery to treat androgenic alopecia.
{"title":"Impact of formulation design and lyophilisation on the physicochemical characteristics of finasteride nanosystems.","authors":"Malik Muhammad Irfan, Shefaat Ullah Shah, Kifayat Ullah Shah, Nicolas Anton, Idoux-Gillet Ysia, Guillaume Conzatti, Kifayat Ullah Shah, Perennes Elise, Thierry Vandamme","doi":"10.1080/02652048.2023.2178537","DOIUrl":"https://doi.org/10.1080/02652048.2023.2178537","url":null,"abstract":"<p><p>The fundamental purpose of this study was to develop a stable lyophilised finasteride nanosystem (FNS-NS) for topical delivery. The FNS-NS was fabricated using an ultrasonication technique. The impact of two different cryoprotectants on the physicochemical characteristics of FNS-NS before and after lyophilisation was thoroughly investigated. The lyophilised FNS-NS had spherical shape with particle size lied between 188.6 nm ± 4.4 and 298.7 nm ± 4.7, low PDI values (0.26 ± 0.02 to 0.32 ± 0.02) and zeta potential ranging from -38.3 to +53.3 mV. The confocal laser microscopy depicted a comparatively higher cellular internalisation achieved for undecorated FNS-NS with respect to its chitosan-decorated counterpart. The lyophilised FNS-NS was stable for 90 days at proper storage conditions. The FNS-NS with 15% trehalose had appropriate physicochemical attributes that could be a promising carrier for topical delivery to treat androgenic alopecia.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 2","pages":"106-123"},"PeriodicalIF":3.9,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9174638","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}
Scaffolds are implanted to spur the regeneration of damaged tissues. The inappropriate construction of scaffolds laden with cells is not efficient. The optimisation of the scaffolds' constituents is essential for tissue repair. In this study, a scaffold embedded with Raloxifene drug was optimised via Response Surface Methodology (RSM), targeting controlled cell proliferation. The independent variables for RSM (fibronectin, collagen I, glutaraldehyde, and Raloxifene) were screened in Swiss target prediction software (probability ≥99%) to optimise dependent variables (porosity, cell viability, degradation, and swelling) by ANOVA and characterised with FTIR, SEM and contact angle measurement. The scaffold was tested for antimicrobial property, and proliferation and attachment of mouse mesenchymal stem cells. The ANOVA analysis with p value ≤ 0.0001 suggested the optimal concentration of biomaterials and drugs. The optimised scaffold displayed 80% porosity with pore size 33 ± 3 µm. We also observed significant cell attachment and proliferation (p value ≤ 0.05) in optimised scaffold. The scaffold may be further evaluated for its potential for tissue repair.
{"title":"Design, development and characterisation of an optimised scaffold to enhance cell proliferation for tissue repair.","authors":"Subodh Kumar, Chanakya Lahiri, Somya Chaaudhary, Prateek Paul, Yogesh Kumar Verma","doi":"10.1080/02652048.2023.2175922","DOIUrl":"https://doi.org/10.1080/02652048.2023.2175922","url":null,"abstract":"<p><p>Scaffolds are implanted to spur the regeneration of damaged tissues. The inappropriate construction of scaffolds laden with cells is not efficient. The optimisation of the scaffolds' constituents is essential for tissue repair. In this study, a scaffold embedded with Raloxifene drug was optimised via Response Surface Methodology (RSM), targeting controlled cell proliferation. The independent variables for RSM (fibronectin, collagen I, glutaraldehyde, and Raloxifene) were screened in Swiss target prediction software (probability ≥99%) to optimise dependent variables (porosity, cell viability, degradation, and swelling) by ANOVA and characterised with FTIR, SEM and contact angle measurement. The scaffold was tested for antimicrobial property, and proliferation and attachment of mouse mesenchymal stem cells. The ANOVA analysis with <i>p</i> value ≤ 0.0001 suggested the optimal concentration of biomaterials and drugs. The optimised scaffold displayed 80% porosity with pore size 33 ± 3 µm. We also observed significant cell attachment and proliferation (<i>p</i> value ≤ 0.05) in optimised scaffold. The scaffold may be further evaluated for its potential for tissue repair.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 2","pages":"82-97"},"PeriodicalIF":3.9,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9181407","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}
Pub Date : 2023-03-01DOI: 10.1080/02652048.2023.2175923
U R Mahajan, I Emmanuel, A Shrinivasa Rao, S T Mhaske
This study aims to enhance the latent heat storage properties of the microcapsules by altering the amount of crosslinking agent from 3 to 20%w/w, the core-to-shell ratio from 1:1 to 2:1, and the amount of initiator from 1 to 3%. The phase change material n-tetradecane (C-14) was microencapsulated by using poly (methyl methacrylate -co- methacrylic acid) as a shell material through an oil by water-seeded emulsion polymerisation technique. The structural, morphological, and thermal properties of microcapsules were evaluated by using Fourier transform infrared spectroscopy, optical microscopy, scanning electron microscopy, differential scanning calorimetry analysis, and thermogravimetric analysis. The average particle size of the microcapsules ranges from 01 to 15 µm. The results showed that the microcapsules have a higher melting enthalpy value of 127.3 ± 0.06 J/g with a microencapsulation efficiency of 66.72% when a 20% w/w crosslinker was used. The thermal stability of the phase change material (PCM) was increased by ∼30 ± 2 °C by encapsulation.
{"title":"Microencapsulation of n-tetradecane with poly (methyl methacrylate-co-methacrylic acid) shell by seeded emulsion polymerisation and its thermal energy storage characteristics.","authors":"U R Mahajan, I Emmanuel, A Shrinivasa Rao, S T Mhaske","doi":"10.1080/02652048.2023.2175923","DOIUrl":"https://doi.org/10.1080/02652048.2023.2175923","url":null,"abstract":"<p><p>This study aims to enhance the latent heat storage properties of the microcapsules by altering the amount of crosslinking agent from 3 to 20%<i>w/w</i>, the core-to-shell ratio from 1:1 to 2:1, and the amount of initiator from 1 to 3%. The phase change material n-tetradecane (C-14) was microencapsulated by using poly (methyl methacrylate -co- methacrylic acid) as a shell material through an oil by water-seeded emulsion polymerisation technique. The structural, morphological, and thermal properties of microcapsules were evaluated by using Fourier transform infrared spectroscopy, optical microscopy, scanning electron microscopy, differential scanning calorimetry analysis, and thermogravimetric analysis. The average particle size of the microcapsules ranges from 01 to 15 µm. The results showed that the microcapsules have a higher melting enthalpy value of 127.3 ± 0.06 J/g with a microencapsulation efficiency of 66.72% when a 20% <i>w/w</i> crosslinker was used. The thermal stability of the phase change material (PCM) was increased by ∼30 ± 2 °C by encapsulation.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 2","pages":"98-105"},"PeriodicalIF":3.9,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9166961","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}
Pub Date : 2023-03-01DOI: 10.1080/02652048.2023.2172469
Ruan Reis Nascimento, Julie Pauline Gaitan Tabares, Paulo Neilson Marques Dos Anjos, Luana Novaes Santos, Denise de Oliveira Silva, Rodrigo Luis Silva Ribeiro Santos
The objectives of this work are to develop nanocarrier systems for the Ru(II)-p-cymene naproxen antitumor metallodrug, [Ru(η6-p-cymene)(npx)Cl] or Rupcy, based on polymeric nanoparticles (NPs) composed by the biodegradable poly(lactic acid) (PLA) and the hydrophilic polymerised β-cyclodextrin (PolyCD); to validate an analytical method for determination of Ru incorporated into the metallodrug loaded-NPs. The PolyCD was prepared by single step condensation and polymerisation reaction and incorporated as a polymer blend during the fabrication of PLA/PolyCD blends NPs and also as a core/shell structure built by adsorption of the PolyCD onto the surface of PLA NPs to give PLA(core)/PolyCD(shell) NPs. Three different loaded-systems incorporating the metallodrug (Rupcy-PLA NPs (1), Rupcy-PLA/PolyCD blends (2), and Rupcy-PLA(core)/PolyCD(shell) NPs (3)) were prepared by nanoprecipitation. The characterisation was performed by Proton Nuclear Magnetic Resonance, Matrix Assisted Laser Desorption/Ionization Time-of-Flight, Fourier-Transform Infra-red and UV-VIS Electronic Absorption Spectroscopies, Thermogravimetric Analysis, Differential Scanning Calorimetry, Dynamic Light Scattering, and Electrophoretic Light Scattering. Ru was determined by Microwave Induced Plasma Optical Emission Spectrometry (MIP-OES) with validation of the method. The metallodrug entrapment efficiency was around 90% (w/w) and drug loading was at 3-4% (w/w). The characterised metallodrug-loaded systems exhibited monomodal size distributions and appropriate hydrodynamic diameters [218.3 ± 13.5 (1), 205.4 ± 14.4 (2), 231.5 ± 22.0 (3) nm] and zeta potential values [-31.5 ± 2.2 (1), -26.1 ± 4.5 (2), -28.8 ± 6.1 (3) mV]. The validation of the MIP-OES method by evaluating selectivity, linearity, precision, accuracy, and limits of detection and quantification succeeded. The NPs parameters are compatible with colloidally stable systems. The MIP-OES method showed to be simple, reliable, and feasible to quantify indirectly the amount of the metallodrug-loaded into the PLA NPs.
{"title":"Poly(lactic acid)/β-cyclodextrin based nanoparticles bearing ruthenium(II)-arene naproxen complex: preparation and characterisation. Analytical validation for metal determination by microwave-induced plasma optical emission spectrometry.","authors":"Ruan Reis Nascimento, Julie Pauline Gaitan Tabares, Paulo Neilson Marques Dos Anjos, Luana Novaes Santos, Denise de Oliveira Silva, Rodrigo Luis Silva Ribeiro Santos","doi":"10.1080/02652048.2023.2172469","DOIUrl":"https://doi.org/10.1080/02652048.2023.2172469","url":null,"abstract":"<p><p>The objectives of this work are to develop nanocarrier systems for the Ru(II)-p-cymene naproxen antitumor metallodrug, [Ru(η<sup>6</sup>-p-cymene)(npx)Cl] or Rupcy, based on polymeric nanoparticles (NPs) composed by the biodegradable poly(lactic acid) (PLA) and the hydrophilic polymerised β-cyclodextrin (PolyCD); to validate an analytical method for determination of Ru incorporated into the metallodrug loaded-NPs. The PolyCD was prepared by single step condensation and polymerisation reaction and incorporated as a polymer blend during the fabrication of PLA/PolyCD blends NPs and also as a core/shell structure built by adsorption of the PolyCD onto the surface of PLA NPs to give PLA(core)/PolyCD(shell) NPs. Three different loaded-systems incorporating the metallodrug (Rupcy-PLA NPs (<b>1</b>), Rupcy-PLA/PolyCD blends (<b>2</b>), and Rupcy-PLA(core)/PolyCD(shell) NPs (<b>3</b>)) were prepared by nanoprecipitation. The characterisation was performed by Proton Nuclear Magnetic Resonance, Matrix Assisted Laser Desorption/Ionization Time-of-Flight, Fourier-Transform Infra-red and UV-VIS Electronic Absorption Spectroscopies, Thermogravimetric Analysis, Differential Scanning Calorimetry, Dynamic Light Scattering, and Electrophoretic Light Scattering. Ru was determined by Microwave Induced Plasma Optical Emission Spectrometry (MIP-OES) with validation of the method. The metallodrug entrapment efficiency was around 90% (w/w) and drug loading was at 3-4% (w/w). The characterised metallodrug-loaded systems exhibited monomodal size distributions and appropriate hydrodynamic diameters [218.3 ± 13.5 (<b>1</b>), 205.4 ± 14.4 (<b>2</b>), 231.5 ± 22.0 (<b>3</b>) nm] and zeta potential values [-31.5 ± 2.2 (<b>1</b>), -26.1 ± 4.5 (<b>2</b>), -28.8 ± 6.1 (<b>3</b>) mV]. The validation of the MIP-OES method by evaluating selectivity, linearity, precision, accuracy, and limits of detection and quantification succeeded. The NPs parameters are compatible with colloidally stable systems. The MIP-OES method showed to be simple, reliable, and feasible to quantify indirectly the amount of the metallodrug-loaded into the PLA NPs.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 2","pages":"67-81"},"PeriodicalIF":3.9,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9181414","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}
Aim: The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.
Methods: Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. In vitro release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex-vivo efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.
Results: The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.
Conclusions: The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.
{"title":"Preparation and characterisation of self-emulsifying drug delivery system (SEDDS) for enhancing oral bioavailability of metformin hydrochloride using hydrophobic ion pairing complexation.","authors":"Seyedeh Nika Rezvanjou, Mohammad Reza Niavand, Omid Heydari Shayesteh, Ehsan Mehrani Yeganeh, Davood Ahmadi Moghadam, Katayoun Derakhshandeh, Reza Mahjub","doi":"10.1080/02652048.2023.2170488","DOIUrl":"https://doi.org/10.1080/02652048.2023.2170488","url":null,"abstract":"<p><strong>Aim: </strong>The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.</p><p><strong>Methods: </strong>Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. <i>In vitro</i> release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex<i>-vivo</i> efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.</p><p><strong>Results: </strong>The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.</p><p><strong>Conclusions: </strong>The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"53-66"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10746231","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}
Pub Date : 2023-01-01DOI: 10.1080/02652048.2023.2167011
Tobeka Naki, William Morwa Reagile Matshe, Mohammed Olusegun Balogun, Suprakas Sinha Ray, Samuel Ayodele Egieyeh, Blessing Atim Aderibigbe
Aim: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.
Methods: The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies.
Results: 1H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC50 values in the range of 13-44.4 µm which was more effective than tacrine (IC50 =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.
Conclusion: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.
{"title":"Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer's disease.","authors":"Tobeka Naki, William Morwa Reagile Matshe, Mohammed Olusegun Balogun, Suprakas Sinha Ray, Samuel Ayodele Egieyeh, Blessing Atim Aderibigbe","doi":"10.1080/02652048.2023.2167011","DOIUrl":"https://doi.org/10.1080/02652048.2023.2167011","url":null,"abstract":"<p><strong>Aim: </strong>To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and <i>E</i>)-<i>N</i>-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.</p><p><strong>Methods: </strong>The conjugates were characterised by <sup>1</sup>HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by <i>in vitro</i> anti-acetylcholinesterase and drug release studies.</p><p><strong>Results: </strong><sup>1</sup>H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC<sub>50</sub> values in the range of 13-44.4 µm which was more effective than tacrine (IC<sub>50</sub> =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.</p><p><strong>Conclusion: </strong>The drug release profile, particle sizes, and <i>in vitro</i> studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"15-28"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10780347","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}
Pub Date : 2023-01-01DOI: 10.1080/02652048.2023.2168081
Jéssica Roberta Pereira Martins, Antonia Livânia Linhares de Aguiar, Karina Alexandre Barros Nogueira, Acrisio José Uchôa Bastos Filho, Thais da Silva Moreira, Márjory Lima Holanda Araújo, Claudia Pessoa, Josimar O Eloy, Ivanildo José da Silva Junior, Raquel Petrilli
We aimed to encapsulate R-PE to improve its stability for use as a fluorescent probe for cancer cells. Purified R-PE from the algae Solieria filiformis was encapsulated in polymeric nanoparticles using PCL. Nanoparticles were characterised and R-PE release was evaluated. Also, cellular uptake using breast and prostate cancer cells were performed. Nanoparticles presented nanometric particle size (198.8 ± 0.06 nm) with low polydispersity (0.13 ± 0.022), negative zeta potential (-18.7 ± 1.10 mV), and 50.0 ± 7.3% encapsulation. FTIR revealed that R-PE is molecularly dispersed in PCL. DSC peak at 307 °C indicates the presence of R-PE in the nanoparticle. Also, in vitro, it was demonstrated low release for nanoparticles and degradation for the free R-PE. Finally, cellular uptake demonstrated the potential of R-PE/PCL nanoparticles for cancer cell detection. Nanoparticles loaded with R-PE can overcome instability and allow application as a fluorescent probe for cancer cells.
{"title":"Nanoencapsulation of R-phycoerytrin extracted from <i>Solieria filiformis</i> improves protein stability and enables its biological application as a fluorescent dye.","authors":"Jéssica Roberta Pereira Martins, Antonia Livânia Linhares de Aguiar, Karina Alexandre Barros Nogueira, Acrisio José Uchôa Bastos Filho, Thais da Silva Moreira, Márjory Lima Holanda Araújo, Claudia Pessoa, Josimar O Eloy, Ivanildo José da Silva Junior, Raquel Petrilli","doi":"10.1080/02652048.2023.2168081","DOIUrl":"https://doi.org/10.1080/02652048.2023.2168081","url":null,"abstract":"<p><p>We aimed to encapsulate R-PE to improve its stability for use as a fluorescent probe for cancer cells. Purified R-PE from the algae <i>Solieria filiformis</i> was encapsulated in polymeric nanoparticles using PCL. Nanoparticles were characterised and R-PE release was evaluated. Also, cellular uptake using breast and prostate cancer cells were performed. Nanoparticles presented nanometric particle size (198.8 ± 0.06 nm) with low polydispersity (0.13 ± 0.022), negative zeta potential (-18.7 ± 1.10 mV), and 50.0 ± 7.3% encapsulation. FTIR revealed that R-PE is molecularly dispersed in PCL. DSC peak at 307 °C indicates the presence of R-PE in the nanoparticle. Also, <i>in vitro</i>, it was demonstrated low release for nanoparticles and degradation for the free R-PE. Finally, cellular uptake demonstrated the potential of R-PE/PCL nanoparticles for cancer cell detection. Nanoparticles loaded with R-PE can overcome instability and allow application as a fluorescent probe for cancer cells.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"37-52"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10814097","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}
Aim: Silybum marianum extract (SME) possesses neuroprotective potency through its high antioxidant content. We attempted to increase the effectiveness of SME by encapsulating them in chitosan. Neuroprotective potency of SME and SME-loaded chitosan nanoparticles (SME-CNPs) were shown in SH-SY5Y cell line against H2O2-induced oxidative stress.
Methods: We produced CNPs and SME-CNPs by ionic gelation method and properly determined their physical characteristics. Encapsulation efficiency, loading capacity, and in vitro release tests were performed for SME-CNPs. The neurotoxicity and neuroprotective efficiency in SH-SY5Y cell line against H2O2 was also investigated.
Results: The size of SME-CNPs was 168.2 ± 11.12 nm with zeta potential 10.6 ± 1.0 mV. The encapsulation efficiency and loading capacity were successfully achieved at 96.6% and 1.89% respectively. SME and SME-CNPs improved cell viability higher than 80%, and SME-CNPs exhibited significant neuroprotective effects against H2O2 damage.
Conclusions: It was concluded that SME and SME-CNPs highly prevent damage caused by H2O2 and reduce cell damage in vitro by their neuroprotective effects.
{"title":"Synthesis characterisation and neuroprotectivity of <i>Silybum marianum</i> extract loaded chitosan nanoparticles.","authors":"Hatice Feyzan Ay, Serap Yesilkir-Baydar, Rabia Cakir-Koc","doi":"10.1080/02652048.2023.2167012","DOIUrl":"10.1080/02652048.2023.2167012","url":null,"abstract":"<p><strong>Aim: </strong><i>Silybum marianum</i> extract (SME) possesses neuroprotective potency through its high antioxidant content. We attempted to increase the effectiveness of SME by encapsulating them in chitosan. Neuroprotective potency of SME and SME-loaded chitosan nanoparticles (SME-CNPs) were shown in SH-SY5Y cell line against H<sub>2</sub>O<sub>2</sub>-induced oxidative stress.</p><p><strong>Methods: </strong>We produced CNPs and SME-CNPs by ionic gelation method and properly determined their physical characteristics. Encapsulation efficiency, loading capacity, and <i>in vitro</i> release tests were performed for SME-CNPs. The neurotoxicity and neuroprotective efficiency in SH-SY5Y cell line against H<sub>2</sub>O<sub>2</sub> was also investigated.</p><p><strong>Results: </strong>The size of SME-CNPs was 168.2 ± 11.12 nm with zeta potential 10.6 ± 1.0 mV. The encapsulation efficiency and loading capacity were successfully achieved at 96.6% and 1.89% respectively. SME and SME-CNPs improved cell viability higher than 80%, and SME-CNPs exhibited significant neuroprotective effects against H<sub>2</sub>O<sub>2</sub> damage.</p><p><strong>Conclusions: </strong>It was concluded that SME and SME-CNPs highly prevent damage caused by H<sub>2</sub>O<sub>2</sub> and reduce cell damage <i>in vitro</i> by their neuroprotective effects.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"29-36"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10753116","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}
Pub Date : 2023-01-01DOI: 10.1080/02652048.2022.2160845
Thapakorn Tree-Udom, Chalermrat Simavong, Prapasiri Phetklung, Kanjanaporn Chompoonuch, Sagaw Prateepchinda, Supatchaya Jaemsai, Andrew William King, Oraphan King
The aim is to prepare, characterise, and evaluate the biological activities and key molecular interactions of L-ascorbic acid and phosphatidylcholine (PC-AA) complex vesicles. PC-AA complexes were prepared and characterised using DLS, TEM, FTIR, UV-Vis, in-vitro release, bioactivities, and cytotoxicity. The key interactions of the AA with the PC were studied with MD simulations. PC-AA complex provides improved stability towards the degradation of AA in aqueous solutions while also slowing its release profile. The PC-AA complexes with an optimal molar ratio of PC: AA = 2.5:1 was shown to have a hydrodynamic diameter of 368.67 ± 4.65 nm and an EE of 68.16 ± 0.23%. At low concentration, the PC-AA complexes have no toxicity towards human dermal fibroblast cells over 48 h. Importantly, MD suggests that AA only forms the PC-AA complex when in its neutral form which is the desired active form. PC-AA complex could be a potential active to use in medicinal and cosmeceutical applications.
目的是制备、表征和评价l -抗坏血酸和磷脂酰胆碱(PC-AA)复合物囊泡的生物活性和关键的分子相互作用。制备了PC-AA配合物,并用DLS、TEM、FTIR、UV-Vis、体外释放度、生物活性和细胞毒性对其进行了表征。通过MD模拟研究了AA与PC的关键相互作用。PC-AA配合物提高了AA在水溶液中降解的稳定性,同时也减缓了其释放。以PC: AA = 2.5:1为最佳摩尔比的PC-AA配合物的水动力直径为368.67±4.65 nm, EE为68.16±0.23%。在低浓度下,PC-AA复合物对人真皮成纤维细胞在48小时内无毒性。重要的是,MD表明AA仅在中性形式下形成PC-AA复合物,而中性形式是期望的活性形式。PC-AA配合物在医药和药妆领域具有潜在的应用价值。
{"title":"L-Ascorbic acid and phosphatidylcholine complex vesicles: formation and elucidation of their biological activities, and their molecular interactions.","authors":"Thapakorn Tree-Udom, Chalermrat Simavong, Prapasiri Phetklung, Kanjanaporn Chompoonuch, Sagaw Prateepchinda, Supatchaya Jaemsai, Andrew William King, Oraphan King","doi":"10.1080/02652048.2022.2160845","DOIUrl":"https://doi.org/10.1080/02652048.2022.2160845","url":null,"abstract":"<p><p>The aim is to prepare, characterise, and evaluate the biological activities and key molecular interactions of L-ascorbic acid and phosphatidylcholine (PC-AA) complex vesicles. PC-AA complexes were prepared and characterised using DLS, TEM, FTIR, UV-Vis, in-vitro release, bioactivities, and cytotoxicity. The key interactions of the AA with the PC were studied with MD simulations. PC-AA complex provides improved stability towards the degradation of AA in aqueous solutions while also slowing its release profile. The PC-AA complexes with an optimal molar ratio of PC: AA = 2.5:1 was shown to have a hydrodynamic diameter of 368.67 ± 4.65 nm and an EE of 68.16 ± 0.23%. At low concentration, the PC-AA complexes have no toxicity towards human dermal fibroblast cells over 48 h. Importantly, MD suggests that AA only forms the PC-AA complex when in its neutral form which is the desired active form. PC-AA complex could be a potential active to use in medicinal and cosmeceutical applications.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"1-14"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9319185","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}
This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease® were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T6% (the time taken for the drug to release equal to 6% w/w). The powder properties were assessed by measuring particle size and microstructure using SEM, FT-IR, and PXRD. Furthermore, selected batch was assessed for their drug content, encapsulation efficiency, in vitro release, bitterness, and stability studies. EPO-Surelease® (1: 4) microcapsules had an average diameter (D50) of 37.69 ± 3.61 μm with a span of 2.395. The drug contents and encapsulation efficiency of EPO-Surelease®(1:4) were 10.89% and 63.7%, respectively. EPO-Surelease® (1:4) microcapsules prepared by spray drying with aqueous polymer dispersion can effectively mask the bitter taste of CAM.
{"title":"The preparation and characterisation of tasteless core-shell clarithromycin microcapsules.","authors":"Yu Fu, Yunjing Zhu, Xue Liang, Yihan Kong, Xiaolin Wang, Anan Zhang, Zhiqing Zhao, Jingxin Gou, Yanjiao Wang, Tian Yin, Yu Zhang, Haibing He, Xing Tang","doi":"10.1080/02652048.2022.2146221","DOIUrl":"https://doi.org/10.1080/02652048.2022.2146221","url":null,"abstract":"<p><p>This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease<sup>®</sup> were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T<sub>6%</sub> (the time taken for the drug to release equal to 6% <i>w</i>/<i>w</i>). The powder properties were assessed by measuring particle size and microstructure using SEM, FT-IR, and PXRD. Furthermore, selected batch was assessed for their drug content, encapsulation efficiency, in vitro release, bitterness, and stability studies. EPO-Surelease<sup>®</sup> (1: 4) microcapsules had an average diameter (D50) of 37.69 ± 3.61 μm with a span of 2.395. The drug contents and encapsulation efficiency of EPO-Surelease<sup>®</sup>(1:4) were 10.89% and 63.7%, respectively. EPO-Surelease<sup>®</sup> (1:4) microcapsules prepared by spray drying with aqueous polymer dispersion can effectively mask the bitter taste of CAM.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"39 7-8","pages":"654-667"},"PeriodicalIF":3.9,"publicationDate":"2022-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10873180","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}